scholarly journals Effect of Stereochemical Configuration on the Transport and Metabolism of Catechins from Green Tea across Caco-2 Monolayers

Molecules ◽  
2019 ◽  
Vol 24 (6) ◽  
pp. 1185
Author(s):  
Zeyi Ai ◽  
Shuyuan Liu ◽  
Fengfeng Qu ◽  
Haojie Zhang ◽  
Yuqiong Chen ◽  
...  
Keyword(s):  
Green Tea ◽  
Epigallocatechin Gallate ◽  
Dimensional Structure ◽  
Cancer Resistance ◽  
Epicatechin Gallate ◽  
Efflux Transport ◽  
Transcellular Transport ◽  
P Glycoprotein ◽  
Gallocatechin Gallate ◽  
Resistance Protein

The transcellular transport and metabolism of eight green tea catechins (GTCs) were studied in Caco-2 monolayers, with the aim of investigating the effect of cis–trans isomerism on the membrane permeability and biotransformation of GTCs. The results showed that the catechin stereochemistry significantly affects the efflux transport rather than the absorption transport in the Caco-2 monolayers. The trans catechins showed a better transcellular permeability than their corresponding cis (epi) catechins in the efflux transport, as the efflux amount of trans catechins were all significantly higher than that of the cis (epi) catechins at each concentration and each time point tested. Moreover, the relative contents of the (+)-catechin (C)-O-sulfate, (+)-gallocatechin (GC)-O-sulfate, (−)-catechin gallate (CG)-O-sulfate, and (−)-gallocatechin gallate (GCG)-O-sulfate in the efflux transport were 2.67, 16.08, 50.48, and 31.54 times higher than that of the (−)-epicatechin (EC)-O-sulfate, (−)-epigallocatechin (EGC)-O-sulfate, (−)-epicatechin gallate (ECG)-O-sulfate, and (−)-epigallocatechin gallate (EGCG)-O-sulfate, respectively. It indicated that more metabolites were observed after the transcellular efflux of trans catechins. Furthermore, after two hours of incubation, the GTCs could significantly increase the expression of multidrug resistance-associated protein 2 (MRP2) and breast cancer-resistance protein (BCRP), and decrease the expression of P-glycoprotein in the Caco-2 cells. The regulation of GTCs on P-glycoprotein, MRP2, and BCRP could also be significantly influenced by the chemical and dimensional structure. In a conclusion, catechin stereochemistry significantly affects the transport and metabolism of GTCs when refluxed in the Caco-2 monolayers.

scholarly journals Anti-Trypanosoma cruzi Activity of Green Tea (Camellia sinensis) Catechins

2004 ◽  
Vol 48 (1) ◽  
pp. 69-74 ◽  
Author(s):  
Cristina Paveto ◽  
María C. Güida ◽  
Mónica I. Esteva ◽  
Virginia Martino ◽  
Jorge Coussio ◽  
...  
Keyword(s):  
Trypanosoma Cruzi ◽  
Green Tea ◽  
Camellia Sinensis ◽  
Developmental Stages ◽  
Arginine Kinase ◽  
Epigallocatechin Gallate ◽  
Array Detector ◽  
Epicatechin Gallate ◽  
Active Compounds ◽  
Gallocatechin Gallate

ABSTRACT The trypanocidal action of green tea catechins against two different developmental stages of Trypanosoma cruzi is reported for the first time. This activity was assayed with the nonproliferative bloodstream trypomastigote and with the intracellular replicative amastigote parasite forms. An ethyl acetate fraction from Camellia sinensis green tea leaves, which contains most of the polyphenolic compounds and the maximal trypanocidal activity, was obtained by fractionation of the aqueous extract with organic solvents. The active compounds present in this extract were further purified by LH-20 column chromatography and were identified by high-performance liquid chromatography analysis with a photo diode array detector and gas chromatography coupled to mass spectroscopy. The following flavan-3-ols derivatives, known as catechins, were identified: catechin, epicatechin, gallocatechin, epigallocatechin, catechin gallate, epicatechin gallate, gallocatechin gallate, and epigallocatechin gallate. The purified compounds lysed more than 50% of the parasites present in the blood of infected BALB/c mice at concentrations as low as 0.12 to 85 pM. The most active compounds were gallocatechin gallate and epigallocatechin gallate, with minimal bactericidal concentrations that inhibited 50% of isolates tested of 0.12 and 0.53 pM, respectively. The number of amastigotes in infected Vero cells decreased by 50% in the presence of each of these compounds at 100 nM. The effects of the catechins on the recombinant T. cruzi arginine kinase, a key enzyme in the energy metabolism of the parasite, were assayed. The activity of this enzyme was inhibited by about 50% by nanomolar concentrations of catechin gallate or gallocatechin gallate, whereas the other members of the group were less effective. On the basis of these results, we suggest that these compounds could be used to sterilize blood and, eventually, as therapeutic agents for Chagas' disease.

