具有双重活性的新一代 MDR 调节剂：P-糖蛋白抑制剂和 iNOS 诱导剂。
A new generation of MDR modulating agents with dual activity: P-gp inhibitor and iNOS inducer agents.
机构信息
Dipartimento Farmacochimico, Università degli Studi di Bari, Bari, Italy.
出版信息
Toxicol In Vitro. 2011 Feb;25(1):222-30. doi: 10.1016/j.tiv.2010.11.004. Epub 2010 Nov 13.
MultiDrug Resistance (MDR) is due to the ability of some ATPase transporters to efflux chemotherapeutic agents out from tumor cells decreasing the endocellular concentration for the pharmacological effect, causing cancer cells chemoresistance. In the present work, a set of MDR modulating agents (MC89, MC70, PB28, IG9) able to modulate transmembrane ATP-dependent transporter, P-glycoprotein (P-gp), and also to induce inducible nitric oxide synthase (iNOS) expression in a panel of tumor cell lines are presented. All selected compounds, known as potent P-gp modulating agents, stimulated nitric oxide (NO) via iNOS in U937, Caco-2 and MCF7-Adr cell lines. The results displayed a new pharmacological strategy to revert MDR and lead to develop a new class of MDR reverting agents devoid of the limits of P-gp inhibitors third generation.
多药耐药性（MDR）是由于某些 ATP 酶转运蛋白将化疗药物从肿瘤细胞中排出，降低了细胞内的药物浓度，从而产生药理作用，导致癌细胞产生耐药性。在本工作中，一组能够调节跨膜 ATP 依赖性转运蛋白 P-糖蛋白（P-gp）的多药耐药调节剂（MC89、MC70、PB28、IG9），并在一系列肿瘤细胞系中诱导诱导型一氧化氮合酶（iNOS）表达。所有选定的化合物，作为有效的 P-gp 调节剂，通过 iNOS 在 U937、Caco-2 和 MCF7-Adr 细胞系中刺激一氧化氮（NO）的产生。结果显示了一种逆转多药耐药性的新的药理学策略，并导致开发一类新的多药耐药逆转剂，避免了第三代 P-gp 抑制剂的局限性。
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