从海洋细菌短小芽孢杆菌中分离得到的抗锥虫生物碱。
Antitrypanosomal alkaloids from the marine bacterium Bacillus pumilus.
机构信息
Center for Biodiversity and Drug Discovery, Institute for Scientific Research and High Technology Services, City of Knowledge, P.O. Box 0843-01103, Panama.
出版信息
Molecules. 2012 Sep 18;17(9):11146-55. doi: 10.3390/molecules170911146.
Fractionation of the ethyl acetate extract of the marine bacterium Bacillus pumilus isolated from the black coral Antipathes sp. led to the isolation of five compounds: cyclo-(L-Leu-L-Pro) (1), 3-hydroxyacetylindole (2), N-acetyl-β-oxotryptamine (3), cyclo-(L-Phe-L-Pro) (4), and 3-formylindole (5). The structures of compounds 1-5 were established by spectroscopic analyses, including HRESITOF-MS and NMR (1H, 13C, HSQC, HMBC and COSY). Compounds 2, 3 and 5 caused the inhibition on the growth of Trypanosoma cruzi (T. cruzi), with IC50 values of 20.6, 19.4 and 26.9 μM, respectively, with moderate cytotoxicity against Vero cells. Compounds 1-5 were found to be inactive when tested against Plasmodium falciparum and Leishmania donovani, therefore showing selectivity against T. cruzi parasites.
从黑珊瑚 Antipathes sp. 中分离出的海洋细菌 Bacillus pumilus 的乙酸乙酯提取物进行分段处理，得到了五个化合物：环-(L-Leu-L-Pro) (1)、3-羟基乙酰吲哚 (2)、N-乙酰-β-氧色胺 (3)、环-(L-Phe-L-Pro) (4)和 3-甲酰吲哚 (5)。通过包括 HRESITOF-MS 和 NMR (1H、13C、HSQC、HMBC 和 COSY) 在内的光谱分析确定了化合物 1-5 的结构。化合物 2、3 和 5 对 Trypanosoma cruzi（T. cruzi）的生长有抑制作用，IC50 值分别为 20.6、19.4 和 26.9 μM，对 Vero 细胞具有中等的细胞毒性。当测试对疟原虫和利什曼原虫时，化合物 1-5 没有活性，因此对 T. cruzi 寄生虫表现出选择性。
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