Guggulsterone is an FXR antagonist in coactivator association assays but acts to enhance transcription of bile salt export pump.

J Biol Chem 2003 Jan 13

Cui J, Huang L, Zhao A, Lew JL, Yu J, Sahoo S, Meinke PT, Royo I, Pelaez F, Wright SD.

Atherosclerosis Endocrinology, Merck Research Laboratories, Rahway, NJ 07065.

Guggulipid is an extract of the guggul tree Commiphora mukul and has been widely used to treat hyperlipidemia in humans. The plant sterol guggulsterone (GS) is the active agent in this extract. Recent studies have shown that GS can act as an antagonist ligand for farnesoid X receptor (FXR) and decrease expression of bile acid-activated genes. Here we show that GS, although an FXR antagonist in coactivator association assays, enhances FXR agonist-induced transcription of bile salt export pump (BSEP), a major hepatic bile acid transporter. In HepG2 cells, in the presence of an FXR agonist such as chenodeoxycholate (CDCA) or GW4064, GS enhanced endogenous BSEP expression with a maximum induction of 400% to 500% that induced by an FXR agonist alone. This enhancement was also readily observed in FXR-dependent BSEP promoter activation using a luciferase reporter construct. In addition, GS alone slightly increased BSEP promoter activation in the absence of an FXR agonist. Consistent with the results in HepG2, guggulipid treatment in Fisher rats increased BSEP mRNA. Interestingly, in these animals expression of the orphan nuclear receptor SHP (small heterodimer partner), a known FXR target, was also significantly increased, while expression of other FXR targets including cholesterol 7 -hydroxylase (Cyp 7a1), sterol 12 -hydroxylase (Cyp 8b1) and the intestinal bile acid binding protein (I-BABP), remained unchanged. Thus, we propose that GS is a selective bile acid receptor modulator (SBARM) that regulates expression of a subset of FXR targets. Guggulipid treatment in rats lowered serum triglyceride and raised serum HDL levels. Taken together, these data suggest that guggulsterone defines a novel class of FXR ligands characterized by antagonist activities in coactivator association assays but with the ability to enhance the action of agonists on BSEP expression in vivo.

PMID: 12525500 [PubMed - as supplied by publisher]

The hypolipidemic natural product guggulsterone acts as an antagonist of the bile acid receptor.

Mol Endocrinol 2002 Jul;16(7):1590-7

Wu J, Xia C, Meier J, Li S, Hu X, Lala DS.

Department of Biotechnology, Pharmacia Corp., St. Louis, Missouri 63198, USA.

Ayurveda, the ancient Indian system of health care and medicine, has a well-organized materia medica in which plants form a dominant part. A key illustration of the exploitation of this knowledge toward the development of a modern drug is the isolation and characterization of two antihyperlipidemic compounds, Z-, and E-guggulsterone from the tree Commiphora mukul, the exudate of which has been traditionally used for mitigating lipid disorders. Here, we demonstrate that Z-guggulsterone and an analog, 80-574 currently in clinical trials, act as antagonists of the bile acid receptor (BAR), a member of the intracellular receptor superfamily. These compounds antagonize the activity of BAR in vitro, and in cell culture systems on promoters and endogenous target genes. In biochemical assays, they are able to displace coactivator peptides from the receptor in a dose-dependent manner. The mechanism by which they act as BAR antagonists is likely through their inability to recruit coactivator proteins, failure to release corepressor proteins from unliganded receptor, and ability to compete with BAR agonists to block coactivator recruitment. Our data suggest these compounds may mediate at least some of their effects via the BAR.

PMID: 12089353 PubMed

A natural product that lowers cholesterol as an antagonist ligand for FXR.

Science 2002 May 31;296(5573):1703-6

Urizar NL, Liverman AB, Dodds DT, Silva FV, Ordentlich P, Yan Y, Gonzalez FJ, Heyman RA, Mangelsdorf DJ, Moore DD.

Department of Molecular and Cellular Biology, Baylor College of Medicine, 1 Baylor Plaza, Houston, TX 77030, USA.

