【作者】 孟庆国； 衣松涛； 何杰； 王振华； 姜永涛； 陈猛； 刘珂；

【Author】 MENG, Qing-Guo YI, Song-Tao HE, Jie WANG, Zhen-Hua JIANG, Yong-Tao CHEN,Meng LIU, Ke (School of Pharmacy, Yantai University, Yantai, 264005; Shandong Luye Pharmaceutical Co. Ltd., 264003)

【机构】 烟台大学药学院； 山东绿叶制药有限公司；

【摘要】 基于药物代谢实验结果,设计合成了六个原人参二醇及原人参三醇新衍生物,化合物的结构经1H NMR;13C NMR;ESI-MS确证,部分新化合物经HMQC,HMBC,DEPT 90,DEPE 135。体外细胞毒实验表明,原人参二醇双羟基衍生物对人肝癌细胞株SMMC-7721和人前列腺癌细胞株PC-3M的增殖具有明显的抑制作用,其IC50分别为8．92 μg／ml和10．95 μg／ml,抑制作用明显强于原人参二醇,体外抗肿瘤活性与注射用硫酸长春新碱接近。更多还原

【Abstract】 On the basis of metabolism results from Gesenzosids, six new derivatives of protopanaxadiol and protopanaxatriol have been designed and synthesized. The structures of these compounds have been determined by 1H NMR; 13C NMR; and ESI-MS, or by HMQC, HMBC, DEPT 90, DEPT 135. In vitro cytotoxic experiment indicates that 20(S)-24,25-dihydroxyl-protopanaxadiol has distinct restrain action to the multiplication of the cell strain SMMC-7721 of liver and the cell strain PC-3M of costal not inactived with IC50 8.92μg/mL and 10.95 μg/mL, respectively. The anti-tumor activity is stronger than that of protopanaxadiol and similar to that of the vitriol leurocristine injection.更多还原