Bioavailability of Black Tea Theaflavins: Absorption, Metabolism, and Colonic Catabolism

Pereira-Caro, Gema; Moreno-Rojas, José Manuel; Brindani, Nicoletta; Rio, Daniele Del; Lean, Michael E. J.; Hara, Yukihiko; Crozier, Alan

doi:10.1021/acs.jafc.7b01707

Cited by 99 publications

(81 citation statements)

References 48 publications

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“…In a human study, after consumption of 700 mg of TFs, the maximum concentration of TFs in plasma was only 1.0 ng/mL . Recently, Pereira‐Pereira‐Caro et al found that TFs were not absorbed in either the upper or lower gastrointestinal tract. Therefore, in this study, we decided to administer TFs topically, instead of by oral administration.…”

Section: Discussionmentioning

confidence: 97%

Effects of theaflavins on tissue inflammation and bone resorption on experimental periodontitis in rats

Kuraji

Taya

et al. 2018

J of Periodontal Research

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Background and ObjectiveTheaflavins (TFs), the major polyphenol in black tea, have the ability to reduce inflammation and bone resorption. The aim of this study was to evaluate the effects of TFs on experimental periodontitis in rats.Material and MethodsThirty rats were divided into five groups: Control (glycerol application without ligation), Ligature (glycerol application with ligation), TF1 (1 mg/mL TF application with ligation), TF10 (10 mg/mL TF application with ligation), and TF100 (100 mg/mL TF application with ligation). To induce experimental periodontitis, ligatures were placed around maxillary first molars bilaterally. After ligature placement, 100 μL glycerol or TFs were topically applied to the rats daily, and rats were euthanized 7 days after ligature placement. Micro‐computed tomography was used to measure bone resorption in the left side of the maxilla, and quantitative polymerase chain reaction was used to measure the expression of interleukin (IL)‐6, growth‐regulated gene product/cytokine‐induced neutrophil chemoattractant (Gro/Cinc‐1, rat equivalent of IL‐8), matrix metalloproteinase‐9 (Mmp‐9), receptor activator of nuclear factor‐kappa Β ligand (Rankl), osteoprotegerin (Opg), and the Rankl/Opg ratio in gingival tissue. With tissue from the right side of the maxilla, hematoxylin and eosin staining was used for histological analysis, immunohistochemical staining for leukocyte common antigen (CD45) was used to assess inflammation, and tartrate‐resistant acid phosphatase (TRAP) staining was used to observe the number of osteoclasts.ResultsThe TF10 and TF100 groups, but not the TF1 group, had significant inhibition of alveolar bone loss, reduction in inflammatory cell infiltration in the periodontium, and significantly reduced numbers of CD45‐positive cells and TRAP‐positive osteoclasts compared with the Ligature group. Correspondingly, the TF10 and TF100 groups had significantly downregulated gene expression of IL‐6, Gro/Cinc‐1(IL‐8), Mmp‐9, and Rankl, but not of Opg. Consequently, Rankl/Opg expression was significantly increased in the Ligation group but was attenuated in the TF10 and TF100 groups.ConclusionThe results of this study suggest that topical application of TFs may reduce inflammation and bone resorption in experimental periodontitis. Therefore, TFs have therapeutic potential in the treatment of periodontal disease.

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Section: Discussionmentioning

confidence: 97%

Effects of theaflavins on tissue inflammation and bone resorption on experimental periodontitis in rats

Kuraji

Taya

et al. 2018

J of Periodontal Research

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“…Thus, the contribution of other transporters to the rosuvastatin–black tea interaction cannot be excluded. However, given the poor oral bioavailability of TFs, hepatic or renal transporter‐related drug interactions may not be clinically important (Pereira‐Caro et al, ).…”

Section: Discussionmentioning

confidence: 99%

Black tea extract and theaflavin derivatives affect the pharmacokinetics of rosuvastatin by modulating organic anion transporting polypeptide (OATP) 2B1 activity

