FISCALINS - NEW SUBSTANCE-P INHIBITORS PRODUCED BY THE FUNGUS NEOSARTORYA-FISCHERI - TAXONOMY, FERMENTATION, STRUCTURES, AND BIOLOGICAL PROPERTIES

被引：124

作者：

WONG, SM

MUSZA, LL

KYDD, GC

KULLNIG, R

GILLUM, AM

COOPER, R

机构：

[1] Sterling Winthrop Pharmaceuticals Research Division, Malvern, PA, 19355

来源：

JOURNAL OF ANTIBIOTICS | 1993年 / 46卷 / 04期

关键词：

D O I：

10.7164/antibiotics.46.545

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：

Three new compounds, named fiscalins A, B, and C, were found in culture broth produced by a Neosartorya fischeri. These compounds inhibit the binding of radiolabeled substance P ligand to the human neurokinin (NK-1) receptor, with Ki values of 57, 174, and 68 mum, respectively. Detailed spectroscopic and amino acid analyses led to the elucidation of structures for the three fiscalins. The structures contain an indolyl moiety linked to an athranilic acid derived tricyclic system. The absolute configuration of fiscalin A was determined by X-ray crystallography and chiral amino acid analysis. The presence of fiscalins was detected directly in crude cellular extracts using LC-MS methods.

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页码：545 / 553

页数：9

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