How and Why It Works?
VemoHerb® Muscle Kick
contains dry extracts from Bulgarian Tribulus terrestris, Leuzea carthamoides, Ginkgo biloba, Piper Nigrum
We can proudly say that the high quality, proprietary ingredients present in this unique product, together with the perfect match of the formula, guarantee the ultimate experience and results of our customers. This positions VemoHerb® Muscle Kick
as a choice No 1, outperforming any similar product. Our long-lasting experience, combined with almost 2 years spent in developing this unique product, make the balanced synergistic effect of this formula the perfect option for every ultimate sports performance goal.
VemoHerb® Muscle Kick
is a dietary supplement based on four high quality concentrated extracts – dry extract from the plant Bulgarian Tribulus terrestris
, dry extract from Leuzea carthamoides
, dry extract from Ginkgo biloba
, dry extract from Piper nigrum
Dry extract from Bulgarian Tribulus terrestris
Dry extract from Leuzea Carthamoides
The properties of the genuine Bulgarian Тribulus extract are due to the presence of steroidal saponins of furostanol type (60% determined as protodioscin). [1, 2] The steroidal saponins are active substances, which support the natural production of sexual hormones (androgens and estrogens),[3, 4, 5] influence positively the normal function of central nervous system [6, 7], and are defined as active components with anabolic character.* They work on the normal testosterone levels in the male organism, naturally supporting the hormonal balance and the normal function of prostate, without affecting their functional mechanism and without side effects.* [2, 3, 4, 8, 9, 10]
In women they work on the normal levels of pregnenolone, progesterone, estrogens, which may help support the physical and psycho-emotional health of a woman.* [5, 11, 12]
The protodioscin [1, 2, 13] supports the natural production of luteinizing hormone from the adenohypophysis and the normal sex hormones levels.*[3, 4, 14] It helps support a positive nitrogen balance and improves the protein synthesis, including the one in the muscles.* This supports the body’s abilities and endurance in cases of physical and mental overwork.* [2, 15]
The genuine Bulgarian Тribulus extract is very suitable for bodybuilders and athletes in the preparatory and the active period, as well as in the period of recovery after physical exhaustion from exercise.* [15, 16, 17]
For more information about the exceptional properties of Dry extract from Bulgarian Tribulus terrestris you can read HERE
The properties of the Leuzea extract are due to the purified active ingredient - 95% beta-ecdysterone.  Ecdysones show muscle growth properties and help the body resist the damaging effect of stress.* [18 – 24]
Phytoecdysteroids stimulate protein synthesis [18, 19, 22, 24, 25], and in dosages of 5-10 mg per kg bodyweight, they are considered protein stimulants, promoting fast muscle growth and strength.* [19, 21, 22,24, 26, 27] As polyhydroxysterols, they naturally affect the metabolism of carbohydrates and nucleic acids, help the normal glycogen synthesis and increase the content of high energy phosphate compounds.* [25, 27] This promotes the growth of the skeleton muscles, influences positively the endurance, reflexes and physical condition of the athletes.* [19, 21, 22, 24, 25, 27]
A number of studies show the anabolic activity of beta-ecdysterone, as well as its harmlessness and safety for use during hard trainings or physical overwork.* [20 – 23, 28, 29] The beta-ecdysterone positively influences the normal function of the central nervous system.* [18, 25, 30] In professional sport it is used for achieving physical and psychical stability, without any side effects on the cardiovascular and the immune systems. [18, 25, 30]
You can read for the long history of Leuzea Carthamoides HERE
Dry extract from Ginkgo biloba
Our extremely effective and concentrated extract from the leaves of Ginkgo biloba
is standardized at 24% ginkgo flavone glycosides. The extract has become highly popular among the sports fields, due to its outstanding benefits [31 - 39]:
- it is beneficial for blood and oxygen flow in the body and can thus support concentration and sports performance*
- its antioxidant activity aids for removing the free radicals from the muscles, that will otherwise break them down*
- increases muscle growth and supports recovery after intense exercise*
- naturally supports the metabolism*
Plenty of studies also suggest that Ginkgo biloba
extract works on the normal cortisol levels, and supports the normal blood pressure levels, especially during workouts.* [31, 32] The combination of Ginkgo biloba
extract and L-arginine boosts its action even more, promoting fast muscle growth and strength, as a result of the supported blood flow to the muscles.* 
For more detailed information regarding benefits of Ginkgo biloba
Dry extract from Piper nigrum
The Piper nigrum
extract in VemoHerb® Muscle Kick
is standardized to the active ingredient piperine (min. 95%). Numerous studies suggest that when only 5 mg of such concentrated Piper nigrum
extract is combined with the other ingredients, it can increase the absorption of those ingredients by 30-2000%!* 
L-Arginine is considered a semi-essential amino acid, which means that the body produces it naturally but in limited quantities, and it can be supplemented additionally through the diet.* L-Arginine is very popular in sports nutrition due to its nitrogen retention properties, because nitrogen is a key factor in the muscle protein synthesis.* L-Arginine is a precursor of nitric oxide, and it is known that nitric oxide participates in the vasodilation (the dilation of blood vessels).* Nitric oxide helps to increase blood flow into the muscles which is the main factor that produces pumps during exercise.* Recent research suggests that nitric oxide is directly connected with muscle building.* Latest data also suggests that L-arginine supports the natural production of Creatine in the body.* It is also shown to support the utilization of oxygen in the body, due to the increased vasodilation.* [42, 43]
**see the References [1-43] in the Science tab
Our attitude in VemoHerb is to “keep it simple and effective”. That’s why we always invest in manufacturing the highest quality raw materials and developing the ideal formulation of the ingredients, so that they combine in the perfect synergistic mechanism, complementing each other, and leading to the maximum sport performance of the body.* We do not believe in the endless list of compounds in the “miracle panaceas” that are flooding the market nowadays, because it is just not feasible to make a good working combination of a dozen substances that could match synergistically in appropriate dosage. Beware of such kind of “miracle” but ineffective products!
The product is a food supplement not a medical drug. The product is not a substitute for a varied diet. Do not exceed the recommended daily dose. It is not recommended for pregnant, nursing women and children!
|*These statements have not been evaluated by the Food and Drug Administration. This product is not intended to diagnose, treat, cure or prevent any disease.
References to How and Why It Works:
1. Kostova, I. & Dinchev, D. Saponins in Tribulus terrestris – Chemistry and Bioactivity. Phytochem Rev (2005) 4: 111.
Tribulus terrestris is a valuable herb known for its application in the folk medicine in many parts of the world. Furostanol and spirostanol saponins of tigogenin, neotigogenin, gitogenin, neogitogenin, hecogenin, neohecogenin, diosgenin, chlorogenin, ruscogenin and sarsasapogenin type are frequently found in this plant. Four sulphated saponins of tigogenin and diosgenin type are also isolated. Extracts and steroidal saponins have been found to possess various pharmacological activities. Preparations based on the saponin fraction of T. terrestris are used for treatment of infertility and libido disorders in men and women, as well as for treatment of cardiac diseases. Food supplements containing T. terrestris extracts are on sale in USA and Europe with claim of a general stimulating action.
2. Wenyi Zhu, Yijie Du, Hong Meng, Yinmao Dong and Li Li – A review of traditional pharmacological uses, phytochemistry, and pharmacological activities of Tribulus terrestris
Tribulus terrestris L. (TT) is an annual plant of the family Zygophyllaceae that has been used for generations to energize, vitalize, and improve sexual function and physical performance in men. The fruits and roots of TT have been used as a folk medicine for thousands of years in China, India, Sudan, and Pakistan. Numerous bioactive phytochemicals, such as saponins and flavonoids, have been isolated and identified from TT that are responsible alone or in combination for various pharmacological activities. This review provides a comprehensive overview of the traditional applications, phytochemistry, pharmacology and overuse of TT and provides evidence for better medicinal usage of TT.
3. Milanov, S., E. Maleeva, M. Tashkov. – Tribestan effect on the concentration of some hormones in the serum of healthy subjects (1981).
