Non-Involvement of the Human Monocarboxylic Acid Transporter 1 (MCT1) in the Transport of Phenolic Acid

Watanabe, Hisahiko; Yashiro, Takashi; Tohjo, Yuichi; Konishi, Yutaka

doi:10.1271/bbb.60093

Cited by 21 publications

(8 citation statements)

References 23 publications

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“…The pH dependence of ferulic acid permeation due to ionization does not exclude an involvement of a facilitated mechanism of transport coupled to a proton pump. Indeed, phenolic acids have been earlier proposed to be transported by a MCT (Konishi and Shimizu, 2003;Konishi and Kobayashi, 2004), recently suggested to be an isoform different from MCT1 (Watanabe et al, 2006). Protons and energy have also been shown to be necessary for the transport of some drugs possessing a carboxylic acid moiety such as ibuprofen.…”

Section: Discussionmentioning

confidence: 99%

Transport and Metabolism of Ferulic Acid through the Colonic Epithelium

Poquet¹,

Clifford²,

Williamson³

2007

Drug Metab Dispos

149

121

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ABSTRACT:Ferulic acid is an important antioxidant found in food, beverages, supplements, and herbal medicines. However, its mechanism of absorption in the colon has never been examined, even though this is its main site of in vivo absorption. Ferulic acid was efficiently transported as the free form through an in vitro model for the colonic epithelium consisting of cocultured Caco-2 and mucusproducing HT29-MTX cells, with only a small amount transported as feruloyl-glucuronide or sulfate, together with some free dihydroferulic acid. This pattern of metabolism and permeation was also seen with the use of rat everted ascending and descending colon sacs. In the cell model, free ferulic acid permeated by passive diffusion, as judged by the linearity of the uptake over time and nonsaturable concentration dependence. The permeation was independent of tight junctions but strongly linked to the hydrophobicity of the different phenolic acids tested, suggesting a transcellular rather than a paracellular transport. Using inhibitors, we showed that only a small proportion (<20%) of the free ferulic acid transport was carrier-mediated. The production of metabolites in the basal chamber was lowered by 3-[[3-[2-(7-chloroquinolin-2-yl)-vinyl]phenyl]-(2-dimethylcarbamoylethylsulfanyl)methylsulfanyl] propionic acid (MK571) and increased by cyclosporin A, implying an involvement of multidrug resistance protein and P-glycoprotein transporters in the efflux of metabolites, respectively to the serosal and luminal sides. These results show that the form of ferulic acid available to the blood after passage across the colonic barrier would be mainly the free form, together with only a small percentage of conjugated and reduced ferulic acid.

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Section: Discussionmentioning

confidence: 99%

Transport and Metabolism of Ferulic Acid through the Colonic Epithelium

Poquet¹,

Clifford²,

Williamson³

2007

Drug Metab Dispos

149

121

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“…It is expressed on both sides of the intestinal cell and transports phenolics especially phenolic acids from the lumen and extracellular fluid into enterocytes (Ziegler et al, 2016). Watanabe et al (2006) reported that MCT 1 was involved in the uptake of salicylic acid but not p-coumaric acid and fluorescein, thus they doubted the phenolics transportability of MCT 1. Meanwhile, some contradictory reports about localization (only apical or only basal membrane) of MCT 1 were compared in this study.…”

Section: Influx Transport Of Enterocytesmentioning

confidence: 99%

Bioaccessibility and bioavailability of phenolic compounds

Shahidi¹,

Peng²

2018

JFB

148

120

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Modern epidemiological and interventional studies have demonstrated that various bioactivities including antioxidant, antiproliferative, immune-regulatory, hormonal-regulation abilities and neuro-/hepato-/cardioprotective effects result from consumption of a phenolic-rich diet. The health benefits of ingesting phenolics are greatly dependent on their bioaccessibility and bioavailability in the digestive tract and circulatory system. This contribution attempts to review the bioaccessibility and bioavailability of phenolic compounds by focusing on the body’s internal mechanism including digestion, absorption, transport, modification, excretion, and colonic fermentation. The bioaccessibility and bioavailability of different phenolics vary depending on the physical condition of an individual, including digestive/absorptive/metabolic/response capability and effective dose. External factors such as processing methods and interaction with various food matrices also play a vital role on the bioavailability of dietary phenolic compounds. On the other hand, some novel phenolics have been synthesized to enable them rendering new bioactivities. The key internal factors influencing the bioaccessibility and bioavailability are also reviewed in this contribution. In addition, suggestions have been made for future measurement and assessment of bioavailability, together with prospects for food/nutraceutical/pharmaceutical application of novel phenolics.

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“…Efflux transporters such as P-gp, BCRP blocked by several polyphenols, e.g. flavonoids [124] Efflux transporters cell→basolateral Effect of polyphenols on efflux transporters such as MRP3 [194][195][196] Transporters gut lumen→cell SRB-1, CD36, NPC1L1, ABCG5/G8: affecting carotenoid uptake -influence of polyphenols [19,197,198] Colon Phase I/II interactions Piperine increased curcumin absorption [146]…”

Section: Efflux Transporters Cell→gut Lumenmentioning

confidence: 99%

Mind the gap—deficits in our knowledge of aspects impacting the bioavailability of phytochemicals and their metabolites—a position paper focusing on carotenoids and polyphenols

Bohn

McDougall

Alegrı́a

et al. 2015

Molecular Nutrition Food Res

218

145

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Various secondary plant metabolites or phytochemicals, including polyphenols and carotenoids, have been associated with a variety of health benefits, such as reduced incidence of type 2 diabetes, cardiovascular diseases, and several types of cancer, most likely due to their involvement in ameliorating inflammation and oxidative stress. However, discrepancies exist between their putative effects when comparing observational and intervention studies, especially when using pure compounds. These discrepancies may in part be explained by differences in intake levels and their bioavailability. Prior to exerting their bioactivity, these compounds must be made bioavailable, and considerable differences may arise due to their matrix release, changes during digestion, uptake, metabolism, and biodistribution, even before considering dose‐ and host‐related factors. Though many insights have been gained on factors affecting secondary plant metabolite bioavailability, many gaps still exist in our knowledge. In this position paper, we highlight several major gaps in our understanding of phytochemical bioavailability, including effects of food processing, changes during digestion, involvement of cellular transporters in influx/efflux through the gastrointestinal epithelium, changes during colonic fermentation, and their phase I and phase II metabolism following absorption.

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Non-Involvement of the Human Monocarboxylic Acid Transporter 1 (MCT1) in the Transport of Phenolic Acid

Cited by 21 publications

References 23 publications

Transport and Metabolism of Ferulic Acid through the Colonic Epithelium

Transport and Metabolism of Ferulic Acid through the Colonic Epithelium

Bioaccessibility and bioavailability of phenolic compounds

Mind the gap—deficits in our knowledge of aspects impacting the bioavailability of phytochemicals and their metabolites—a position paper focusing on carotenoids and polyphenols

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