2013•Zhonghua zhongyiyao zazhiRequires access

Study on the absorption mechanism of brucine in vitro and its transport interaction with liquiritin in Caco-2 cell monolayer model

Yong Chen

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Abstract

Objective: To study the absorption mechanism of brucine in vitro and its transport interaction with liquiritin in Caco-2 cell monolayer model.Methods: The cumulative transport concentration(TRcum),apparent permeability coefficient(PappB→A and PappA→B) of brucine were determined after Caco-2 cell monolayer model were treated by brucine and combined with liquiritin.The effects of drug concentration,conveying time,P-glycoprotein inhibitor verapamil and medium pH value on the transport of brucine in Caco-2 cell monolayer model were also investigated.Results: The Papp value of brucine was larger than 10-6cm/s,and the ratio of Papp B→A versus Papp A→B was less than 1.5.The co-treatment of brucine combined with liquiritin increase the ratio of Papp B→A versus Papp A→B,whereas the co-treatment of brucine combined with verapamil decreased the ratio of Papp B→A versus Papp A→B.Moreover,the Papp A→B in medium pH6.0 was less than that in medium pH7.4.Conclusion: The absorption of brucine in Caco-2 cell monolayer model was well and the passive transference was its main intestinal absorption mechanism.P-glycoprotein and liquiritin inhibited the absorption of brucine,and medium pH had important effect on the transport of brucine.

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Objective: To study the absorption mechanism of brucine in vitro and its transport interaction with liquiritin in Caco-2 cell monolayer model.Methods: The cumulative transport concentration(TRcum),apparent permeability coefficient(PappB→A and PappA→B) of brucine were determined after Caco-2 cell monolayer model were treated by brucine and combined with liquiritin.The effects of drug concentration,conveying time,P-glycoprotein inhibitor verapamil and medium pH value on the transport of brucine in Caco-2 cell monolayer model were also investigated.Results: The Papp value of brucine was larger than 10-6cm/s,and the ratio of Papp B→A versus Papp A→B was less than 1.5.The co-treatment of brucine combined with liquiritin increase the ratio of Papp B→A versus Papp A→B,whereas the co-treatment of brucine combined with verapamil decreased the ratio of Papp B→A versus Papp A→B.Moreover,the Papp A→B in medium pH6.0 was less than that in medium pH7.4.Conclusion: The absorption of brucine in Caco-2 cell monolayer model was well and the passive transference was its main intestinal absorption mechanism.P-glycoprotein and liquiritin inhibited the absorption of brucine,and medium pH had important effect on the transport of brucine.

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Available abstract

Objective: To study the absorption mechanism of brucine in vitro and its transport interaction with liquiritin in Caco-2 cell monolayer model.Methods: The cumulative transport concentration(TRcum),apparent permeability coefficient(PappB→A and PappA→B) of brucine were determined after Caco-2 cell monolayer model were treated by brucine and combined with liquiritin.The effects of drug concentration,conveying time,P-glycoprotein inhibitor verapamil and medium pH value on the transport of brucine in Caco-2 cell monolayer model were also investigated.Results: The Papp value of brucine was larger than 10-6cm/s,and the ratio of Papp B→A versus Papp A→B was less than 1.5.The co-treatment of brucine combined with liquiritin increase the ratio of Papp B→A versus Papp A→B,whereas the co-treatment of brucine combined with verapamil decreased the ratio of Papp B→A versus Papp A→B.Moreover,the Papp A→B in medium pH6.0 was less than that in medium pH7.4.Conclusion: The absorption of brucine in Caco-2 cell monolayer model was well and the passive transference was its main intestinal absorption mechanism.P-glycoprotein and liquiritin inhibited the absorption of brucine,and medium pH had important effect on the transport of brucine.

Key concepts: Brucine, Liquiritin, Verapamil, Chemistry, Monolayer, Caco-2, Absorption (acoustics), Chromatography

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