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苦参总黄酮体内外抗肿瘤作用实验研究

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目的:考察苦参总黄酮(kushen flavonoids,KS-Fs)的体内外抗肿瘤作用.方法:采用甲基噻唑基四唑(methyl thiazolyl tetrazolium,MTT)比色法检测KS-Fs对多种肿瘤细胞株的生长抑制作用;构建S180肉瘤、H22肝癌和Lewis肺癌小鼠肿瘤模型和人非小细胞肺癌H460、食管癌Eca-109裸小鼠移植肿瘤模型,研究KS-Fs体内抗肿瘤作用;急性毒性试验考察KS-Fs的毒副作用.结果:KS-Fs和苦参酮(kurarinone,Kur)在体外有比苦参总碱(kushen alkaloids,KS-As)更强的细胞毒作用(半数抑制率:KS-Fs 4.9~29.4 道道地地μg/ml,Kur 2.0~13.1 μg/ml,KS-As>200 μg/ml).体内研究表明KS-Fs和Kur不仅能有效抑制小鼠H22肝癌、S180肉瘤、Lewis肺癌(瘤质量抑瘤率6O%~80%),而且能显著抑制人非小细胞肺癌H460和人食管癌Eca-109裸小鼠移植肿瘤的生长(瘤质量抑瘤率在41%~47%).小鼠口服和静脉注射KS-Fs的最大耐受剂量分别大干2.8 g/kg和750 mg/kg,远远超过苦参碱(口服半数致死量为1.18 g/kg),且无明显毒副作用.结论:研究表明KS-Fs或Kur是新颖的高效低毒的抗肿瘤候选药物.
Antitumor activities of kushen flavonoids in vivo and in vitro
Objective: To explore the antitumor activities of kushen (Sophora flavescens) flavonoids (KS-Fs) in vivo and in vitro. Methods: Cell proliferation was assayed by using methyl thiazolyl tetrazolium (MTT) method. H22 hepatocellular carcinoma and S180 sarcoma were induced in ICR mice. Lewis lung carcinoma was induced in C57BL/6 mice. H460 and Eca-109 tumor were induced in Balb/c nude mice by injecting 5 ×105 or 5 ×106 tumor cells in the right flank, respectively. Results: KS-Fs could inhibit the growth of a variety of human tumor cell lines (A549, SPC-A-1, NCI-H460, etc.) in vitro. The antitumor efficacies were confirmed in the mice models of H22, S180 and Lewis lung tumors and the nude mice models of human H460 and Eca-109 xenografted tumors. The oral or intravenous maximum tolerated dose of KS-Fs was more than 2.8 g/kg or 750 mg/kg respectively, far more than the oral medial lethal dose of kushen alkaloids (≤1.18 g/kg). No adverse reactions were observed. Conclusion: These results suggest that KS-Fs or kurarinone may be developed as a novel antitumor agent.

Sophora flavescensflavonesantineoplastic agentsmice

孙明瑜、左剑、段继峰、韩军、范士明、张炜、朱丽芳、姚明辉

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上海中医药大学曙光医院,上海中医药大学肝病研究所,上海,201203

上海和记黄埔医药有限公司药理部,上海,201203

第二军医大学药学院生药学教研室,上海,200433

复旦大学上海医学院药理系,上海,200032

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苦参 黄酮类 抗肿瘤药 小鼠

2008

结合医学学报(英文版)
上海市中西医结合学会,上海长海医院

结合医学学报(英文版)

CSTPCD
影响因子:0.711
ISSN:2095-4964
年,卷(期):2008.6(1)
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