小孢子
立体化学
孢菌
细胞毒性
生物
绝对构型
IC50型
化学
生物化学
植物
体外
雄蕊
小孢子
花粉
作者
Shuai Liu,Hao‐Fu Dai,Gamall Makhloufi,Christian Heering,Christoph Janiak,Rudolf Hartmann,Attila Mándi,Tibor Kurtán,Wernér E.G. Müller,Matthias U. Kassack,Wenhan Lin,Zhen Liu,Peter Proksch
标识
DOI:10.1021/acs.jnatprod.6b00473
摘要
Seven new 14-membered macrolides, pestalotioprolides C (2), D-H (4-8), and 7-O-methylnigrosporolide (3), together with four known analogues, pestalotioprolide B (1), seiricuprolide (9), nigrosporolide (10), and 4,7-dihydroxy-13-tetradeca-2,5,8-trienolide (11), were isolated from the mangrove-derived endophytic fungus Pestalotiopsis microspora. Their structures were elucidated by analysis of NMR and MS data and by comparison with literature data. Single-crystal X-ray diffraction analysis was used to confirm the absolute configurations of 1, 2, and 10, while Mosher's method and the TDDFT-ECD approach were applied to determine the absolute configurations of 5 and 6. Compounds 3-6 showed significant cytotoxicity against the murine lymphoma cell line L5178Y with IC50 values of 0.7, 5.6, 3.4, and 3.9 μM, respectively, while compound 5 showed potent activity against the human ovarian cancer cell line A2780 with an IC50 value of 1.2 μM. Structure-activity relationships are discussed. Coculture of P. microspora with Streptomyces lividans caused a roughly 10-fold enhanced accumulation of compounds 5 and 6 compared to axenic fungal control.
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