VemoHerb Guggulsterone

21.80 

Description

Supports the metabolism and fat burning process naturally. *

Dietary supplement, based on dry extract from Commiphora mukul (Guggul) standardized at 35 mg Guggulsteroids and 35 mg Е&Z Guggulsterones.

Guggulsterones are plant steroids, which are found in the resin of the plant Commiphora mukul (common also as Guggul). This powerful ancient herb has recently been re-discovered by the nowadays modern Western culture.

How and Why It Works?

Guggulsterones have been used for thousands of years to help maintain normal metabolism, and to support fat loss and normal cholesterol levels, without side effects.* [1-3]

Scientific studies indicate that Guggulsterones support the reduction of bodyweight and this is mostly attributed to the positive effect which they have on the normal function of thyroid gland, responsible for controlling the metabolic rate.* [4] When the hormone levels of the thyroid increase, the metabolic rate is boosted, and vice versa. Following that mechanism, when a caloric restriction is present due to a lower food intake (as it occurs during weight loss diets), the defensive reaction of the body is to decrease the metabolism rate by lowering the thyroid hormone levels. It is a well-known fact that when you eat less than you need for basic biological function, your body slows down your metabolism in order to keep its reserves for longer time. For example, you normally need 2000 kcal per day, but once you start diet you take 1000 kcal in order to lose weight. However, your clever organism compensates that scarcity and as the metabolism is slowed down, your body is now satisfied with 1000 kcal (and not with 2000 kcal). That means once you start eating normally (2000 kcal) it is already too much for your organism, and it quickly gains back the weight you lost during the diet. [5] In such cases during diets, the role of VemoHerb® Guggulsterone is to ensure that the metabolism stays at normal levels, despite the calorie decrease.* [6] Hence, they promote the weight loss program for the maximum desirable effect.* This is the most healthy and safe way to lose weight.*

Some studies also suggest that Guggulsterones help in maintaining the normal balance of HDL (good cholesterol) and LDL (bad cholesterol), adding extra benefits to the magnificent properties of this incredible herb.* [1, 3, 7]

Recommended for:

Guggulsterones are a perfect supplement for anyone who is looking for a safe and effective way of supporting the weight loss process, especially in cases of prolonged dieting.* [8, 9, 10, 11] Guggulsterones do not affect negatively the normal functions of the central nervous and the cardiovascular systems, and some studies suggest that they can support them.* [12, 13] Thus, they are generally considered as one of the safest available weight loss supplements on the market.* [9, 14] Guggulsterones influence positively the thyroid gland’s activity, and in that way assist the regulation of the metabolic rate in a natural way.* They support the weight loss rate, since more calories are burned by the body everyday.* [6, 8-11]

VemoHerb® Guggulsterone is based on one of the most potent natural Guggul extracts available today, thus ensuring the premium quality of the product and the cutting edge results of our customers.

The pack contains

90 capsules

Active substances in one capsule

350 mg dry extract from Commifora mukul (Guggul) standardized at 35 mg Guggulsteroids and 35 mg Е&Z Guggulsterones

Recommended daily dose

1 – 2 capsules, 3 times a day

Directions for use

Take the capsule between the meals or as directed on the label

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! Not recommended for people who have functional problems with their thyroid gland.

Some scientific evidence suggests

Other scientific studies suggest that Commiphora mukul extract is one effective tool for weight loss, when applied along with low calorie diets. [6, 8, 9, 10, 11] Guggulsterones have been reported to have inhibiting effect on fat cells and assist the regulated fats accumulation. [11, 15]

Other scientific studies [16 – 21]

These evidences are limited and not conclusive.

 

References

1. Yu BZ, Kaimal R, Bai S, El Sayed KA, Tatulian SA, Apitz RJ, Jain MK, Deng R, Berg OG – Effect of guggulsterone and cembranoids of Commiphora mukul on pancreatic phospholipase A(2): role in hypocholesterolemia.