Tribestan effect has been studied on the serum concentration of hypophyseal hormones, of ACTH, STH, LH, FSH, adrenal hormone aldosterone and cortisol and sex hormones - testosterone and estradiol. The experiments have been carried out on 8 males and 8 females, aged 28 - 45 years of age. The product was perorally administered in a single dose of 250 mg, three times daily for 5 days. Serum samples were withdrawn at 8 a.m. and 12 a.m., prior to and post treatment. The product has been established not to change essentially the concentrations of adrenal hormones and of ACTH. The hypophyseal-gonadal axis however has significantly been affected in the females with predominantly increased concentration of FSH and estradiol and in the males - mainly of LH and the testosterone. The mechanism of that action is presumed to be complicated and realized both by direct effect on gonadal apparatus and by the tropic hormones. The probable established changes in the concentration of the hormones studied do not get out of the frames of the physiological limits. The lyophilized extract of Tribulus terrestris, introduced in veterinary practice as TB-68, has pronounced sex-stimulating function. The initial studies of this product showed that it stimulates the spermatogenesis of albino rats (Vankov S., et al., 1973) and enhanced the ovulation of female rats (Vankov S. et al. 1973). Zarkova S. (1976) has also established in rats an increased number of spermatogonia, spermatocytes as well as increase of neutral mucopolysaccharides in seminiferous tubules of the testes. Gendzhev Z. and S. Zarkova, in other experiments (1978) proved the increase of spermatic reserve in the epididymis of rats. With the view to the need of human medicine of a product stimulating sexual function, Tribestan was formulated on the base of the indicated phytochemical product. It contains saponins of furostanol type (Tomova M. et al., 1978). The first studies of Tribestan confirmed its high sex-stimulating activity in experimental animals (Zarkova S., 1981). Later, the clinical studies established a similar stimulating effect in humans as well (Protich M. at al. 1981). The present study was carried out with a view to throwing light on some aspects of the mechanism of that action of Tribestan, aiming at attaining an effect from the product on the serum concentration of some hypophyseal, sexual and adrenal hormones.
4. Gauthaman, K. and Ganesan, A. – The hormonal effects of Tribulus terrestris and its role in the management of male erectile dysfunction – an evaluation using primates, rabbit and rat. Phytomedicine (2008) 15: 44.
Hormonal effects of Tribulus terrestris (TT) were evaluated in primates, rabbit and rat to identify its usefulness in the management of erectile dysfunction (ED). TT extract was administered intravenously, as a bolus dose of 7.5, 15 and 30 mg/kg, in primates for acute study. Rabbits and normal rats were treated with 2.5, 5 and 10mg/kg of TT extract orally for 8 weeks, for chronic study. In addition, castrated rats were treated either with testosterone cypionate (10mg/kg, subcutaneously; biweekly for 8 weeks) or TT orally (5mg/kg daily for 8 weeks). Blood samples were analyzed for testosterone (T), dihydrotestosterone (DHT) and dehydroepiandrosterone sulphate (DHEAS) levels using radioimmunoassay. In primates, the increases in T (52%), DHT (31%) and DHEAS (29%) at 7.5mg/kg were statistically significant. In rabbits, both T and DHT were increased compared to control, however, only the increases in DHT (by 30% and 32% at 5 and 10mg/kg) were statistically significant. In castrated rats, increases in T levels by 51% and 25% were observed with T and TT extract respectively that were statistically significant. TT increases some of the sex hormones, possibly due to the presence of protodioscin in the extract. TT may be useful in mild to moderate cases of ED.
5. Justino Mameri Filho; Mauro Abi Haidar; José Maria Soares Júnior; Edmund Chada Baracat – Effects of the association of estrogen and androgen in postmenopausal women
PURPOSE: to evaluate the effects of the association of estrogen and androgen on the quality of life and sexuality of women during climacterium.
METHODS: ninety-six postmenopausal women with vasomotor symptoms and sexual dysfunction were included. The participants were randomly divided into three treatment groups with 32 pacients each: placebo, conjugated equine estrogens (CEE) (0.625 mg per day) and CEE (0.625 mg per day) associated with methyltestosterone (2.5 mg per day). The length of the treatment period was three months. The Women Health Questionnaire (WHQ) and the Modified Sexuality Questionnaire were applied to evaluate the quality of life and sexuality before and after the treatment. Some parameters of cardiovascular risk, endometrial echo and hepatic toxicity were evaluated. ANOVA was used for data analysis followed by the Fisher test and the Shapiro-Wilk post hoc test.
RESULTS: the improvement in WHQ parameters was significant in the hormonal treatment groups (CEE and CEE + methyltestosterone) compared to the placebo group. However, there were no differences in somatic symptoms among the three groups. The association of estrogen with androgen significantly improved sexual function (score (mean): 64 vs 67, p<0.05) and depressive humor (score (mean): 75 vs 80, p<0.05) compared to estrogen alone. This therapy also presented a large number of WHQ questions with a high score (p<0.05). The use of CEE associated with methyltestosterone decreased the total cholesterol (212±42 and 194±43, before and after the treatment, respectively) and HDL colesterol (56±16 and 48±14, before and after the treatment, respectively), and slightly increased the endometrial echo (4.7±2.3 and 5.5±2.3, before and after the treatment, respectively). No signifcant changes in liver enzymes during the treatment period was detected.
CONCLUSIONS: estrogen associated with methyltestosterone resulted in significant improvement in the quality of life and sexuality of postmenopausal women. This effect was superior to estrogen alone and placebo. The effect of treatment with the estrogen-androgen association was evident regarding depressive humor and sexual function questions of the WHQ.
6. Mengquan Lia Yue Guanb Jiaqi Liua Fengguo Zhaia Xiuping Zhanga Lixin Guana – Cellular and Molecular Mechanisms in Vascular Smooth Muscle Cells by which Total Saponin Extracted from Tribulus Terrestris Protects Against Artherosclerosis
Total saponin extracted from Tribulus terrestris (TSETT) has been reported to protect against atherosclerosis. We here investigate the cellular and molecular mechanisms of TSETT underlying protection against atherosclerosis.
Cell proliferation was measured with Methyl thiazolyl tetrazolium (MTT); Intracellular H2O2 was measured with DCFH-DA, a fluorescent dye; Intracellular free Ca(2+) was measured with a confocal laser scanning microscopy; Genes expression was measured with gene array and real-time quantitative polymerase chain reaction (RT-PCR); Phosphorylation of extracellular signal-regulated kinase 1/2 (phospho-ERK1/2) was measured with cell-based enzyme-linked immunosorbent assay (ELISA) and western blotting.
TSETT significantly suppressed the increase in cells proliferation induced by angiotensin II, significantly suppressed the increase in the intracellular production of H2O2 induced by angiotensin II, significantly inhibited the increase in intracellular free Ca(2+) induced by H2O2, significantly inhibited the increase in phospho-ERK1/2 induced by angiotensin II; significantly inhibited the increase in mRNA expression of c-fos, c-jun and pkc-α induced by angiotensin II.
These findings provide a new insight into the antiatherosclerotic properties of TSETT and provide a pharmacological basis for the clinical application of TSETT in anti-atherosclerosis.
7. Zhai, Fg., Li, HZ., Zhou, FB., Lin, F., Guan, LX. – Effects of saponins of Tribulus terrestris on PPARγ and NF-κB signaling pathways expression in rat brain following cerebral ischemic injury. Med Recapitulate (2015) 21: 4539.
Objective To study and explore the effect of tribulus terrestris on the expression of peroxisome proliferators γ( PPAR γ) and nuclear factor κB( NF-κB) inflammatory signaling pathways in rat brain tissue after focal cerebral ischemia,and further explore its potential mechanisms. Methods According to random number table method,40 SD rats were randomly equally divided into sham operation group,cerebral ischemia-reperfusion model group,low-dose saponins of tribulus terrestris group and high-dose saponins of tribulus terrestris group. Cerebral ischemia reperfusion model was established with suture emboli method in middle cerebral artery of rats. Neurological deficit scores was measured 24 hours after the cerebral reperfusion. Content of NF-κB,tumor necrosis factor-α( TNF-α) and interleukin-1β( IL-1β) in rat brain was detected by ELISA; expression levels of PPARγ protein in rat brain was determined by Western blot. Results Compared with the model group,nerve function injury of low dose tribulus terrestris saponin treatment group and high dose group obviously reduced( 1. 8 ± 0. 7) scores,( 1. 3 ± 0. 5) scores vs( 2. 3 ± 0. 7) scores,the difference was statistically significant( P 0. 05). NF-κB,TNF-α and IL-1 β level of low dose saponins of tribulus group ( 16. 4 ± 1. 3) μg / mg,( 257 ± 110) pg / mg,( 148 ± 16) pg / mgand high dose group( 15. 0 ± 1. 2) μg/mg,( 665 ± 72) pg/mg,( 139 ± 14) pg/mgwere lower than those of the model group( 18. 4 ± 1. 5) μg/mg,( 916 ± 128) pg/mg,( 169 ± 16) pg/mg( P 0. 05). Conclusion Saponins of tribulus terrestris exerts the neuroprotective effect on cerebral ischemia-reperfusion injury in rats through inhibiting the inflammatory reaction,which may be associated with the increase of the PPARγ protein expression and inhibition of NF-κB inflammation signal pathway.