Extracts of the resin of the guggul tree (Commiphora mukul) lower LDL (low-density lipoprotein) cholesterol levels in humans. The plant sterol guggulsterone [4,17(20)-pregnadiene-3,16-dione] is the active agent in this extract. We show that guggulsterone is a highly efficacious antagonist of the farnesoid X receptor (FXR), a nuclear hormone receptor that is activated by bile acids. Guggulsterone treatment decreases hepatic cholesterol in wild-type mice fed a high-cholesterol diet but is not effective in FXR-null mice. Thus, we propose that inhibition of FXR activation is the basis for the cholesterol-lowering activity of guggulsterone. Other natural products with specific biologic effects may modulate the activity of FXR or other relatively promiscuous nuclear hormone receptors.

PMID: 11988537 [PubMed - indexed for MEDLINE]

A safe, effective, herbal antischistosomal therapy derived from myrrh.

Am J Trop Med Hyg 2001 Dec;65(6):700-4

Sheir Z, Nasr AA, Massoud A, Salama O, Badra GA, El-Shennawy H, Hassan N, Hammad SM.

Department of Internal Medicine, Faculty of Medicine, Students' University Hospital, Mansoura University, Egypt.

Schistosomiasis is a widespread helminthic disease. Treatment of schistosomiasis is based on chemotherapy with praziquantel, which is the drug of choice. Since resistance to praziquantel has been demonstrated, alternative drugs must be considered. Myrrh is an oleo-gum resin from the stem of the plant Commiphora molmol. This study was carried out on 204 patients with schistosomiasis. The drug was given at a dose of 10 mg/kg of body weight/day for three days, and induced a cure rate of 91.7%. Re-treatment of cases who did not respond with a dose of 10 mg/kg of body weight/day for six days gave a cure rate of 76.5%, increasing the overall cure rate to 98.09%. The drug was well tolerated, and side effects were mild and transient. Twenty cases provided biopsy specimens six months after treatment and none of them showed living ova.

PMID: 11791960 [PubMed - indexed for MEDLINE]

Furanosesquiterpenoids of Commiphora myrrha.

J Nat Prod 2001 Nov;64(11):1460-2

Zhu N, Kikuzaki H, Sheng S, Sang S, Rafi MM, Wang M, Nakatani N, DiPaola RS, Rosen RT, Ho CT.

Department of Food Science, Rutgers University, New Brunswick, New Jersey 08901, USA.

An investigation on the gum exudates of Commiphora myrrha has led to the isolation of six sesquiterpenoids. On the basis of spectroscopic data interpretation, they were determined as two new furanosesquiterpenoids, rel-1S,2S-epoxy-4R-furanogermacr-10(15)-en-6-one (1) and rel-2R-methyl-5S-acetoxy-4R-furanogermacr-1(10)Z-en-6-one (2), and four known furanosesquiterpenoids, rel-3R-methoxy-4S-furanogermacra-1E,10(15)-dien-6-one (3), rel-2R-methoxy-4R-furanogermacr-1(10)E-en-6-one (4), furanogermacra-1(10)Z,4Z-dien-6-one, and curzerenone [6,7-dihydro-5beta-isopropenyl-3,6beta-dimethyl-6-vinylbenzofuran-4(5H)-one]. This is the first report of the relative stereochemistry for the known compounds 3 and 4. Compound 1 exhibited weak cytotoxic activity against a MCF-7 breast tumor cell line in a clonogenic assay, while the other five compounds were inactive in this assay.

PMID: 11720534 [PubMed - indexed for MEDLINE]

Simultaneous determination of E- and Z-guggulsterones in dietary supplements containing Commiphora mukul extract (guggulipid) by liquid chromatography.

J AOAC Int 2001 Jan-Feb;84(1):24-8

Nagarajan M, Waszkuc TW, Sun J.

Enzymatic Therapy, Green Bay, WI 54311, USA.

Guggulipid, the standardized product from the extraction of the ole-gum-resin from the Commiphora mukul plant, has been marketed as a hypolipidemic agent. The ketosteroids, cis- and trans-4,17(20)-pregnadiene-3,16-dione, known as E- and Z-guggulsterones, respectively, are the main ingredients in guggulipid. A liquid chromatographic method was developed for simultaneous determination of E- and Z-guggulsterones in guggulipid preparations using synthetic E- and Z-guggulsterone standards. Realtively low amounts of guggulsterones (E and Z) were found in commercial guggulipid preparations in comparison with the manufacturer's claim of 2.5%. The mixture of E- and Z-guggulsterones was extracted and separated on a Symmetry C18 reversed-phase column, with a mobile phase of acetonitrile--water (46 + 54, v/v) and detected at 242 nm. The retention times of E- and Z-guggulsterones are approximately 8 and 11 min, respectively. Assay quantitation was based on the calibration curve obtained from a mixture of synthetic standard E- and Z-guggulsterones. Experimental data on selectivity, linearity, accuracy, and recoveries are presented.

