Hypolipidemic effects in monkeys of ML-236B,a competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase |
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Authors: | Masao Kuroda Yoshio Tsujita Kazuhiko Tanzawa Dr Akira Endo |
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Affiliation: | (1) Fermentation Research Laboratories, Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, 140 Tokyo, Japan |
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Abstract: | The fungal metabolite ML-236B, a competitive inhibitor of 3-hydroxy-3-methylglutaryl CoA reductase, has been shown to be significantly
effective in lowering serum cholesterol levels in cynomolgus monkeys at doses of 20–50 mg/kg per day. Levels of serum phospholipids
and triglycerides were, however, not significantly changed by the administration of the drug. Of the serum lipoprotein fractions,
a β-lipoprotein corresponding to low density lipoprotein was preferentially reduced by the drug treatment. Fecal excretion
of neutral sterols was unaffected but that of bile acids was slightly elevated by the administration of ML-236B. |
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