Guggulsterone (7) and cembranoids (8-12) from Commiphora mukul stem bark resin guggul were shown to be specific modulators of two independent sites that are also modulated by bile salts (1-6) to control cholesterol absorption and catabolism. Guggulsterone (7) antagonized the chenodeoxycholic acid (3)-activated nuclear farnesoid X receptor (FXR), which regulates cholesterol metabolism in the liver. The cembranoids did not show a noticeable effect on FXR, but lowered the cholate (1)-activated rate of human pancreatic IB phospholipase A2 (hPLA2), which controls gastrointestinal absorption of fat and cholesterol. Analysis of the data using a kinetic model has suggested an allosteric mechanism for the rate increase of hPLA2 by cholate and also for the rate-lowering effect by certain bile salts or cembranoids on the cholate-activated hPLA2 hydrolysis of phosphatidylcholine vesicles. The allosteric inhibition of PLA2 by certain bile salts and cembranoids showed some structural specificity. Biophysical studies also showed specific interaction of the bile salts with the interface-bound cholate-activated PLA2. Since cholesterol homeostasis in mammals is regulated by FXR in the liver for metabolism and by PLA2 in the intestine for absorption, modulation of PLA2 and FXR by bile acids and selected guggul components suggests novel possibilities for hypolipidemic and hypocholesterolemic therapies.

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2. Yamada T, Sugimoto K – Guggulsterone and Its Role in Chronic Diseases.

Guggulsterone is a plant sterol derived from gum resin of Commiphora wightii. The gum resin from guggul plants has been used for thousand years in Ayurveda to treat various disorders, including internal tumors, obesity, liver disorders, malignant sores and ulcers, urinary complaints, intestinal worms, leucoderma, sinuses, edema, and sudden paralytic seizures. Guggulsterone has been identified a bioactive components of this gum resin. This plant steroid has been reported to work as an antagonist of certain nuclear receptors, especially farnesoid X receptor, which regulates bile acids and cholesterol metabolism. Guggulsterone also mediates gene expression through the regulation of transcription factors, including nuclear factor-kappa B and signal transducer and activator of transcription 3, which plays important roles in the development of inflammation and tumorigenesis. Guggulsterone has been shown to downregulate the expression of proteins involved in anti-apoptotic, cell survival, cell proliferation, angiogenic, metastatic, and chemoresistant activities in tumor cells. This review aimed to clarify the cell signal pathways targeted by guggulsterone and the bioactivities of guggulsterone in animal models and humans.

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3. Das S, Datta A, Bagchi C, Chakraborty S, Mitra A, Tripathi SK – A Comparative Study of Lipid-Lowering Effects of Guggul and Atorvastatin Monotherapy in Comparison to Their Combination in High Cholesterol Diet-Induced Hyperlipidemia in Rabbits.

BACKGROUND:

Hypolipidemic activity of gugulipid has been widely described in traditional literature.

OBJECTIVE:

This study was done to evaluate hypolipidemic activity of guggul and atorvaststin monotherapy in comparison to their combination in rabbits.

MATERIALS AND METHODS:

Male New Zealand White rabbits (body weight 1.3-1.8 kg and age 8-10 weeks) were made hyperlipidemic by feeding cholesterol (0.5 g/kg) for three weeks and randomly divided into a control and three treatment groups receiving: atorvastatin (3.7 mg/kg), guggul (3.5 mg/kg) and their combination (same dose) for the next three weeks. Body weight measurements, estimation of serum lipid profile were done at the beginning, after three and six weeks, respectively. Histopathological examination of liver, heart and aorta was done after six weeks. Statistical analysis was done with SPSS version 16.0 using one-way and repeated measures analysis of variance (ANOVA) followed by post-hoc multiple comparison test with two tailed P value < 0.05 as significant.

RESULTS:

All treated groups had significant reduction in cholesterol, triglyceride, low-density lipoprotein (LDL) and very low-density lipoprotein (VLDL) in comparison to pre-treatment values and control group, and had significant increase in high-density lipoprotein (HDL) in comparison to pre-treatment values.

CONCLUSION:

Combination of atorvastatin and guggul was comparable to their monotherapies in improving lipid profile.

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4. Tripathi YB, Malhotra OP, Tripathi SN. – Thyroid Stimulating Action of Z-Guggulsterone Obtained from Commiphora mukul.

