阿加丁是一种由枝顶孢属真菌FO-7314产生的新型几丁质酶抑制剂。

Argadin, a new chitinase inhibitor, produced by Clonostachys sp. FO-7314.

作者信息

Arai N, Shiomi K, Yamaguchi Y, Masuma R, Iwai Y, Turberg A, Kölbl H, Omura S

机构信息

Research Center for Biological Function, The Kitasato Institute, Tokyo, Japan.

出版信息

Chem Pharm Bull (Tokyo). 2000 Oct;48(10):1442-6. doi: 10.1248/cpb.48.1442.

DOI:10.1248/cpb.48.1442

PMID:11045447

Abstract

A new chitinase inhibitor, designated as argadin (1), was isolated from the cultured broth of a fungal strain FO-7314. The strain was identified as Clonostachys sp. from the morphological characteristics. Argadin was purified from the cultured mycelium by a combination of cation exchange, adsorption and gel filtration chromatographic methods. The structure of argadin was elucidated as cyclo(Nomega-acetyl-L-arginyl-D-prolyl-homoseryl-histidyl-L- 2-aminoadipyl) in which homoseryl gamma-methylene bonded to histidyl alpha-amino residue. The IC50 value of argadin against Lucilia cuprina (blowfly) chitinase was 150 nM at 37 degrees C and 3.4 nM at 20 degrees C. Argadin arrested the moult of cockroach larvae upon injection into the ventral abdominal part.

摘要

一种新的几丁质酶抑制剂，命名为精胍菌素（1），是从真菌菌株FO-7314的培养液中分离得到的。根据形态学特征，该菌株被鉴定为枝顶孢属。通过阳离子交换、吸附和凝胶过滤色谱法相结合的方法，从培养的菌丝体中纯化出精胍菌素。精胍菌素的结构被确定为环（Nω-乙酰-L-精氨酰-D-脯氨酰-高丝氨酰-组氨酰-L-2-氨基己二酰），其中高丝氨酰γ-亚甲基与组氨酰α-氨基残基相连。精胍菌素在37℃时对铜绿丽蝇（绿头苍蝇）几丁质酶的IC50值为150 nM，在20℃时为3.4 nM。将精胍菌素注射到蟑螂幼虫腹部腹面后，它会阻止幼虫蜕皮。