来自多花多孔菌的新型苯并呋喃脯氨酰内肽酶抑制剂Kynapcin - 13和 - 28。

kynapcin-13 and -28, new benzofuran prolyl endopeptidase inhibitors from polyozellus multiplex.

作者信息

Kim Sang-In, Park In-Hye, Song Kyung-Sik

机构信息

Division of Applied Biology and Chemistry, College of Agriculture and Life Sciences, Kyungpook National University, Daegu, Korea.

出版信息

J Antibiot (Tokyo). 2002 Jul;55(7):623-8. doi: 10.7164/antibiotics.55.623.

DOI:10.7164/antibiotics.55.623

PMID:12243451

Abstract

Two new benzofurans, 5,6-dihydroxybenzofuran-2,3-dicarboxylic acid dimethyl ester (kynapcin-13) and 5,6,5',6'-tetrahydroxy[3,3']bibenzofuranyl-2,2'-dicarboxylic acid 2'-methyl ester (kynapcin-28) were isolated from Polyozellus multiplex, and shown to non-competitively inhibit prolyl endopeptidase (PEP), with the IC50 values of 76.80 and 0.98 microM, respectively. Kynapcin-13 and -28 were less inhibitory to other serine proteases such as chymotrypsin, trypsin, and elastase.

摘要

从多花多孔菌中分离出两种新的苯并呋喃，即5,6 - 二羟基苯并呋喃 - 2,3 - 二羧酸二甲酯（kynapcin - 13）和5,6,5',6'- 四羟基[3,3']联苯并呋喃基 - 2,2'- 二羧酸2'- 甲酯（kynapcin - 28），它们被证明可非竞争性抑制脯氨酰内肽酶（PEP），IC50值分别为76.80和0.98微摩尔。Kynapcin - 13和 - 28对其他丝氨酸蛋白酶如胰凝乳蛋白酶、胰蛋白酶和弹性蛋白酶的抑制作用较小。