PMID: 11234828 [PubMed - indexed for MEDLINE]

Alternative therapies: Part II. Congestive heart failure and hypercholesterolemia.

Am Fam Physician 2000 Sep 15;62(6):1325-30 Morelli V, Zoorob RJ.

Louisiana State University School of Medicine in New Orleans, USA.

Natural supplements are widely used by the American public but, while claims of their therapeutic effects abound, medical research does not always support their effectiveness. Clinical trials using Q10 for the management of congestive heart failure have had conflicting results; hawthorn is prescribed in Germany for the treatment of this condition, but no trials have been conducted in the United States. Although initial research about the use of garlic in the management of hypercholesterolemia was encouraging, follow-up studies have failed to verify these results. Substituting soy protein for high-fat animal protein diets, however, does have a beneficial effect on serum lipid levels. So far, cholestin (a natural product containing several statins) has proved to be a cost-saving lipid-lowering medication, and fenugreek may offer modest improvement as well. Gugulipid is also promising but requires further research.

PMID: 11011861 [PubMed - indexed for MEDLINE]

Gugulu (Commiphora mukul) induces triiodothyronine production: possible involvement of lipid peroxidation.

Life Sci 1999;65(12):PL137-41

Panda S, Kar A.

School of Life Sciences, Devi Ahilya University, Vigyan Bhawan, Indore, India.

An investigation was made to find out the importance of gugulu (Commiphora mukul) in thyroid function of mice and to reveal the possible involvement of lipid peroxidation (LPO), if any. While no marked change in the concentrations of serum thyroxine (T4) was observed, triiodoth yronine (T3) concentration and T3/T4 ratio were enhanced following the administration of gugulu extract (0.2 g/kg b. wt./d for 15 days). A concomitant decrease in LPO was also noticed in liver, the principal site of T3 generation, suggesting that gugulu induced increase in T3 concentration is LPO mediated.

PMID: 10503949 [PubMed - indexed for MEDLINE]

Hypolipidemic and antioxidant effects of Commiphora mukul as an adjunct to dietary therapy in patients with hypercholesterolemia.

Cardiovasc Drugs Ther 1994 Aug;8(4):659-64

Singh RB, Niaz MA, Ghosh S.

Heart Research Laboratory, Medical Hospital and Research Centre, Moradabad, India.

The effects of the administration of 50 mg of guggulipid or placebo capsules twice daily for 24 weeks were compared as adjuncts to a fruit- and vegetable-enriched prudent diet in the management of 61 patients with hypercholesterolemia (31 in the guggulipid group and 30 in the placebo group) in a randomized, double-blind fashion. Guggulipid decreased the total cholesterol level by 11.7%, the low density lipoprotein cholesterol (LDL) by 12.5%, triglycerides by 12.0%, and the total cholesterol/high density lipoprotein (HDL) cholesterol ratio by 11.1% from the postdiet levels, whereas the levels were unchanged in the placebo group. The HDL cholesterol level showed no changes in the two groups. The lipid peroxides, indicating oxidative stress, declined 33.3% in the guggulipid group without any decrease in the placebo group. The compliance of patients was greater than 96%. The combined effect of diet and guggulipid at 36 weeks was as great as the reported lipid-lowering effect of modern drugs. After a washout period of another 12 weeks, changes in blood lipoproteins were reversed in the guggulipid group without such changes in the placebo group. Side effects of guggulipid were headache, mild nausea, eructation, and hiccup in a few patients.

PMID: 7848901 [PubMed - indexed for MEDLINE]

Ayurveda's role in preventing disease.

Indian J Med Sci 1998 Feb;52(2):70-7

Svoboda RE.

Ayurvedic Institute, Albuquerque, NM 87192-1445, USA.

