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

被引:103
作者
Arai, N
Shiomi, K
Yamaguchi, Y
Masuma, R
Iwai, Y
Turberg, A
Kölbl, H
Omura, S
机构
[1] Kitasato Inst, Biol Funct Res Ctr, Minato Ku, Tokyo 1088642, Japan
[2] Bayer AG, Biol Technol Ctr, Business Grp Anim Hlth, D-51368 Leverkusen, Germany
关键词
chitinase inhibitor; cyclic peptide; Clonostachys; argadin; microbial metabolite;
D O I
10.1248/cpb.48.1442
中图分类号
R914 [药物化学];
学科分类号
100701 [药物化学];
摘要
ii new chitinase inhibitor, designated as argadin (1), a as 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(N-omega-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.
引用
收藏
页码:1442 / 1446
页数:5
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