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天然产物作为癌症多药耐药调节剂。

Natural products as multidrug resistance modulators in cancer.

机构信息

Laboratory of Natural Products, Department of Pharmaceutical Sciences and Natural Products, Central University of Punjab, Mansa Road, Bathinda, 151001, India.

Laboratory of Natural Products, Department of Pharmaceutical Sciences and Natural Products, Central University of Punjab, Mansa Road, Bathinda, 151001, India.

出版信息

Eur J Med Chem. 2019 Aug 15;176:268-291. doi: 10.1016/j.ejmech.2019.05.027. Epub 2019 May 11.

Abstract

Cancer is a prominent cause of death globally. Currently, many drugs that are in clinical practice are having a high prevalence of side effect and multidrug resistance. Risk of tumors acquiring resistance to chemotherapy (multidrug resistance) remains a significant hurdle to the successful treatment of various types of cancer. Membrane-embedded drug transporters, generally overexpressed in cancer, are the leading cause among multiple mechanisms of multidrug resistance (MDR). P-glycoprotein (P-gp) also MDR1/ABCB1, multidrug resistance associated protein 1 (MRP1/ABCC1), MRP2 and breast cancer resistance protein (BCRP/ABCG2) are considered to be a prime factor for induction of MDR. To date, several chemical substances have been tested in a number of clinical trials for their MDR modulatory activity which are not having devoid of any side effects that necessitates to find newer and safer way to tackle the current problem of multidrug resistance in cancer. The present study systematically discusses the various classes of natural products i.e flavonoids, alkaloids, terpenoids, coumarins (from plants, marine, and microorganisms) as potential MDR modulators and/or as a source of promising lead compounds. Recently a bisbenzyl isoquinoline alkaloid namely tetrandrine, isolated from Chinese herb Stephania tetrandra (Han-Fang-Chi) is in clinical trials for its MDR reversal activity.

摘要

癌症是全球主要的死亡原因。目前,许多临床应用的药物具有很高的副作用和多药耐药性。肿瘤对化疗(多药耐药性)产生耐药的风险仍然是成功治疗各种类型癌症的一个重大障碍。膜嵌入的药物转运蛋白通常在癌症中过度表达,是多种多药耐药性(MDR)机制中的主要原因。P-糖蛋白(P-gp)也称为 MDR1/ABCB1、多药耐药相关蛋白 1(MRP1/ABCC1)、MRP2 和乳腺癌耐药蛋白(BCRP/ABCG2)被认为是诱导 MDR 的主要因素。迄今为止,已有几种化学物质在多项临床试验中进行了测试,以评估其对 MDR 的调节活性,但这些物质都没有完全没有副作用,因此需要寻找更新、更安全的方法来解决癌症中当前的多药耐药问题。本研究系统地讨论了各种天然产物类别,即黄酮类、生物碱类、萜类、香豆素类(来自植物、海洋和微生物),作为潜在的 MDR 调节剂和/或有前途的先导化合物的来源。最近,从中国草药Stephania tetrandra(汉防己)中分离出的双苄基异喹啉生物碱即汉防己甲素,正在进行临床试验,以评估其逆转 MDR 的活性。

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