Reference

Pregnane X receptor and natural products: beyond drug-drug interactions

All Rights Reserved.Some chemicals with cas registry numbers like 95975-55-6 are also used. Pregnane X receptor and natural products: beyond drug-drug interactions. Staudinger, Jeff L.; Ding, Xunshan; Lichti, Kristin (Department of Pharmacology and Toxicology, University of Kansas, Lawrence, KS 66045, USA). Expert Opinion on Drug Metabolism & Toxicology, 2(6), 847-857 (English) 2006 Informa Healthcare. CODEN: EODMAP. ISSN: 1742-5255. DOCUMENT TYPE: Journal; General Review CA Section: 1 (Pharmacology) A review. The pregnane X receptor (PXR, NR1I2) is a member of the nuclear receptor superfamily that is activated by a myriad of compds. and natural products in clin. use. Activation of PXR represents the basis for several clin. important drug-drug interactions. Although PXR activation has undesirable effects in patients on combination therapy, it also mediates the hepatoprotective effects exhibited by some herbal remedies. This review focuses on PXR activation by natural products and the potential therapeutic opportunities presented. In particular, the biol. effects of St. John's Wort, gugulipid, kava kava, Coleus forskolii, Hypoxis, Sutherlandia, qing hao, wu wei zi, gan cao and other natural products are discussed. The impact of these natural products on drug metab. and hepatoprotection is highlighted in the context of activation and antagonism of PXR. .

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

Cardioprotective activity of synthetic guggulsterone (E and Z-isomers) in isoproterenol-induced myocardial ischemia in rats: a comparative study. Chander, Ramesh; Rizvi, Farhan; Khanna, A. K.; Pratap, Ram (Division of Biochemistry, Central Drug Research Institute, Lucknow 226001, India). Indian Journal of Clinical Biochemistry, 18(2), 71-79 (English) 2003 Association of Clinical Biochemists of India. CODEN: IJCBEY. ISSN: 0970-1915. DOCUMENT TYPE: Journal CA Section: 2 (Mammalian Hormones) Guggulsterone, a mixt. of cis (E) and trans (Z) isomers (7:3 wt./wt.) was synthesized from 16-DPA. The isomers were sepd. by column chromatog. 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 biochem. parameters in ischemic rats. The cardioprotective activity of guggulsterone and of both the isomers were compared with that of gemfibrozil at the same doses. 95975-55-6 and 7683-59-2 which are cas registry numbers of chemicals are mentioned. Guggulsterone and both the isomers at tested concns. (5-20mM) inhibited oxidative degrdn. of lipids in human low-d. lipoprotein and rat liver microsomes induced by metal ions in vitro. The drug counteracted against the generation of superoxide anions (O2) 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 mukul that contains isomers E & Z in the ratio of wt./wt. are the same. .