Activation of transient receptor potential ankyrin 1 by quercetin and its analogs

Nakamura, Toshiyuki; Miyoshi, Noriyuki; Ishii, Takeshi; Nishikawa, Miyu; Ikushiro, Shinichi; Watanabe, Tatsuo

doi:10.1080/09168451.2015.1132148

Cited by 15 publications

(10 citation statements)

References 34 publications

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“…Moringa leaves have also been reported to contain various types of flavonol glycosides, as well as kaempferol, rutin, and quercetin [54]. Additionally, these flavonols are TRPA1 agonists [55].…”

Section: Discussionmentioning

confidence: 99%

Moringin, A Stable Isothiocyanate from Moringa oleifera, Activates the Somatosensory and Pain Receptor TRPA1 Channel In Vitro

Borgonovo

Petrocellis²,

Moriello³

et al. 2020

Molecules

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Moringa oleifera Lam. is a tropical plant widely used in traditional medicines and as a food supplement. It is characterized by the presence of glucosinolates and isothiocyanates; the stable isothiocyanate 4-[(α-l-rhamnosyloxy)benzyl]isothiocyanate (moringin) has been widely studied for its bioactivity as hypoglycemic, antimicrobial, anticancer and in particular for its involvement in nociception and neurogenic pain. Moringa extracts and pure moringin were submitted to in vitro assays with the somatosensory TRPA1 ion channel, proving that moringin is a potent and effective agonist of this receptor involved in nociceptive function and pain states. Moringin do not activate or activates very weakly the vanilloids somatosensory channels TRPV1,2,3 and 4, and the melastatin cooling receptor TRPM8. The comparison of moringin’s activity with other known agonists of natural origin is also discussed.

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Section: Discussionmentioning

confidence: 99%

Moringin, A Stable Isothiocyanate from Moringa oleifera, Activates the Somatosensory and Pain Receptor TRPA1 Channel In Vitro

Borgonovo

Petrocellis²,

Moriello³

et al. 2020

Molecules

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“…Recently, Nakamura T et al . found that methylated quercetin may bind with the transient receptor potential ankyrin 1 (TRPA1) and acts as agonist for this molecule, which may be the receptor for quercetin 48 . Quercetin exerts suppressive effects on the expression of collagen in lung fibroblasts by regulating the translocation of the nuclear factor E2-related factor-2 (Nrf2), an important transcription factor that regulates the expression of HO-1 from the cytoplasm to the nuclei 14 .…”

Section: Discussionmentioning

confidence: 99%

Quercetin Inhibits Fibroblast Activation and Kidney Fibrosis Involving the Suppression of Mammalian Target of Rapamycin and β-catenin Signaling

Ren

Liu

et al. 2016

Sci Rep

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Quercetin, a flavonoid found in a wide variety of plants and presented in human diet, displays promising potential in preventing kidney fibroblast activation. However, whether quercetin can ameliorate kidney fibrosis in mice with obstructive nephropathy and the underlying mechanisms remain to be further elucidated. In this study, we found that administration of quercetin could largely ameliorate kidney interstitial fibrosis and macrophage accumulation in the kidneys with obstructive nephropathy. MTORC1, mTORC2, β-catenin as well as Smad signaling were activated in the obstructive kidneys, whereas quercetin could markedly reduce their abundance except Smad3 phosphorylation. In cultured NRK-49F cells, quercetin could inhibit α-SMA and fibronectin (FN) expression induced by TGFβ1 treatment. MTORC1, mTORC2, β-catenin and Smad signaling pathways were stimulated by TGFβ1 at a time dependent manner. Similar to those findings in the obstructive kidneys, mTORC1, mTORC2 and β-catenin, but not Smad signaling pathways were remarkably blocked by quercetin treatment. Together, these results suggest that quercetin inhibits fibroblast activation and kidney fibrosis involving a combined inhibition of mTOR and β-catenin signaling transduction, which may act as a therapeutic candidate for patients with chronic kidney diseases.

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“…Several phytochemicals that interact with TRP channels were shown to be potential treatments for COVID-19 [ [121] , [122] , [123] , [124] , [125] , [126] , [127] , [128] , [129] , [130] , [131] , [132] , [133] , [134] , [135] , [136] , [137] , [138] , [139] , [140] , [141] , [142] ]. However, the implication of TRP channel in their mechanism of action had not been investigated yet.…”

Section: Resultsmentioning

confidence: 99%

“…Quercetin is a well known a ligand for TRPM7, TRPV1 and TRPA1 channels [ [133] , [134] , [135] ]. In a prospective, randomized, controlled, and open-label study, a daily dose of 1000 mg of quercetin was given for 30 days to 152 COVID-19 outpatients to study its adjuvant effect in treating the early symptoms and in preventing the severe consequences of the disease.…”

Section: Resultsmentioning

confidence: 99%

TRP channels in COVID-19 disease: Potential targets for prevention and treatment

Jaffal

Abbas

2021

Chemico-Biological Interactions

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Coronavirus disease 2019 [COVID-19] is a global health threat caused by severe acute respiratory syndrome coronavirus 2 [SARS-CoV2] that requires two proteins for entry: angiotensin-converting enzyme 2 [ACE2] and trans-membrane protease serine 2 [TMPRSS2]. Many patients complain from pneumonia, cough, fever, and gastrointestinal (GI) problems. Notably, different TRP channels are expressed in various tissues infected by SARS-CoV-2. TRP channels are cation channels that show a common architecture with high permeability to calcium [Ca 2+ ] in most sub-families. Literature review shed the light on the possible role of TRP channels in COVID-19 disease. TRP channels may take part in inflammation, pain, fever, anosmia, ageusia, respiratory, cardiovascular, GI and neurological complications related to COVID-19. Also, TRP channels could be the targets for many active compounds that showed effectiveness against SARS-CoV-2. Desensitization or blocking of TRP channels by antibodies, aptamers, small molecules or venoms can be an option for COVID-19 prevention and future treatment. This review provides insights into the involvement of TRP channels in different symptoms and mechanisms of COVID-19, potential treatments targeting these channels and highlights missing gaps in literature.

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Activation of transient receptor potential ankyrin 1 by quercetin and its analogs

Cited by 15 publications

References 34 publications

Moringin, A Stable Isothiocyanate from Moringa oleifera, Activates the Somatosensory and Pain Receptor TRPA1 Channel In Vitro

Moringin, A Stable Isothiocyanate from Moringa oleifera, Activates the Somatosensory and Pain Receptor TRPA1 Channel In Vitro

Quercetin Inhibits Fibroblast Activation and Kidney Fibrosis Involving the Suppression of Mammalian Target of Rapamycin and β-catenin Signaling

TRP channels in COVID-19 disease: Potential targets for prevention and treatment

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