3-Anhydro-6-hydroxy-ophiobolin A,a new sesterterpene inhibiting the growth of methicillin-resistant Staphylococcus aureus and inducing the cell death by apoptosis on K562, from the phytopathogenic fungus Bipolaris oryzae |
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| Authors: | Quan-Xin Wang Jian-Ling Yang Qiu-Yue Qi Li Bao Xiao-Li Yang Miao-Miao Liu Pei Huang Li-Xin Zhang Ji-Long Chen Lei Cai Hong-Wei Liu |
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| Institution: | 1. State Key Lab of Mycology, Institute of Microbiology, Chinese Academy of Sciences, No. 8 Beiertiao, Zhongguancun, Haidian District, Beijing 100190, PR China;2. School of Life Science, University of Science and Technology of China, No. 96 Jinzhai-Road, Hefei 230026, PR China;3. Key Laboratory of Pathogenic Microbiology and Immunology, Institute of Microbiology, Chinese Academy of Sciences, No. 8 Beiertiao, Zhongguancun, Haidian District, Beijing 100190, PR China |
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| Abstract: | A new ophiobolin derivative, 3-anhydro-6-hydroxy-ophiobolin A (1), as well as two known ophiobolin derivatives 3-anhydro-ophiobolin A (2) and 3-anhydro-6-epi-ophiobolin A (3) were isolated from the PDB culture of a phytopathogenic fungus Bipolaris oryzae. The structure of 1 was elucidated through 2D NMR and other spectroscopic techniques. Compound 1 exhibited strong antimicrobial activity against Bacille Calmette–Guerin, Bacillus subtilis, Staphylococcus aureus, and methicillin-resistant Staphylococcus aureus with MIC value of 12.5 μg/mL, and potent antiproliferative activity against cell lines HepG2 and K562 with IC50 of 6.49 μM and 4.06 μM, respectively. Further studies on the cytotoxicity of compound 1 against K562 cells demonstrated that it induced apoptosis, observed by flow cytometric method. Preliminary structure–activity relationships of these ophiobolins and the mechanism of apoptosis induced by 1 were analyzed. |
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| Keywords: | Ophiobolin derivative Antimicrobial Cell apoptosis |
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