Modern medical science is currently in the throes of a revolution which is likely to have a dramatic impact on both the theory of medicine and the way it is practised. The mechanistic model which served biomedicine well for many years is gradually collapsing, thanks to the efforts of dedicated researchers who have looked beyond that model's flaws. Thus we now know that networks of chemical communication exist between the nervous and immune systems, and that prayer at a distance can positively affect the conditions of those who are seriously ill, even when the prayer and the patient are not known to one another. Another participant in this exciting climate of change and ferment is Ayurveda, India's ancient medical system. While Ayurveda has already contributed much to modern medicine (reserpine, gugulipid, plastic surgery), its real contributions are yet to be made. While some of these are likely to come in matters of materia medica and technique, most will likely be derived from Ayurveda's way of seeing the world, its "darshana." This paper outlines a few of the ways in which Ayurveda's "vision" is likely to facilitate medicine's ability to teach people not just how to avoid disease but how to proactively develop and maintain a healthy "state."

PMID: 9770867 [PubMed - indexed for MEDLINE]

Recent nutritional approaches to the prevention and therapy of cardiovascular disease.

Prog Cardiovasc Nurs 1997 Summer;12(3):3-23

Kendler BS.

Manhattan College, NY, USA.

Nutritional factors play an important role in the development and treatment of cardiovascular disease (CVD). However, health care professionals may overlook, or even disregard, some of these factors for several reasons, including inadequate training and conflicting reports in the biomedical literature. This review provides a synopsis of more than two-dozen nutritional approaches to primary and secondary prevention and therapy of CVD. Favorable cardiovascular effects have been reported with the use of unsaturated fatty acids, vegetarian and semi-vegetarian diets, dietary fiber, plant sterols, alcoholic beverages, vitamins (niacin, E, C, B6, B12, folate), minerals (potassium, calcium, magnesium, selenium), conditionally-essential nutrients (coenzyme Q10, L-carnitine, taurine) and botanical agents (garlic, hawthorn, gugulipid). In contrast, trans-fatty acids, oxysterols, homocysteinemia, carbohydrate intolerance, and excessive sodium chloride and iron have been associated with undesirable cardiovascular effects. A nutritional approach to CVD provides a pivotal adjuvant to traditional pharmaceutical and/or surgical interventions by maximizing the likelihood of success in decreasing CVD morbidity and mortality and minimizing the economic and social costs associated with this disease.

PMID: 9287363 [PubMed - indexed for MEDLINE]

Effects of S-allyl cysteine sulfoxide isolated from Allium sativum Linn and gugulipid on some enzymes and fecal excretions of bile acids and sterols in cholesterol fed rats.

Indian J Exp Biol 1995 Oct;33(10):749-51

Sheela CG, Augusti KT.

Department of Bio-Chemistry, University of Kerala, Thiruvananthapuram, India.

S-allyl cysteine sulfoxide, isolated from garlic, A. sativum, is more or less as active as gugulipid in controlling hypercholestermia, obesity and derangement of enzyme activities in cholesterol diet fed rats. The beneficial effects of the drugs are partly due to their inhibitory effects on transaminases, alkaline phosphatase, lipogenic enzymes and HMG CoA reductase and partly due to their stimulatory effects on plasma lecithin-cholesterol acyl transferase lipolytic enzymes and fecal excretion of sterols and bile acids.

PMID: 8575806 [PubMed - indexed for MEDLINE]

Conceptual and methodologic challenges of assessing the short-term efficacy of Guggulu in obesity: data emergent from a naturalistic clinical trial.

J Postgrad Med 1995 Jan-Mar;41(1):5-7

Bhatt AD, Dalal DG, Shah SJ, Joshi BA, Gajjar MN, Vaidya RA, Vaidya AB, Antarkar DS.

Swami Prakashananda Ayurveda Research Centre, Juhu, Bombay.

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.

PMID: 10740691 [PubMed - indexed for MEDLINE]

Antiperoxide effects of S-allyl cysteine sulphoxide isolated from Allium sativum Linn and gugulipid in cholesterol diet fed rats.

Indian J Exp Biol 1995 May;33(5):337-41

Sheela CG, Augusti KT.

Department of Biochemistry, University of Kerala, India.

Cholesterol containing diet significantly increased not only the body weight, but also the weight of liver and adipose tissue of rats. This is accompanied by a significant increase in blood lipids, atherogenic index and lipid peroxidation and a significant decrease in reduced glutathione level, superoxide dismutase and catalase activities in tissues. Treatment with S-allyl cysteine sulphoxide reverses the deleterious effects of cholesterol diet significantly and almost as effectively as gugulipid.

PMID: 7558192 [PubMed - indexed for MEDLINE]

Nodulocystic acne: oral gugulipid versus tetracycline.

J Dermatol 1994 Oct;21(10):729-31

Thappa DM, Dogra J.

