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新型葛根素纳米混悬剂对结肠癌的体内外抗癌活性,具有高效低毒的特点。

In vitro and in vivo anticancer activity of a novel puerarin nanosuspension against colon cancer, with high efficacy and low toxicity.

机构信息

School of Chemistry and Pharmaceutical Engineering, Shandong Polytechnic University, Jinan 250353, China.

出版信息

Int J Pharm. 2013 Jan 30;441(1-2):728-35. doi: 10.1016/j.ijpharm.2012.10.021. Epub 2012 Oct 23.

Abstract

The present study aims to evaluate the anticancer activity of puerarin nanosuspensions in human colon cancer HT-29 cell line in vitro and in vivo. Puerarin nanosuspensions were prepared by the high-pressure homogenization (HPH) technique. The HT-29 cells were incubated with increasing concentrations of puerarin solution and nanosuspensions for indicated times. MTT evaluated cellular viability and investigated the effect of puerarin on cell proliferation of HT-29. Annexin V-FITC/PI staining method was conducted to determine the influences of the puerarin nanosuspensions on cell cycle and apoptosis. The in vivo anticancer activity of the puerarin nanosuspensions was observed in HT-29 cancer bearing mice. The puerarin nanosuspensions were well re-dispersed in aqueous media a mean diameter about 400-500 nm. Cytotoxicity assay, observation of morphological changes and early apoptosis revealed that the puerarin nanosuspensions could significantly enhance the in vitro anti-proliferation against HT-29 cells compared to the puerarin free solution. The prepared puerarin nanosuspensions in vivo evaluation showed higher anticancer efficacy and lower toxicity compared to the free solution, as shown by changes in tumor volumes, body weights, and survival rates. Based on these data, the potential of the puerarin nanosuspensions to serve as a cancer chemotherapeutic agent for colon cancer could be suggested.

摘要

本研究旨在评估葛根素纳米混悬剂在体外和体内对人结肠癌细胞 HT-29 的抗癌活性。葛根素纳米混悬剂通过高压均质(HPH)技术制备。将 HT-29 细胞与不同浓度的葛根素溶液和纳米混悬剂孵育指定时间。MTT 评估细胞活力,并研究葛根素对 HT-29 细胞增殖的影响。用 Annexin V-FITC/PI 染色法确定葛根素纳米混悬剂对细胞周期和凋亡的影响。在 HT-29 荷瘤小鼠中观察葛根素纳米混悬剂的体内抗癌活性。葛根素纳米混悬剂在水性介质中重新分散,平均粒径约为 400-500nm。细胞毒性试验、形态变化观察和早期凋亡表明,与游离葛根素溶液相比,葛根素纳米混悬剂能显著增强对 HT-29 细胞的体外抗增殖作用。体内评价表明,与游离溶液相比,制备的葛根素纳米混悬剂具有更高的抗癌疗效和更低的毒性,表现为肿瘤体积、体重和存活率的变化。基于这些数据,可以推测葛根素纳米混悬剂有可能成为结肠癌的化疗药物。

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