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[链霉菌属CPCC 202950大米发酵产生的一种新型苯甲酰胺衍生物]

[A new benzamide derivative from rice fermentation of Streptomyces sp. CPCC 202950].

作者信息

Chang Shan-Shan, Chen Ming-Hua, Wang Ren-Zhong, Wu Ye-Xiang, Yang Guo-Hong, Dong Biao, Yu Li-Yan, Gao Zeng-Ping, Si Shu-Yi

机构信息

School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, China.

Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China.

出版信息

Zhongguo Zhong Yao Za Zhi. 2017 Jun;42(11):2097-2101. doi: 10.19540/j.cnki.cjcmm.2017.0093.

Abstract

Eight compounds were isolated from the rice fermentation of Streptomyces sp. CPCC 202950 by a combination of various chromatographic techniques including column chromatography over silica, Sephadex LH-20, flash C₁₈, and reversed-phase HPLC. Their structures were identified as 3-[(3'-amino-3'-oxoprop-1'-en-2'-yl)oxy]benzamide (1), m-hydroxybenzamide (2), leptosphaepin (3), 5-methyluracil (4), feruloylamide (5), p-hydroxyphenylacetoamide (6), vanillamide (7), cyclo (L-val-L-ala) (8). Among them, 1 was a new benzamide analogue, and 2 was a new natural product. In the preliminary assays, none of the compounds 1-8 exhibited obvious inhibition of HIV-1 protease activity, and toxic with the Hela, HepG2, and U2OS cells. (IC₅₀ > 10 μmol•L⁻¹).

摘要

通过硅胶柱色谱、葡聚糖凝胶LH-20、快速C₁₈和反相高效液相色谱等多种色谱技术相结合,从链霉菌属CPCC 202950的大米发酵产物中分离出8种化合物。它们的结构被鉴定为3-[(3'-氨基-3'-氧代丙-1'-烯-2'-基)氧基]苯甲酰胺(1)、间羟基苯甲酰胺(2)、细交链孢菌酮酸(3)、5-甲基尿嘧啶(4)、阿魏酰胺(5)、对羟基苯乙酰胺(6)、香草酰胺(7)、环(L-缬氨酸-L-丙氨酸)(8)。其中,1是一种新的苯甲酰胺类似物,2是一种新的天然产物。在初步试验中,化合物1-8均未表现出对HIV-1蛋白酶活性的明显抑制作用,且对Hela、HepG2和U2OS细胞无毒(半数抑制浓度>10 μmol•L⁻¹)。

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