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Ophiobolins P-T, five new cytotoxic and antibacterial sesterterpenes from the endolichenic fungus Ulocladium sp.

机译:Ophiobolins P-T,五个来自内分泌真菌Ulocladium sp。的新的细胞毒性和抗菌的酯基萜烯。

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摘要

Five ophiobolane sesterterpenes, ophiobolins P-T, and three known compounds, 6-epi-21, 21-O-dihydroophiobolin G, 6-epi-ophiobolin G and 6-epi-ophiobolin K, were isolated from the acetone extract of the endolichenic fungus Ulocladium sp. by using OSMAC method. Their structures were elucidated on the basis of spectroscopic analysis. The absolute configuration of the 18,19-diol moieties in ophiobolin Q was assigned using the Frelek's method. The cytotoxic effects on KB and HepG2 cell lines, antibacterial activity against Bacillus subtilis, methicillin-resistant Staphylococcus aureus, and Bacille Calmette-Guerin were evaluated for all isolated compounds. Ophiobolin T and 6-epi-ophiobolin G exhibited the most potent cytotoxic activity against HepG2 with IC50 of 0.24 and 0.37 mu M, respectively. In antibacterial assay, ophiobolins P and T showed moderate antibacterial activity against B. subtilis and meticillin-resistant S. aureus. Ophiobolin T also displayed moderate antibacterial activity against the Bacille Calmette-Guerin strain
机译:从苔藓内生真菌Ulocladium的丙酮提取物中分离出了五种蛇药酯,蛇药素PT和三种已知化合物6-epi-21,21-O-二氢蛇药素G,6-表蛇药素G和6-表蛇药素K。 sp。通过使用OSMAC方法。在光谱分析的基础上阐明了它们的结构。使用Frelek方法确定ophiobolin Q中18,19-二醇部分的绝对构型。对于所有分离的化合物,均评估了对KB和HepG2细胞系的细胞毒性作用,对枯草芽孢杆菌,耐甲氧西林的金黄色葡萄球菌和芽孢杆菌卡介苗的抗菌活性。蛇夫草素T和6-表鬼臼乙素G对HepG2表现出最强的细胞毒活性,IC50分别为0.24和0.37μM。在抗菌测定中,ophiobolins P和T对枯草芽孢杆菌和耐甲氧西林金黄色葡萄球菌表现出中等的抗菌活性。蛇夫草素T对Bacille Calmette-Guerin菌株也显示出中等的抗菌活性

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