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| 野黄芩苷对Caco-2细胞中P-gp蛋白表达及活性的影响 |
| Effect of Scutellarin on the Expression and Activity of P-gp in Caco-2 Cells |
| 投稿时间：2014-12-01 |
| DOI： |
| 中文关键词: 野黄芩苷 P-gp 蛋白表达 罗丹明123 Caco-2 |
| 英文关键词:Scutellarin P-gp Protein expression Rhodamine-123 Caco-2 |
| 基金项目:广东省重点实验室建设项目（编号：2011A060901014）、国家科技支撑计划项目（编号：2012BAI29B09）、广东省重大科技专项（编号：2012A080202013）和十二五重大专项（编号：2012ZX09506 001 004） |
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| 中文摘要: |
| 摘 要 目的： 研究野黄芩苷对Caco-2细胞中P 糖蛋白（P-gp）表达及活性的影响。 方法: 野黄芩苷（25，50及100 μmol·L-1）与Caco-2细胞共孵育24 h，48 h及72 h后，通过western blot方法检测野黄芩苷对Caco-2细胞中P-gp蛋白表达的影响；通过罗丹明123转运试验，测定罗丹明123在Caco-2细胞内的累积量变化，以考察野黄芩苷对P-gp活性的影响。结果:野黄芩苷对Caco-2细胞中P-gp蛋白表达具有诱导作用，孵育24 h后，野黄芩苷（25，50及100 μmol·L-1）对P-gp蛋白的上调倍数分别为2.34，2.65，2.00；孵育48 h后，野黄芩苷上调P-gp蛋白表达2.70，4.66，3.13倍；孵育72 h后，野黄芩苷（25，50及100 μmol·L-1）对P-gp蛋白的上调倍数分别为2.82，2.62，1.84。野黄芩苷上调Caco-2细胞中P-gp蛋白表达的同时增加P-gp外排泵活性，孵育24 h后，野黄芩苷（25，50及100 μmol·L-1）降低胞内罗丹明123累积量至70.6%，66.6%，76.6%；孵育48 h后，胞内罗丹明123累积量降低至55.6%，37.5%，65.2%；孵育72 h后，胞内罗丹明123累积量降低至45.5%，53.9%，60.3%。结论: 野黄芩苷诱导Caco-2细胞中P-gp的蛋白表达，并能增加P-gp外排泵活性。 |
| 英文摘要: |
| ABSTRACT Objective: To investigate the effect of scutellarin on P-gp protein expression and activity in Caco-2 cells. Methods: Scutellarin (25, 50 and 100 μmol·L-1) was incubated with Caco-2 cells respectively for 24 h, 48 h and 72 h. The expression of P-gp was determined by western blot assay and the activity of P-gp was determined by Rhodamine-123 assay. Results: P-gp protein expression levels were significantly increased by scutelarin. After the incubation for 24 h with scutellarin, P-gp protein expression was up regulated 2.34, 2.65 and 2.00fold in Caco-2 cells. After the incubation with scutellarin for 48 h, P-gp protein expression was up regulated 2.70, 4.66 and 3.13 fold. After the incubation with scutellarin for 72 h, P-gp protein expression was up regulated 2.82, 2.62 and 1.84 fold. The intracellular accumulation of Rhodamine-123 was significantly decreased by scutellarin, indicating that the efflux transport activity of P-gp was increased by scutellarin in Caco-2 cells. Conclusion:Scutellarin can significantly up regulate P-gp protein expression and increase the efflux transport activity of P-gp in Caco-2 cells. |
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