8. Roaiah, M., El Khayat, Y., GamalEl Din, S. and Abd El Salam, M. – Pilot Study on the Effect of Botanical Medicine (Tribulus terrestris) on Serum Testosterone Level and Erectile Function in Aging Males With Partial Androgen Deficiency (PADAM). J Sex Marital Ther. (2016) 42: 297.
This study was conducted on 30 consecutive male patients presenting to Kasr-Al Ainy Andrology outpatient clinic complaining of manifestations of partial androgen deficiency in aging males (PADAM). In this study (750 mg/day) of Tribulus terrestris in 3 divided doses, each of 250 mg, as an endogenous testosterone enhancer had been tried for a duration of 3 months and the evaluation of its effect had been monitored for each patient concerning its effect on serum testosterone (total and free) and luteinizing hormone (LH), as well as its impact on erectile function, which was evaluated by the International Index of Erectile Function-5 (IIEF-5) questionnaire for those patients. Results showed a statistically significant difference in the level of testosterone (total and free) and IIEF-5, but no statistically significant difference in the level of LH before and after treatment. Also, the study showed statistically significant correlation between testosterone (total and free) and IIEF-5, but no statistically significant correlation between the level of LH and the IIEF-5 before and after treatment.
9. Mrinalini Kumari, Praveen Kumar and Poonam Singh – Safety Evaluation of Tribulus Terrestris on the Male Reproductive Health of Laboratory Mouse
Tribulus terrestris (TT) has emerged as an instant plant for the treatment of sexual dysfunctions and fertility related disorders in the males. The present study was aimed to assess the safety efficacy of the fruit extract of TT on the male reproduction. Animals of Group I served as control while that of II and III were administered with 100mg/kgBW/day and 200mg/kgBW/day of the fruit extract of TT, respectively, for 28 days. Testicular histology, sperm parameters, serum clinical biochemistry (SGOT, SGPT and creatinine) and tissue biochemistry (fructose in the seminal vesicle, sialic acid in the epididymis, antioxidant enzymes activity, LPO, LDH and ALP in the testis) were carried out to establish the safety of the fruit extract. Safety of the extract was evidenced by the unaltered body weight and serum clinical biochemistry. Administration of the fruit extract of TT neither interfered with the weights of the reproductive organs nor altered the sperm indices in the cauda epididymidis as well as the spermatogenic activity in the testis. The unaltered androgen - dependent biochemical markers i.e. sialic acid in the epididymis and fructose in the seminal vesicle indicated the normal status of the testosterone level. Unaltered activities of testicular antioxidant enzymes and the level of LPO suggest that the fruit extract does not cause oxidative stress. Further the unaltered activities of LDH and ALP in the testis represent normal physiological activity of the organ that could be correlated with the uninterrupted spermatogenic activity. It can, therefore, be concluded that the fruit extract of this herb could effectively be used as a natural remedy in treatment of male reproductive disorders without causing any side effects. ISSN
10. Dr. Pavleta Tabakova, Dr. Mitko Dimitrov, Dr. Bozihdar Tashkov (Head Physician), Director of Studies: (Prof. Dr. S. Dokumov) – Clinical treatment with Tribestan (Pharmachim) in women with climacteric syndrome
Climacterium is a complicated biological process with versatile symptoms associated with the gradual dying out of the hormonal activity of ovaries on the background of a general aging of the female organism.
Climacterium is a psychological process with duration from two to more years, most often at the age of 40-55. The visible manifestation is the cessation of menstruation - advancing of menopause. The initial period of gradual dying out of ovarian function, known as premenopause is with various duration in individual women.
A disorder of the cyclic activity of hypothalamic-hypophyseal axis with predomination of parasympathicus occurs on the background of age readjustment of the central nervous system. Various neuro-vegetative symptoms, neuro-psychic disorders, metabolic changes etc. are observed during climacterium. Hypothalamic reactivity is intensified leading to the increase of the production of hypophysiotropic hormones.
The ovulatory activity of ovaries declines and the receptive function versus hormones partially fades. The reduced production of ovarian hormones leads to a compensatory effect (growth) of gonadotrophic hormones. On its part, that however is the cause of hyperthyroidism, virilization, acromegalic manifestations etc.
The option of the research, based on the experience from the treatment of 50 patients with natural and postoperative climacterium during that experiment, as well as on the data from the previous pilot study on another 12 women with the same clinical picture is that Tribestan (Pharmachim) can successfully be used in the treatment of climacteric syndrome in females, both natural or postcastration. The absence of any adverse effects, the ready tolerance and its excellent effect makes it a desired agent for the treatment of all patients with similar complaints.
11. Akhtari, E., Raisi, F., Keshavarz, M., Hosseini, H., Sohrabvand, F., Bioos, S., Kamalinejad, M. and Ghobadi, A. – Tribulus terrestris for treatment of sexual dysfunction in women: randomized double-blind placebo - controlled study. Daru (2014) 22: 40.
Tribulus terrestris as a herbal remedy has shown beneficial aphrodisiac effects in a number of animal and human experiments. This study was designed as a randomized double-blind placebo-controlled trial to assess the safety and efficacy of Tribulus terrestris in women with hypoactive sexual desire disorder during their fertile years. Sixty seven women with hypoactive sexual desire disorder were randomly assigned to Tribulus terrestris extract (7.5 mg/day) or placebo for 4 weeks. Desire, arousal, lubrication, orgasm, satisfaction, and pain were measured at baseline and after 4 weeks after the end of the treatment by using the Female Sexual Function Index (FSFI). Two groups were compared by repeated measurement ANOVA test. Thirty women in placebo group and thirty women in drug group completed the study. At the end of the fourth week, patients in the Tribulus terrestris group had experienced significant improvement in their total FSFI (p < 0.001), desire (p < 0.001), arousal (p = 0.037), lubrication (p < 0.001), satisfaction (p < 0.001) and pain (p = 0.041) domains of FSFI. Frequency of side effects was similar between the two groups. Tribulus terrestris may safely and effectively improve desire in women with hypoactive sexual desire disorder. Further investigation of Tribulus terrestris in women is warranted.
12. de Souza, K., Vale, F. and Geber, S. – Efficacy of Tribulus terrestris for the treatment of hypoactive sexual desire disorder in postmenopausal women: a randomized, double-blinded, placebo-controlled trial. Menopause (2016) 23: 1252.
The objective of this study was to evaluate the efficacy of Tribulus terrestris for the treatment of hypoactive sexual desire disorder in postmenopausal women and evaluate its effect on the serum levels of testosterone.
We performed a prospective randomized, double-blinded, placebo-controlled study, during 18 months. A total of 45 healthy sexually active postmenopausal women reporting diminished libido were selected to participate in the study and were randomly assigned to receive 750 mg/d of T terrestris or placebo for 120 days. Randomization was performed using sealed envelopes. All participants answered the Female Sexual Function Index and the Sexual Quotient-female version questionnaires and had their serum levels of prolactin, thyroid-stimulating hormone, total testosterone, and sex hormone-binding globulin measured. A total of 36 participants completed the study, because 3 from each group were excluded due to side effects and 3 dropped out due to personal reasons. FSFI questionnaire results demonstrated an improvement in all domains in both groups (P < 0.05) except for lubrication which was improved only in the study group. QS-F results showed a significant improvement in the domains of desire (P < 0.01), arousal/lubrication (P = 0.02), pain (P = 0.02), and anorgasmia (P < 0.01) in women who used T terrestris, whereas no improvement was observed in the placebo group (P > 0.05). Moreover, free and bioavailable testosterone levels showed a significant increase in the T terrestris group (P < 0.05). Tribulus terrestris might be a safe alternative for the treatment of hypoactive sexual desire disorder in postmenopausal women, because it was effective in reducing symptoms with few side effects. Its probable mechanism of action involves an increase in the serum levels of free and bioavailable testosterone.
13. M. Ganzera1, e. bedir, i.a. khan – Determination of Steroidal Saponins in Tribulus terrestris by Reversed-Phase High-Performance Liquid Chromatography and Evaporative Light Scattering Detection, 2001 Wiley‐Liss, Inc. and the American Pharmaceutical Association J Pharm Sci 90:1752–1758, 2001.
