四纤维蛋白溶菌素，一种新型纤维蛋白原受体拮抗剂。I. 分类、发酵、分离、特性及生物学活性。

Tetrafibricin, a novel fibrinogen receptor antagonist. I. Taxonomy, fermentation, isolation, characterization and biological activities.

作者信息

Kamiyama T, Umino T, Fujisaki N, Fujimori K, Satoh T, Yamashita Y, Ohshima S, Watanabe J, Yokose K

机构信息

Nippon Roche Research Center, Kanagawa, Japan.

出版信息

J Antibiot (Tokyo). 1993 Jul;46(7):1039-46. doi: 10.7164/antibiotics.46.1039.

DOI:10.7164/antibiotics.46.1039

PMID:8360097

Abstract

Tetrafibricin is a novel fibrinogen receptor antagonist produced by Streptomyces neyagawaensis NR0577. It was isolated from the culture broth by Diaion HP-21 adsorption, MeOH extraction, MCI GEL CHP-20P column chromatography, preparative HPLC and Toyopearl HW-40 SF column chromatography. The physico-chemical properties of tetrafibricin indicated that the structure of tetrafibricin is different from the known peptide fibrinogen receptor antagonists and closely related to the polyene macrolide antibiotics. Tetrafibricin strongly inhibited the binding of fibrinogen to its receptors with an IC50 of 46 nM. It also inhibited ADP-, collagen-, and thrombin-induced aggregation of human platelets with IC50s of 5.6, 11.0 and 7.6 microM, respectively.

摘要

四纤维蛋白溶菌素是由根岸链霉菌NR0577产生的一种新型纤维蛋白原受体拮抗剂。它通过Diaion HP - 21吸附、甲醇萃取、MCI GEL CHP - 20P柱色谱、制备型高效液相色谱和Toyopearl HW - 40 SF柱色谱从发酵液中分离得到。四纤维蛋白溶菌素的物理化学性质表明，其结构不同于已知的肽类纤维蛋白原受体拮抗剂，与多烯大环内酯类抗生素密切相关。四纤维蛋白溶菌素强烈抑制纤维蛋白原与其受体的结合，IC50为46 nM。它还分别以5.6、11.0和7.6 microM的IC50抑制ADP、胶原和凝血酶诱导的人血小板聚集。