聚合物纳米粒共载槲皮素和咖啡酸苯乙酯提高结肠癌细胞的抗肿瘤疗效。
Co-delivery of quercetin and caffeic-acid phenethyl ester by polymeric nanoparticles for improved antitumor efficacy in colon cancer cells.
机构信息
Department of Molecular Biology and Genetics, Faculty of Arts and Science, Yildiz Technical University, Istanbul, Turkey.
出版信息
J Microencapsul. 2021 Sep;38(6):381-393. doi: 10.1080/02652048.2021.1948623. Epub 2021 Jul 5.
AIM
This study aimed to synthesise quercetin- caffeic-acid phenethyl ester (CAPE)-co-loaded poly(lactic-co-glycolic-acid) (PLGA) nanoparticles (QuCaNP) and investigate their anti-cancer activity on human colorectal carcinoma HT-29 cells.
METHODS
QuCaNPs were synthesised using single-emulsion (o/w) solvent evaporation method. Particle size, zeta potential, polydispersity index, release profile, and surface morphology of QuCaNPs were determined. Cytotoxicity, anti-migration, anti-proliferation and apoptotic activities of QuCaNPs were studied.
RESULTS
Mean diameter of QuCaNP was 237.8 ± 9.670 nm, with a polydispersity index (PDI) of 0.340 ± 0.027. Encapsulation efficiency was 74.28% (quercetin) and 65.24% (CAPE). Particle size and drug content of QuCaNP remained stable for 30 days at -20 °C. The half-maximal inhibitory concentration (IC) values of QuCaNP-treated HT-29 cells were calculated as 11.2 µg/mL (24 h) and 8.2 µg/mL (48 h). QuCaNP treatment increased mRNA levels of caspase-3 (2.38 fold) and caspase-9 (2-fold) and expressions of key proteins in the intrinsic apoptosis pathway in HT-29 cells.
CONCLUSION
Overall, our results demonstrated QuCaNPs exhibits improved anti-cancer activity on HT-29 cells.
目的
本研究旨在合成槲皮素-咖啡酸苯乙酯（CAPE）-共载聚乳酸-共-羟基乙酸（PLGA）纳米粒（QuCaNP），并研究其对人结肠直肠癌细胞 HT-29 的抗癌活性。
方法
采用单乳液（o/w）溶剂蒸发法合成 QuCaNPs。测定 QuCaNPs 的粒径、Zeta 电位、多分散指数、释放曲线和表面形态。研究了 QuCaNPs 的细胞毒性、抗迁移、抗增殖和凋亡活性。
结果
QuCaNP 的平均直径为 237.8±9.670nm，多分散指数（PDI）为 0.340±0.027。槲皮素的包封效率为 74.28%，CAPE 的包封效率为 65.24%。QuCaNP 在-20°C 下稳定 30 天，粒径和药物含量保持稳定。QuCaNP 处理 HT-29 细胞的半最大抑制浓度（IC）值分别为 11.2μg/mL（24 小时）和 8.2μg/mL（48 小时）。QuCaNP 处理可增加 HT-29 细胞中 caspase-3（2.38 倍）和 caspase-9（2 倍）的 mRNA 水平，并表达内在凋亡途径中的关键蛋白。
结论
总的来说，我们的结果表明 QuCaNP 对 HT-29 细胞表现出增强的抗癌活性。
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