FR171456, a novel cholesterol synthesis inhibitor produced by Sporormiella minima No. 15604. II. Biological activities.
Novel cholesterol synthesis inhibitors FR171456 and FR173945 were isolated from the culture broth of Sporormiella minima No. 15604. FR171456 strongly inhibited the cholesterol synthesis and up-regulated the LDL-receptor expression in human hepatoma cell line Hep G2. Single oral administration of FR171456 inhibited in vivo hepatic sterol synthesis in rats. And FR171456 shows a significant serum cholesterol-lowering effect in a cholesterol fed rabbit model.
Hatori
Hidetaka
H
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., 5-2-3 Tokodai, Tsukuba, Ibaraki 300-2698, Japan. hidetaka_hatori@po.fujisawa.co.jp
Shibata
Toshihiro
T
Nishikawa
Motoaki
M
Ueda
Hirotsugu
H
Hino
Motohiro
M
Fujii
Takashi
T
D000818:Animals; D000924:Anticholesteremic Agents / Q000494:pharmacology*; D001203:Ascomycota / Q000737:chemistry*; D045744:Cell Line, Tumor; D002784:Cholesterol / Q000031:analogs & derivatives / Q000097:blood / Q000378:metabolism* / Q000494:pharmacology*; D006801:Humans; D008297:Male; D015394:Molecular Structure; D011817:Rabbits; D051381:Rats; D017207:Rats, Sprague-Dawley; D011973:Receptors, LDL / Q000378:metabolism*; D015854:Up-Regulation / Q000187:drug effects
D000924:Anticholesteremic Agents; C487953:FR171456; D011973:Receptors, LDL; D002784:Cholesterol