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Study on mechanism of low bioavailability of black tea theaflavins by using Caco-2 cell monolayer

Fengfeng Qu, Zeyi Ai, Shuyuan Liu, Haojie Zhang, Yuqiong Chen, Yaomin Wang, Dejiang Ni

2021Drug Delivery27 citationsDOIOpen Access PDF

Abstract

cm/s in the absorptive transport. All the theaflavins showed an efflux ratio of over 1.24. And it is further confirmed that P-glycoprotein (P-gp), multidrug resistance associated proteins (MRPs) and breast cancer resistance protein (BCRP) were all shown to contribute to the efflux transport of four theaflavins, with P-gp playing the most important role, followed by MRPs and BCRP. Moreover, theaflavins increased the expression of P-gp, MRP1, MPR3, and BCRP while decreased the expression of MRP2 at the transcription and translation levels. Additionally, the gallated theaflavins were degraded into simple theaflavins and gallic acids when transported through Caco-2 monolayers. Overall, the structural instability, efflux transporters, and cell metabolism were all responsible for the low bioavailability of four theaflavins in Caco-2 monolayers.

Topics & Concepts

TheaflavinBioavailabilityAbcg2EffluxChemistryCaco-2CytotoxicityGallic acidPharmacologyBiochemistryIn vitroTransporterPolyphenolMedicineATP-binding cassette transporterAntioxidantGeneTea Polyphenols and EffectsPhytoestrogen effects and researchTannin, Tannase and Anticancer Activities