This paper describes the first analytical method suitable for the determination of steroidal saponins in Tribulus terrestris. A separation by high performance liquid chromatography (HPLC) was achieved by using a reversed‐phase (RP‐18) column, evaporative light scattering (ELS) detection, and a water/acetonitrile gradient as the mobile phase. The marker compound, protodioscin, was detected at a concentration as low as 10.0 μg/mL. Several different samples of plant material were successfully analyzed, and depending on origin and plant part used for extraction, significant differences in the composition of the saponins were observed. The analysis of market products showed considerable variations of 0.17 to 6.49% in the protodioscin content.
14. Karimi Jashni, Malekzadeh Shiravani, Hoshmand – The effect of the Tribulus terrestris extract on spermatogenesis in the rat
According to our antecedents, in addition to other pharmacological properties, Tribulus terrestris
increases sexual functioning and libido in men. Due to the fact that the benefits of herbal drugs should be approved clinically in the laboratory, the present study aimed to investigate the effect of Tribulus terrestris extract on the primary spermatocyte in rat. Material and Methods: In this experimental study, thirty five mature male Wistar rats with average weight of 180 ± 10 g and age of 2-3 months were randomly divided into five groups of seven each. Group I served as a control and group II as a experiment group (normal saline, 2.5 ml) and groups III, IV and V were treated with three different doses of oral TT extract (2.5, 5 and 10 mg/kg body weight, respectively) once daily for 8 weeks. After the last treatment, the rats were sacrificed and their testis was removed, fixed and studied using light microscope. The data were analyzed using Anova.
The results of this study showed that the mean number of primary spermatocytes in the 3rd
experimental group (10 mg/kg/body) increased significantly compared with the control group
(P<0.01). But Tribulus terrestris extract had no effect on the mean number of primary spermatocytes in the other experimental groups.
The above results showed that Tribulus terrestris can probably balance the functions of the male
reproductive system and can be used in treatment of male infertility, while effecting the testis
15. Naveen Khatak & Pradeep Kumar Singh – Beneficial effect of aqueous extract of tribulus terrestris on serum glutamate pyruvic transaminase in albino rat
In recent times focus on plant research has increased all over the world and a large number of evidences have collected to show immense potential of medicinal plant used in various traditional system. More than 1300 plants have been studied during last ten-years period (Solecki, 1975). Seven of these are medicinal plants still used throughout the herbal world (Bensky and Gamble, 1993). The ancient cultures people methodically and scientifically collect information on herbs and developed well-defined herbal pharmacopoeias. Indeed swell into 20th century much of the pharmacopoeia of scientific medicine was derived from the herbal lore of native people. Many drugs including strychnine, aspirin, taxol, curare and ergot are of herbal origin. About one quarter of the prescription drugs dispensed by community pharmacies in the United States contain at least one active ingredient derived from the plant material (Farnsworth et al., 1985 and Acherknecht, 1973).
Tribulus terrestris has many medicinal uses. It has been a constituent in tonics in Indian Ayurveda practice, where it is known by its Sanskrit name “gokshura”. (MHFW, Government of India, 2001). It is also used as an aphrodisiac in Ayurveda. Some have compared the tonic properties of Tribulus terrestris to the effects of ginseng, but these occur due to entirely different mechanisms. Serum Glutamate Pyruvic Transaminase (SGPT) is the member of the transaminase family of enzymes. Transaminase referred to as transaminase amino trasnferases; facilitate mainly in the liver, catalyses the transfer of amino groups between L-alanine and glutamate to meet physiological needs. SGPT is found in large amounts in the liver and small amounts of this enzyme are found in the heart, muscle and kidney. When the liver is injured or inflamed, the levels of in the blood usually rise; therefore, this test is performed to check for signs of liver diseases. When body tissue or an organ such as the heart or liver is damaged, additional SGPT is released into the blood stream. The amount of SGPT in the blood is directly related to the extent of the tissue damage (Nicholas and Strevens, 2003 and De Ritis et al., 1972). Therefore, the aim of this present work is to examine the effect of the oral administration of aqueous extract of Tribulus terrestris on Serum Glutamate Pyruvic Transaminase in Albino rat (Rattus norvegicus).
16. K. Milasius, R. Dadeliene, Ju. Skernevicius – The influence of the Tribulus terrestris extract on the parameters of the functional preparadness and athletes’ organism homeostase
The influence of the Tribulus terrestris extract on the parameters of the functional preparadness and athletes. organism homeostase was investigated. It was established the positive impact of dietary supplement .Tribulus. (Optimum Nutrition, USA) using per 1 capsule 3 times a day during 20 days on athletes. physical power in various energy producing zones: anaerobic alactic muscular power and anaerobic alactic glycolytic power statistically reliable increased. Tribulus terrestris extract, after 20 days of consuming it, did not have essential effect on erythrocytes, haemoglobin and thrombocytes indices. During the experimental period statistically importantly increased percentage of granulocytes and decreased percentage of leucocytes show negative impact of this food supplement on changes of leucocytes formula in athletes. blood. Creatinkinase concentration in athletes. Blood statistically importantly has increased and creatinine amount has had a tendency to decline during 20 days period of consuming Tribulus terrestris extract. The declining tendency of urea, cholesterol and bilirubin concentrations has appeared. The concentration of blood testosterone increased statistically reliable during the first half (10 days) of the experiment; it did not grow during the next 10 days while consuming Tribulus still.
17. Jameel Mohd, Ansari Javed Akhtar, Ali Abuzer, Ahamad Javed, Ali M., Tamboli Ennus – Pharmacological scientific evidence for the promise of tribulus terrestris
The usage of plants, plant extracts or plant-derived pure chemicals for disease management, become a therapeutic modality, which has stood the test of time. In the present r eview, we focus on pharmacological profile (in tabular form) of Tribulus terrestris L., apart from Phytochemistry, Taxonomy and Traditional uses. Data were l ocated, selected and extracted from SCI database, Medline, Pubmed, Highwire a nd Google Scholar. Fruits and seeds of Tribulus terrestris L., (Zygophyllaceae) are of immense importance in oriental medicine because they are used as an aphrodisiac, diuretic and anthelmintic, as well as to treat coughs and kidney failure. Tribulus terrestris L. has reported to have antimicrobial, antihypertension, diuretic, antiacetylcholine, haemolytic activity, spermatogenesis
and libido enhancer, antitumor activity and effects on cardiovascular system. Furostanol and spirostanol saponins, flavonoid glycosides, alkaloids, steroidal saponins named terrestrosins A, B, C, D and E, F-gitonis, gitnin and amides have been reported to occur in Tribulus terrestris L. T raditionally T. terrestris is used in folk medicine a s a tonic, aphrodisiac, palliative, a stringent, stomachic, antihypertensive, diuretic, lithon-triptic, cordial drug and uri nary anti-infective. The ash of the whole plant is good for external application in rheumatic-arthritis.
18. Kokoska, L. and Janovska, D. – Chemistry and pharmacology of Rhaponticum carthamoides: A review. Phytochemistry (2009) 70: 842.
Rhaponticum carthamoides (Willd.) Iljin is a perennial herb, commonly known as a maral root or Russian leuzea, which has been used for centuries in eastern parts of Russia for its marked medicinal properties. This review based on 117 literary sources, with many of them being originally published in non-English languages (mainly in Russian), discusses the current knowledge of traditional uses, chemistry, biological effects and toxicity of this species. Several different classes of compounds were previously isolated from various parts of R. carthamoides of which the main groups are steroids, particularly ecdysteroids, and phenolics (flavonoids and phenolic acids) accompanied with polyacetylenes, sesquiterpene lactones, triterpenoid glycosides and terpenes (essential oil). A comprehensive account of the chemical constituents is given in this review (figures of 120 structures are shown). Various types of preparations, extracts and individual compounds derived from this species have been found to possess a broad spectrum of pharmacological effects on several organs such as the brain, blood, cardiovascular and nervous systems as well as on different biochemical processes and physiological functions including proteosynthesis, work capacity, reproduction, and sexual function. Moreover, the extracts and preparations from the plant, which are hopefully safe, exhibited various additional biological effects e.g. antioxidant, immunomodulatory, anticancerogenic, antimicrobial.
19. Gorelick-Feldman, J., MacLean, D., Ilic, N., Poulev, A., Lila, M., Cheng, D. and Raskin, I. – Phytoecdysteroids Increase Protein Synthesis in Skeletal Muscle Cells. J Agric Food Chem. (2008) 56: 3532.
Phytoecdysteroids, which are structurally similar or identical to insect molting hormones, produce a range of effects in mammals, including increasing growth and physical performance. To study the mechanism of action of phytoecdysteroids in mammalian tissue, an in vitro cellular assay of protein synthesis was developed. In C2C12 murine myotubes and human primary myotubes, phytoecdysteroids increased protein synthesis by up to 20%. In vivo, ecdysteroids increased rat grip strength. Ecdysteroid-containing plant extracts produced similar results. The effect was inhibited by a phosphoinositide kinase-3 inhibitor, which suggests a PI3K-mediated mechanism.
