›› 2017, Vol. 2 ›› Issue (2): 1-5.

• 药学 •    下一篇

美洲大蠊提取物逆转Bel-7402/5-Fu多药耐药性实验研究

  

  1. (1. 大理大学药学与化学学院,云南大理671000;2.上海交通大学药学院,上海200240)
  • 收稿日期:2016-08-09 修回日期:2016-09-15 出版日期:2017-02-15 发布日期:2017-02-15
  • 作者简介:李婷,硕士研究生,主要从事抗肿瘤药理学研究.
  • 基金资助:

    云南省应用基础研究计划资助项目(2013FA043)

Research of Extracts from Periplaneta americana on Reversing Multi-drug Resistance to Bel-7402/5-Fu

  1. (1. College of Pharmacy and Chemistry, Dali University, Dali, Yunnan 671000, China; 2. School of Pharmacy, Shanghai Jiaotong
    University, Shanghai 200240, China)
  • Received:2016-08-09 Revised:2016-09-15 Online:2017-02-15 Published:2017-02-15

摘要:

目的:探讨美洲大蠊提取物逆转Bel-7402/5-Fu多药耐药性的作用及机制。方法:MTT法检测Bel-7402/5-Fu的多药耐
药性及美洲大蠊CⅡ-3和脱脂膏的无毒剂量;Bel-7402/5-Fu 细胞线粒体膜电位及Bcl-2、Bax、Caspase-9、Caspase-3蛋白表达
情况。结果:Bel-7402/5-Fu对5-Fu表现出较高的耐药性,耐药倍数为66.42。CⅡ-3的使用剂量低于93.37 μg/mL,脱脂膏的使
用剂量低于47.81 μg/mL。CⅡ-3和脱脂膏能降低线粒体膜电位,且CⅡ-3较脱脂膏作用强;能抑制Bel-7402/5-Fu细胞Bcl-2
蛋白表达,抑制作用随药物剂量增加而加强;促进Bax 蛋白表达,促进作用随剂量增加而加强;激活下游通路中Caspase-3,
Caspase-9 蛋白表达,且与剂量成正相关。结论:美洲大蠊提取物CⅡ-3和脱脂膏能够有效逆转Bel-7402/5-Fu 的多药耐药
性,其作用机制主要通过降低线粒体膜电位和调控Bcl-2、Bax、Caspase-9、Caspase-3蛋白的表达。

关键词: 美洲大蠊, 逆转, 肝癌, 多药耐药性

Abstract:

Objective: To investigate the effect and mechanism of extracts from Periplaneta americana on reversing multi- drug
resistance to Bel-7402/5-Fu. Methods: Multi-drug resistance to cancer agents and nontoxic dose of the Periplaneta americana extract
CⅡ-3 and skim cream were evaluated by MTT assay. The effect of mitochondrial membrane potential and expressions of Bcl-2, Bax,
Caspase-9 and Caspase-3 were detected in Bel-7402/5-Fu cells affected with CⅡ-3 and skim cream. Results: Bel-7402/5-Fu cells
showed high resistance to 5-Fu, the resistance ratio was 66.42. The dose of CⅡ-3 was lower than 93.37 μg/mL, and the dose of skim
cream was lower than 47.81 μg/mL. CⅡ-3 and the skimmed cream could decrease mitochondrial membrane potential and CⅡ-3 was
stronger than the skimmed cream. CⅡ-3 and the skimmed cream could inhibit the Bcl-2 protein expression of Bel-7402/5-Fu and the
inhibition effect increased with the dose amount; could promote the expression of Bax protein and the promoting effect increased with
the dose amount; could activate downstream pathways of Caspase-9, Caspase-3, and the promoting effect increased with the dose
amount. Conclusion: The Periplaneta americana extract CⅡ-3 and the skimmed cream can effectively reverse MDR in Bel-7402/5-
Fu cells. The mechanism is to decrease of mitochondrial membrane potential, and regulate the expression of Bcl-2, Bax, Caspase-9
and Caspase-3 protein.

Key words: Periplaneta americana, reversion, Hepatocellular carcinoma, multi-drug resistance

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