CAJ | 학술논문

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100μmol· 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100μmol·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100μmol·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100μmol·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。
목적：연구야황금감대Caco-2세포중P-당단백（P-gp）표체급활성적영향。방법：야황금감（25，50급100μmol· L-1）여Caco-2세포공부육24 h，48 h급72 h후，통과western blot방법검측야황금감대Caco-2세포중P-gp단백표체적영향；통과라단명123전운시험，측정라단명123재Caco-2세포내적루적량변화，이고찰야황금감대P-gp활성적영향。결과：야황금감대Caco-2세포중P-gp단백표체구유유도작용，부육24 h후，야황금감（25，50급100μmol·L-1）대P-gp단백적상조배수분별위2.34，2.65，2.00；부육48 h후，야황금감상조P-gp단백표체2.70，4.66，3.13배；부육72 h후，야황금감（25，50급100μmol·L-1）대P-gp단백적상조배수분별위2.82，2.62，1.84。야황금감상조Caco-2세포중P-gp단백표체적동시증가P-gp외배빙활성，부육24 h후，야황금감（25，50급100μmol·L-1）강저포내라단명123루적량지70.6%，66.6%，76.6%；부육48 h후，포내라단명123루적량강저지55.6%，37.5%，65.2%；부육72 h 후，포내라단명123루적량강저지45.5%，53.9%，60.3%。결론：야황금감유도Caco-2세포중P-gp적단백표체，병능증가P-gp외배빙활성。
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 ex-pression 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. 00-fold 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 ef-flux 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.