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作 者:李珊 柳熠鑫 任菲菲 李相晨 张志清[1] LI Shan;LIU Yixin;REN Feifei;LI Xiangchen;ZHANG Zhiqing(The Second Hospital of Hebei Medical University,Shijiazhuang 050000,Hebei,China)
机构地区:[1]河北医科大学第二医院,河北石家庄050000
出 处:《中国临床药理学与治疗学》2023年第3期331-340,共10页Chinese Journal of Clinical Pharmacology and Therapeutics
基 金:河北省自然科学基金(H2021206384)。
摘 要:多药耐药(multidrug resistance, MDR)是临床上肿瘤患者复发及化疗失败的主要因素,其发生机制较为复杂,目前研究最为深入的机制之一为肿瘤细胞膜上P-糖蛋白(P-glycoprotein, P-gp)过表达所致。大多数化疗药物为P-gp的底物,肿瘤细胞会通过P-gp介导的主动转运将化疗药物转运到胞外,使细胞内有效药物浓度降低,从而产生耐药性,导致临床疗效下降。P-gp的逆转剂可通过下调P-gp表达和转运活性,减少化疗药物从胞内泵出,增强肿瘤细胞对化疗药物的敏感性,从而提高治疗效果。本文将对可逆转P-gp介导的MDR的天然植物活性成分及其调控机制进行总结,为临床及相关研究提供参考。Multidrug resistance(MDR)is the main factor of tumor recurrence and chemotherapy failure in clinical practice.Its mechanism is relatively complex,and one of the most thoroughly studied mechanism is the overexpression of P-glycoprotein(P-gp)on tumor cell membrane.Most of the chemotherapy drugs are p-gp substrates,and tumor cells will transport the chemotherapy drugs to the extracellular through p-gp mediated active transport,so that the concentration of effective drugs in the cell is reduced,resulting in drug resistance,leading to the decline of clinical efficacy.The reversal agent of P-gp can reduce the intracellular pumping of chemotherapeutic drugs by regulating the expression and transport activity of P-gp,and enhance the sensitivity of tumor cells to chemotherapeutic drugs,thus improving the therapeutic effect.In this paper,we will summarize the natural plant active ingredients that can reverse P-gp mediated MDR to provide reference for clinical and related studies.
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