A ketosteroid has been isolated from the oleo-resin of COMMIPHORA MUKUL and its structure (4,17(20)trans pregnandiene 3,16-dione; Z-guggulsterone) established from its physico-chemical properties, specially UV, IR, NMR and mass-spectra. The isolated ketosteroid showed a strong thyroid stimulatory action when administered to albino rats. Its administration (1 mg/100 g body weight) brought about an increase in iodine-uptake by thyroid and enhanced activities of thyroid peroxidase and protease as well as oxygen consumption by isolated slices of liver and biceps muscle.

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5. Katzeff HL, Selgrad C. – Maintenance of thyroid hormone production during exercise-induced weight loss.

Calorie restriction reduces thyroxine (T4) and 3,5,3′-triiodothyronine (T3) production, but the effects of exercise-induced weight loss on thyroid hormone metabolism in rodents are unclear. We studied the effects of chronic exercise on T4 and T3 metabolism comparing exercising (exercise) rats pair fed to sedentary (control) rodents and to weight-matched underfed sedentary animals (underfed; caloric intake 75% of ad libitum-fed controls). The exercise group utilized voluntary running wheels (28 days), and thyroid hormone metabolism was assessed using a three-compartment kinetics model. The exercise and underfed groups were equivalent in weight, but protein mass was greater in the exercise vs. underfed groups (30.4 +/- 0.5 vs. 27.9 +/- 0.5 g; P less than 0.05). During exercise, the T4 plasma clearance rate (PCR) was decreased (-39.2%; P less than 0.01) and the T4 concentration in serum was increased (48.6%; P less than 0.01), resulting in an unchanged T4 plasma appearance rate (PAR) vs. the control group. The decrease in T4 PCR in the exercise group was associated with a lower transport rate of T4 out of the slow pool (P less than 0.01). In the underfed group there was a reduction in both T4 serum concentration and PAR (-36%; P less than 0.01) compared with the control group, which was associated with a decrease in the volume of distribution (-25%; P less than 0.01). T3 PAR decreased 38.7% (P less than 0.01) during underfeeding but only 16.9% (P = not significant) during exercise vs. the control group.(ABSTRACT TRUNCATED AT 250 WORDS).

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6. Panda S, Kar A. – Guggulu (Commiphora mukul) potentially ameliorates hypothyroidism in female mice.

The efficacy of guggulu, the gum resin of Commiphora mukul in regulating hypothyroidism was evaluated in female mice. In addition to estimating serum levels of thyroxine and triiodothyronine, hepatic 5′ monodeiodinase, hepatic glucose-6-phospatase and lipid-peroxidation (LPO), the activities of the anti-oxidative enzymes, superoxide dismutase (SOD) and catalase (CAT), were investigated. While 6-n-propyl-2-thiouracil (PTU, 10.00 mg/kg/d for 30 days) induced hypothyroidism in mice, as evidenced by a decrease in thyroid hormone concentration and in hepatic 5’D-I activity, simultaneous administration of guggulu (200 mg/kg/d for 30 days) reversed this effect, indicating its potential to stimulate thyroid function. Although in PTU treated animals a marginal increase in hepatic LPO was observed, when simultaneously treated with guggulu, it was decreased. A parallel increase in the activity of endogenous antioxidants, SOD and CAT, in the latter group indicated the safe and antiperoxidative nature of the drug. These findings suggest the possible use of guggulu in the amelioration of hypothyroidism.

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7. Mithila MV, Khanum F. – The appetite regulatory effect of guggulsterones in rats: a repertoire of plasma hormones and neurotransmitters.

Guggulsterone or guggulipid is a steroidal constituent present in the neutral fraction of gum resin of Commiphora mukul, commonly known as guggul. The traditional uses of guggul-resin extract are well documented in the Ayurveda-where it is prescribed to treat a variety of ailments including lipid-related disorders such as obesity and arteriosclerosis. The hypolipidemic activity of the extracts known since ancient times can be traced to the two closely related steroidal ketones, E-guggulsterone and Z-guggulsterone. In this study, we have investigated the dose dependent (100, 200, 400 mg/kg body weight) effect of guggulsterones on appetite regulating hormones [ghrelin, leptin, cholecystokinin (CCK)] and neurotransmitters (serotonin and dopamine), which play a major role in the energy homeostasis and thus influence obesity related factors. We have also studied its effect on food intake, body weight and plasma triglycerides and glucose in rats. Guggulsterones at the dose of 400 mg/kg body weight was able to significantly reduce food intake and limit body weight gain over a period of 15 days. It also significantly decreased the plasma ghrelin, glucose, triglyceride levels and increased plasma leptin, serotonin, dopamine levels, but did not show much effect on CCK levels.

