Inhibition of Platelet Aggregation by „Guggulu” Steroids

Mester, L.; M, Mester de Parajd; Nityanand, S

doi:10.1055/s-0028-1097351

Cited by 32 publications

(18 citation statements)

References 1 publication

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“…The effect of guggulsterones and was very similar to the inhibitory effect of clofibrate. This finding has therapeutic value in myocardial infarction and thromboembolism 70 .…”

Section:  Effect On Platelet Aggregation and Fibrinolytic Activitymentioning

confidence: 53%

Commiphora wightii (Arn.) Bhandari. Review of Its Botany, Medicinal Uses, Pharmacological Activities and Phytochemistry

Bhardwaj¹,

Alia²

2019

J. Drug Delivery Ther.

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The oldest remedies identified to mankind are herbal medicines. India is recognized worldwide for its Ayurvedic treatment. As only little studies are done on this plant, the purpose of current review is to make accessible up-to-date information on, botany, morphology, ecological biodiversity, medicinal uses, phytochemistry and pharmacological activities on diverse parts of Commiphora wightii (Arn.) Bhandari (C. wightii). This review was assembled using scientific literature from electronic search engine such as Springerlink, BioMed Central, PubMed, Scopus, ScienceDirect, Scielo, Medline and Science domain. Supplementary literatures were obtained from books, book chapters, dissertations, websites and other scientific publications. C. wightii (Syn. Commiphora mukul Hook. ex. Stocks) or Guggulu tree. C. wightii is a shrub or small tree belonging to Burseraceae family. C. wightii contains volatile oil, gum resin, gugulipids, guggulsterones, guggulsterols, mukolol and other steroids. Guggulu is very much used in Ayuvedic system of medicine as astringent, anti-septic, expectorant, aphrodisiac, carminative, anti-spasmodic, emmenagogue. In Ayurveda, it is the best among herbs that are used for Medoroga and Vata disorders. It is widely used for obesity and it is also known as fat burning agent all over the world. It helps to lower cholesterol and triglycerides level. It is very effective in rheumatoid arthritis, gout and sciatica. It is also one of the most important Rasayana of Ayurveda. In addition it treats sluggish liver, stimulates libido, nervous diseases, bronchial congestion, cardiac and circulatory problems, weak digestion, wounds, abscess, foetid ear, fractures, gynaecological problems and various skin diseases. C. wightii is a very important and trustworthy herb in Ayurvedic medicine. This alternative system of medicine is gaining increasing fame universal. There is a required to isolate active constituents, their biological test, molecular mechanisms, experimental defense and legalization of therapeutic uses of C. wightii. The collected information will be obliging to locate up study protocol for current drugs and Ayurvedic formulation extension in remedial and luxury a variety of ailments.

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“…The effect of guggulsterones and was very similar to the inhibitory effect of clofibrate. This finding has therapeutic value in myocardial infarction and thromboembolism 70 .…”

Section:  Effect On Platelet Aggregation and Fibrinolytic Activitymentioning

confidence: 53%

Commiphora wightii (Arn.) Bhandari. Review of Its Botany, Medicinal Uses, Pharmacological Activities and Phytochemistry

Bhardwaj¹,

Alia²

2019

J. Drug Delivery Ther.

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“…Guggulsterones have been shown to be the active ingredient in gugulipid (Beg et al, 1996). Guggulsterones also exhibit thyroid-stimulating activity (Tripathi et al, 1984) and inhibit platelet aggregation (Mester et al, 1979). Recent studies indicate that guggulsterones may lower cholesterol through antagonism of FXR, a member of the nuclear receptor superfamily of ligand-activated transcription factors.…”

Section: Discussionmentioning

confidence: 99%

Guggulsterone Activates Multiple Nuclear Receptors and Induces CYP3A Gene Expression through the Pregnane X Receptor