20. Wu, J., Gao, L., Shang, L., Wang, G., Wei, N., Chu, T., Chen, S., Zhang, Y., Huang, J., Wang, J. and Lin, R. – Ecdysterones from Rhaponticum carthamoides (Willd.) Iljin reduce hippocampal excitotoxic cell loss and upregulate mTOR signaling in rats. Fitoterapia (2017) 119: 158.
Glutamate-induced excitotoxicity is a key pathological mechanism in many neurological disease states. Ecdysterones derived from Rhaponticum carthamoides (Willd.) Iljin (RCI) have been shown to alleviate glutamate-induced neuronal damage; although their mechanism of action is unclear, some data suggest that they enhance signaling in the mechanistic target of rapamycin (mTOR) signaling pathway. This study sought to elucidate the mechanisms underlying ecdysterone-mediated neuroprotection. We used in silico target prediction and simulation methods to identify putative ecdysterone binding targets, and to specifically identify those that represent nodes where several neurodegenerative diseases converge. We then used histological analyses in a rat hippocampal excitotoxicity model to test the effectiveness of ecdysterones in vivo. We found that RCI-derived ecdysterones should bind to glutamatergic NMDA-type receptors (NMDARs); specifically, in vivo modeling showed binding to the GRIN2B subunit of NMDARs, which was found also to be a node of convergence in several neurodegenerative disease pathways. Computerized network construction by using pathway information from the Kyoto Encyclopedia of Genes and Genomes (KEGG) database showed putative links between GRIN2B and mTOR pathway elements including phosphoinositide-3kinase (PI3K), mTOR, and protein kinase C (PKC); these elements are associated with neuronal survival. Brain tissue western blots of ecdysterone-treated rats showed upregulated PI3K, Akt, mTOR, and phosphorylated Akt and mTOR, and down regulated GRIN2B and the apoptotic enzyme cleaved caspase-3. Ecdysterone treatment also prevented glutamate-induced rat hippocampal cell loss. In summary, RCI-derived ecdysterones appear to prevent glutamatergic excitotoxicity by increasing mTOR/Akt/PI3K signaling activity.
21. Toth, Noemi; Szabo, Andras; Kacsala, Peter; Heger, Julia; Zador, Erno – 20Hydroxyecdysone increases fiber size in a musclespecific fashion in rat.
20Hydroxyecdysone (20E) is an ecdysteroid hormone that regulates moulting in insects. Interestingly, 20E is also found most abundantly in plant species and has anabolic effects in vertebrates, i.e. increasing muscle size without androgen influence. The effect of 20E on slow and fast fiber types of skeletal muscle has not been reported yet. Here we present that 20E affects the size (crosssectional area, CSA) of the different fiber types in a musclespecific manner. The effect on fiber size was modified by the distance from the site of the treatment and the presence of a regenerating soleus muscle in the animal. Besides the fiber size, 20E also increased the myonuclear number in the fibers of normal and regenerating muscles, suggesting the activation of satellite cells. According to our results 20E may provide an alternative for substitution of anabolicandrogenic steroids in therapeutic treatments against muscle atrophy.
22. Chermnykh NS, Shimanovskiĭ NL, Shutko GV, Syrov VN – The action of methandrostenolone and ecdysterone on the physical endurance of animals and on protein metabolism in the skeletal muscles
The results of the comparative study on the myotropic activity of methandrostenolone and ecdysterone and their effects on physical endurance of animals suggested that ecdysterone possessing a wider spectrum of the anabolic action on the contractile proteins of the skeletal muscles exerts a more pronounced influence on physical endurance of animals without their preliminary training.
23. Pablo Kizelsztein, Dmitry Govorko, Slavko Komarnytsky, Alysa Evans, Zhong Wang, William T. Cefalu, and Ilya Raskin – 20-Hydroxyecdysone decreases weight and hyperglycemia in a diet-induced obesity mice model
The steroid hormone 20-hydroxyecdysone (20HE) is an essential signaling molecule that modulates molting response in insects and may function as a putative anabolic factor in vertebrate animals, although no mammalian 20HE receptor has been identified. Here we show that in H4IIE cell culture, 20HE treatment decreased expression of phosphoenolpyruvate carboxykinase (PEPCK) and glucose-6-phosphatase (G6Pase), reduced glucose production, and induced Akt2 phosphorylation sensitive to the phosphoinositide-3 kinase pathway-specific inhibitor LY-294002. Daily oral administration of 20HE (10 mg/kg for 13 wk) ameliorated obesity and insulin resistance in C57BL/6J mice fed a high-fat diet and produced a significant decrease of body weight gain and body fat mass compared with nontreated animals as demonstrated by dual-energy X-ray absorptiometry analysis. In addition, plasma insulin levels and glucose tolerance were significantly lowered by 20HE treatment. These changes were accompanied by the reduced hepatic expression of PEPCK and G6Pase and increased adiponectin production by visceral fat tissue. These studies demonstrate the anti-obesity and anti-diabetic effects of 20HE and begin to elucidate its putative cellular targets both in vitro and in vivo.
24. Jonathan Gorelick-Feldman, David MacLean, Nebojsa Ilic, Alexander Poulev, Mary Ann Lila, Diana Cheng and Ilya Raskin – Phytoecdysteroids Increase Protein Synthesis in Skeletal Muscle Cells
Phytoecdysteroids, which are structurally similar or identical to insect molting hormones, produce a range of effects in mammals, including increasing growth and physical performance. To study the mechanism of action of phytoecdysteroids in mammalian tissue, an in vitro cellular assay of protein synthesis was developed. In C2C12 murine myotubes and human primary myotubes, phytoecdysteroids increased protein synthesis by up to 20%. In vivo, ecdysteroids increased rat grip strength. Ecdysteroid-containing plant extracts produced similar results. The effect was inhibited by a phosphoinositide kinase-3 inhibitor, which suggests a PI3K-mediated mechanism.
25. Donald Yance, CN, AHG, SFO – Rhaponticum carthamoides
Rhaponticum carthamoides (Willd.) Iljin, syn. Leuzea carthamoides (Willd.) DC, is a largeperennial herb in the Compositae family. R. carthamoides has a wood-like horizontal rhizome, multiple long, hard roots, and is capable of growing to a height of over 6 feet. R. carthamoides grows in the pristine alpine and subalpine zones and alpine meadows of Southern Siberia. The roots and rhizomes are the medicinal parts, with the biological activity determined by phytoecdystone quantity, including ecdysterone.
This herb is a hidden jewel. R. carthamoides extract (RCE) has demonstrated a normalizing effect on the central nervous and cardiovascular systems. RCE improves sleep, appetite, moods, mental and physical state, and the functional ability of humans under working conditions. It is a classic adaptogen possessing a wide spectrum of anabolic activities, acting on the contractile proteins of the skeletal muscles, as well as on other areas of the body including the liver, heart, kidneys, and brain. It builds lean muscle, reduces body fat, improves work and/or athletic performance, improves mental acuity, relieves depression, is a tonic for the vital organ systems, is a reliable blood- building tonic, and delays the effects of aging. It is useful for both andropause and menopause.
26. R. Lafont and L. Dinan – Practical uses for ecdysteroids in mammals including humans: and update
Ecdysteroids are widely used as inducers for gene-switch systems based on insect ecdysteroid receptors and genes of interest placed under the control of ecdysteroid-response elements. We review here these systems, which are currently mainly used in vitro with cultured cells in order to analyse the role of a wide array of genes, but which are expected to represent the basis for future gene therapy strategies. Such developments raise several questions, which are addressed in detail.
First, the metabolic fate of ecdysteroids in mammals, including humans, is only poorly known, and the rapid catabolism of ecdysteroids may impede their use as in vivo inducers.
A second set of questions arose in fact much earlier with the pioneering “heterophylic” studies of Burdette in the early sixties on the pharmacological effects of ecdysteroids on mammals. These and subsequent studies showed a wide range of effects, most of them being beneficial for the organism (e.g. hypoglycaemic, hypocholesterolaemic, anabolic). These effects are reviewed and critically analysed, and some hypotheses are proposed to explain the putative mechanisms involved.
All of these pharmacological effects have led to the development of a wide array of ecdysteroid-containing preparations, which are primarily used for their anabolic and/or “adaptogenic” properties on humans (or horses or dogs). In the same way, increasing numbers of patents have been deposited concerning various beneficial effects of ecdysteroids in many medical or cosmetic domains, which make ecdysteroids very attractive candidates for several practical uses.