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8. Bhatt AD, Dalal DG, Shah SJ, Joshi BA, Gajjar MN, Vaidya RA, Vaidya AB, Antarkar DS. – Conceptual and methodologic challenges of assessing the short-term efficacy of Guggulu in obesity: data emergent from a naturalistic clinical trial.

An open comparative trial was conducted in 58 adult obese patients (Body Mass Index > or = 25 kg/square metre). Group I (n = 27), non-drug, was advised diet (1200-1600 cals) and a brisk walk for 30 minutes. Group II, in addition, received Guggulu (Medohar) 1.5-3 gms/day for 30 days. Mean difference in weight loss between Guggulu and non-drug group was 0.32 kg (ns) on day 15 and 0.58 kg on day 30 (ns). The mean weight reduction in patients (> 90 kgs) was 1.92 kg (ns) and 2.25 kg (ns) higher in Guggulu group. All patients weighing > 90 kg lost weight in Guggulu group whilst 3 in non-drug group did not lose weight. Guggulu was tolerated well. The data from this pilot study suggest a synergistic diet-Guggulu interaction over 30 days in patients weighing > 90 kgs which needs to be confirmed in a large placebo controlled study.

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9. Jose Antonio, Carlon M.Colker, Georgeann, C.Torina, QuihuShi, WilliamBrink, Douglas Kaiman – Effects of a standardized guggulsterone phosphate supplement on body composition in overweight adults.

The purpose of this study was to determine the effects of a guggulsterone phosphate salt compound on body composition and mood states in overweight adults. In a double-masked, randomized, placebo-controlled study, 20 subjects with a body-mass index >25 kg/m2 were separated into 1 of 3 groups. The experimental group received guggulsterones 750 mg and phosphate 1650 mg daily, the placebo group received maltodextrin capsules, and the control group received no treatment for 6 weeks. Subjects were instructed to follow the American Heart Association Step One diet and a 3-day-per-week circuit exercise program. Body weight decreased significantly in the experimental group (3.2%, P < 0.05) and fat mass decreased significantly in the experimental (20.6%) and control (8.6%) groups (P < 0.01). However, between-group differences in weight loss were not statistically significant. Profile of Mood States (POMS)-fatigue decreased significantly in the experimental group (63.7%, P< 0.01), whereas POMS-vigor increased significantly in the experimental group (32.3%, P < 0.01) and decreased significantly in the placebo group (15.6%, P < 0.01). Results of this study suggest that ingestion of a guggulsterone phosphate salt compound concurrent with regular exercise will result in a significant loss of body weight and improved mood states.

10. Sharma B, Salunke R, Srivastava S, Majumder C, Roy P. – Effects of guggulsterone isolated from Commiphora mukul in high fat diet induced diabetic rats.

Sedentary lifestyle, consumption of energy-rich diet, obesity and longer lifespan are some of the major reasons for the rise of metabolic disorders like type II diabetes, obesity, hypertension and dyslipidemia among people of various age groups. High fat diet induced diabetic rodent models resembling type II diabetic condition in human population were used to assess the anti-diabetic and hypolipidemic activity of guggulsterone (isolated from Commiphora mukul resin). Four groups of rats were fed high fat diet, for 16 weeks. On feeding the normal rats with fat rich diet they showed increased serum glucose, cholesterol and triglyceride levels along with increase in insulin resistance significantly (p<0.05) in comparison to control animals. Different biochemical parameters like GTT, glycogen content, glucose homeostatic enzymes (like glucose-6-phosphatase, hexokinase), insulin release in vivo and expression profiles of various genes involved in carbohydrate and lipid metabolism clearly demonstrated the hypoglycemic effect of this extract. Guggulsterone demonstrated a differential effect with a significantly improved PPARgamma expression and activity in in vivo and in vitro conditions, respectively. However, it inhibited 3T3-L1 preadipocytes differentiation in vitro. The results presented here suggest that the guggulsterone has both hypoglycemic and hypolipidemic effect which can help to cure type II diabetes.

