LC-DAD/MS/MS检测石地钱中大环双联苄及其微管抑制活性的细胞筛选

摘要

目的:研究苔类植物石地钱中具有微管抑制活性的大环双联苄类化合物.方法:在具有微管抑制活性的石地钱提取部分中,利用LC-DAD/MS/MS方法检测其中的大环双联苄,通过制备高效液相分离和纯化此类化合物、光谱方法鉴定其结构,利用稳定表达EYFP-tubulin的HeLa细胞株考察其抑制微管活性.结果:LC-DAD/MS/MS检测到11个双联苄类化合物,经分离纯化得到其中8个并鉴定为:异地前素c(1)、片叶苔素C(2)、新地前素A(3)、地前素A(4)、异片叶苔素C(5)、片叶苔素B(6),羽苔素E(7)和地前素C(8).化合物4和8具有显著的抑制微管解聚活性.结论:化合物3-7均为首次从该植物中分得,并首次报道联苄类化合物具有微管抑制活性.%AIM: To investigate the microtubule inhibitory active macrocyclic bisbibenzyls from the liverwort Reboulia hemi- sphaerica.METHODS: LC-DAD/MS/MS was used to detect macrocyclic bisbibenzyls from the microtubule depolymerization active extract of R.Hemisphaerica.Preparative HPLC was applied for the isolation and purification of compounds, the structures of which were identified by spectroscopic technology.The antimicrotubule activities of these compounds were examined on human tumor cell line HeLa (cervical carcinoma) stably expressing EYFP-tubulin.RESULTS: Eleven bisbibenzyls were detected and eight of them were obtained and were further identified to be isomarchantin C (1), riccardin C (2), neomarchantin A (3), marchantin A (4), isoriccardin C (5), riccardin B (6), plagiochin E (7), and marchantin C (8).Compounds 4 and 8 showed strong microtubule depolymerization activi- ties.CONCLUTION: Compounds 3-7 have been isolated from this plant for the first time.This is also the first report that bisbibenzyl is the novel class of natural molecule having antimicrotubule activity.