A novel bone resorption inhibitor, A-75943 isolated from Streptomyces sp. SANK 61296.
A novel bone resorption inhibitor, A-75943, was isolated from Streptomyces sp. SANK 61296. Its structure was determined to be (1"S,2'R,3"S,4S',5"S)-2-[(3",5"- dimethyl-2"-oxocyclohexan-1"-yl)-6'-oxotetrahydropyran-4'-yl ]acetamide by spectral analyses and chemical conversion of cycloheximide. A-75943 inhibited bone resorption in vitro in a concentration-dependent manner with an IC50 of 0.35 microM, and also displayed an inhibitory effect on bone resorption in thyroid and parathyroid-extracted rats.
Morishita
T
T
Biomedical Research Laboratories, Sankyo Co., Ltd., Tokyo, Japan.
Sato
A
A
Ando
T
T
Oizumi
K
K
Miyamoto
M
M
Enokita
R
R
Okazaki
T
T
D000818:Animals; D015519:Bone Density / Q000187:drug effects*; D001862:Bone Resorption / Q000188:drug therapy*; D005285:Fermentation; D066298:In Vitro Techniques; D008297:Male; D013058:Mass Spectrometry; D011714:Pyrans / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D013055:Spectrophotometry, Infrared; D013302:Streptomyces / Q000145:classification / Q000378:metabolism*
D011714:Pyrans; C114111:A 75943