Bioactive sulfonyl metabolites from the Red Sea endophytic fungus Penicillium aculeatum

Bioactive sulfonyl metabolites from the Red Sea endophytic fungus Penicillium aculeatum
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DOI:
10.1080/14786419.2021.1917571
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发表时间:
2021-04
影响因子:
2.2
通讯作者:
Usama W. Hawas;Lamia T Abou El-Kassem;E. Ahmed;Rana A. Alghamdi
Usama W. Hawas;Lamia T Abou El-Kassem;E. Ahmed;Rana A. Alghamdi
中科院分区:
化学3区
文献类型:
--
作者:
Usama W. Hawas;Lamia T Abou El-Kassem;E. Ahmed;Rana A. Alghamdi

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摘要从海洋红藻钝顶青霉(Laurencia Obtusa)的内生真菌尖顶青霉(Penicillium Aculeata)的发酵液中分离得到2个新的磺酰代谢物(1)和2个新的磺酰代谢物(1)和4个已知的代谢产物。通过广泛的核磁共振和质谱学分析确定了化合物的结构。化合物2对白色念珠菌具有抑菌活性,抑菌直径分别为20.5 mm和18.0 mm。此外,化合物2对MCF-7的细胞毒作用最强,而化合物1对HCT-116的抑制作用相对较弱,与药物对照紫杉醇相比,其IC50值分别为2.18和5.23µM。图形摘要
Abstract Two new sulfonyl metabolites, pensulfonoxy (1) and pensulfonamide (2), together with four known metabolites were obtained from the fermentation extract of Penicillium aculeatum, an endophytic fungus isolated from the marine red alga Laurencia obtusa. The structures of the compounds were established on the basis of extensive NMR and MS spectroscopic analysis. The ethyl acetate extract exhibited potent antibacterial inhibitory activity against Escherichia coli, while compound 2 exhibited antifungal activity against Candida albicans with inhibition diameters of 20.5 and 18.0 mm, respectively. Moreover, compound 2 also displayed the most potent preferential cytotoxicity against MCF-7, while compound 1 displayed relatively mild activity against HCT-116 with IC50 values of 2.18 and 5.23 µM, respectively, compared to the drug control, paclitaxel. Graphical Abstract