Department of Dermatology, C.G.H.S., Bajaj Nagar, Jaipur, India.

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.

PMID: 7798429 [PubMed - indexed for MEDLINE]

Effect of gugulipid on bioavailability of diltiazem and propranolol.

J Assoc Physicians India 1994 Jun;42(6):454-5

Dalvi SS, Nayak VK, Pohujani SM, Desai NK, Kshirsagar NA, Gupta KC.

Dept of Pharmacology, Seth GS Medical College, Parel, Bombay.

The effect of single oral dose of 1 gm gugulipid was studied on bioavailability of single oral dose of propranolol (40 mg) and diltiazem (60 mg) in 10 and 7 normal healthy male volunteers respectively. It was a randomised within group crossover study. Blood samples were collected at hourly intervals upto 8 hrs. Gugulipid significantly reduced (P < .01) peak plasma concentration (Cmax) and area under curve (AUC 0-8 hrs) of both the drugs in normal volunteers. Such interaction in patients receiving propanolol or diltiazem with gugulipid may lead to diminished efficacy or nonresponsiveness due to significant reduction in bioavailability.

PMID: 7852226 [PubMed - indexed for MEDLINE]

Beneficial effects of Allium sativum, Allium cepa and Commiphora mukul on experimental hyperlipidemia and atherosclerosis--a comparative evaluation.

J Postgrad Med 1991 Jul;37(3):132-5

Lata S, Saxena KK, Bhasin V, Saxena RS, Kumar A, Srivastava VK.

Department of Pharmacology, L. L. R. M. Medical College, Meerut, Uttar Pradesh.

Oral administration of petroleum ether extract of Allium sativum, Allium cepa and ethylacetate extract of Commiphora mukul in albino rats significantly prevented rise in serum cholesterol and serum triglyceride level, caused by atherogenic diet. All the three agents were also found to confer significant protection against atherogenic diet induced atherosclerosis.

PMID: 1784023 [PubMed - indexed for MEDLINE]

Stimulation of low density lipoprotein receptor activity in liver membrane of guggulsterone treated rats.

Pharmacol Res 1990 Jan-Feb;22(1):37-44

Singh V, Kaul S, Chander R, Kapoor NK.

Division of Biochemistry, Central Drug Research Institute, Lucknow, India.

Chronic feeding of guggulsterone to rats showed hypolipidaemic activity in blood serum and liver membrane lipids. The decrease in serum cholesterol is associated with enhanced uptake of LDL by the liver through receptor mediated endocytosis, located on the surface of the cell membrane. In the present communication it has been shown that membranes prepared from liver of guggulsterone treated rats exhibit up to 87% increase in binding sites for human 125I-LDL. Significant decrease in lipid levels of serum as well as of membrane were observed. Lipid lowering activity of the drug in relation to LDL catabolism and other possible mechanisms have been explained.

PMID: 2330337 [PubMed - indexed for MEDLINE]

Clinical trials with gugulipid. A new hypolipidaemic agent.

J Assoc Physicians India 1989 May;37(5):323-8

Nityanand S, Srivastava JS, Asthana OP.

Multicentric clinical trials of the efficacy of gugulipid conducted at Bombay, Bangalore, Delhi, Jaipur, Lucknow, Nagpur and Varanasi have been reported. Two hundred and five patients completed 12 week open trial with gugulipid in a dose of 500 mg tds after 8 week diet and placebo therapy. One patient showed gastrointestinal symptoms which did not necessitate withdrawal of the drug. A significant lowering of serum cholesterol (av. 23.6%) and serum triglycerides (av. 22.6%) was observed in 70-80% patients Double-blind, crossover study was completed in 125 patients with gugulipid therapy and in 108 patients with clofibrate therapy. Two patients had flu-like syndrome with clofibrate and opted out from the study. With gugulipid the average fall in serum cholesterol and triglycerides was 11 and 16.8% respectively and with clofibrate 10 and 21.6% respectively. The lipid lowering effect of both drugs became evident 3-4 week after starting the drug and had no relationship with age, sex, and concomitant drug intake. Hypercholesterolaemic patients responded better to gugulipid therapy than hypertriglyceridaemic patients who responded better to clofibrate therapy. In mixed hyperlipidaemic patients response to both drugs was comparable. HDL-cholesterol was increased in 60% cases who responded to gugulipid therapy. Clofibrate had no effect on HDL-cholesterol. A significant decrease in LDL-cholesterol was observed in the responder group to both drugs.

