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首页> 外文期刊>RSC Advances >Cytotoxic and antimicrobial indole alkaloids from an endophytic fungus Chaetomium sp. SYP-F7950 of Panax notoginseng
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Cytotoxic and antimicrobial indole alkaloids from an endophytic fungus Chaetomium sp. SYP-F7950 of Panax notoginseng

机译：内生真菌Chaetomium sp。的细胞毒性和抗菌吲哚生物碱。三七SYP-F7950

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Two new compounds chetoseminudin F ( 1 ) and G ( 2 ) together with eleven known compounds were isolated from the solid fermentation products of the endophytic fungus Chaetomium sp. SYP-F7950. The structures of the isolated compounds were elucidated by extensive spectroscopic analyses, including 1D and 2D NMR, and HRFABMS experiments. The absolute configurations of chetoseminudin F ( 1 ) and G ( 2 ) were determined by comparing the electronic circular dichroism (ECD) spectrum with those of the reported references. A plausible biogenetic pathway for compounds 1–6 and 9–13 was proposed. These isolates were also evaluated for their antimicrobial and antitumor activity, revealing that chetoseminudin F ( 1 ) displayed more potent cytotoxicity against MDA-MB-231 cells with an IC _(50) value of 26.49 μmol L ~(?1) more than the common chemotherapeutic agent (paclitaxel). In antimicrobial assay, compounds 6 , 9 , 11 and 12 had strong antibacterial activity against Staphylococcus aureus , Bacillus subtilis , Enterococcus faecium and antifungal activity against Candida albicans with minimum inhibitory concentration (MIC) values ranging from 0.12 to 9.6 μg mL ~(?1) ; meanwhile compounds 6 , 8 , 9 and 12 exhibited strong cytotoxicity with IC _(50) values of 2.75–8.68 μmol L ~(?1) against tumor cell lines A549 and MDA-MB-231. In addition, morphological observation showed that treatment with compounds 6 , 9 and 12 increased the mean length of B. subtilis by 1.6 to 1.8-fold. In silico molecular docking was applied to study the binding interactions between the compounds and the active sites of filamentous temperature-sensitive protein Z (FtsZ) from B. subtilis . Compounds 6 , 9 and 12 displayed the low binding energies, strong H-bond interactions with FtsZ. On the basis of the antimicrobial activities, cellular phenotype observation and docking studies, compounds 6 , 9 and 12 are considered to be a promising antimicrobial inhibitor of FtsZ.
机译：从内生真菌Chaetomium sp。的固体发酵产物中分离出两种新的化合物chetoseminudin F（1）和G（2）以及十一种已知化合物。 SYP-F7950。通过广泛的光谱分析，包括1D和2D NMR以及HRFABMS实验，阐明了分离出的化合物的结构。通过将电子圆二色性（ECD）光谱与报道的参考文献进行比较，确定了chetoseminudin F（1）和G（2）的绝对构型。提出了化合物1-6和9-13的合理生物遗传途径。还对这些分离物的抗微生物和抗肿瘤活性进行了评估，发现chetoseminudin F（1）对MDA-MB-231细胞显示出更强的细胞毒性，IC_（50）值为26.49μmolL〜（？1）。常见的化疗药物（紫杉醇）。在抗菌试验中，化合物6、9、11和12对金黄色葡萄球菌，枯草芽孢杆菌，粪肠球菌和白色念珠菌具有很强的抗菌活性，最小抑菌浓度（MIC）值为0.12至9.6μgmL〜（？1 ）;同时，化合物6、8、9和12对肿瘤细胞A549和MDA-MB-231的IC_（50）值为2.75–8.68μmolL〜（？1），具有较强的细胞毒性。另外，形态学观察表明，用化合物6、9和12处理使枯草芽孢杆菌的平均长度增加了1.6至1.8倍。利用计算机分子对接技术研究化合物与枯草芽孢杆菌丝状温度敏感蛋白Z（FtsZ）的活性位点之间的结合相互作用。化合物6、9和12显示出低的结合能，与FtsZ的强H键相互作用。基于抗微生物活性，细胞表型观察和对接研究，化合物6、9和12被认为是有希望的FtsZ抗微生物抑制剂。

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