It may be questioned whether all these pharmacological actions are compatible with the development of ecdysteroid-inducible gene switches for gene therapy, and also if ecdysteroids should be classified among doping substances.
27. David Winston, Steven Maimes – Adaptogens: Herbs for Strength, Stamina, and Stress Relief
The definitive guide to adaptogenic herbs, formerly known as “tonics,” that counter the effects of age and stress on the body.
Reveals how adaptogens increase the body’s resistance to adverse influences
Provides a history of the use of these herbal remedies and the actions, properties, preparation, and dosage for each herb
We all deal with stress every day, and every day our bodies strive to adapt and stay balanced and healthy. In Adaptogens, authors David Winston and Steven Maimes provide a comprehensive look into adaptogens, non-toxic herbs such as ginseng, eleuthero, and licorice, that produce a defensive response to stress in our bodies. Formerly known as rejuvenating herbs or tonics, adaptogens help the body to “adapt” to the many influences it encounters. They increase stamina and counter the normal effects of aging and thus are becoming important tools in sports medicine and in the prevention and treatment of chronic fatigue and other stress-related disorders.
Winston and Maimes present the historical uses of these herbal remedies in India, Russia, China, and the Americas and explain how they work and why they are so effective at combating stress-induced illness. Monographs for each adaptogen also present the latest scientific research and include the origin, traditional use, actions, properties, preparation, and dosage for each herb.
28. Gadzhieva, RM, Portugalov, SN, Paniushkin, VV, Kondrat'eva II. – A comparative study of the anabolic action of ecdysten, leveton and Prime Plus, preparations of plant origin Eksp Klin Farmakol. (1995) 58: 46.
A new class of anabolic substances includes different saponins, originated from Leuzea rhaponticum sp. The effect of these substances on the human body was studied by caliperometric measurements of body folds. All tested substances taken orally for three weeks diminished fat content under conditions of daily aerobic-anaerobic training. Ekdisten and Prime Plus (combination of ekdisten and pure protein) elevated the muscle mass. The same effect of leventon was less pronounced. We showed that all substances studied elevated the magnitude of "total work", estimated per 1 kg of body weight. Ekdisten and Prime Plus again appeared to be most efficient. The prospects of using the saponins in sport medicine are discussed.
29. Syrov, VA, Kurmukov, AG. – On the anabolic activity of phytoecdisone-ecdisterone extracted from Rhaponticum carthamoides. Farmakol Toksikol. (1976) 39: 690.
Introduction of phytiexdizone-exdisterone (0.5 mg/100 g) to rats for 7 days is shown to be attended by an accelerated body weight gain and also by a rising weight of the liver, heart, kidneys and musculus tibialis anterior. In these organs the total amount of protein increases. All of the above-stated changes are more marked when the substance is given to growing rats (70--80 g). In experiments on castrated sexually immature rats the androgenic action of exdisterone, unlike that of methandrostenolone, is not demonstrable.
30. Ladislav Kokoska, Dagmar Janovska – Chemistry and pharmacology of Rhaponticum carthamoides: A review
Rhaponticum carthamoides (Willd.) Iljin is a perennial herb, commonly known as a maral root or Russian leuzea, which has been used for centuries in eastern parts of Russia for its marked medicinal properties. This review based on 117 literary sources, with many of them being originally published in non-English languages (mainly in Russian), discusses the current knowledge of traditional uses, chemistry, biological effects and toxicity of this species. Several different classes of compounds were previously isolated from various parts of R. carthamoides of which the main groups are steroids, particularly ecdysteroids, and phenolics (flavonoids and phenolic acids) accompanied with polyacetylenes, sesquiterpene lactones, triterpenoid glycosides and terpenes (essential oil). A comprehensive account of the chemical constituents is given in this review (figures of 120 structures are shown). Various types of preparations, extracts and individual compounds derived from this species have been found to possess a broad spectrum of pharmacological effects on several organs such as the brain, blood, cardiovascular and nervous systems as well as on different biochemical processes and physiological functions including proteosynthesis, work capacity, reproduction, and sexual function. Moreover, the extracts and preparations from the plant, which are hopefully safe, exhibited various additional biological effects e.g. antioxidant, immunomodulatory, anticancerogenic, antimicrobial, antiparasitic and insect antifeedant or repellent activities. The results of data analysis on the chemical, pharmacological and toxicological characteristics of R. carthamoides support the view that this species has beneficial therapeutic properties and indicate its potential as an effective adaptogenic herbal remedy. Finally, some suggestions for further research on chemical and pharmacological properties are given in this review.
31. Zhang, Xue – Effect of Western medicine therapy assisted by Ginkgo biloba tablet on vascular cognitive impairment of none dementia.
To discuss the clinical effects of Western medicine therapy assisted by Ginkgo biloba tablet (GBT) on patients with vascular cognitive impairment of none dementia (VCIND).
A total of 80 patients with VCIND were divided into two groups randomly: Conventional treatment group (control group) and combined treatment group. Conventional treatment group was given conventional treatment with anti-platelet aggregation. In this group, 75 mg aspirin was given three times a day for 3 months. While in combined treatment group, 19.2 mg GBT was given three times a day for 3 months together with conventional treatment (anti-platelet aggregation drugs). Montreal cognitive assessment (MoCA) and transcranial Doppler (TCD) were used to observe changes of cognitive ability and cerebral blood flow in VCIND patients before and after treatment in both groups. Then the clinical data were analyzed so as to compare the efficacy in two groups.
After 3 month-treatment in combined treatment group, the scores of executive ability, attention, abstract, delayed memory, orientation in the MoCA were significantly increased compared with those before treatment and those in control group after treatment. Besides, blood flow velocity of anterior cerebral artery increased significantly than that before treatment and that in control group after treatment.
GBT tablet can improve the therapeutic efficacy as well improve cognitive ability and cerebral blood flow supply of patients with VCIND.
32. Santos, Galduróz, Barbieri, Castiglioni, Ytaya, Bueno – Cognitive performance, SPECT, and blood viscosity in elderly non-demented people using Ginkgo biloba.
The aging process is associated with several cognitive alterations. This study looks at the effects of taking dried extract of Ginkgo biloba, which has been used in several countries in an attempt to minimize these effects. The subjects were 48 men aged 60 - 70 matched between control and experimental groups for educational level. Evaluation was based on a number of neuropsychological tests in an attempt to cover the largest possible number of functions including Single Photon Emission Computer Tomography (SPECT) and measures of blood viscosity. The study was run on a double-blind basis with placebo and Ginkgo biloba groups evaluated over a period of 8 months. After treatment, the experimental group showed a reduction in blood viscosity, improved cerebral perfusion in specific areas and improved global cognitive functioning. The control group showed the opposite - higher blood viscosity, a reduction in cerebral perfusion (in specific areas), and cognitive deterioration in different functions. Although the mechanisms by which Ginkgo biloba may contribute to overall enhancement of the parameters evaluated have not been specified, this plant extract certainly appears to be effective in the treatment of cognitive deficits in older people. Further research into its use is called for on the basis of the results obtained here.
33. J. Klein, O. Weichel , M. Hilgert , J. Rupp, S. S. Chatterjee , H. Nawrath – Excitotoxic Hippocampal Membrane Breakdown and its Inhibition by Bilobalide: Role of Chloride Fluxes
We have previously shown that hypoxia and N-methyl-D-aspartate (NMDA) receptor activation induce breakdown of choline-containing phospholipids in rat hippocampus, a process which is mediated by calcium influx and phospholipase A2activation. Bilobalide, a constituent of Ginkgo biloba, inhibited this process in a potent manner (Weichel et al., Naunyn-Schmiedeberg’s Arch. Pharmacol. 360, 609 - 615, 1999). In this study, we used fluorescence microscopy and radioactive flux measurements to show that bilobalide does not interfere with NMDA-induced calcium influx. Instead, bilobalide seems to inhibit NMDA-induced fluxes of chloride ions through ligand-operated chloride channels. In our experiments, substitution of chloride in the superfusion medium fully blocked the effect of NMDA on choline release from hippocampal slices, while the presence of chloride transport inhibitors (furosemide, DIDS) was partially antagonistic. The inhibitory effect of bilobalide and of HA-966, a glycine B receptor antagonist, on NMDA-induced choline release was attenuated in the presence of glycine. The inhibitory effect of bilobalide, but not that of HA-966, was also antagonized by GABA. The inhibitory effect of MK-801, an NMDA channel blocker, on choline release was insensitive to glycine. We conclude from our findings that bilobalide inhibits an NMDA-induced chloride flux through glycine/GABA-operated channels, thereby preventing NMDA-induced breakdown of membrane phospholipids. This effect is expected to contribute to the neuroprotective effects of ginkgo biloba extracts.