PMID: 2693440 [PubMed - indexed for MEDLINE]

Hypolipidemic activity of guggal resin (Commiphora mukul) and garlic (Alium sativum linn.) in dogs (Canis familiaris) and monkeys (Presbytis entellus entellus Dufresne).

Biochem Exp Biol 1980;16(4):421-4

Dixit VP, Joshi S, Sinha R, Bharvava SK, Varma M.

1. The identification of cholesterol as a constituent in the genesis of coronary artery disease in man and experimental animals are well documented. 2. The hypolipidemic effects of Commiphora mukul (guggulu) and Alium sativum (Garlic powder) were screened in dog and Presbytis monkeys. 3. Progressive decrease in the mean values of cholesterol, triglycerides and phospholipids were conspicuous for forty eight hours following the administration of guggulu/garlic powder. 4. 25 mg/kg body weight garlic powder was more effective in lowering the serum cholesterol and triglycerides as compared with that of guggulu. 5. A comparative hypolipidemic action of the two compounds is discussed.

PMID: 7346059 [PubMed - indexed for MEDLINE]

Comparison of the anti-inflammatory activity of Commiphora mukul (an indigenous drug) with those of phenylbutazone and ibuprofen in experimental arthritis induced by mycobacterial adjuvant.

Arzneimittelforschung 1977 Jul;27(7):1455-7

Sharma JN, Sharma JN.

In the present investigation a method of induction of experimental arthritis in animals was modified to provide a better model replica of human arthritis. Inflammatory syndrome, resembling rheumatoid arthritis in man, was induced in the right hock joint of albino rabbits by intra-articular injection of the killed mycobacterial adjuvant in liquid paraffin. Development of this arthritic syndrome was studied from a period of five months with and without drugs. Anti-inflammatory agents such as phenylbutazone, ibuprofen and fraction "A" of gum-guggual from Commiphora mukkul were administered orally at a daily dose of 100, 100 and 500 mg/kg, respectively, for a period of five months. All three drugs decreased the thickness of the joint swelling during the course of drug treatment. These results indicate the beneficial role of phenylbutazone, ibuprofen and fraction "A" of gum-guggul in experimental arthritis.

PMID: 578471 [PubMed - indexed for MEDLINE]

New triterpenes, myrrhanol A and myrrhanone A, from guggul-gum resins, and their potent anti-inflammatory effect on adjuvant-induced air-pouch granuloma of mice.

Bioorg Med Chem Lett 2001 Apr 23;11(8):985-9

Kimura I, Yoshikawa M, Kobayashi S, Sugihara Y, Suzuki M, Oominami H, Murakami T, Matsuda H, Doiphode VV.

Department of Clinical Pharmacology, Graduate School of Pharmaceutical Sciences, Toyama Medical and Pharmaceutical University, Sugitani, Japan. ikukokim@ms.toyama-mpu.ac.jp

Myrrhanol A, a new triterpene isolated from guggul (Balsamodendron or Commiphora mukul Hook.)-gum resin, displays a potent anti-inflammatory effect on exudative pouch fluid, angiogenesis, and granuloma weights in adjuvant-induced air-pouch granuloma of mice. Its effects were more marked than those of hydrocortisone and the 50% aqueous methanolic extract of the crude drug. Myrrhanol A is a plausible candidate for a potent anti-inflammatory agent.

PMID: 11327606 [PubMed - indexed for MEDLINE]

Bioactive constituents from gum guggul (Commiphora wightii).

Phytochemistry 2001 Apr;56(7):723-7

Zhu N, Rafi MM, DiPaola RS, Xin J, Chin CK, Badmaev V, Ghai G, Rosen RT, Ho CT.

Department of Food Science and Center for Advanced Food Technology, Rutgers University, New Brunswick, NJ 08901, USA.

Bioactivity-directed fractionation and purification afforded cytotoxic components of Commiphora wightii. The exudates of C. wightii were extracted with EtOAc and the extract was subjected to repeated column chromatography. A fraction showing cytotoxic activity was characterized as a mixture of two ferulates with an unusual skeleton by spectral and chemical methods, including by NMR, GC-MS and chemical derivatization. This fraction also showed moderate scavenging effect against 2,2-diphenyl-1-picrylhydrazyl (DPPH) radicals.

PMID: 11314959 [PubMed - indexed for MEDLINE]