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[Transport mechanism of swertiamain metabolite across Caco-2 model].

Cheng Tang, Yanjun Zhang, Tiejun Zhang, Chengwang Tian, Changxiao Liu

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Abstract

OBJECTIVE: To investigate the intestinal absorption mechanism of swertiamain metabolite {(Z)-5-ethylidene-8-hydroxy-3,4,5,6,7,8-hexahydro-1H-pyrano [3,4-c]pyridine-1-one, EHPO}. METHOD: The time depended hi-directional transport of EHPO in Caco-2 monolayer model was investigated with the factors of concentration, pH and verapamil. EHPO concentration was measured by HPLC assay and the apparent permeability coefficients (Papp) were calculated. RESULT: In the this cell model, EHPO could be absorbed through Caco-2 soon. The P(app AP-BL) was equal to the P(app BL-AP), and Papp keep almost constant with the selected concentration investigated. But the Papp could be influenced by pH and verapamil (100 mg x L(-1)). CONCLUSION: The absorption of EHPO in Caco-2 cell model is a passive one. And absorption of EHPO in the intestines is quite good.

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What this paper is about

OBJECTIVE: To investigate the intestinal absorption mechanism of swertiamain metabolite {(Z)-5-ethylidene-8-hydroxy-3,4,5,6,7,8-hexahydro-1H-pyrano [3,4-c]pyridine-1-one, EHPO}. METHOD: The time depended hi-directional transport of EHPO in Caco-2 monolayer model was investigated with the factors of concentration, pH and verapamil. EHPO concentration was measured by HPLC assay and the apparent permeability coefficients (Papp) were calculated. RESULT: In the this cell model, EHPO could be absorbed through Caco-2 soon. The P(app AP-BL) was equal to the P(app BL-AP), and Papp keep almost constant with the selected concentration investigated. But the Papp could be influenced by pH and verapamil (100 mg x L(-1)). CONCLUSION: The absorption of EHPO in Caco-2 cell model is a passive one. And absorption of EHPO in the intestines is quite good.

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Available abstract

OBJECTIVE: To investigate the intestinal absorption mechanism of swertiamain metabolite {(Z)-5-ethylidene-8-hydroxy-3,4,5,6,7,8-hexahydro-1H-pyrano [3,4-c]pyridine-1-one, EHPO}. METHOD: The time depended hi-directional transport of EHPO in Caco-2 monolayer model was investigated with the factors of concentration, pH and verapamil. EHPO concentration was measured by HPLC assay and the apparent permeability coefficients (Papp) were calculated. RESULT: In the this cell model, EHPO could be absorbed through Caco-2 soon. The P(app AP-BL) was equal to the P(app BL-AP), and Papp keep almost constant with the selected concentration investigated. But the Papp could be influenced by pH and verapamil (100 mg x L(-1)). CONCLUSION: The absorption of EHPO in Caco-2 cell model is a passive one. And absorption of EHPO in the intestines is quite good.

Key concepts: Caco-2, Verapamil, Chemistry, Metabolite, Absorption (acoustics), Chromatography, Permeability (electromagnetism), Cell

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