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来自于中华稻蝗来源的稀有放线菌 Amycolatopsis sp. HCa1 的细胞毒蒽环类抗生素。

Cytotoxic angucyclines from Amycolatopsis sp. HCa1, a rare actinobacteria derived from Oxya chinensis.

机构信息

Institute of Functional Biomolecules, State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing, China.

出版信息

Planta Med. 2011 Dec;77(18):2057-60. doi: 10.1055/s-0031-1280097. Epub 2011 Aug 9.

DOI:10.1055/s-0031-1280097
PMID:21830188
Abstract

Two new angucyclines, named (2R,3R)-2-hydroxy-8- O-methyltetrangomycin (1) and (2R,3R)-2-hydroxy-5-O-methyltetrangomycin (2), together with eight known compounds (3-10), were isolated from the culture of Amycolatopsis sp. HCa1, a rare actinobacteria isolated from the gut of Oxya chinensis. The new structures were elucidated through extensive spectroscopic data analysis, and their absolute configurations were assigned by application of the modified Mosher's method and CD spectrum comparison. Their IN VITRO cytotoxic activities against four cell lines including human cervical cancer cell line (HeLa), human gastric adenocarcinoma cell line (SGC-7901), human lung adenocarcinoma cell line (SPC-A-1), and mouse macrophage cell line (RAW264.7) were then investigated. Compounds 3, 4, 9, and 10 showed potent cytotoxic activities towards the HeLa cells with IC (50) values of 0.27, 0.11, 0.56, and 0.39 µM, respectively.

摘要

从中华稻蝗肠道中分离得到的稀有放线菌 Amycolatopsis sp. HCa1 的发酵产物中分离得到了两个新的蒽环类化合物,分别命名为(2R,3R)-2-羟基-8-O-甲基四放线菌素(1)和(2R,3R)-2-羟基-5-O-甲基四放线菌素(2),以及另外 8 个已知化合物(3-10)。通过广泛的光谱数据分析阐明了新结构,并通过应用改进的 Mosher 法和 CD 光谱比较确定了它们的绝对构型。然后研究了它们对四种细胞系(人宫颈癌细胞系(HeLa)、人胃腺癌细胞系(SGC-7901)、人肺腺癌细胞系(SPC-A-1)和小鼠巨噬细胞系(RAW264.7))的体外细胞毒性活性。化合物 3、4、9 和 10 对 HeLa 细胞表现出很强的细胞毒性活性,IC(50)值分别为 0.27、0.11、0.56 和 0.39µM。

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