Kondo

Narumi

Okuhara

et al. 2019

Biopharm & Drug Disp

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Theaflavins (TFs) are derived from black tea, an important source of dietary polyphenols. Although the potential interactions between dietary polyphenols and drugs have been demonstrated through in vitro and in vivo studies, little information is available concerning the influence of TFs on drug disposition. Organic anion transporting polypeptide 2B1 (OATP2B1) is expressed in human enterocytes and plays a role in the intestinal absorption of numerous drugs. The current study evaluated the effects of black tea extracts on the pharmacokinetics of rosuvastatin in rats, and investigated the effect of four major TFs (theaflavin, theaflavin-3-gallate, theaflavin-3′-gallate and theaflavin-3,3′-digallate) on the transport activity of OATP2B1. Black tea extracts significantly decreased the maximum plasma concentration (C max ) and area under the plasma concentration-time curve (AUC 0 -8 ) of rosuvastatin by 48% and 37%, respectively (p < 0.001 and p < 0.01, respectively).Moreover, OATP2B1-mediated rosuvastatin and estrone-3-sulfate uptake was significantly reduced in the presence of TFs. A kinetic study revealed that the uptake efficiency (in terms of V max /K m ) of rosuvastatin was decreased following treatment with TFs. Black tea extracts also reduced OATP2B1-mediated rosuvastatin uptake.These results suggest that black tea reduces the plasma concentrations of rosuvastatin by inhibiting the intestinal OATP2B1-mediated transport of rosuvastatin.

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“…In this regard it is of note that 5C‐RFMs are also derived from catechins and gallocatechins, such as (−)‐epigallocatechin‐3‐ O ‐gallate 12 , which occur in tea (van der Hooft et al., ). Furthermore, 5C‐RFMs also originate to some degree from colonic catabolism of procyanidins (Appeldoorn, Vincken, Aura, Hollman, & Gruppen, ; Stoupi, Williamson, Drynan, Barron, & Clifford, ), but they appear not to be formed from theaflavins, and presumably thearubigins, after the ingestion of black tea (Pereira‐Caro et al., ).…”

Section: Bioavailabilitymentioning

confidence: 99%

The Bioavailability, Transport, and Bioactivity of Dietary Flavonoids: A Review from a Historical Perspective

Williamson

Kay

Crozier

2018

Comp Rev Food Sci Food Safe

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393

288

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Flavonoids are plant-derived dietary components with a substantial impact on human health. Research has expanded massively since it began in the 1930s, and the complex pathways involved in bioavailability of flavonoids in the human body are now well understood. In recent years, it has been appreciated that the gut microbiome plays a major role in flavonoid action, but much progress still needs to be made in this area. Since the first publications on the health effects of flavonoids, their action is understood to protect against various stresses, but the mechanism of action has evolved from the now debunked simple direct antioxidant hypothesis into an understanding of the complex effects on molecular targets and enzymes in specific cell types. This review traces the development of the field over the past 8 decades, and indicates the current state of the art, and how it was reached. Future recommendations based on this historical analysis are (a) to focus on key areas of flavonoid action, (b) to perform human intervention studies focusing on bioavailability and protective effects, and (c) to carry out cellular in vitro experiments using appropriate cells together with the chemical form of the flavonoid found at the site of action; this could be the native form of compounds found in the food for studies on digestion and the intestine, the conjugated metabolites found in the blood after absorption in the small intestine for studies on cells, or the chemical forms found in the blood and tissues after catabolism by the gut microbiota.

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Bioavailability of Black Tea Theaflavins: Absorption, Metabolism, and Colonic Catabolism

Cited by 99 publications

References 48 publications

Effects of theaflavins on tissue inflammation and bone resorption on experimental periodontitis in rats

Effects of theaflavins on tissue inflammation and bone resorption on experimental periodontitis in rats

Black tea extract and theaflavin derivatives affect the pharmacokinetics of rosuvastatin by modulating organic anion transporting polypeptide (OATP) 2B1 activity

The Bioavailability, Transport, and Bioactivity of Dietary Flavonoids: A Review from a Historical Perspective

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