title: FR171456, a novel cholesterol synthesis inhibitor produced by Sporormiella minima No. 15604. II. Biological activities.
abstract: 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.
authors.affiliation: Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., 5-2-3 Tokodai, Tsukuba, Ibaraki 300-2698, Japan. hidetaka_hatori@po.fujisawa.co.jp
authors.forename: Hidetaka
authors.initials: H
authors.lastname: Hatori
authors.forename: Toshihiro
authors.initials: T
authors.lastname: Shibata
authors.forename: Motoaki
authors.initials: M
authors.lastname: Nishikawa
authors.forename: Hirotsugu
authors.initials: H
authors.lastname: Ueda
authors.forename: Motohiro
authors.initials: M
authors.lastname: Hino
authors.forename: Takashi
authors.initials: T
authors.lastname: Fujii
mesh_terms: 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
chemical_list: D000924:Anticholesteremic Agents; C487953:FR171456; D011973:Receptors, LDL; D002784:Cholesterol