文献：mPEG-DPPE/CaP纳米粒子联合递送雷公藤内酯醇和姜黄素用于卵巢癌靶向*

链接：https://www.ingentaconnect.com/contentone/asp/jbn/2018/00000014/00000010/art00008

作者：刘雷； 熊晓媛; 沉明; 茹、丹； 高培; 张翔宇; 黄灿; 孙英； 李、何； 段友容

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雷公藤内酯醇已被证实具有*癌潜力并被广泛用于*癌研究。然而，肝肾毒性限制了其在癌症*中的应用。本研究开发了一种基于mPEG-DPPE/磷酸钙的药物递送系统，共负载雷公藤内酯醇和姜黄素（TP和Curc-NPs）。通过计算药物相互作用系数（CDI）来确定两种药物的最佳浓度。当雷公藤内酯醇浓度为25.22 ng/mL，姜黄素浓度为6.62 μ g/mL时，两种药物对SKOV-3*细胞达到最大的协同杀伤作用。采用超声乳化法制备TP和Curc-NPs。流式细胞术检测结果显示，TP和Curc-NPs可将细胞周期阻滞于S期和G2/M期，并表现出较强的诱导细胞凋亡能力。细胞内活性氧(ROS)检测结果表明姜黄素能降低雷公藤甲素引起的细胞内ROS水平。qTR-PCR检测热休克蛋白(HSP)mRNA水平,结果表明TP和Curc-NPs均能降低HSP70mRNA水平,而对HSP90mRNA水平无明显降低作用。动物实验证明TP和Curc-NPs具有良好的疗效,抑瘤率达68.78%;病理检查结果表明纳米粒对重要脏器无明显毒性作用。综上所述,TP和Curc-NPs在体内外对卵巢癌均有协同作用,姜黄素可能通过*氧化应激作用减轻雷公藤甲素引起的毒性,TP和Curc-NPs可能是一种有前景的卵巢癌*策略。

Triptolide has proven to possess anticancer potential and been widely used for anti-cancer research. However, the liver and kidney toxicity has limited its application in cancer treatment. In this study, a drug delivery system based on mPEG-DPPE/calcium phosphate was developed to co-load triptolide and curcumin (TP and Curc-NPs). The coefficient of drug interaction (CDI) was calculated to determine the optimal concentration of the two drugs. When the concentration of triptolide was 25.22 ng/mL and the concentration of curcumin was 6.62 μg/mL, the two drugs reached the maximum synergistic killing effects on SKOV-3 tumor cells. The TP and Curc-NPs was prepared using ultrasonic emulsification. Flow cytometry results revealed that the TP and Curc-NPs arrested cell-cycle in the S and G2/M phases and exhibited a strong ability to induce apoptosis. Intracellular reactive oxygen species (ROS) results indicated that curcumin could reduce the intracellular ROS level caused by triptolide. The mRNA levels of heat shock protein (HSP) were detected by qTR-PCR and the results showed that the TP and Curc-NPs could lower the HSP70 mRNA level while could not reduce the HSP90 mRNA level. The animal experiments demonstrated the favorable curative effects of the TP and Curc-NPs, and the tumor inhibition rate reached 68.78%. The results of the pathological examinations demonstrated that the nanoparticles had no significant toxic effects on important organs. In conclusion, the TP and Curc-NPs exerted synergistic effects on ovarian cancer in vitro and in vivo, and the toxicity caused by triptolide may be reduced by curcumin through anti-oxidative stress effects. The TP and Curc-NPs could be a promising strategy for ovarian cancer.

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