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Study on mechanism of low bioavailability of black tea theaflavins by using Caco-2 cell monolayer.
- Source :
-
Drug Delivery . 2021, Vol. 28 Issue 1, p1737-1747. 11p. - Publication Year :
- 2021
-
Abstract
- This study aimed to clarify the bioavailability mechanism of theaflavins by using the Caco-2 monolayer in vitro model. Prior to the transport of theaflavin (TF), theaflavin-3-gallate (TF3G), theaflavin-3'-gallate (TF3'G), and theaflavin-3, 3'-digallate (TFDG), we found the cytotoxicity of theaflavins was in the order of TF3'G>TFDG>TF3G>TF, suggesting the galloyl moiety enhances the cytotoxicity of theaflavins. Meantime, the galloyl moiety made theaflavins unstable, with the stability in the order of TF>TFDG>TF3G/TF3'G. Four theaflavins showed poor bioavailability with the Papp values ranging from 0.44X10-7 to 3.64X10-7 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. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 10717544
- Volume :
- 28
- Issue :
- 1
- Database :
- Academic Search Index
- Journal :
- Drug Delivery
- Publication Type :
- Academic Journal
- Accession number :
- 154908605
- Full Text :
- https://doi.org/10.1080/10717544.2021.1949074