埃坡霉素B对A549人肺腺癌细胞的体内外抗肿瘤药效学研究

中国临床药理学与治疗学 ›› 2014, Vol. 19 ›› Issue (11): 1201-1205.

• 基础研究 • 下一篇

埃坡霉素B对A549人肺腺癌细胞的体内外抗肿瘤药效学研究

杨德宣, 李琳娜, 王珊珊, 袁守军

军事医学科学院放射与辐射医学研究所,北京 100850

收稿日期:2013-11-06 修回日期:2014-10-29 出版日期:2014-11-26 发布日期:2014-12-09
通讯作者: 袁守军,男,博士,研究员,研究方向:肿瘤药理。Tel: 010-66930271 E-mail: yuansj@nic.bmi.ac.cn
作者简介:杨德宣,男,硕士,实验师,研究方向:肿瘤药理。Tel: 010-66931215 E-mail: dexuanyang@163.com
基金资助:
重大新药创制国家科技重大专项综合性新药研究开发技术大平台项目(2012ZX09301003-001)

Evaluation of anti-tumor effect of epothilone B on human lung cancer A549 cell in vitro and in vivo

YANG De-xuan, LI Lin-na, WANG Shan-shan, YUAN Shou-jun

Institute of Radiation Medicine, Academy of Military Medical Sciences, Beijing 100850, China

Received:2013-11-06 Revised:2014-10-29 Online:2014-11-26 Published:2014-12-09

摘要/Abstract

摘要： 目的观察埃坡霉素B在体内外对A549人肺腺癌细胞生长的抑制作用。方法用MTT法观察埃坡霉素B体外作用 72 h 对A549人肺腺癌细胞增殖的抑制作用;用A549人肺腺癌裸鼠移植瘤模型评价埃坡霉素B在 1.0、0.5、0.25 mg/kg 剂量下,给药2~3次后的体内抗肿瘤活性。结果实验结果显示,埃坡霉素B在体外对人肺腺癌细胞A549抑制作用的IC₅₀为(0.53±0.11) nmol/L,实际检测的最大抑制率为 68.6%。体内实验表明受试物对A549人肺腺癌裸鼠移植瘤具有较强的抑制作用,并呈现出良好的剂量依赖性。给予 1.0、0.5、0.25 mg/kg 受试物,第一次实验,其对A549裸鼠移植瘤的抑制率分别为78.6%、58.8%和 48.3%;第二次实验,其对A549裸鼠移植瘤的抑制率分别为84.2%、76%和 68.2%。阳性药物紫杉醇 15 mg/kg 多次给药的抑瘤率分别为 56.0%和 85.7%。结论埃坡霉素B在体内外对A549人肺腺癌具有较强的抑制作用。

关键词: 埃坡霉素B, A549, 肺腺癌, 抗肿瘤活性, 移植瘤

Abstract: AIM: To investigate the inhibitory effect of Epothilone B on the human lung cancer A549 cell line in vitro and in vivo. METHODS: The MTT method was used to evaluate the inhibitory effect of Epothilone B on proliferation of A549 cell line for 72 h; Xenotransplanted nude mice model with human lung cancer A549 was used to evaluate Epothilone B antitumor activity on 1.0, 0.5, 0.25 mg/kg concentration. RESULTS: MTT inspection showed that the IC₅₀ of Epothilone B was (0.53±0.11) nmol/L. In addition, the maximum inhibition rate was 68.6%. The data from experiments in vivo indicated that Epothilone B had a strong inhibitory effect in dose-dependent manner on A549 human lung cancer xenografts in nude mice. The inhibition rates were 78.6%, 58.8% and 48.3% for the first experiment when the administrated concentration was 1.0, 0.5, 0.25 mg/kg, and the inhibition rates of the second experiment were 84.2%, 76.0% and 68.2%, moreover, the inhibition rates of paclitaxel at a multiple dose of 15 mg/kg were 56.0% and 85.7%, respectively. CONCLUSION: Our results indicate that Epothilone B can inhibit the proliferation of A549 cell line in vitro and the growth of xenotransplanted human tumors in nude mice.

Key words: Epothilone B, A549, human lung cancer, anti-tumor effect, xenograft

中图分类号:

R965.2

杨德宣, 李琳娜, 王珊珊, 袁守军. 埃坡霉素B对A549人肺腺癌细胞的体内外抗肿瘤药效学研究[J]. 中国临床药理学与治疗学, 2014, 19(11): 1201-1205.

YANG De-xuan, LI Lin-na, WANG Shan-shan, YUAN Shou-jun. Evaluation of anti-tumor effect of epothilone B on human lung cancer A549 cell in vitro and in vivo[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2014, 19(11): 1201-1205.

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埃坡霉素B对A549人肺腺癌细胞的体内外抗肿瘤药效学研究

Evaluation of anti-tumor effect of epothilone B on human lung cancer A549 cell in vitro and in vivo

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