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11. Rayalam S, Yang JY, Della-Fera MA, Park HJ, Ambati S, Baile CA. – Anti-obesity effects of xanthohumol plus guggulsterone in 3T3-L1 adipocytes.

Xanthohumol (XN) and guggulsterone (GS) have each been shown to inhibit adipogenesis and induce apoptosis in adipocytes. In the present study effects of the combination of XN + GS on 3T3-L1 adipocyte apoptosis and adipogenesis were investigated. Mature adipocytes were treated with XN and GS individually and in combination. XN and GS individually decreased cell viability, but XN + GS caused an enhanced decrease in viability and potentiated induction of apoptosis. Likewise, XN + GS caused a potentiated increase in caspase-3/7 activation, whereas neither of the compounds showed any effect individually. In addition, western blot analysis revealed that XN + GS increased Bax expression and decreased Bcl-2 expression, whereas individual compounds did not show any significant effect. XN and GS both decreased lipid accumulation. Individually, XN at 1.5 microM and GS at 3.12 microM decreased lipid accumulation by 26 +/- 4.5% (P < .001) each, whereas XN1.5 + GS3.12 decreased lipid accumulation by 78.2 +/- 1.8% (P < .001). Moreover, expression of the adipocyte-specific proteins was down-regulated with XN1.5 + GS3.12, but no effect was observed with the individual compounds. Finally, XN + GS caused an enhanced stimulation of lipolysis. Thus, combination of XN and GS is more potent in exerting anti-obesity effects than additive effects of the individual compounds.

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12. Ojha SK, Nandave M, Arora S, Mehra RD, Joshi S, Narang R, Arya DS. – Effect of Commiphora mukul extract on cardiac dysfunction and ventricular function in isoproterenol-induced myocardial infarction.

In present study, hydroalcoholic extract of C. mukul significantly improved the cardiac function and prevented myocardial ischemic impairment manifested in the form of increased heart rate, decreased arterial pressure, increased left ventricular end diastolic pressure, and altered myocardial contractility indices. C. mukul treatment additionally also produced a significant increase in lactate dehydrogenase levels and prevented decline of protein content in heart. C. mukul preserved the structural integrity of myocardium. Reduced leakage of myocyte enzyme lactate dehydrogenase and maintenance of structural integrity of myocardium along with favorable modulation of cardiac function and improved cardiac performance indicate the salvage of myocardium with C. mukul treatment. Guggulsterones which are considered to be responsible for most of the therapeutic properties of C. mukul may underlie the observed cardioprotective effect of C. mukul against cardiac dysfunction in isoproterenol-induced ischemic rats.

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13. Shen T, Li GH, Wang XN, Lou HX. – The genus Commiphora: a review of its traditional uses, phytochemistry and pharmacology.

ETHNOPHARMACOLOGICAL RELEVANCE:

The resinous exudates of the Commiphora species, known as ‘myrrh’, are used in traditional Chinese medicine for the treatment of trauma, arthritis, fractures and diseases caused by blood stagnation. Myrrh has also been used in the Ayurvedic medical system because of its therapeutic effects against inflammatory diseases, coronary artery diseases, gynecological disease, obesity, etc.

AIM OF THE REVIEW:

Based on a comprehensive review of traditional uses, phytochemistry, pharmacological and toxicological data on the genus Commiphora, opportunities for the future research and development as well as the genus’ therapeutic potential are analyzed.

METHODS:

Information on the Commiphora species was collected via electronic search (using Pubmed, SciFinder, Scirus, Google Scholar and Web of Science) and a library search for articles published in peer-reviewed journals. Furthermore, information also was obtained from some local books on ethnopharmacology. This paper covers the literature, primarily pharmacological, from 2000 to the end of December 2011.

