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新型金担子素的分离、结构及抗真菌活性

Isolation, structures, and antifungal activities of new aureobasidins.

作者信息

Yoshikawa Y, Ikai K, Umeda Y, Ogawa A, Takesako K, Kato I, Naganawa H

机构信息

Biotechnology Research Laboratories, Takara Shuzo Co., Ltd., Shiga, Japan.

出版信息

J Antibiot (Tokyo). 1993 Sep;46(9):1347-54. doi: 10.7164/antibiotics.46.1347.

Abstract

Aureobasidins are a group of cyclic depsipeptides with antifungal activity and are produced by Aureobasidium pullulans. Aureobasidins are composed of eight amino acids and one hydroxy acid such as 2-hydroxy-3-methylpentanoic acid (Hmp), and highly lipophilic. Five new aureobasidins, S1, S2a, S2b, S3 and S4, which have higher hydrophilicity in reversed phase HPLC than the known aureobasidins A-R, were discovered in a fermentation broth of A. pullulans R106 by means of on-line liquid chromatography/mass spectrometry with electrospray ionization. We identified the structures of the compounds and studied their antifungal activities. Three of the new aureobasidins, S2b, S3 and S4, which have hydroxylated Hmp as the hydroxy acid, were highly active against Candida spp. and Cryptococcus neoformans.

摘要

金耳素是一类具有抗真菌活性的环缩肽,由出芽短梗霉产生。金耳素由八个氨基酸和一种羟基酸(如2-羟基-3-甲基戊酸,Hmp)组成,具有高度亲脂性。通过在线液相色谱/电喷雾电离质谱法,在出芽短梗霉R106的发酵液中发现了五种新的金耳素,即S1、S2a、S2b、S3和S4,它们在反相高效液相色谱中的亲水性高于已知的金耳素A-R。我们确定了这些化合物的结构并研究了它们的抗真菌活性。三种以羟基化Hmp作为羟基酸的新金耳素S2b、S3和S4,对念珠菌属和新型隐球菌具有高度活性。

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