FR901512, a novel HMG-CoA reductase inhibitor produced by an agonomycetous fungus No. 14919. II. Taxonomy of the producing organism, fermentation, isolation and physico-chemical properties.
Novel compounds FR901512 and FR901516 were isolated from the fermentation broth of agonomycete strain No. 14919. FR901512 and FR901516 possess unique tetralin ring in their structure. These compounds were potent inhibitors of the cholesterol synthesis in human hepatoma cell line Hep G2. FR901512 shows strong 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitory activity with an IC50 value of 0.95 nM.
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
Sato
Bunji
B
Sato
Ikuko
I
Shibata
Toshihiro
T
Tsurumi
Yasuhisa
Y
Sakamoto
Kazutoshi
K
Takase
Shigehiro
S
Ueda
Hirotsugu
H
Hino
Motohiro
M
Fujii
Takashi
T
D045744:Cell Line, Tumor; D002784:Cholesterol / Q000378:metabolism; D004952:Esters / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D005658:Fungi / Q000737:chemistry / Q000145:classification / Q000378:metabolism*; D006801:Humans; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D013764:Tetrahydronaphthalenes / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology
D004952:Esters; C487955:FR901512; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; D013764:Tetrahydronaphthalenes; D002784:Cholesterol