Huang Xue-Jiao, Xiong Nan, Chen Bo-Chen, Luo Fan, Huang Min, Ding Zhi-Shan, Qian Chao-Dong
Institute of Molecular Medicine, College of Life Science, Zhejiang Chinese Medical University, Hangzhou, 310053 Zhejiang People's Republic of China.
Institute of Medical Technology, College of Life Science, Zhejiang Chinese Medical University, Hangzhou, 310053 Zhejiang People's Republic of China.
Indian J Microbiol. 2021 Jun;61(2):195-202. doi: 10.1007/s12088-021-00932-8. Epub 2021 Mar 22.
Biphenanthrene compound, 4, 8, 4', 8'-tetramethoxy (1, 1'-biphenanthrene)-2, 7, 2', 7'-tetrol (LF05), recently isolated from fibrous roots of , exhibits antibacterial activity against several Gram-positive bacteria. In this study, we investigated the antibacterial properties, potential mode of action and cytotoxicity. Minimum inhibitory concentrations (MICs) tests showed LF05 was active against all tested Gram-positive strains, including methicillin-resistant (MRSA) and staphylococcal clinical isolates. Minimum bactericidal concentration (MBC) tests demonstrated LF05 was bactericidal against ATCC 29213 and 168 whereas bacteriostatic against ATCC 43300, WX 0002, and other strains of . Time-kill assays further confirmed these observations. The flow cytometric assay indicated that LF05 damaged the cell membrane of ATCC 29213 and 168. Consistent with this finding, 4 × MIC of LF05 caused release of ATP in 168 within 10 min. Checkerboard test demonstrated LF05 exhibited additive effect when combined with vancomycin, erythromycin and berberine. The addition of rat plasma or bovine serum albumin to bacterial cultures caused significantly loss in antibacterial activity of LF05. Interestingly, LF05 was highly toxic to several tumor cells. Results of these studies indicate that LF05 is bactericidal against some Gram-positive bacteria and acts as a membrane structure disruptor. The application of biphenanthrene in the treatment of infection, especially local infection, deserves further study.
最近从[植物名称]须根中分离出的联菲化合物4, 8, 4', 8'-四甲氧基(1, 1'-联菲)-2, 7, 2', 7'-四醇(LF05)对多种革兰氏阳性菌具有抗菌活性。在本研究中，我们对其抗菌特性、潜在作用模式和细胞毒性进行了研究。最低抑菌浓度(MIC)试验表明，LF05对所有测试的革兰氏阳性菌株均有活性，包括耐甲氧西林金黄色葡萄球菌(MRSA)和葡萄球菌临床分离株。最低杀菌浓度(MBC)试验表明，LF05对金黄色葡萄球菌ATCC 29213和枯草芽孢杆菌168具有杀菌作用，而对金黄色葡萄球菌ATCC 43300、WX 0002和其他枯草芽孢杆菌菌株具有抑菌作用。时间杀菌试验进一步证实了这些观察结果。流式细胞术分析表明，LF05破坏了金黄色葡萄球菌ATCC 29213和枯草芽孢杆菌168的细胞膜。与此发现一致的是，4倍MIC的LF05在10分钟内导致枯草芽孢杆菌168中ATP的释放。棋盘试验表明，LF05与万古霉素、红霉素和黄连素联合使用时表现出相加作用。向细菌培养物中添加大鼠血浆或牛血清白蛋白会导致LF05的抗菌活性显著丧失。有趣的是，LF05对几种肿瘤细胞具有高毒性。这些研究结果表明，LF05对一些革兰氏阳性菌具有杀菌作用，并作为膜结构破坏剂起作用。联菲在治疗[细菌名称]感染，尤其是局部感染方面的应用值得进一步研究。
