玉足海参中具有细胞毒活性的三萜皂苷成分研究  

Cytotoxic Triterpene Glycosides from Sea cucumber Holothuria leucospilota

作　　者：韩华[1,2] 易杨华[2] 张文[2] 王晓华[3] 潘敏翔[4] 李玲[2] 

机构地区：[1]浙江大学动物科学学院,杭州310058 [2]第二军医大学药学院海洋药物研究中心,上海200433 [3]中国人民解放军第202医院药剂科,沈阳110003 [4]中国人民解放军第306医院药学部,北京100101

出　　处：《中国药学杂志》2012年第15期1194-1198,共5页Chinese Pharmaceutical Journal

基　　金：国家高技术研究发展计划"863计划"(2006AA09Z417);国家自然科学基金资助项目(20772155)

摘　　要：目的研究玉足海参(Holothuria leucospilota)具有生物活性的三萜皂苷类成分。方法应用大孔树脂柱色谱、正相硅胶柱色谱、反相硅胶柱色谱和HPLC对玉足海参体内三萜皂苷活性成分进行分离纯化,根据化合物的理化性质和波谱数据鉴定其结构。结果分离并鉴定了3个三萜皂苷类化合物,分别为:leucospilotaside D(1)、holothurin B(2)和holothurin B2(3)。化合物1～3对人宫颈癌细胞HeLa,人胃癌细胞BEL-7402和人乳腺癌细胞MCF-7的抑制率较强。结论化合物1为首次从玉足海参中分离得到。3个化合物均显示显著的体外细胞毒活性。OBJECTIVE To study the bioactive triterpene glycosides in sea cucumber Holothuria leucospilota. METHODS Triterpene glycosides in the sea cucumber were isolated and purified by column chromatography on DA-101, silica gel, reversed-phase silica and reversed HPLC. Their chemical structures were identified on the basis of chemical properties and spectral data~ The eytotox- ieities of the compounds obstained were tested with human cervical carcinoma HeLa cells, gastric carcinoma BEL-7402 cells, and breast carcinoma MCF-7 cells. RESULTS Three triterpene glycosides were obstained from the sea cucumber studied and their struc- tures were identified as leucospilotaside D （ 1 ）, holothurin B （2）, and holothurin B2 （3）. Their inhibition ratios for HeLa, BEL-7402, and MCF-7 cells were high. CONCLUSION Compound 1 is obstained from Holothuria leucospilota for the first time. All glycosides show marked in vitro antitumor activity.

关 键 词：玉足海参 三萜皂苷 细胞毒活性 leucospilotaside D holothurin B holothurin B2 

分 类 号：R931.6[医药卫生—生药学]