RESULTS:

The resinous exudates from the bark of plants of the genus Commiphora are important indigenous medicines, and have a long medicinal application for arthritis, hyperlipidemia, pain, wounds, fractures, blood stagnation, in Ayurvedic medicine, traditional Chinese medicine and other indigenous medical systems. Phytochemical investigation of this genus has resulted in identification of more than 300 secondary metabolites. The isolated metabolites and crude extract have exhibited a wide of in vitro and in vivo pharmacological effects, including antiproliferative, antioxidant, anti-inflammatory and antimicrobial. The bioactive steroids guggulsterones have attracted most attention for their potent hypolipidemic effect targeting farnesoid X receptor, as well as their potent inhibitory effects on tumor cells and anti-inflammatory efficiency.

CONCLUSIONS:

The resins of Commiphora species have emerged as a good source of the traditional medicines for the treatment of inflammation, arthritis, obesity, microbial infection, wound, pain, fractures, tumor and gastrointestinal diseases. The resin of C. mukul in India and that of C. molmol in Egypt have been developed as anti-hyperlipidemia and antischistosomal agents. Pharmacological results have validated the use of this genus in the traditional medicines. Some bioassays are difficult to reproduce because the plant materials used have not been well identified, therefore analytical protocol and standardization of extracts should be established prior to biological evaluation. Stem, bark and leaf of this genus should receive more attention. Expansion of research materials would provide more opportunities for the discovery of new bioactive principles from the genus Commiphora.

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14. Jeong-Yeh Yang, Mary Anne Della-Fera and Clifton A. Baile – Guggulsterone inhibits adipocyte differentiation and induces apoptosis in 3T3-L1 cells.

OBJECTIVE:

To determine the effects of guggulsterone (GS), the active substance in guggulipid, on apoptosis, adipogenesis, and lipolysis using 3T3-L1 cells.

METHODS AND PROCEDURES:

For apoptosis and lipolysis experiments, mature adipocytes were treated with GS isomers. Viability, apoptosis, and caspase 3/7 activation were quantified using MTS, enzyme-linked immunosorbent assay (ELISA), caspase-Glo 3/7 activity assay, respectively. The expression of cytochrome c was demonstrated by western blot. Lipolysis was quantified by measuring the release of glycerol. For adipogenesis experiments, postconfluent preadipocytes were incubated with GS isomers for up to 6 days during maturation. Adipogenesis was quantified by measuring lipid content using Nile Red dye. Western blot was also used to demonstrate the adipocyte-specific transcription factors peroxisome proliferator-activated receptor gamma2 (PPARgamma2), CCAAT/enhancer binding protein alpha (C/EBPalpha), and C/EBPbeta.

RESULTS:

In mature adipocytes cis-GS decreased viability, whereas the trans-GS isomer had little effect. Both isomers caused dose-dependent increases in apoptosis and cis-GS was more effective than trans-GS in inducing apoptosis. cis- and trans-GS also increased caspase-3 activity and release of cytochrome c from mitochondria. In maturing preadipocytes, both isomers were equally effective in reducing lipid content. The adipocyte-specific transcription factors PPARgamma2, C/EBPalpha, and C/EBPbeta were downregulated after treatment with cis-GS during the maturation period. Furthermore, cis-GS increased basal lipolysis of mature adipocytes, but trans-GS had no effect.

DISCUSSION:

These results indicate that GS isomers may exert antiobesity effects by inhibiting differentiation of preadipocytes, and by inducing apoptosis and promoting lipolysis of mature adipocytes. The cis-GS isomer was more potent than the trans-GS isomer in inducing apoptosis and lipolysis in mature adipocytes.

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15. Thappa DM, Dogra J. – Nodulocystic acne: oral gugulipid versus tetracycline.

Twenty patients with nodulocystic acne were randomly allocated to one of two treatment schedules: 1) Tetracycline 500 mg or 2) Tab. Gugulipid (equivalent to 25 mg guggulsterone). Both were taken twice daily for 3 months, and both produced a progressive reduction in the lesions in the majority of patients. With tetracycline, the percentage reduction in the inflammatory lesions was 65.2% as compared to 68% with gugulipid; on comparison, this difference was statistically insignificant (P > 0.05). Follow-up at 3 months showed a relapse in 4 cases on tetracyline and 2 cases on gugulipid. An interesting observation was that the patients with oily faces responded remarkably better to gugulipid.

