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Objective:To investigate the transport mechanism of punicalagin in MDCK monolayer model .Methods:The safe con-centration of punicalagin in MDCK cells was determined by CCK8 assay.Millicell -ERS was used to measure cell monolayer TEER value to determine the integrity of the cell monolayer .The effects of direction , drug concentration , time, P-gp inhibitor and EDTA-Na2 on the absorption and transport of punicalagin were studied systematically .And then the drug concentration was analyzed by HPLC to calculate the apparent permeability coefficient (Papp) and efflux ratio(ER).Results: Punicalagin transport in MDCK cells was time and concentration dependent .Punicalagin showed poor absorption in MDCK cells .Papp from apical to basolateral side ( AP-BL) within the concentration range of 100-300μg· ml-1 was (6.13 ±0.12) ×10 -7 cm· s-1 , (6.96 ±0.26) ×10 -7 cm· s-1 and (5.94 ±0.10) ×10 -7 cm· s-1 , respectively .P-gp inhibitor and EDTA-Na2 could significantly increase the transport of punicalagin in AP-BL direc-tion, while the transport decreased at 4℃.Conclusion:The transport mechanism of punicalagin might be passive diffusion as the dom-inating process involving active transportation .Punicalagin is one of P-gp substrates with exocytosis and absorbed via the paracellular route.
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ABSTRACT Ellagitannin is a complex compound of plant polyphenols, and it is an effective substance in many commonly used natu-ral drugs. Ellagitannin has been widely used in medicine, cosmetics, food, health care products and the other fields. The article re-viewed the structure source, biological activity and metabolic outcomes of ellagitannin in order to provide basis for the in-depth resear-ches and the resource development of natural medicines rich in tannins.
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Objective: To study the in vitro antilipid-peroxidation effects of tannins extract from Sanguisorba officinalis on heart, liver, brain and kidney of rats.Methods: The in vitro inhibitory effects of tannins extract from Sanguisorba officinalis on lipid-peroxidation of heart, liver, brain and kidney of rats induced by Fe2+-cysteine (Fe2+-Cys), Fe2+-vitamin C (Fe2+-Vit C) and Fe2+-H2O2 were determined by spectrophotometry.Results: The inhibitory effects of tannins extract from Sanguisorba officinalis on MDA produced by lipid-peroxidation of brain, heart, liver homogenate, kidney and mitochondria of rats induced by Fe2+-Cys, Fe2+-Vit C and Fe2+-H2O2 were all significant.Conclusion: Tannins from Sanguisorba officinalis has good in vitro protective effects on antilipid-peroxidation of heart, liver, brain and kidney of rats, which is worth studying further.
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Objective:To study the effect of tannins from Pericarpium Granati on hepatic microsomal enzyme in rats. Methods:Thirty Wistar rats were randomly divided into five groups:the blank control group, high, medium and low dose groups of tannins from Pericarpium Granati, the positive control group of phenobarbital sodium. The blank control group was given physiological saline. The three different doses groups were respectively given tannins from Pericarpium Granati orally at the dose of 150,100 and 75 mg·kg-1 · d-1 for 7 days. The positive control group was given phenobarbital sodium 80 mg·kg-1 ·d-1 with intramuscular injection for 5 days. At the end of the experiment, the activity ofⅠandⅡphase metabolic enzymes in liver microsomes of each group was determined by UV. Results:Compared with the blank control group, the high, medium and low dose groups of tannins from Pericarpium Granati could sig-nificantly decrease the content of CYP 450 and CYPb5, and inhabit the activity of ADM (P<0. 01);the high and medium dose group could significantly inhibit ERD enzyme activity (P<0. 01);the high dose group could significantly reduce GST enzyme activity (P<0. 01). Conclusion:Tannins from Pericarpium Granati has notably inhibitory effect on hepatic microsomal enzyme in rats, which can reduce the expression of CYP3A and CYP2E1 in a dose-dependent manner.
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ABSTRACT Ellagitannin is a complex compound of plant polyphenols, and it is an effective substance in many commonly used natu-ral drugs. Ellagitannin has been widely used in medicine, cosmetics, food, health care products and the other fields. The article re-viewed the structure source, biological activity and metabolic outcomes of ellagitannin in order to provide basis for the in-depth resear-ches and the resource development of natural medicines rich in tannins.