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糖多孢菌 BCC 21906 产生的具有细胞毒性的抗疟安格洛昔酮类化合物 saccharosporones A、B 和 C。

Saccharosporones A, B and C, cytotoxic antimalarial angucyclinones from Saccharopolyspora sp. BCC 21906.

机构信息

National Center for Genetic Engineering and Biotechnology BIOTEC, Thailand Science Park, Klong Luang, Pathumthani 12120, Thailand.

出版信息

J Antibiot (Tokyo). 2013 Jun;66(6):305-9. doi: 10.1038/ja.2013.16. Epub 2013 Apr 3.

DOI:10.1038/ja.2013.16
PMID:23549355
Abstract

Three new angucyclinones, saccharosporones A, B and C, together with (+)-ochromycinone, (+)-rubiginone B2, tetrangulol methyl ether and fujianmycin A, were obtained from fermentation of the terrestrial actinomycete of the genus Saccharopolyspora BCC 21906 isolated from a soil collected in Chanthaburi Province, Thailand. Structures of the new compounds and their relative configurations were assigned by NMR spectral data interpretation. Saccharosporones A and B exhibited antimalarial activity against Plasmodium falciparum K1 with IC50 values of 4.1 and 3.9 μM. Both metabolites also possessed cytotoxic activities against cancer cell lines (KB, MCF-7 and NCI-H187) and nonmalignant Vero cell, while saccharosporone C only showed cytotoxic activity against NCI-H187.

摘要

从泰国庄他武里省采集的土壤中分离到的陆地放线菌 Saccharopolyspora BCC 21906 的发酵产物中,得到了三个新的安格利酮,即 saccharosporones A、B 和 C,以及 (+)-ochromycinone、(+)-rubiginone B2、tetrangulol 甲基醚和 fujianmycin A。通过 NMR 谱数据解释,确定了新化合物的结构及其相对构型。saccharosporones A 和 B 对疟原虫 K1 表现出抗疟活性,IC50 值分别为 4.1 和 3.9 μM。这两种代谢物还对癌细胞系(KB、MCF-7 和 NCI-H187)和非恶性 Vero 细胞具有细胞毒性,而 saccharosporone C 仅对 NCI-H187 具有细胞毒性。

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