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16. Ajaz A. Bhat, Kirti S. Prabhu, Shilpa Kuttikrishnan, Roopesh Krishnankutty, Jayaprakash Babu,Ramzi M. Mohammad, and Shahab Uddin – Potential therapeutic targets of Guggulsterone in cancer

Natural compounds capable of inducing apoptosis in cancer cells have always been of considerable interest as potential anti-cancer agents. Many such compounds are under screening and development with their potential evolution as a clinical drug benefiting many of the cancer patients. Guggulsterone (GS), a phytosterol isolated gum resin of the tree Commiphora mukul has been widely used in Indian traditional medicine as a remedy for various diseses. GS has been shown to possess cancer chemopreventive and therapeutic potential as established by in vitro and in vivo studies. GS has been shown to target constitutively activated survival pathways such as PI3-kinase/AKT, JAK/STAT, and NFκB signaling pathways that are involved in the regulation of growth and inflammatory responses via regulation of antiapoptotic and inflammatory genes. The current review focuses on the molecular targets of GS, cellular responses, and the animal model studies in various cancers. The mechanistic action of GS in different types of cancers also forms a part of this review. The perspective of translating this natural compound into a clinically approved drug with its pros and cons is also discussed.

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17. Shen T, Zhang L, Wang YY, Fan PH, Wang XN, Lin ZM, Lou HX. – Steroids from Commiphora mukul display antiproliferative effect against human prostate cancer PC3 cells via induction of apoptosis.

Two new stigmastane-type steroids, stigmasta-5,22E-diene-3β,11α-diol (1) and stigmasta-5,22E-diene-3β,7α,11α-triol (2), together with eight known compounds, were isolated from the resinous exudates of Commiphora mukul. Their structures were established by extensive analysis of their HR-MS, 1D- and 2D-NMR (COSY, HMQC, HMBC and NOESY) spectra. The isolates were evaluated for their antiproliferative activities against four human cancer cell lines. Compound 2 demonstrated inhibitory effects with IC(50) values of 5.21, 9.04, 10.94 and 16.56 μM, respectively, against K562, MCF-7, PC3 and DU145 human cancer cell lines. Further study showed that 2 was able to enforce the PC3 cell cycle arrest in the G2/M phase, and induce the apoptosis of PC3 cells by activation of Bax, caspases 3 and 9, and by inhibition of Bcl-2. It was also found that 1 inhibited proliferation of PC3 cells via G0/G1 phase arrest of the cell cycle.

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18. Guoqin Jiang, Xiao Xiao, Yan Zeng, Kalyanam Nagabhushanam, Muhammed Majeed and Dong Xiao – Targeting beta-catenin signaling to induce apoptosis in human breast cancer cells by z-guggulsterone and Gugulipid extract of Ayurvedic medicine plant Commiphora mukul.

z-Guggulsterone (z-Gug) and Gugulipid (GL) have been used to treat a variety of ailments. We now report their anti-cancer effect and mechanism against human breast cancer.

METHODS:

Using the human estrogen receptor-positive (MCF-7) and triple-negative (MDA-MB-231) breast cancer cells as well as the normal human mammary epithelial cell line (HMEC), we evaluated the anti-breast-cancer efficacy and apoptosis inducing activity of GL. We determined the cellular and molecular mechanism of GL-inhibited breast cancer cell growth.

RESULTS:

GL significantly inhibited growth of MCF-7 and MDA-MB-231 cells with an IC50~2 μM at pharmacologically relevant concentrations standardized to its major active constituent z-Gug. The GL-induced growth inhibition correlated with apoptosis induction as evidenced by an increase in cytoplasmic histone-associated DNA fragmentation and caspase 3 activity. The GL-induced apoptosis was associated with down-regulation of the β-Catenin signaling pathway. The decreased expression of Wnt/β-Catenin targeting genes, such as cyclin D1, C-myc and survivin, and the inhibition of the activity of the transcription factor (T-cell factor 4, TCF-4) were observed in GL-treated breast cancer cells. The GL treatment resulted in a significant reduction of β-Catenin /TCF-4 complex in both of the cancer cells. The GL-induced apoptotic cell death was significantly enhanced by RNA Interference of β-Catenin and TCF-4. On the other hand, the normal human mammary epithelial cell HMEC, compared with the human breast cancer cells, is significantly more resistant to growth inhibition and apoptosis induction by GL.

