MDCK-MDR1细胞药物体外吸收模型的建立及验证
取对数生长期的mdck-wt接种于6孔板中,每孔约2×105个/孔细胞,加入打靶质粒2ug:genjet6ul形成的转染复合物悬浮mdck细胞,37℃反应20min,加入新鲜培养基,48h后以1:3比例传3孔,第二天加g418(800ug/ml)进行筛选,大概7天后大量细胞死亡,停止加药,待细胞进入对数生长期后铺单克隆。每3天换药一次,待细胞大量死亡,...
MDCK-hMDR1细胞系的渗透性,并同时测定了添加Pgp抑制剂与不加抑制剂时细胞下层到上层的渗透 性,判定其是否为Pgp的作用底物。 ML120B是IKK2的受体拮抗剂,是理想的抗过敏性鼻炎候选药物 [2] ,分子式为C 19 H 15 ClN 4 O 2 ,结 构式见图1。
摘要: 目的测定ML120B的细胞膜渗透性.方法采用MDCK-hMDR1单层膜细胞测定ML120B的体外跨膜转运率及转运机制.结果药物的被动转运渗透性为678.9nm·s-1,不加P-糖蛋白(Pgp)抑制剂的外排率Efflux值为0.8,添加Pgp抑制剂的Efflux值为0.5.结论ML120B属于高渗透性药物,并不是Pgp的作用底物.关键词: 药剂学;ML120B;...
a triple culture of primary rat BCECs with pericytes and astrocytes, the Caco-2 and MDCK-MDR1 models identified more Pgp drug substrates than the rat brain BBB model [22]. Further- more, the rat brain BBB model resulted in the best cor- relation with in vivo drug permeability data in...
结果:在Caco-2、L-MDR1和MRP2细胞,5、50、500μmol·L-15-ASA从底端(B)→顶端(A)方向和A→B方向的转运率和表观渗透系数(Papp)均无统计学差异(P>0.05)。在Caco-2细胞,与未用5-ASA组相比,各浓度5-ASA组(50μmol·L-1~5mmol·L-1)对地高辛的Papp和B→A方向的净转运率无明显影响(P>0.05)。结论...
(NCEs), often BBB surrogate models such asMDR1-transfected MDCKII (Madin-Darby canine kidney strain II) and LLC-PK1 (Lilly Laboratories cells—porcine kidney 1) cells or a human colon carcinoma cell line (Caco-2) are used as general barrier models, because these polarized epithelial cells ...
In the MDCKII-MDR1 cells, berberine and berbamine inhibited both theefflux Papp of CSA and digoxin. Our data suggests that OGR extract, berberine,and berbamine can inhibit P-gp thereby may increase the bioavailability of drugsthat are substrates of P-gp....
Human intestinal epithelial Caco-2 cells, T84 cells, and MDCKII cells transfected with human MDR1, were used to investigate the mechanistic basis of transi... S Lowes,NL Simmons - 《British Journal of Pharmacology》 被引量: 68发表: 2002年 Coexpression of invasive markers (uPA, CD44) and ...
Objectives: To investigate the effects of bergapten of Angelicae Dahuricae Radix on the transport of vincristine and its possible mechanism.Methods: The apparent permeability coefficient(Papp) for the transport of vincristine through the membrane of MDCK-MDR1 cells was used as an indicator of the ...