The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
FR901512, a Novel HMG-CoA Reductase Inhibitor Produced by an Agonomycetous Fungus No. 14919
II. Biological Profiles
HIDETAKA HATORIBUNJI SATOIKUKO SATOTOSHIHIRO SHIBATAHIROTSUGU UEDAMOTOHIRO HINOTAKASHI FUJII
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2004 Volume 57 Issue 6 Pages 390-393

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Abstract

FR901512, a new specific inhibitor of HMG-CoA reductase, was isolated from the culture of an agonomycetous fungus No. 14919. FR901512 inhibited cholesterol synthesis from [14C] acetate in Hep G2 cells with an IC50 of 1.0nM. An increase of cell surface LDL receptors observed on the FR901512 treated human hepatoma cell line Hep G2 cells. Single oral administration of FR901512 strongly inhibited sterol synthesis in rats. Daily oral administration of FR901512 to beagle dogs decreased plasma cholesterol levels.

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© Japan Antibiotics Research Association
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