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19. Dong Xiao and Shivendra V. Singh – z-Guggulsterone, a constituent of Ayurvedic medicinal plant Commiphora mukul, inhibits angiogenesis in vitro and in vivo.

Our previous studies have shown that z-guggulsterone, a constituent of Indian Ayurvedic medicinal plant Commiphora mukul, inhibits the growth of human prostate cancer cells by causing apoptosis. We now report a novel response to z-guggulsterone involving the inhibition of angiogenesis in vitro and in vivo. The z-guggulsterone treatment inhibited capillary-like tube formation (in vitro neovascularization) by human umbilical vein endothelial cells (HUVEC) and migration by HUVEC and DU145 human prostate cancer cells in a concentration- and time-dependent manner. The z- and E-isomers of guggulsterone seemed equipotent as inhibitors of HUVEC tube formation. The z-guggulsterone-mediated inhibition of angiogenesis in vitro correlated with the suppression of secretion of proangiogenic growth factors [e.g., vascular endothelial growth factor (VEGF) and granulocyte colony-stimulating factor], down-regulation of VEGF receptor 2 (VEGF-R2) protein level, and inactivation of Akt. The z-guggulsterone-mediated suppression of DU145 cell migration was increased by knockdown of VEGF-R2 protein level. Ectopic expression of constitutively active Akt in DU145 cells conferred protection against z-guggulsterone-mediated inhibition of cell migration. Oral gavage of 1 mg z-guggulsterone/d (five times/wk) to male nude mice inhibited in vivo angiogenesis in DU145-Matrigel plug assay as evidenced by a statistically significant decrease in tumor burden, microvessel area (staining for angiogenic markers factor VIII and CD31), and VEGF-R2 protein expression. In conclusion, the present study reveals that z-guggulsterone inhibits angiogenesis by suppressing the VEGF-VEGF-R2-Akt signaling axis. Together, our results provide compelling rationale for further preclinical and clinical investigation of z-guggulsterone for its efficacy against prostate cancer.

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20. Xu HB, Xu LZ, Mao XP, Fu J. – Guggulsterone of Commiphora mukul resin reverses drug resistance in imatinib-resistant leukemic cells by inhibiting cyclooxygenase-2 and P-glycoprotein.

The purpose of this study was to investigate the effects of guggulsterone on cyclooxygenase-2 and P-glycoprotein mediated drug resistance in imatinib-resistant K562 cells (K562/IMA). MTT cytotoxicity assay, flow cytometry, western blot analysis, and ELISA were performed to investigate the anti-proliferative effect, the reversal action of drug resistance, and the inhibitory effect on cyclooxygenase-2, P-glycoprotein, BCR/ABL kinase, and PGE2 release in K562/IMA cells by guggulsterone. The results showed that co-administration of guggulsterone resulted in a significant increase in chemo-sensitivity of K562/IMA cells to imatinib, compared with imatinib treatment alone. Rhodamine123 accumulation in K562/IMA cells was significantly enhanced after incubation with guggulsterone (60, 120 μM), compared with untreated K562/IMA cells (p<0.05). When imatinib (1 μM) was combined with guggulsterone (60, 120 μM), the mean apoptotic population of K562/IMA cells was 15.47% and 24.91%. It was increased by 3.82 and 6.79 times, compared with imatinib (1 μM) treatment alone. Furthermore, guggulsterone had significantly inhibitory effects on the levels of cyclooxygenase-2, P-glycoprotein and prostaglandin E2. However, guggulsterone had little inhibitory effect on the activity of BCR/ABL kinase. The present study indicates guggulsterone induces apoptosis by inhibiting cyclooxygenase-2 and down-regulating P-glycoprotein expression in K562/IMA cells.

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