Abstract
Objective. To investigate the absorption property of the representative hydrolyzable tannin, namely corilagin, and its hydrolysates gallic acid (GA) and ellagic acid (EA) from the Fructus Phyllanthi tannin fraction (PTF) in vitro. Methods. Caco-2 cells monolayer model was established. Influences of PTF on Caco-2 cells viability were detected with MTT assay. The transport across monolayers was examined for different time points, concentrations, and secretory directions. The inhibitors of P-glycoprotein (P-gp), multidrug resistance proteins (MRPs), organic anion transporting polypeptide (OATP) and sodium/glucose cotransporter 1 (SGLT1), and tight junction modulators were used to study the transport mechanism. LC-MS method was employed to quantify the absorption concentration. Results. The apparent permeability coefficient (P app) values of the three compounds were below 1.0 × 10−6 cm/s. The absorption of corilagin and GA were much lower than their efflux, and the uptake of both compounds was increased in the presence of inhibitors of P-gp and MRPs. The absorption of EA was decreased in the company of OATP and SGLT1 inhibitors. Moreover, the transport of corilagin, GA, and EA was enhanced by tight junction modulators. Conclusion. These observations indicated that the three compounds in PTF were transported via passive diffusion combined with protein mediated transport. P-gp and MRPs might get involved in the transport of corilagin and GA. The absorption of EA could be attributed to OATP and SGLT1 protein.
Highlights
IntroductionHydrolyzable tannins belong to the family of polyphenol, which integrated in some kinds of foods and medicinal herbs, such as Punica granatum and Terminalia chebula Retz
Hydrolyzable tannins belong to the family of polyphenol, which integrated in some kinds of foods and medicinal herbs, such as Punica granatum and Terminalia chebula Retz.Recently, researches of hydrolyzable tannins are getting more and more attentions on account of their benefits for our health [1]
The absorbance of the marker was measured at 490 nm using the microplate reader (Molecular Devices, Sunnyvale, CA, USA), and the concentration of sodium fluorescein was calculated by standard curve
Summary
Hydrolyzable tannins belong to the family of polyphenol, which integrated in some kinds of foods and medicinal herbs, such as Punica granatum and Terminalia chebula Retz. Researches of hydrolyzable tannins are getting more and more attentions on account of their benefits for our health [1]. As a typical hydrolyzable tannin, corilagin is a potential antitumor compound [2, 3]. It exhibits antiviral, antihyperalgesic, and antibacterial activities [4,5,6]. (Euphorbiaceae) is a famous medicinal plant distributed in Asia countries especially in Gallic acid (GA) and ellagic acid (EA) are two hydrolysates of corilagin, both of which possess strong antioxidant and anticancer effects [7,8,9,10].
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