Theaflavins inhibit glucose transport across Caco-2 cells through the downregulation of the Ca2+/AMP-activated protein kinase-mediated glucose transporter SGLT1

Li, Baorui; Fu, Lei; Abe, Chizumi; Nectoux, Alexia M.; Yamamoto, Ayaka; Matsui, Toshiro

doi:10.1016/j.jff.2020.104273

Cited by 14 publications

(12 citation statements)

References 39 publications

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“…Previous studies have reported that polyphenols in black tea can regulate the activity of Ca 2+ and nitric oxide synthase in SkM, as well as enhance muscle contraction . In addition, TFs have also been reported to promote Ca 2+ transport in Coca-2 cells to regulate intestinal glucose metabolism …”

Section: Discussionmentioning

confidence: 98%

“…13 In addition, TFs have also been reported to promote Ca 2+ transport in Coca-2 cells to regulate intestinal glucose metabolism. 49 After Ca 2+ enters the cell, it often directly activates the CaMKK2 activity, thereby activating a series of downstream biological activities. 50 The formation of SkM slow-twitch muscle fibers mainly relies on calcium-dependent signaling pathways, such as Ca 2+ /calmodulin-activated phosphatase, calcineurin-and Ca 2+ -/calmodulin-dependent protein kinase, and the CaMKK signaling pathway in SkM.…”

Section: ■ Discussionmentioning

confidence: 99%

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Theaflavin Promotes Mitochondrial Abundance and Glucose Absorption in Myotubes by Activating the CaMKK2-AMPK Signal Axis via Calcium-Ion Influx

Liu

et al. 2021

J. Agric. Food Chem.

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Drinking tea has been proven to have a positive biological effect in regulating human glucose and lipid metabolism and preventing type 2 diabetes (T2D). Skeletal muscle (SkM) is responsible for 70% of the sugar metabolism in the human body, and its dysfunction is an important factor leading to the development of obesity, T2D, and muscle diseases. As one of the four known theaflavins (TFs) in black tea, the biological role of theaflavin (TF1) in regulating SkM metabolism has not been reported. In this study, mature myotubes induced by C2C12 cells in vitro were used as models. The results showed that TF1 (20 μM) promoted mitochondrial abundance and glucose absorption in myotubes by activating the CaMKK2-AMPK signaling axis via Ca2+ influx. Moreover, it promoted the expression of slow muscle fiber marker genes (Myh7, Myl2, Tnnt1, and Tnnc1) and PGC-1α/SIRT1, as well as enhanced the oxidative phosphorylation capacity of myotubes. In conclusion, this study preliminarily clarified the potential role of TF1 in regulating SkM glucose absorption as well as promoting SkM mitochondrial biosynthesis and slow muscle fiber formation. It has potential research and application values for the prevention/alleviation of SkM-related T2D and Ca2+-related skeletal muscle diseases through diet.

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Section: Discussionmentioning

confidence: 98%

Section: ■ Discussionmentioning

confidence: 99%

Theaflavin Promotes Mitochondrial Abundance and Glucose Absorption in Myotubes by Activating the CaMKK2-AMPK Signal Axis via Calcium-Ion Influx

Liu

et al. 2021

J. Agric. Food Chem.

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“…Theaflavin 3-gallate is a major component of black tea which is already known for its anti-oxidant properties and is the most consumed beverage in the world. Since theaflavin 3-gallate is already consumed by humans through tea and crosses cell–cell barriers in the body 47 , it is an excellent potential inhibitor against SARS-CoV-2. Either the molecule alone or in formulations with other such anti-viral compounds as a cocktail can provide an effective first line of defense against diseases associated with coronaviruses.…”

Section: Discussionmentioning

confidence: 99%

Theaflavin 3-gallate inhibits the main protease (Mpro) of SARS-CoV-2 and reduces its count in vitro

Chauhan

Bhardwaj

Kumar

et al. 2022

Sci Rep

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The main protease (Mpro) of SARS-CoV-2 has been recognized as an attractive drug target because of its central role in viral replication. Our previous preliminary molecular docking studies showed that theaflavin 3-gallate (a natural bioactive molecule derived from theaflavin and found in high abundance in black tea) exhibited better docking scores than repurposed drugs (Atazanavir, Darunavir, Lopinavir). In this study, conventional and steered MD-simulations analyses revealed stronger interactions of theaflavin 3-gallate with the active site residues of Mpro than theaflavin and a standard molecule GC373 (a known inhibitor of Mpro and novel broad-spectrum anti-viral agent). Theaflavin 3-gallate inhibited Mpro protein of SARS-CoV-2 with an IC50 value of 18.48 ± 1.29 μM. Treatment of SARS-CoV-2 (Indian/a3i clade/2020 isolate) with 200 μM of theaflavin 3-gallate in vitro using Vero cells and quantifying viral transcripts demonstrated reduction of viral count by 75% (viral particles reduced from Log106.7 to Log106.1). Overall, our findings suggest that theaflavin 3-gallate effectively targets the Mpro thus limiting the replication of the SARS-CoV-2 virus in vitro.

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“…Thea avin 3-gallate is a major component of black which is already known for its anti-oxidant properties and is the most consumed beverage in the world. Since thea avin 3-gallate is already consumed by humans through tea for ages and being edible, crossing cell-cell barriers in the body 40 makes it a good potential inhibitor to be used against SARS-CoV-2. Either the molecule alone or in formulations with other such anti-viral compounds as a cocktail can provide an effective rst line of defense against diseases associated with coronaviruses.…”

Section: Discussionmentioning

confidence: 99%

Theaflavin 3-gallate inhibits the main protease (Mpro) of SARS-CoV-2 and reduces its count in vitro

Chauhan

Bhardwaj

Kumar

et al. 2022

Preprint

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Main protease (Mpro) of SARS-CoV-2 is crucial for its replication/infection and has been recognized as an attractive drug target. In this study, we identified theaflavin 3-gallate as an inhibitor of Mpro protein of SARS-CoV-2 with IC50 value of 18.48 ± 1.29 µM. Compared to theaflavin, theaflavin 3-gallate exhibited superior antiviral activity and at a concentration of 200 µM reduced the viral count by 75% (viral particles reduced from 106.7 to 106.1). Time-dependent analyses of conventional and steered MD-simulations revealed stronger interactions of theaflavin 3-gallate with the active site residues of Mpro than the standard molecule GC373 and theaflavin. Taken together, our findings suggest that theaflavin 3-gallate can be developed into a potential lead molecule against SARS-CoV-2.

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Theaflavins inhibit glucose transport across Caco-2 cells through the downregulation of the Ca2+/AMP-activated protein kinase-mediated glucose transporter SGLT1

Cited by 14 publications

References 39 publications

Theaflavin Promotes Mitochondrial Abundance and Glucose Absorption in Myotubes by Activating the CaMKK2-AMPK Signal Axis via Calcium-Ion Influx

Theaflavin Promotes Mitochondrial Abundance and Glucose Absorption in Myotubes by Activating the CaMKK2-AMPK Signal Axis via Calcium-Ion Influx

Theaflavin 3-gallate inhibits the main protease (Mpro) of SARS-CoV-2 and reduces its count in vitro

Theaflavin 3-gallate inhibits the main protease (Mpro) of SARS-CoV-2 and reduces its count in vitro

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