Xu Shengtao, Pei Lingling, Li Dahong, Yao Hong, Cai Hao, Yao Hequan, Wu Xiaoming, Xu Jinyi
State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, China; Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, China.
State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, China; Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, China; Key Laboratory of Structure-Based Drug Design & Discovery of Ministry of Education and School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, 103 Wen Hua Road, Shenyang 110016, China.
Fitoterapia. 2014 Dec;99:300-6. doi: 10.1016/j.fitote.2014.10.005. Epub 2014 Oct 12.
A series of enmein-type derivatives were synthesized and assayed for their antimycobacterial effects. The structures of the synthesized compounds were established by (1)H NMR, (13)C NMR and mass spectral analysis. All the compounds were screened for their antimycobacterial properties against Mycobacterium phlei, Mycobacterium smegmatis and Mycobacterium marinum. Compounds 2, 6g and 6i were found to exhibit potent antimycobacterial activity against M. phlei at a concentration of 0.5 μg/mL, which was comparable to that of positive drug streptomycin. Furthermore, five compounds were tested against Mycobacterium tuberculosis H₃₇Rv based on the promising preliminary screening results. Among them, compound 10 showed potent activity with IC₅₀ value of 17.1 μg/mL against M. tuberculosis H₃₇Rv strain. Thus, compound 10 could emerge as a promising lead for further research work.
合成了一系列延命草素型衍生物，并对其抗分枝杆菌作用进行了测定。通过¹H NMR、¹³C NMR和质谱分析确定了合成化合物的结构。对所有化合物针对草分枝杆菌、耻垢分枝杆菌和海分枝杆菌的抗分枝杆菌特性进行了筛选。发现化合物2、6g和6i在浓度为0.5 μg/mL时对草分枝杆菌表现出强效抗分枝杆菌活性，这与阳性药物链霉素相当。此外，基于有前景的初步筛选结果，对五种化合物针对结核分枝杆菌H₃₇Rv进行了测试。其中，化合物10表现出强效活性，对结核分枝杆菌H₃₇Rv菌株的IC₅₀值为17.1 μg/mL。因此，化合物10可能成为进一步研究工作的有前景的先导物。