Versatile Health Benefits of Catechin from Green Tea (Camellia sinensis)

2019 ◽  
Vol 15 (1) ◽  
pp. 3-10 ◽  
Author(s):  
Satheesh Babu Natarajan ◽  
Suriyakala Perumal Chandran ◽  
Sahar Husain Khan ◽  
Packiyaraj Natarajan ◽  
Karthiyaraj Rengarajan
Keyword(s):  
Green Tea ◽  
Camellia Sinensis ◽  
Health Benefits ◽  
Epigallocatechin Gallate ◽  
Extraction Methods ◽  
Major Constituent ◽  
Epicatechin Gallate ◽  
Wide Range ◽  
Green Tea Catechin ◽  
Anti Inflammatory

Background: Tea (Camellia sinensis, Theaceae) is the second most consumed beverage in the world. Green tea is the least processed and thus contain rich antioxidant level, and believed to have most of the health benefits. </p><p> Methods: We commenced to search bibliographic collection of peer reviewed research articles and review articles to meet the objective of this study. </p><p> Results: From this study, we found that the tea beverage contains catechins are believed to have a wide range of health benefits which includes neuroprotective, anti-inflammatory, antiulcer, antiviral, antibacterial, and anti-parasitic effects. The four major catechin compounds of green tea are epigallocatechin (EGC), epicatechin (EC), epigallocatechin gallate (EGCG), and epicatechin gallate (ECG), of which EGCG is the major constituent and representing 50-80% of the total catechin content. And also contain xanthine derivatives such as caffeine, theophylline, and theobromine, and the glutamide derivative theanine. It also contains many nutritional components, such as vitamin E, vitamin C, fluoride, and potassium. We sum up the various green tea phytoconstituents, extraction methods, and its medicinal applications. </p><p> Conclusion: In this review article, we have summarized the pharmacological importance of green tea catechin which includes antioxidant potential, anti-inflammatory, antimicrobial, anticancer, antidiabetic and cosmetic application.

scholarly journals High Intrinsic Expression of P-glycoprotein and Breast Cancer Resistance Protein in Canine Mammary Carcinomas Regardless of Immunophenotype and Outcome

Animals ◽  
2021 ◽  
Vol 11 (3) ◽  
pp. 658
Author(s):  
Michela Levi ◽  
Luisa Vera Muscatello ◽  
Barbara Brunetti ◽  
Cinzia Benazzi ◽  
Federico Parenti ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Epidermal Growth Factor Receptor ◽  
Growth Factor ◽  
Breast Cancer Resistance Protein ◽  
Triple Negative ◽  
Growth Factor Receptor ◽  
Cancer Resistance ◽  
P Glycoprotein ◽  
Epidermal Growth ◽  
Resistance Protein

P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) are major actors in multidrug resistance (MDR) phenomenon in both human and canine mammary carcinomas (CMCs). The aim of this study was to investigate an association between the intrinsic expression of P-gp and BCRP compared to the immunophenotypes and outcome in CMCs. Fifty CMCs were evaluated at immunohistochemistry (IHC) for P-gp, BCRP, Estrogen receptor alpha (ER), Progesterone receptors (PR), Human Epidermal Growth Factor Receptor type 2 (HER2), basal cytokeratins 5/6 (CK5/6), Epidermal Growth Factor Receptor 1 (EGFR), and Ki67 proliferation index. P-gp and BCRP positive cases were, respectively, 52% and 74.5%, with a significantly higher expression of BCRP than P-gp. Five immunophenotypes were defined in 37 out of 50 CMCs: 9 (24.3%) Luminal A, 5 (13.5%) Luminal B, 9 (24.3%) HER2 overexpressing, 9 (24.3%) Triple-negative basal-like, and 5 (13.5%) Triple-negative non-basal-like. In all CMCs at least one marker was expressed. Follow-up data were available for 25 animals. The average cancer-specific survival was 739 ± 444 days. A number of CMCs bear a high expression of P-gp and BCRP but no significant association was found between their expression and the immunophenotypes, Ki67 index, the histological grade, and tumor-related death.

scholarly journals P-Glycoprotein and Breast Cancer Resistance Protein Restrict Apical-to-Basolateral Permeability of Human Brain Endothelium to Amyloid-β

2009 ◽  
Vol 29 (6) ◽  
pp. 1079-1083 ◽  
Author(s):  
Leon M Tai ◽  
A Jane Loughlin ◽  
David K Male ◽  
Ignacio A Romero
Keyword(s):  
Breast Cancer ◽  
Human Brain ◽  
Breast Cancer Resistance Protein ◽  
Amyloid Β ◽  
Cancer Resistance ◽  
Glycoprotein P ◽  
P Glycoprotein ◽  
Resistance Protein ◽  
The Brain

The clearance of amyloid beta (Aβ) from the brain represents a novel therapeutic target for Alzheimer's disease. Conflicting data exist regarding the contribution of adenosine triphosphatebinding cassette transporters to the clearance of Aβ through the blood-brain barrier. Therefore, we investigated whether Aβ could be a substrate for P-glycoprotein (P-gp) and/or for breast cancer resistance protein (BCRP) using a human brain endothelial cell line, hCMEC/D3. Inhibition of P-gp and BCRP increased apical-to-basolateral, but not basolateral-to-apical, permeability of hCMEC/D3 cells to 125l Aβ 1–40. Our in vitro data suggest that P-gp and BCRP might act to prevent the blood-borne Aβ 1–40 from entering the brain.

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