Microbial secondary metabolites inhibitor from

Many attempts have been made to find cholesterol biosynthesis inhibitors for development as hypocholesterolemic agents. Microbial secondary metabolites have been used as valuable natural sources in the development of novel cholesterol biosynthesis inhibitors. Mevastatin and lovastatin were isolated from the fungi, Penicillium citrinum and Aspergillus terreus, respectively, as potent inhibitors of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase which is involved in the rate-limiting step of cholesterol synthesis in mammals. These findings have led to the development of statins , which are drugs of choice in the treatment of hypercholesterolemia. 

An important class of active agents that potently inhibit HMG-CoA reductase has evolved from extensive studies for microbial secondary metabolites. Since Brown and Goldstein have reported that the rate of cholesterol biosynthesis is determined by the activity of HMG-CoA reductase [19,20,21], this enzyme has been known to be a prime target for discovery of novel therapeutics against hypercholesterolemia. Several fimgal secondary metabolites were isolated as useful inhibitors of endogenous cholesterol biosynthesis and developed as commercially available hypolipidemics. Endo and Hasumi have extensively reviewed natural, semisynthetic and synthetic HMG-CoA reductase inhibitors in 1993 [22],... 

Screening of Oncogene Function Inhibitors from Microbial Secondary Metabolites... 

The present volume reflects these developments, and there is a growing emphasis on bioactive natural products. Articles in this volume include those on structure-activity relationships of highly sweet natural products, chemical constituents of cchinodenns, diterpenoids from Rabdosia and Eremophila sp., structural studies on saponins, marine sesquiterpene quinoncs and antimicrobial activity of amphibian venoms. The reviews on bioactive metabolites of Phomopsis, cardenolide detection by ELISA, xenocoumacins and bioactive dihydroisocoumarins, CD studies of carbohydrate-molybdate complexes, oncogene function inhibitors from microbial secondary metabolites and Gelsemium and Lupin alkaloids present frontier developments in several areas of natural product chemistry. It is hoped that the present volume, which contains articles by eminent authorities in each field, will be received with the same enthusiasm as the previous volumes of this series. 

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