| 引用本文: | 杨建苗,王田田,韩旻,许东航,李范珠.线粒体靶向药物联合氯喹克服肿瘤多药耐药研究[J].中国现代应用药学,2021,38(15):1793-1797. |
| YANG Jianmiao,WANG Tiantian,HAN Min,XU Donghang,LI Fanzhu.Study on Mitochondrial Targeted Drugs Combined with Chloroquine to Overcome Multidrug Resistance in Cancer[J].Chin J Mod Appl Pharm(中国现代应用药学),2021,38(15):1793-1797. |
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| 线粒体靶向药物联合氯喹克服肿瘤多药耐药研究 |
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杨建苗1,2, 王田田3,4, 韩旻3, 许东航4, 李范珠1
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1.浙江中医药大学, 杭州 310053;2.浙江省台州医院, 浙江 临海 317000;3.浙江大学药学院, 杭州 310058;4.浙江大学医学院附属第二医院, 杭州 310009
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| 摘要: |
| 目的 研究线粒体靶向药物三苯基膦修饰的多柔比星（triphenylphosphine-doxorobicin，TPP-DOX）联合自噬抑制剂氯喹逆转慢性白血病耐药细胞K562/ADR的耐药作用。方法 制备线粒体靶向药物TPP-DOX；采用CCK8法检测TPP-DOX、DOX及二者联合氯喹引起的K562/DOX细胞毒性情况；流式分析TPP-DOX、DOX及二者联合氯喹入胞情况及周期抑制情况；比色法分析凋亡因子caspase-3和caspase-9的表达。结果 TPP-DOX联合氯喹可明显逆转K562/DOX耐药情况，提高caspase-3和caspase-9的表达。TPP-DOX并不能引起细胞周期阻滞，说明TPP-DOX并未通过入核发挥作用。结论 TPP-DOX联合氯喹可有效克服K562/DOX细胞耐药情况。 |
| 关键词: 线粒体靶向 氯喹 多药耐药 三苯基膦 多柔比星 |
| DOI：10.13748/j.cnki.issn1007-7693.2021.15.001 |
| 分类号:R965.1 |
| 基金项目:浙江省自然科学基金项目（LY18H300004，LY15H300001）；台州市科技计划项目（1801ky04） |
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| Study on Mitochondrial Targeted Drugs Combined with Chloroquine to Overcome Multidrug Resistance in Cancer |
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YANG Jianmiao1,2, WANG Tiantian3,4, HAN Min3, XU Donghang4, LI Fanzhu1
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1.Zhejiang Chinese Medical University, Hangzhou 310053, China;2.Taizhou Hospital of Zhejiang Province, Linhai 317000, China;3.College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China;4.The Second Affiliated Hospital of Zhejiang University, School of Medicine, Hangzhou 310009, China
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| Abstract: |
| OBJECTIVE To study the reversal effect of mitochondrial targeting drug triphenylphosphine-doxorobicin (TPP-DOX) combined with autophagy inhibitor chloroquine on drug resistance of K562/ADR cells in chronic leukemia. METHODS Mitochondrion targeting drug TPP-DOX was prepared. Then CCK8 method was used to measure cell cytotoxicity of K562/DOX after the treatment of TPP-DOX, DOX and their chloroquine combinations. Cell uptake and cell cycle arrest of TPP-DOX, DOX and their chloroquine combination were measured through flow cytometer. The expression of caspase-3 and caspase-9 were examined by using a colorimetric method. RESULTS TPP-DOX combined with chloroquine significantly reversed the drug resistance of K562/DOX cell, and increased the expression of caspase-3 and caspase-9. TPP-DOX couldn't cause cell cycle arrest, indicating that TPP-DOX did not play a role through nuclear entry. CONCLUSION TPP-DOX and chloroquine successfully overcame the drug resistance of K562/DOX. |
| Key words: mitochondrion targeting chloroquine multidrug resistance triphenylphosphine doxorubicin |
