New antimicrobial compounds produced by endophytic Penicillium janthinellum isolated from Panax notoginseng as potential inhibitors of FtsZ
New antimicrobial compounds produced by endophytic Penicillium janthinellum isolated from Panax notoginseng as potential inhibitors of FtsZ
复制标题
从三七中分离出的内生青霉产生的新抗菌化合物作为 FtsZ 的潜在抑制剂
DOI：
10.1016/j.fitote.2018.10.006
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发表时间：
2018-11-01
期刊：
影响因子：
3.4
通讯作者：
Zhang, Yi-Xuan
中科院分区：
文献类型：
--
作者：
Xie, Jun;Wu, Ying-Ying;Zhang, Yi-Xuan
从三七根、茎、叶中分离到真菌180株，隶属于20属47种。一个分离物，内生真菌Penicilliun janthinellum SYPF 7899，表现出最强的抗菌活性，并研究其次级代谢产物的产生。共从黄拟青霉的固体培养物中分离出三个新化合物，包括旋转异构体la、lb和2，以及八个已知化合物（3-10）。这些化合物的结构是根据1D，2D NMR和电子圆二色谱（ECD）光谱分析以及理论计算确定的。化合物1对枯草芽孢杆菌和金黄色葡萄球菌表现出显著的抑制活性，MIC值分别为15和18 μ g/ml。其他化合物表现出中等或较弱的活性。此外，形态学观察显示B细胞呈杆状。枯草芽孢杆菌生长成长丝，在用化合物1处理后，其长度达到原始细胞长度的1.5- 2倍。S.金黄色葡萄球菌表现出类似的反应，并且在用化合物1处理后膨胀至2倍体积。利用计算机分子对接技术研究了这些化合物与来自B的丝状温度敏感蛋白Z（FtsZ）活性位点之间的相互作用。subtilis和S.金黄色。化合物Ia、Ib和2显示出与FtsZ的高结合能、强H -键相互作用和疏水相互作用。基于抗菌活性、细胞表型观察和对接研究，化合物1被认为是FtsZ的有希望的抗菌抑制剂。
A total of 180 fungal isolates, belonging to 20 genera and 47 species, were obtained from the roots, stems and leaves of Panax notoginseng. One isolate, the endophytic fungus Penicilliun janthinellum SYPF 7899, displayed the strongest antibacterial activity and was studied for its production of secondary metabolites. In total, three new compounds, including rotational isomers la, 1b and 2 were isolated from the solid cultures of P. janthinellun, as well as eight known compounds (3-10). These structures were determined on the basis of 1D, 2D NMR and electronic circular dichroism (ECD) spectroscopic analyses as well as theoretical calculations. Compound 1 exhibited significant inhibitory activities against Bacillus subtilis and Staphylococcus aureus with MIC values of 15 and 18 jig/ml, respectively. The other compounds showed moderate or weak activities. In addition, morphological observation showed the rod -shaped cells of B. subtilis growing into long filaments, which reached 1.5-to 2 -fold of the length of the original cells after treatment with compound 1. The coccoid cells of S. aureus exhibited a similar response and swelled to a 2 -fold volume after treatment with compound 1. In silico molecular docking was explored to study the binding interactions between the compounds and the active sites of filamentous temperature -sensitive protein Z (FtsZ) from B. subtilis and S. aureus. Compound la, lb and 2 showed high binding energies, strong H -bond interactions and hydrophobic interactions with FtsZ. Based on the antimicrobial activities, cellular phenotype observation and docking studies, compound 1 is considered to be a promising antimicrobial inhibitor of FtsZ.