34. Yoshitake, Yoshitake, Kehr – The Ginkgo biloba extract EGb 761(R) and its main constituent flavonoids and ginkgolides increase extracellular dopamine levels in the rat prefrontal cortex.
BACKGROUND AND PURPOSE:
Experimental and clinical data suggest that extracts of Ginkgo biloba improve cognitive function. However, the neurochemical correlates of these effects are not yet fully clarified. The purpose of this study was to examine the effects of acute and repeated oral administration of the standardized extract EGb 761((R)) on extracellular levels of dopamine, noradrenaline and serotonin (5-HT), and the dopamine metabolites 3,4-dihydroxyphenylacetic acid (DOPAC) and homovanillic acid (HVA) in the prefrontal cortex (PFC) and striatum of conscious rats.
Monoamines and their metabolites were monitored by the use of microdialysis sampling and HPLC with electrochemical or fluorescence detection.
A single oral dose of EGb 761 (100 mg.kg(-1)) had no effect on monoamine levels. However, following chronic (100 mg.kg(-1)/14 days/once daily) treatment, the same dose significantly increased extracellular dopamine and noradrenaline levels, while 5-HT levels were unaffected. Chronic treatment with EGb 761 showed dose-dependent increases in frontocortical dopamine levels and, to a lesser extent, in the striatum. The extracellular levels of HVA and DOPAC were not affected by either acute or repeated doses. Treatment with the main constituents of EGb 761 revealed that the increase in dopamine levels was mostly caused by the flavonol glycosides and ginkgolide fractions, whereas bilobalide treatment was without effect.
CONCLUSIONS AND IMPLICATIONS:
The present results demonstrate that chronic but not acute treatment with EGb 761 increased dopaminergic transmission in the PFC. This finding may be one of the mechanisms underlying the reported effects of G. biloba in improving cognitive function.
35. Helene Amieva, Celine Meillon, Catherine Helmer, Pascale Barberger-Gateau, Jean Franc¸ois Dartigues – Ginkgo Biloba Extract and Long-Term Cognitive Decline:A 20-Year Follow-Up Population-Based Study
Numerous studies have looked at the potential benefits of various nootropic drugs such as Ginkgo biloba extract (EGb761®; Tanakan®) and piracetam (Nootropyl®) on age-related cognitive decline often leading to inconclusive results due to small sample sizes or insufficient follow-up duration. The present study assesses the association between intake of EGb761® and cognitive function of elderly adults over a 20-year period.
METHODS AND FINDINGS:
The data were gathered from the prospective community-based cohort study 'Paquid'. Within the study sample of 3612 non-demented participants aged 65 and over at baseline, three groups were compared: 589 subjects reporting use of EGb761® at at least one of the ten assessment visits, 149 subjects reporting use of piracetam at one of the assessment visits and 2874 subjects not reporting use of either EGb761® or piracetam. Decline on MMSE, verbal fluency and visual memory over the 20-year follow-up was analysed with a multivariate mixed linear effects model. A significant difference in MMSE decline over the 20-year follow-up was observed in the EGb761® and piracetam treatment groups compared to the 'neither treatment' group. These effects were in opposite directions: the EGb761® group declined less rapidly than the 'neither treatment' group, whereas the piracetam group declined more rapidly (β = -0.6). Regarding verbal fluency and visual memory, no difference was observed between the EGb761® group and the 'neither treatment' group (respectively, β = 0.21 and β = -0.03), whereas the piracetam group declined more rapidly (respectively, β = -1.40 and β = -0.44). When comparing the EGb761® and piracetam groups directly, a different decline was observed for the three tests (respectively β = -1.07, β = -1.61 and β = -0.41).
Cognitive decline in a non-demented elderly population was lower in subjects who reported using EGb761® than in those who did not. This effect may be a specific medication effect of EGb761®, since it was not observed for another nootropic medication, piracetam.
Ginkgo (Ginkgo biloba) is one of the oldest living tree species. It is also one of the best-selling herbal supplements in the United States and Europe.
Ginkgo has a long history of use in treating blood disorders and memory issues. It is best known today as way to potentially keep your memory sharp. Laboratory studies have shown that ginkgo improves blood circulation by opening up blood vessels and making blood less sticky. It is also an antioxidant.
For those reasons, ginkgo may improve vein and eye health. Although not all studies agree, ginkgo may help treat dementia (including Alzheimer disease) and intermittent claudication, or poor circulation in the legs. It may also protect memory in older adults.
Ginkgo leaves contain flavonoids and terpenoids, which are both antioxidants. In your body, harmful particles called free radicals build up as you age, and may contribute to heart disease, cancer, and Alzheimer disease. Antioxidants like those found in ginkgo fight off free radicals, and stop them from damaging DNA and other cells.
37. Kennedy, Scholey, Wesnes – Modulation of cognition and mood following administration of single doses of Ginkgo biloba, ginseng, and a ginkgo/ginseng combination to healthy young adults.
It has previously been demonstrated in separate studies that single doses of Ginkgo biloba, Panax ginseng, and a combination of the two extracts can improve different aspects of cognitive performance in healthy young volunteers. The present study directly compared the effects of single doses of G. biloba, ginseng, and a product combining the two on aspects of mood and cognitive performance in the same cohort of healthy, young adult volunteers. The study followed a randomised placebo-controlled, double-blind, balanced, cross-over design. Twenty participants received 360 mg of ginkgo, 400 mg of ginseng, 960 mg of a product combining the two extracts, and a matching placebo. Treatment order was dictated by random allocation to a Latin square, with a 7-day wash-out period between treatments. Cognitive testing comprised completion of the Cognitive Drug Research (CDR) computerised assessment battery and two serial subtraction mental arithmetic tasks. Mood was assessed with Bond-Lader visual analogue scales. Following a baseline cognitive assessment, further test sessions took place 1, 2.5, 4, and 6 h after the day's treatment was taken. The results largely supported previous findings. All three treatments were associated with improved secondary memory performance on the CDR battery, with the ginseng condition evincing some improvement in the speed of performing memory tasks and in the accuracy of attentional tasks. Following ginkgo and the ginkgo/ginseng combination performance of both the Serial Threes and Serial Sevens, subtraction tasks was also improved at the later testing sessions. No modulation of the speed of performing attention tasks was evident. Improvements in self-rated mood was also found following ginkgo and to a lesser extent the combination product.
38. Hemmeter, Annen, Bischof, Brüderlin, Hatzinger, Rose, Holsboer-Trachsler. – Polysomnographic effects of adjuvant ginkgo biloba therapy in patients with major depression medicated with trimipramine.
Sleep disturbance and cognitive impairment are frequent complaints of depressed patients under standard antidepressant medication. Therefore, additional therapies are required which specifically focus on the improvement of these deficits without exerting major side effects. Ginkgo biloba extract (EGb) has been shown to improve cognitive abilities in elderly subjects and in patients with disorders of the dementia spectrum. Animal studies surmise that EGb may reduce CRH activity, which is substantially related to depressive mood and behavior, predominantly cognition and sleep. An open non-randomized pilot study has been conducted to investigate the effects of ginkgo biloba extract (EGb Li 1370) on cognitive performance and sleep regulation in depressed inpatients. 16 patients were treated with a trimipramine (T)-monotherapy (200 mg) for six weeks. In eight of the 16 patients, an adjunct EGb therapy (240 mg/d) was applied for four weeks after a baseline week, the other eight patients remained on trimipramine monotherapy (200 mg) during the entire study. Polysomnography, cognitive psychomotor performance and psychopathology were assessed at baseline, after short-term and long-term adjunct EGb treatment, and after one week of ginkgo discontinuation (at the respective evaluation times in the eight patients on T-monotherapy). This report focuses on the results of EGb on sleep EEG pattern. EGb significantly improved sleep pattern by an increase of sleep efficiency and a reduction of awakenings. In addition, sleep stage 1 and REM-density were reduced, while stage 2 was increased. Non-REM sleep, predominantly slow wave sleep in the first sleep cycle, was significantly enhanced compared to trimipramine monotherapy. Discontinuation of EGb reversed most of these effects. Based on the animal data, these results suggest that EGb may improve sleep continuity and enhance Non-REM sleep due to a weakening of tonic CRH-activity. The compensation of the deficient Non-REM component in depression by the EGb application may provide a new additional treatment strategy, especially in the treatment of the depressive syndrome with sleep disturbance.
