Yang Yi, Zhang Yang, Liu Dong, Li-Weber Min, Shao Bing, Lin Wenhan
State Key Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing 100191, People's Republic of China; Beijing Key Laboratory of Diagnostic and Traceability Technologies for Food Poisoning, Beijing Center for Disease Control and Prevention, Beijing 100013, China.
State Key Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing 100191, People's Republic of China.
Fitoterapia. 2015 Jun;103:277-82. doi: 10.1016/j.fitote.2015.04.016. Epub 2015 Apr 30.
Chemical examination of the barks of mangrove plant Ceriops tagal resulted in the isolation of six new dolabrane-type diterpenes with the trivial names of tagalenes A-F (1-6), together with 10 known analogues. The structures of new compounds were elucidated by extensive spectroscopic data analyses. Tagalenes A-C (1-3) are characterized by 18-nordolabrane scaffold, while tagalene F (6) featured by a 2,3-seco dolabrane derivative. Antitumor assay revealed that seven compounds exhibited potent inhibitory effects against a panel of tumor cell lines with IC50<10 μM, while tagalsin C (8) exerted the most potent activities in comparison with the IC50 values of the rest compounds. The primary structure-activity relationship is discussed. Tagalsin C also exerted the potent effects against a panel of drug-resistant human tumor cell lines, indicating it to be a promising molecule for further evaluation as an antitumor lead compound.
对红树植物角果木的树皮进行化学分析，结果分离出六种新的多拉烷型二萜，其俗名为他加林A - F（1 - 6），以及10种已知类似物。通过广泛的光谱数据分析阐明了新化合物的结构。他加林A - C（1 - 3）的特征是具有18 - 去甲多拉烷骨架，而他加林F（6）的特征是2,3 - 裂环多拉烷衍生物。抗肿瘤试验表明，七种化合物对一组肿瘤细胞系表现出强效抑制作用，IC50 < 10 μM，而与其余化合物的IC50值相比，他加辛C（8）表现出最强的活性。讨论了初步的构效关系。他加辛C对一组耐药人肿瘤细胞系也有强效作用，表明它是一种有前景的分子，可作为抗肿瘤先导化合物进行进一步评估。
