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- W1567248722 abstract "Coronary heart disease is the leading cause of morbidity and mortality in the developed countries, which is due to abnormal deposition of lipids in the inner walls of coronary arteries. Higher levels of low-density lipoprotein (LDL) cholesterol are believed to be a major risk factor of coronary heart disease. Thus, inhibition of de novo cholesterol biosynthesis has been known to be one of the most efficient approaches in the regulation of LDL cholesterol levels. 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. HMG-CoA reductase inhibitors have also been shown to decrease the synthesis of other biologically important isoprenoid compounds derived from mevalonate, including ubiquinone and dolichol. And there has been continued interest in developing hypolipidemic agents that inhibit the enzymes involved specifically in the later stages of cholesterol biosynthesis. Cultured animal cells and intact animals have generally been used for the screening of cholesterol biosynthesis inhibitors. Coverage of the review includes chemical and biological aspects of the cholesterol biosynthesis inhibitors originated from microorganisms and their semisynthetic and biotransformed analogues reported to the present." @default.
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- W1567248722 date "2006-01-01" @default.
- W1567248722 modified "2023-10-16" @default.
- W1567248722 title "Cholesterol Biosynthesis Inhibitors of Microbial Origin" @default.
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- W1567248722 doi "https://doi.org/10.1016/s1572-5995(06)80039-6" @default.
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