中国药业
中國藥業
중국약업
CHINA PHARMACEUTICALS
2014年
21期
31-32,33
,共3页
高春艳%聂珍贵%王俊亚%杨红
高春豔%聶珍貴%王俊亞%楊紅
고춘염%섭진귀%왕준아%양홍
胡桃醌%Caco-2细胞%维拉帕米
鬍桃醌%Caco-2細胞%維拉帕米
호도곤%Caco-2세포%유랍파미
juglone%Caco-2 cells model%verapamil
目的:研究维拉帕米对胡桃醌Caco-2细胞转运特性的影响。方法应用Caco-2细胞模型考察时间、浓度对胡桃醌转运吸收特性的影响,应用P-糖蛋白抑制剂维拉帕米对胡桃醌转运吸收机制进行研究,采用高效液相色谱(HPLC)法测定胡桃醌的浓度,计算其表观渗透系数( Papp )。结果 Caco-2细胞模型,随浓度增加和时间延长,胡桃醌的累积转运量逐渐增加;加用维拉帕米(100μmol/L )后,使AP侧到BL侧的表观渗透系数 PappAP→BL显著增加,而从BL侧到AP侧的表观渗透系数 PappBL→AP降低。结论胡桃醌的转运以被动转运为主,存在P-糖蛋白参与的主动外排,加用维拉帕米后胡桃醌经吸收转运增加,提示维拉帕米可能促进吸收。
目的:研究維拉帕米對鬍桃醌Caco-2細胞轉運特性的影響。方法應用Caco-2細胞模型攷察時間、濃度對鬍桃醌轉運吸收特性的影響,應用P-糖蛋白抑製劑維拉帕米對鬍桃醌轉運吸收機製進行研究,採用高效液相色譜(HPLC)法測定鬍桃醌的濃度,計算其錶觀滲透繫數( Papp )。結果 Caco-2細胞模型,隨濃度增加和時間延長,鬍桃醌的纍積轉運量逐漸增加;加用維拉帕米(100μmol/L )後,使AP側到BL側的錶觀滲透繫數 PappAP→BL顯著增加,而從BL側到AP側的錶觀滲透繫數 PappBL→AP降低。結論鬍桃醌的轉運以被動轉運為主,存在P-糖蛋白參與的主動外排,加用維拉帕米後鬍桃醌經吸收轉運增加,提示維拉帕米可能促進吸收。
목적:연구유랍파미대호도곤Caco-2세포전운특성적영향。방법응용Caco-2세포모형고찰시간、농도대호도곤전운흡수특성적영향,응용P-당단백억제제유랍파미대호도곤전운흡수궤제진행연구,채용고효액상색보(HPLC)법측정호도곤적농도,계산기표관삼투계수( Papp )。결과 Caco-2세포모형,수농도증가화시간연장,호도곤적루적전운량축점증가;가용유랍파미(100μmol/L )후,사AP측도BL측적표관삼투계수 PappAP→BL현저증가,이종BL측도AP측적표관삼투계수 PappBL→AP강저。결론호도곤적전운이피동전운위주,존재P-당단백삼여적주동외배,가용유랍파미후호도곤경흡수전운증가,제시유랍파미가능촉진흡수。
Objective To investigate the influence of verapamil on transport characteristics of juglone Caco-2 cells model. Methods The juglone Caco-2 cells model was adopted to investigate the influence of time and concentration on juglone transport and absorption char-acteristics. The P-glycoprotein ( P-gp ) inhibitor verapamil was used to investigate the juglone transport mechanism. The HPLC method was adopted to detect the juglone concentration. The apparent permeability coefficient ( Papp ) was calculated. Results In the Caco-2 cells model, the cumulative transport quantity of juglone was gradually increased with the concentration increase and the time extend-ing. After adding verapamil ( 100 μmol/L ) , Papp(AP→BL) was significantly increased, while Papp(BL→AP) was decreased. Conclusion The ab-sorption of juglone in Caco-2 cells model is dominated by the passive transference, and the active efflux participated by P-gp exists, after adding juglone in Caco-2 cells, the absorption and transference of juglone, which suggesting that verapamil could promote the ab-sorption.