对-氨基苯甲酸-4’ 去甲表鬼臼酯的抗氧化与抗肿瘤作用

摘要/Abstract

摘要： 目的研究对-氨基苯甲酸-4' 去甲表鬼臼酯(4-p-amino-benzoinc acid-4 ‘-demethylepipodophyllotoxin ester, PDE) 的体外抗氧化与抗肿瘤活性。方法体外对SGC-7901 细胞的抗肿瘤活性用MTT 比色法, 体内抗肿瘤活性用动物移植瘤法。用TBA 法测大鼠肝自发性, Fe2 +-抗坏血酸诱发的心、肝、肾组织匀浆丙二醛(MDA) 生成, 分光光度法测H2O2 诱导的红细胞溶血。结果 PDE 剂量依赖性地抑制SGC-7901 细胞生长, 作用48 h IC50为84.7 (51.7 ~ 138.9) mg L, 在体内PDE 10 、20 mg kg 对S180 和H22 肿瘤的抑制率分别为25.2%、46.5%和22.9%、39.3%。PDE 浓度依赖性地抑制大鼠肝组织自发性MDA 生成, IC50 为22.7(16.9 ~ 30.4) mg L, 也能浓度依赖性地抑制Fe2 +-AA 诱导的大鼠心、肝、肾组织匀浆MDA 生成, IC50 分别为30.3(13.9 ~ 66.1) 、29.9(20.9 ~42.7) 和13.3(1.8 ~ 96.9) mg L。PDE 对H2O2 诱导的大鼠红细胞溶血也有一定的抑制作用, 40 、80 mg L 的抑制率分别为26.8%和100.2%。结论 PDE 有明显抗氧化及抗肿瘤作用, 二者有一定的关系。

关键词: 对-氨基苯甲酸-4’去甲表鬼臼酯, 抗氧化, 抗肿瘤

Abstract: AIM: To investigate the antitumor and antioxidation effects of 4-p-amino-benzoinc acid-4'-demethylepipodophyllotoxin ester (PDE). METHODS: The in vitro antitumor effects was measured by MTT method, and in vivo antitumor effects was studied by transplanting tumor model of S180 and H22 in mice.The malondialdehyde (MDA) generation in tissues of rats was measured with the thiobarbituric acid (TBA) reaction.H2O2-induced RBC hemolysis was determined with spectrophotometry. RESULTS: PDE strongly inhibited SGC-7901 cell proliferation for 48 h in a concentration-dependent manner with IC50 of 84.7 (51.7-138.9) mg L.In vivo experiments showed that10, 20 mg kg PDE obviously inhibited the growth of S180 and H22 with inhibition rate 25.2%, 46.5%and 22.9%,39.3%, respectively.PDE also significantly inhibited MDA generation spontaneously [IC50 22.7 (16.9-30.4) mg L] or induced by Fe2 +-AA in homogenate of heart, liver and kidneys of rats with IC50 30.3(13.9-66.1), 29.9(20.9-42.7) and 13.3 (1.8-96.9) mg L, respectively.PDE 40, 80 mg L significantly inhibited haemolysis induced by H2O2 with inhibition rate 26.8% and 100.2%, respectively. CONCLUSION: PDE exhibits antitumor and antioxidation effects and there is relationship between the effects.

Key words: 4-p-amino-phenol-4'-denmethylepidophyllotoxin ester, antioxidation, antitumor

中图分类号:

R965.2

陈晓, 王哲元, 张有成, 李文广. 对-氨基苯甲酸-4’ 去甲表鬼臼酯的抗氧化与抗肿瘤作用[J]. 中国临床药理学与治疗学, 2008, 13(3): 288-292.

CHEN Xiao, WANG Zhe-yuan, ZHANG You-cheng, LI Wen-guang. Anti-tumor and antioxidation effects of 4-p-amino-benzoinc acid-4’-demethylepipodophyllotoxin ester[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2008, 13(3): 288-292.

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