Benzotropolone moiety in theaflavins is responsible for inhibiting peptide-transport and activating AMP-activated protein kinase in Caco-2 cells

  title={Benzotropolone moiety in theaflavins is responsible for inhibiting peptide-transport and activating AMP-activated protein kinase in Caco-2 cells},
  author={Ha-Young Park and Yuri Kunitake and Toshiro Matsui},
  journal={Functional Foods in Health and Disease},
Objective : In the small intestine, peptide transporter 1 (PEPT1) plays a role in the transport of di- and tri-peptides. Recently, we found that theaflavins (TFs), dimeric catechins, inhibited the transport of di-peptides across Caco-2 monolayers by suppressing the expression of PEPT1 through AMP-activated protein kinase (AMPK) activation. In this study, we investigated the structural requirement of theaflavins for the effect, and the mechanism(s) underling theaflavin-induced AMPK activation… Expand
Theaflavins enhance intestinal barrier of Caco-2 Cell monolayers through the expression of AMP-activated protein kinase-mediated Occludin, Claudin-1, and ZO-1
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Condensed catechins and their potential health-benefits.
  • T. Matsui
  • Chemistry, Medicine
  • European journal of pharmacology
  • 2015
This review focuses on the physiological potentials of dimeric and trimeric catechins in the intestine, blood vessels, and muscle organs (promotion of glucose uptake resulting in an anti-diabetic effect), and the roles of non-absorbable theaflavins, absorbable theasinensins, and absorbable procyanidins on target organs are discussed. Expand
Theaflavins inhibit glucose transport across Caco-2 cells through the downregulation of the Ca2+/AMP-activated protein kinase-mediated glucose transporter SGLT1
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Theaflavins prevent the onset of diabetes through ameliorating glucose tolerance mediated by promoted incretin secretion in spontaneous diabetic Torii rats
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  • Medicine
  • Journal of Functional Foods
  • 2021
Abstract The in vivo anti-hyperglycemic effect of non-absorbable theaflavins, polyphenolic ingredients of black tea, was evaluated in spontaneously diabetic Torii (SDT) rats. A mixture of theaflavinsExpand


Theaflavins, dimeric catechins, inhibit peptide transport across Caco-2 cell monolayers via down-regulation of AMP-activated protein kinase-mediated peptide transporter PEPT1.
It is demonstrated that TFs inhibit peptide transport across Caco-2 cell monolayers, probably through suppression of AMPK-mediated PEPT1 expression, which should be considered a new bioactivity of TFs in black tea. Expand
Regulation of expression of the intestinal oligopeptide transporter (Pept-1) in health and disease.
  • S. Adibi
  • Biology, Medicine
  • American journal of physiology. Gastrointestinal and liver physiology
  • 2003
In conclusion, the above studies have produced a wealth of new information on regulation of a key transporter in the intestine that may have useful applications in nutritional and pharmacological treatments, for example, in diabetic patients needing enteral nutrition or in ulcerative colitis patients needing the suppression of the intestinal inflammation. Expand
Catechin-induced activation of the LKB1/AMP-activated protein kinase pathway.
It is suggested that multiple effects of catechins, including anti-obesity and anti-cancer effects, are mediated, at least in part, by the activation of LKB1/AMPK in various tissues, and that these effects vary according to the catechin structure. Expand
The apical (hPepT1) and basolateral peptide transport systems of Caco-2 cells are regulated by AMP-activated protein kinase
The reduction in apical hPepT1 protein and dipeptide uptake after AICAR treatment in Caco-2 cells demonstrates a regulatory effect of AMPK on hPEPT1, along with an influence on both the microvilli and tight junction structures. Expand
Theaflavins attenuate hepatic lipid accumulation through activating AMPK in human HepG2 cellss⃞ Published, JLR Papers in Press, August 24, 2007.
The results show that theaflavins are bioavailable both in vitro and in vivo and may be active in the prevention of fatty liver and obesity and support the idea that AMPK is a critical component of decreased hepatic lipid accumulation by theAFlavin treatments. Expand
Epigallocatechin-3-gallate (EGCG), A Green Tea Polyphenol, Suppresses Hepatic Gluconeogenesis through 5′-AMP-activated Protein Kinase*
An inhibitory role for EGCG is demonstrated in isolated hepatocytes in hepatic gluconeogenesis and new light is shed on the mechanism by which E GCG suppresses gluc oneogenesis. Expand
Cellular and molecular mechanisms of dietary regulation on rat intestinal H+/Peptide transporter PepT1.
The results suggest that the up-regulation of dipeptide transport activity by dietary protein is caused by transcriptional activation of the PepT1 gene by selective amino acids and diPEptides in the diet. Expand
Inhibitory effect(s) of polymeric black tea polyphenols on the formation of B(a)P-derived DNA adducts in mouse skin.
  • R. Krishnan, G. Maru
  • Chemistry, Medicine
  • Journal of environmental pathology, toxicology and oncology : official organ of the International Society for Environmental Toxicology and Cancer
  • 2005
The results suggest that black tea-derived PBPs have one of the chemopreventive properties shown by monomeric green tea polyphenols. Expand
Enzymatic synthesis of tea theaflavin derivatives and their anti-inflammatory and cytotoxic activities.
Derivatives based on a benzotropolone skeleton have been found to inhibit TPA-induced mice ear edema, nitric oxide (NO) synthesis, and arachidonic acid release by LPS-stimulated RAW 264.7 cells. Expand
A cell-penetrating peptide suppresses inflammation by inhibiting NF-κB signaling.
The results suggest that AIP6 is a promising lead peptide for the development of specific NF-κB inhibitors as potential anti-inflammatory agents. Expand