Cytotoxicity of lissoclibadins and lissoclinotoxins, isolated from a tropical ascidian Lissoclinum cf. badium, against human solid-tumor-derived cell lines.
Cytotoxicity of lissoclibadins and lissoclinotoxins, isolated from a tropical ascidian Lissoclinum cf. badium, against human solid-tumor-derived cell lines.
复制标题
从热带海鞘类 Lissoclinum 中分离出的 lissoclibadins 和 lissoclinotoxins 的细胞毒性。
DOI：
10.1248/bpb.30.385
复制
发表时间：
2007
影响因子：
2
通讯作者：
M. Namikoshi
中科院分区：
文献类型：
--
作者：
T. Oda;K. Kamoshita;S. Maruyama;Kuniko Masuda;M. Nishimoto;Jinzhong Xu;K. Ukai;R. E. Mangindaan;M. Namikoshi
从热带海鞘Lissoclinum cf.检测了Badium对9种人癌细胞系的作用，以评价其潜在的抗癌功效。Lissoclibadins 1（1）和2（2），以及Lissoclinotoxin F（4）显示出六种测试化合物中最强的活性，比抗癌药物顺铂更有效。化合物1具有三聚体结构，化合物2和4是具有分别通过反式和顺式取向的二硫键和硫键连接的二聚体结构的结构异构体。利索克利巴定3（3），由两个硫键连接的二聚化合物，和两个单体化合物（5，6）的活性低于1，2和4。Lissoclibadin 2（2）是最令人感兴趣的化合物，其对结肠癌（DLD-1和HCT 116）、乳腺癌（MDA-MB-231）、肾癌（ACHN）和非小细胞肺癌（NCI-H460）细胞系具有有效的抑制活性，并且在对小鼠进行50 mg/kg单次治疗后没有显示出毒性，并且在大鼠血浆中具有优选的稳定性。
The in vitro growth inhibitory activity of lissoclibadins and lissoclinotoxins isolated from the tropical ascidian Lissoclinum cf. badium against nine human cancer cell lines was examined to evaluate their potential anticancer efficacy. Lissoclibadins 1 (1) and 2 (2), and lissoclinotoxin F (4) showed the strongest activity of the six compounds tested, which were more potent than the anticancer drug cisplatin. Compound 1 has a trimeric structure, and compounds 2 and 4 are structural isomers possessing dimeric structures connected by disulfide and sulfide bonds of trans- and cis-orientations, respectively. Lissoclibadin 3 (3), a dimeric compound connected by two sulfide bonds, and two monomeric compounds (5, 6) were less active than 1, 2, and 4. Lissoclibadin 2 (2) was the most interesting compound possessing potent inhibitory activity against colon (DLD-1 and HCT116), breast (MDA-MB-231), renal (ACHN), and non-small-cell lung (NCI-H460) cancer cell lines and showing no toxicity following a 50 mg/kg single treatment to mice, and preferable stability in rat plasma.