Fluostatins A and B, new inhibitors of dipeptidyl peptidase III, produced by Streptomyces sp. TA-3391 -: I.: Taxonomy of producing strain, production, isolation, physico-chemical properties and biological properties

被引:30
作者
Akiyama, T [1 ]
Harada, S [1 ]
Kojima, F [1 ]
Takahashi, Y [1 ]
Imada, C [1 ]
Okami, Y [1 ]
Muraoka, Y [1 ]
Aoyagi, T [1 ]
Takeuchi, T [1 ]
机构
[1] Inst Microbial Chem, Shinagawa Ku, Tokyo 141, Japan
关键词
D O I
10.7164/antibiotics.51.553
中图分类号
Q81 [生物工程学(生物技术)]; Q93 [微生物学];
学科分类号
071005 ; 0836 ; 090102 ; 100705 ;
摘要
New inhibitors of dipeptidyl peptidaseIII (EC 3.4.14.4) from human placenta, designated as fluostatins A and B, were discovered in the fermentation broth of a strain isolated in our institute. The strain has been identified as Streptomyces sp. TA-3391 on the basis of taxonomic studies. Fluostatins A and B were purified by Diaion HP-20 chromatography, ethyl acetate extraction, silica gel chromatography and reverse phase preparative HPLC. With the synthetic substrate, arginyl-arginine-2-naphthylamide, the IC50 values of fluostatins A and B were 0.44 and 24.0 mu g/ml, respectively. Fluostatins A and B were slightly inhibitory against other dipeptidyl peptidases. Fluostatin A showed mixed-type (competitive and noncompeptitive) inhibition was human leucine-enkephalin as a substrate, and the inhibition constant (Ki) was 14.2 mu M.
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页码:553 / 559
页数:7
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