Mohamed Nadia H, Liu Miaomiao, Abdel-Mageed Wael M, Alwahibi Lamya H, Dai Huanqin, Ismail Mady Ahmed, Badr Gamal, Quinn Ronald J, Liu Xueting, Zhang Lixin, Shoreit Ahmed A M
Department of Botany and Microbiology, Faculty of Science, Assiut University, Assiut, Egypt; Department of Biology, Faculty of Science and Art, Samtah, Jazan University, Saudi Arabia.
Key Laboratory of Pathogenic Microbiology and Immunology, Institute of Microbiology, Chinese Academy of Sciences, Beijing 100101, China; University of Chinese Academy of Sciences, Beijing 100049, China; Eskitis Institute, Griffith University, Brisbane, QLD 4111, Australia.
Bioorg Med Chem Lett. 2015 Oct 15;25(20):4615-20. doi: 10.1016/j.bmcl.2015.08.044. Epub 2015 Aug 21.
Three new cardenolides (3, 9 and 10), along with eight known ones, were isolated from the latex of Calotropis procera. The structural determination was accomplished by the 1D- and 2D-NMR spectra as well as HRESIMS analysis. The growth inhibitory activity of the latex and its sub-fractions as well as isolated compounds was evaluated against human A549 and Hela cell lines. The results exhibited that latex had strong growth inhibitory activity with IC50s of (3.37 μM, A-549) and (6.45 μM, Hela). Among the four extracts (hexane, chloroform, ethyl acetate and aqueous), chloroform extract displayed the highest potential cytotoxic activity, with IC50s of (0.985 μM, A-549) and (1.471 μM, Hela). All the isolated compounds displayed various degrees of cytotoxic activity and the highest activity was observed by calactin (1) with IC50s values of (0.036 μM, A-549) and (0.083 μM, Hela). None of these isolated compounds exhibited good antimicrobial activity evaluated by determination of their MICs using the broth microdilution method against various infectious pathogens. The structure-activity relationships for cytotoxic activity were also discussed.
从牛角瓜的乳汁中分离出三种新的强心苷（3、9和10）以及八种已知的强心苷。通过一维和二维核磁共振光谱以及高分辨电喷雾电离质谱分析完成了结构鉴定。评估了乳汁及其亚组分以及分离出的化合物对人A549和Hela细胞系的生长抑制活性。结果表明，乳汁具有很强的生长抑制活性，对A549细胞系的IC50为3.37 μM，对Hela细胞系的IC50为6.45 μM。在四种提取物（己烷、氯仿、乙酸乙酯和水提取物）中，氯仿提取物表现出最高的潜在细胞毒性活性，对A549细胞系的IC50为0.985 μM，对Hela细胞系的IC50为1.471 μM。所有分离出的化合物均表现出不同程度的细胞毒性活性，其中卡拉亭（1）的活性最高，对A549细胞系的IC50值为0.036 μM，对Hela细胞系的IC50值为0.083 μM。通过肉汤微量稀释法测定这些分离出的化合物对各种感染性病原体的最低抑菌浓度，结果表明它们均未表现出良好的抗菌活性。还讨论了细胞毒性活性的构效关系。
