KS - 501和KS - 502，来自申克孢子丝菌的新型钙离子及钙调蛋白依赖性环核苷酸磷酸二酯酶抑制剂

KS-501 and KS-502, new inhibitors of Ca2+ and calmodulin-dependent cyclic-nucleotide phosphodiesterase from Sporothrix sp.

作者信息

Nakanishi S, Ando K, Kawamoto I, Kase H

机构信息

Tokyo Research Laboratories, Kyowa Hakko Kogyo Co., Ltd., Japan.

出版信息

J Antibiot (Tokyo). 1989 Jul;42(7):1049-55. doi: 10.7164/antibiotics.42.1049.

DOI:10.7164/antibiotics.42.1049

PMID:2546910

Abstract

New inhibitors of Ca2+ and calmodulin-dependent cyclic-nucleotide phosphodiesterase, KS-501 and KS-502 were isolated from a fungus, Sporothrix sp. KAC-1985. Inhibitory concentration causing 50% inhibition (IC50) values of KS-501 and KS-502 for bovine brain enzyme were 1.8 and 4.3 microM, respectively. The compounds exhibited no or weak inhibition for calmodulin-independent cyclic-nucleotide phosphodiesterases and protein kinase C.

摘要

从真菌Sporothrix sp. KAC - 1985中分离出新型钙和钙调蛋白依赖性环核苷酸磷酸二酯酶抑制剂KS - 501和KS - 502。KS - 501和KS - 502对牛脑酶的半数抑制浓度（IC50）值分别为1.8和4.3微摩尔。这些化合物对不依赖钙调蛋白的环核苷酸磷酸二酯酶和蛋白激酶C无抑制作用或抑制作用较弱。