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目的:研究蝙蝠葛碱在Caco-2细胞模型中的跨膜转运机制。方法:采用Caco-2细胞模型,进行A-B和B-A双向转运实验,计算表观渗透系数(Papp)、外排比率(ER)和累积转运量,考察蝙蝠葛碱不同质量浓度、细胞两侧pH梯度和螯合剂EGTA对蝙蝠葛碱转运的影响。结果:高、中、低浓度下的ER分别为1.11,4.49和7.24,即中、低浓度下转运有明显极化现象;顶侧pH 7.4和6.5时,ER值分别为3.95和9.38,即pH梯度存在时,蝙蝠葛碱吸收减少,外排增加;加入螯合剂EGTA后,Papp,ER和累积转运量均无显著改变。结论:蝙蝠葛碱的吸收有主动转运机制存在;pH梯度能驱动了蝙蝠葛碱的外排转运,偏碱性环境较酸性环境易于吸收;其吸收途径主要为跨细胞通道转运。
Objective: To study the transmembrane transport mechanism of dauricine in Caco-2 cell model. Methods: Caco-2 cell model was used to study the AB and BA bidirectional transport experiments. The apparent permeability coefficient (Papp), efflux ratio (ER) and cumulative transport volume were calculated. The effects of different concentrations of dauricine, pH gradient And chelator EGTA on dahurium transport. Results: ER at high, medium and low concentrations were 1.11, 4.49 and 7.24, respectively, indicating that there was obvious polarization at medium and low concentrations. The ER values at pH 7.4 and 6.5 at the top were 3.95 and 9.38, respectively In the presence of a gradient, the dauricine absorbed decreased and the efflux increased. After addition of the chelator EGTA, there was no significant change in Papp, ER and cumulative transport. CONCLUSION: The uptake of daunorubic has an active transport mechanism. The pH gradient can drive the outward transport of dauricine. The alkalescent environment is more easily absorbed than the acidic environment. The absorption pathway is mainly transcellular channel transport.