Brobst¹,

Ding²,

Creech³

et al. 2004

J Pharmacol Exp Ther

102

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Gugulipid is an extract of the guggul tree, Commiphora mukul, that is used to treat hyperlipidemia in humans. The lipid-lowering activity is found in the stereoisomers and plant sterols Z-guggulsterone and E-guggulsterone. The molecular basis for the lipidlowering action of guggulsterone has been suggested to be antagonism of the farnesoid X receptor, a member of the nuclear receptor superfamily of ligand-activated transcription factors. To determine whether guggulsterone has the ability to function as an agonist of other nuclear receptor family members, we screened a panel of these proteins for their ability to transactivate reporter genes. Here, we show that guggulsterones activate the estrogen receptor ␣ isoform, progesterone receptor, and pregnane X receptor. Concentration-response analysis using reporter gene assays indicate that guggulsterones activate these three receptors with EC 50 values in the low micromolar range. Furthermore, we show that guggulsterone-mediated activation of the pregnane X receptor induces the expression of CYP3A genes in both rodent and human hepatocytes. Protein interaction assays indicate that guggulsterones interact directly with pregnane X receptor, thereby modulating interaction with protein cofactors. We introduce a novel method to screen herbal remedies for their ability to activate pregnane X receptor. Pregnane X receptor activation is known to cause herb-drug interactions, and our data suggest that gugulipid therapy should be used cautiously in patients taking prescription medications that are metabolized by CYP3A family members. Moreover, our data suggest the need for additional studies of guggulsterones agonist activity against estrogen receptor ␣ isoform and the progesterone receptor.

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“…As guggulipid, guggulsterone also inhibited platelets aggregation (13) and provide protection against myocardial ischemia induced by isoproterenol (14). The protective action of guggulsterone is due to antioxidant property because it inhibits the generation of oxygen free radicals (15).…”

Section: Introductionmentioning

confidence: 99%

Cardioprotective activity of synthetic guggulsterone (E and Z-isomers) in isoproterenol induced myocardial ischemia in rats: A comparative study

Chander

Rizvi

Khanna

et al. 2003

Indian J Clin Biochem

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Guggulsterone, a mixture ofcis (E) and trans (Z) isomers (7:3 w/w) was synthesized from 16-DPA. The isomers were separated by column chromatography and evaluated for cardioprotective and antioxidant activities. Myocardial necrosis induced by isoproterenol in rats caused marked increase in serum creatine phosphokinase and glutamate pyruvate transaminase. Simultaneously in ischemic heart, phospholipase, xanthine oxidase and lipid peroxides were enhanced following depletion of glycogen, phospholipids and cholesterol. Treatment with guggulsterone and its both isomers at the dose of 50 mg/kg po., significantly protected cardiac damage as assessed by the reversal of blood and heart biochemical parameters in ischemic rats. The cardioprotective activity of guggulsterone and of both the isomers were compared with that of gemfibrozil at the same doses. Guggulsterone and both the isomers at tested concentrations (5-20mM) inhibited oxidative degradation of lipids in human low-density lipoprotein and rat liver microsomes induced by metal ions in vitro. The drug counteracted against the generation of superoxide anions (O 2) and hydroxyl radicals (OH) in non-enzymic test systems. It is suggested that cardioprotective and antioxidant activities of synthetic guggulsterone and guggulsterone obtained from gum resin Commiphora mukulthat contains isomers E & Z in the ratio of 46:54w/w are the same. KEY WORDSCis and trans-guggulsterone, cardiprotective activity, antioxidant property, Isoproterenol cardiac ischemia.

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Inhibition of Platelet Aggregation by „Guggulu” Steroids

Abstract: Purified steroidal fractions of ,guggulua show a marked inhibition of ADP, adrenaline and serotonin induced platelet aggregation. Their inhibitory effect is comparable to the .effect o f ,Clofi-&ratea.

Cited by 32 publications

References 1 publication

Commiphora wightii (Arn.) Bhandari. Review of Its Botany, Medicinal Uses, Pharmacological Activities and Phytochemistry

Commiphora wightii (Arn.) Bhandari. Review of Its Botany, Medicinal Uses, Pharmacological Activities and Phytochemistry

Guggulsterone Activates Multiple Nuclear Receptors and Induces CYP3A Gene Expression through the Pregnane X Receptor

Cardioprotective activity of synthetic guggulsterone (E and Z-isomers) in isoproterenol induced myocardial ischemia in rats: A comparative study

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