一种新型蛋白激酶C抑制剂，RK - 286C（4'-去甲基氨基-4'-羟基星形孢菌素）。I.筛选、分类学、发酵及生物活性。

A new inhibitor of protein kinase C, RK-286C (4'-demethylamino-4'-hydroxystaurosporine). I. Screening, taxonomy, fermentation and biological activity.

作者信息

Osada H, Takahashi H, Tsunoda K, Kusakabe H, Isono K

机构信息

Antibiotics Laboratory, RIKEN, Institute of Physical and Chemical Research, Saitama, Japan.

出版信息

J Antibiot (Tokyo). 1990 Feb;43(2):163-7. doi: 10.7164/antibiotics.43.163.

DOI:10.7164/antibiotics.43.163

PMID:2312404

Abstract

In the course of our screening program using a bleb-forming assay, a new inhibitor of protein kinase C (PKC) was found in the fermentation of a streptomycete. The inhibitor, RK-286C (4'-demethylamino-4'-hydroxystaurosporine), inhibited the morphological change of K562 cells, a human chronic erythroleukemia cell, induced by phorbol 12,13-dibutylate at the concentration of 3 microM. The same concentration of the compound inhibited the activity of PKC in vitro and the aggregation of rabbit platelets induced by collagen and arachidonic acid.

摘要

在我们使用气泡形成试验的筛选项目过程中，在一种链霉菌的发酵产物中发现了一种新型蛋白激酶C（PKC）抑制剂。该抑制剂RK-286C（4'-去甲基氨基-4'-羟基星形孢菌素）在3 microM浓度下可抑制佛波醇12,13-二丁酸酯诱导的人慢性红白血病细胞K562的形态变化。相同浓度的该化合物在体外可抑制PKC的活性以及胶原和花生四烯酸诱导的兔血小板聚集。