摘要
多药耐药(MDR)的产生是临床上治疗肿瘤失败的重要原因之一,而MDR的相关机制却十分复杂。目前认为P-糖蛋白(P-gp)是介导MDR的主要因素之一,它能将不同结构和功能的化疗药物排出细胞外,明显降低化疗的成功率。黄酮类化合物存在于多种植物中,具有广泛的药理活性,近年研究发现,黄酮类化合物具有逆转肿瘤MDR作用,能影响外排转运蛋白特别是P-gp的表达和功能。本文从黄酮类化合物抑制P-gp蛋白表达的分子机制、抑制P-gp的外排功能、阻止P-gp与底物结合等方面来阐述黄酮成分抵抗P-gp介导肿瘤MDR特性的机制,为黄酮类化合物在肿瘤治疗方面的应用提供思路和借鉴。
Multidrug resistance（MDR）is one of the important reasons for the failure of chemotherapy in clinic,whereas the mechanism of MDR is very complicated. At present,it is considered that the efflux protein P-glycoprotein（P-gp）is one of the main factors which can lead to MDR,descreasing the successful rate of chemotherapy because chemotherapeutics with different structures and functions can be effluxed by P-gp. Flavonoids are found in many kinds of plants and have a wide range of pharmacological activi-ties. Besides,recent studies have reported that flavonoids can reverse the MDR of tumor and affect the expression and function of ef-flux transporter,especially P-gp. In this review,we elucidate the mechanisms of flavonoids reversing tumor MDR mediated by P-gp from the following aspects：inhibition of P-gp protein expression,inhibition of P-gp efflux function,and prevention of combining P-gp and its substrate,etc. The review can provide some ideas and references for the application of flavonoids in tumor therapy.
出处
《国际药学研究杂志》
CAS
CSCD
北大核心
2016年第5期818-823,共6页
Journal of International Pharmaceutical Research
基金
上海市人才发展资金资助项目(201565)
上海中医药大学第八批大学生科创项目(201510268042)