39. Woelk, Arnoldt, Kieser, Hoerr – Ginkgo biloba special extract EGb 761 in generalized anxiety disorder and adjustment disorder with anxious mood: a randomized, double-blind, placebo-controlled trial.
Ginkgo biloba special extract EGb 761, an anti-dementia drug, enhances cognitive functioning and stabilizes mood in cognitively impaired elderly subjects. Moreover, EGb 761 had been found to alleviate symptoms of anxiety in people with mental decline, therefore it was now tested for clinical efficacy in younger patients suffering from anxiety. One hundred and seven patients with generalized anxiety disorder (GAD, n=82) or adjustment disorder with anxious mood (ADWAM, n=25) according to the diagnostic and statistical manual of mental disorders, third edition - revised (DSM-III-R) were randomized to daily doses of 480 mg EGb 761, 240 mg EGb 761 or placebo for 4 weeks. Intention-to-treat (ITT) analyses were performed on the primary outcome measure, the Hamilton rating scale for anxiety (HAMA), and the secondary variables, the clinical global impression of change (CGI-C), the Erlangen anxiety tension and aggression scale (EAAS), the list of complaints (B-L'), and the patient's global rating of change. The HAMA total scores decreased by -14.3 (+/-8.1), -12.1 (+/-9.0) and -7.8 (+/-9.2) in the high-dose EGb 761, the low-dose EGb 761 and the placebo group, respectively. Changes were significantly different from placebo for both treatment groups with p=0.0003 (high-dose group) and p=0.01 (low-dose). Regression analyses revealed a dose-response trend (p=0.003). EGb 761 was significantly superior to placebo on all secondary outcome measures. It was safe and well tolerated and may thus be of particular value in elderly patients with anxiety related to cognitive decline.
40. L-Arginine/Korean Ginseng/Ginkgo biloba/Damiana-Based Supplement
An amino acid and herbal supplement with libido-enhancing activity. L-arginine/Korean ginseng/Ginkgo biloba/Damiana-based supplement contains a blend of the amino acid L-arginine and the herbs Korean ginseng, Ginkgo biloba, and damiana (Turnera aphrodisiaca) in addition to 14 other vitamins and minerals. The semi-essential amino acid L-arginine is a precursor for nitric oxide (NO); Korean ginseng may enhance the conversion of L-arginine into NO by NO synthase; and Ginkgo biloba may promote microvascular circulation. This agent may increase NO production, resulting in vasodilatation and an enhanced circulation critical to sexual function and arousal. The damiana component may exert an anxiolytic effect and stimulate sexual behavior.
41. Butt, M., Pasha, I., Sultan, M., Randhawa, M., Saeed, F. and Ahmed, W. – Black Pepper and Health Claims: A Comprehensive Treatise. Critical Reviews in Food Science and Nutrition (2013) 53: 875.
For millennia, spices have been an integral part of human diets and commerce. Recently, the widespread recognition of diet-health linkages bolsters their dietary importance. The bioactive components present in them are of considerable significance owing to their therapeutic potential against various ailments. They provide physiological benefits or prevent chronic ailment in addition to the fundamental nutrition and often included in the category of functional foods. Black pepper (Piper Nigrum L.) is an important healthy food owing to its antioxidant, antimicrobial potential and gastro-protective modules. Black pepper, with piperine as an active ingredient, holds rich phytochemistry that also includes volatile oil, oleoresins, and alkaloids. More recently, cell-culture studies and animal modeling predicted the role of black pepper against number of maladies. The free-radical scavenging activity of black pepper and its active ingredients might be helpful in chemoprevention and controlling progression of tumor growth. Additionally, the key alkaloid components of Piper Nigrum, that is, piperine assist in cognitive brain functioning, boost nutrient's absorption and improve gastrointestinal functionality. In this comprehensive treatise, efforts are made to elucidate the antioxidant, antimicrobial, anti-inflammatory, gastro-protective, and antidepressant activities of black pepper. Moreover, the synergistic interaction of black pepper with different drugs and nutrients is the limelight of the manuscript. However, the aforementioned health-promoting benefits associated with black pepper are proven in animal modeling. Thus, there is a need to conduct controlled randomized trials in human subjects, cohort studies, and meta-analyses. Such future studies would be helpful in recommending its application in diet-based regimens to prevent various ailments.
42. Tsuboi, T., Maeda, M. and Hayashi, T. – Administration of L-arginine plus L-citrulline or L-citrulline alone successfully retarded endothelial senescence. PLOS ONE (2018) 13: p.e0192252.
L-citrulline and L-arginine supplementation has been shown to have several beneficial effects on the cardiovascular system. Nitric oxide (NO) protects against the progression of atherosclerosis and is synthesized by nitric oxide synthase (NOS), which converts L-arginine (L-Arg) into L-citrulline (L-Cit). Our previous study revealed that chronic administration of a combination of L-Cit and L- Arg has a better therapeutic effect on high cholesterol-induced atherosclerosis in rabbits. We investigated how L-Arg and L-Cit affect endothelial function, aging and atherosclerosis. Following a 3-day stimulation of human umbilical venous endothelial cells (HUVECs) with high glucose (HG: 22 mM) and L-Arg (300 μM), L-Cit (300 μM) or L-Arg plus L-Cit (LALC: each 150 μM) supplementation, endothelial senescence and function were evaluated. These amino acids were also administered to dyslipidemic type 2 diabetic (ZDFM) rats fed a high cholesterol diet. They were fed L-Arg or L-Cit or LALC for four weeks. Aortic senescence was investigated by measuring senescence-associated ß-galactosidase (SA-ß-gal), telomerase activity, DNA damage and p16INK4a protein expression. Only L-Cit and LALC supplementation retarded the HG-induced endothelial senescence, as evaluated by SA-ß-gal activity, a widely used marker of cellular senescence, p16INK4a expression, a senescence-related protein, and DNA damage. Under HG conditions, L-Cit and LCLA restored telomerase activity to levels observed under normal glucose (NG) conditions. Under HG conditions, L-Cit decreased ROS production, as measured by CM-H2DCFDA and the expression of p67phox, a major component of NADPH oxidase. Under HG conditions, L-Cit and LALC increased NO production, as measured by DAF-2AM. Endothelial NO synthase (eNOS) and phosphorylated eNOS were decreased under HG conditions and L-Cit and LALC significantly increased these levels. Arginase 2 protein expression increased under the HG conditions, and L-Cit and LALC significantly attenuated this effect. In ZDFM rats, SA-ß-gal activity was detected on the aortic endothelial surface; however, L-Cit and LALC reduced these levels. L-Cit and LALC both decreased the proportion of senescent cells. Furthermore, treatment with LALC for 4 weeks increased plasma NO production. Therefore conclusively, L-citrulline supplementation rescued NO levels better than L-arginine supplementation by inhibiting ROS production and arginase 2 protein expression. Consequently, L-Cit and LCLA supplementation retaeded HG-induced endothelial senescence.
43. Smeets, E., Schutzler, S., Wei, J., Azhar, G. and Wolfe, R. – Do anabolic nutritional supplements stimulate human growth hormone secretion in elderly women with heart failure? Physiological Reports (2017) 5: p.e13366.
Growth hormone treatment has gained attention over the past decade as a treatment for heart failure. Human growth hormone (HGH) must be administered by injections (usually daily), so there is considerable advantage to stimulation of endogenous secretion by amino acid-based nutritional supplementation. However, studies investigating the effect of amino acid (AA) supplementation show conflicting results. Therefore, in this study we aimed to investigate the effect of nutritional supplementation on HGH production in elderly women with heart failure. Eight elderly women with heart failure participated in this randomized cross-over study. Plasma HGH concentration was measured before and for 4 h following ingestion of a mixture of protein, carbohydrate, and fat or an AA beverage. HGH concentration was determined with ELISA kits and AA concentrations were analyzed by Liquid Chromatography-Mass Spectrometry (LCMS). Linear mixed models was performed to analyze the effect of time, treatment, and interaction. Plasma arginine and lysine concentrations were significantly higher after consumption of the AA drink compared to the mixture of protein, carbohydrate, and fat. Nonetheless, only ingestion of the protein, carbohydrate, and fat mixture (meal replacement) increased HGH concentration. HGH concentration was increased in elderly women with heart failure following consumption of a meal replacement containing protein, carbohydrate, and fat. Consumption of a mixture of amino acids failed to increase HGH concentration despite significantly greater elevations in plasma amino acid concentrations, including arginine and lysine. The stimulatory effect of the protein/carbohydrate/fat mixture was presumably mediated by factors other than increases in free amino acid concentrations.
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