Recent studies have indicated that multidrug resistance (MDR) can significantly limit the effects of conventional chemotherapy. In this study, PT (Pachymic acid and dehydrotumulosic acid) are the two major triterpenoid components purified and identified in P. cocos. A liposomal co-delivery system encapsulating doxorubicin (DOX) and PT was prepared. Notably, the mechanism of PT reversed P-glycoprotein (P-gp) mediated MDR mainly relied on the inhibition of the P-gp function, which further decreased the levels of P-gp and caveolin-1 proteins. In drug-resistant MCF cells, co-administration with 5 μg/ml PT significantly enhanced sensitivity of DOX. Finally, liposome-mediated co-delivery with PT significantly improved the anti-tumor effect of DOX in tumor-bearing mice when compared to other single therapy groups. In conclusion, this study showed for the first time that DOX and PT act synergistically as an “all-in-one” treatment to reverse MDR during tumor treatment and, thus, should be studied further for a wide range of anti-cancer applications.

最近的研究表明，多药耐药性（MDR）可以大大限制常规化学疗法的作用。在这项研究中，PT（巴豆酸和脱氢肿瘤糖酸）是在椰子中纯化和鉴定的两个主要三萜类成分。。制备了包封阿霉素（DOX）和PT的脂质体共递送系统。值得注意的是，PT逆转P-糖蛋白（P-gp）介导的MDR的机制主要依赖于对P-gp功能的抑制，从而进一步降低了P-gp和caveolin-1蛋白的水平。在耐药的MCF细胞中，与5μg/ ml PT共同给药可显着增强DOX的敏感性。最后，与其他单一治疗组相比，脂质体介导的PT与PT共同递送显着改善了DOX在荷瘤小鼠中的抗肿瘤作用。总之，这项研究首次表明，DOX和PT协同作用是一种“多合一”疗法，可在肿瘤治疗过程中逆转MDR，因此，应在广泛的抗癌应用中进行进一步研究。