人参皂苷结构修饰物HRG的体内抗肿瘤活性研究  

Study on Anti-Tumor Activities of Ginsenoside Structure Modification HRG in Vivo

作　　者：赵凤丽 袁野 孙婷婷 朱雷 黄樱 刘墨祥 李吉萍 

机构地区：[1]扬州大学药理教研室,江苏扬州225001 [2]扬州大学药物研究所,江苏扬州225001

出　　处：《中国药学杂志》2012年第20期1625-1629,共5页Chinese Pharmaceutical Journal

基　　金：国家自然科学基金资助项目(8100159);江苏省卫生厅医学科技发展基金(H200157)

摘　　要：目的探讨新化合物3β,12β,20(S)-三羟基达玛-3-O-β-D-吡喃葡萄糖基(1-2)-β-D-吡喃葡萄糖苷[3β,12β,20(S)-trihy-droxy dammarane-3-O-β-D-glucopyranosyl(1-2)-β-D-glucopyranoside](HRG)即人参皂苷结构修饰物的体内抗肿瘤活性。方法建立肝癌H22鸡胚尿囊膜(CAM)移植瘤模型,观察药物对移植瘤生长、诱导血管生成数、生长抑制率等的影响;将移植瘤切片及HE染色进行光镜组织形态的观察和测定;运用免疫组织化学染色(S-P法)检测移植瘤微血管密度及血管内皮生长因子的表达情况。结果新化合物HRG 25、50、100μg.mL-13个剂量组对肝癌H22-CAM移植瘤生长均有抑制作用,其抑瘤率分别为27.73%、50.02%、64.21%;HRG可显著减少移植瘤诱导血管生成数,且光镜下观察发现各用药组移植瘤组织均存在不同程度坏死,坏死程度与移植瘤诱导血管生成数成反比例关系;HRG可降低移植瘤的微血管密度,并下调血管内皮生长因子的表达。结论 HRG具有体内抗肿瘤活性,能够显著抑制肝癌H22-CAM移植瘤的生长和其诱导的血管生成,其机制可能与降低移植瘤微血管密度和下调血管内皮生长因子表达有关。OBJECTIVE To explore the anti-tumor activities of a new compound 3fl, 1213,20 （S）-trihydroxy dammarane-3-O-β-D- glncopyranosyl （ 1-2 ） -β-D-glucopyranoside （HRG） , which is a substance of ginsenoside structure modification, in vivo. METHODS Liver cancer H22 tumor model on the chick chorioallantoic membrane （CAM） was established to observe the effects of HRG on tumor growth, the number of induced vessels and the growth inhibition rate. The implanted tumors were dyed by hematoxylin-eosin （ HE）, and the morphological properties were studied with light microscope. Immunohistochemistry （SP method） was used to detect the expressions of the implanted tumor＇s MVD and VEGF. RESULTS HRG inhibited the tumor growth at 25, 50 and 100 μg · mL^-1. Compared with the model control group, the inhibitory rates of the tumor growth were 27. 73 % , 50. 02% , and 64. 21% , respectively.HRG significantly reduced the number of tumor-induced vessels. At the same time, there existed different degree necrosis among the treatment groups, and the degree of necrosis had an inverse relationship with the number of tumor-induced vessels. In addition, HRG reduced the MVD of the implanted tunlors, and decreased the expression of VEGF. CONCLUSION HRG has good anti-tumor activities in vivo, and （：an significantly inhibit the growth of liver cancer H22-CAM tumor and the induction of angiogenesis. The mechanisms may be associated with lower tumor MVD and VEGF expression.

关 键 词：3β 12β 20(S)-三羟基达玛-3-O-β-D-吡喃葡萄糖基(1-2)-β-D-吡喃葡萄糖苷 肝癌H22细胞 鸡胚尿囊膜 移植瘤 血管生成 

分 类 号：R285.5[医药卫生—中药学]