Department of Pharmaceutics, College of Pharmacy, Shandong University, Shandong Province, PR China.
Drug Deliv. 2011 May;18(4):265-71. doi: 10.3109/10717544.2010.536271. Epub 2010 Nov 24.
The mechanism for anti-tumor activity of oridonin (ORI) nanosuspension, prepared by the high pressure homogenization method, was studied using MCF-7 human breast carcinoma cells in vitro. MTT assay, observation of morphologic changes, flow cytometric analysis, and western blot analysis indicated that ORI nanosuspension could significantly intensify the in vitro anti-tumor activity to MCF-7 cells, as compared with ORI solution. Furthermore, ORI nanosuspension induced G₂/M stage proliferation arrest and apoptosis in MCF-7 cells depending on its concentration. In addition, western blot analysis indicated that the pro-caspase-3 protein was not cleaved into the activated form and the expression of anti-apoptotic Bcl-2 protein decreased, on the contrary, the expression of pro-apoptotic Bax protein increased in a dose-dependent manner in ORI nanosuspension-treated cells. These observations indicated that the anti-tumor activity of ORI nanosuspension was intensified by cell-cycle arrest and apoptosis induction.
采用高压匀质法制备冬凌草甲素纳米混悬剂，并研究其在 MCF-7 人乳腺癌细胞体外的抗肿瘤活性机制。MTT 法检测、形态学观察、流式细胞术分析和 Western blot 分析表明，与冬凌草甲素溶液相比，冬凌草甲素纳米混悬剂可显著增强对 MCF-7 细胞的体外抗肿瘤活性。此外，冬凌草甲素纳米混悬剂可诱导 MCF-7 细胞发生 G₂/M 期增殖阻滞和凋亡，并呈现浓度依赖性。此外，Western blot 分析表明，在冬凌草甲素纳米混悬剂处理的细胞中，前半胱氨酸蛋白酶-3 蛋白未被切割成活化形式，抗凋亡 Bcl-2 蛋白的表达降低，而促凋亡 Bax 蛋白的表达则呈剂量依赖性增加。这些观察结果表明，冬凌草甲素纳米混悬剂通过细胞周期阻滞和诱导细胞凋亡来增强抗肿瘤活性。
