Extraoral Taste Receptor Discovery: New Light on Ayurvedic Pharmacology

Gîlcă, Marilena; Dragoș, Dorin

doi:10.1155/2017/5435831

Cited by 28 publications

(44 citation statements)

References 358 publications

(346 reference statements)

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“…TAS2Rs have been discovered in various non‐taste cell types, including cardiac myocytes, gut enteroendocrine cells, leukocytes, sperm and upper airway epithelial cells 27,30,31 . We have provided evidence to show that TAS2R14 is functionally expressed in human epidermal keratinocytes.…”

Section: Discussionmentioning

confidence: 84%

“…Studies have shown that extraoral taste receptors mediate various physiological processes including immune responses of the upper airway, nutrient uptake in the gut, and testis development 27,30,31,38 . Wölfle et al showed that keratinocytes upregulated differentiation genes in the presence of bitter tastants and hypothesized that TAS2R signaling in these cells promotes differentiation and epidermal barrier formation 26 .…”

Section: Discussionmentioning

confidence: 99%

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Functionally expressed bitter taste receptor TAS2R14 in human epidermal keratinocytes serves as a chemosensory receptor

Bigliardi

Stelmashenko

et al. 2021

Experimental Dermatology

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Traditionally, it is theorized that skin sensation is initiated when cutaneous sensory afferents and Merkel cells receive sensory stimuli, while epidermal keratinocytes were deemed to have no role. However, mounting evidence has shown that keratinocytes can initiate skin sensation by receiving sensory stimuli and transmitting sensory information to sensory afferents. Knowledge regarding the mechanisms by which keratinocytes receive exogenous stimuli is limited, with TRP channels and olfactory receptors having been proposed to serve as receptors for exogenous stimuli in keratinocytes. Recently, expression analyses have demonstrated the expression of multiple TAS2R genes in human skin. TAS2Rs are chemosensory GPCRs employed by taste cells to detect bitter‐tasting substances. However, only subtypes TAS2R1 and TAS2R38 have been characterized in epidermal keratinocytes. We present evidence suggesting that subtype TAS2R14 is functionally expressed in epidermal keratinocytes. TAS2R14 transcripts and protein were detected in primary and N/TERT‐1 keratinocytes. Additionally, keratinocytes responded to α‐thujone, a TAS2R14 ligand, with an increase in intracellular free Ca2+ concentration. The tastant‐evoked Ca2+ signals were found to be mediated by wild‐type TAS2R14 and heterotrimeric G proteins. We conclude that TAS2R14 serves as a chemosensory receptor in epidermal keratinocytes and hypothesize that it enables the cells to recognize potentially harmful chemical substances.

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Section: Discussionmentioning

confidence: 84%

Section: Discussionmentioning

confidence: 99%

Functionally expressed bitter taste receptor TAS2R14 in human epidermal keratinocytes serves as a chemosensory receptor

Bigliardi

Stelmashenko

et al. 2021

Experimental Dermatology

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“…On the other hand, we need to pay attention to the side effects of bitter tastants for drugs since many bitter tastants are toxins. In fact, the extra-oral expression of TAS2Rs has been hypothesized to cause off-target effects of bitter medications (Clark et al, 2012; Gilca and Dragos, 2017). Therefore, the suitable dose will be critical for developing drugs based on bitter tastants.…”

Section: Discussion and Future Directionsmentioning

confidence: 99%

Toward the Identification of Extra-Oral TAS2R Agonists as Drug Agents for Muscle Relaxation Therapies via Bioinformatics-Aided Screening of Bitter Compounds in Traditional Chinese Medicine

Luo

Jin

et al. 2019

Front. Physiol.

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Significant advances have been made in the past decade in mapping the distributions and the physiological functions of extra-oral bitter taste receptors (TAS2Rs) in nongustatory tissues. In particular, it has been found that TAS2Rs are expressed in various muscle tissues and activation of TAS2Rs can lead to muscle cell relaxation, which suggests that TAS2Rs may be important new targets in muscle relaxation therapy for various muscle-related diseases. So far, however, there is a lack of potent extra-oral TAS2R agonists that can be used as novel drug agents in muscle relaxation therapies. Interestingly, traditional Chinese medicine (TCM) often characterizes a drug's property in terms of five distinct flavors (bitter, sweet, sour, salty, and pungent) according to its taste and function, and commonly regards "bitterness" as an intrinsic property of "good medicine." In addition, many bitter flavored TCM are known in practice to cause muscle relaxation after long term use, and in lab experiments the compounds identified from some bitter flavored TCM do activate TAS2Rs and thus relax muscle cells. Therefore, it is highly possible to discover very useful extra-oral TAS2R agonists for muscle relaxation therapies among the abundant bitter compounds used in bitter flavored TCM. With this perspective, we reviewed in literature the distribution of TAS2Rs in different muscle systems with a focus on the map of bitter flavored TCM which can regulate muscle contractility and related functional chemical components. We also reviewed the recently established databases of TCM chemical components and the bioinformatics software which can be used for high-throughput screening and data mining of the chemical components associated with bitter flavored TCM. All together, we aim to present a knowledge-based approach and technological platform for identification or discovery of extra-oral TAS2R agonists that can be used as novel drug agents for muscle relaxation therapies through screening and evaluation of chemical compounds used in bitter flavored TCM.

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“…6 These are unique concepts in Ayurveda which can potentially be applied to all living things that are a source of food and medicine in this world. 7 CP is described as being pungent (katu) and bitter (tikta) in taste, piercing in quality (teekshna), hot in potency (ushnaveerya), pungent post-digestion (katuvipaka), with special effect of boosting the intellect (medhya). It improves cognition, memory, digestion, relieves constipation, aids wound healing and is also prescribed for anemia like conditions, liver disorders, certain skin diseases and arthritis.…”

Section: Ayurvedamentioning

confidence: 99%

Neuropharmacological and Cognitive Effects of Celastrus paniculatus – A Comprehensive Review

Bhagya¹,

Jaideep²

2020

IJPSRR

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Celastrus paniculatus (CP) has been used for thousands of years in Indian system of medicine, Ayurveda. It is referred to as Jyotishmati and as the name suggests, boosts intelligence. Seed and seed oil are the most used parts of this deciduous plant and oral and intranasal routes are most preferred for delivering this drug in Ayurveda. Studies in laboratory animals have shown CP improves intellect and memory and is beneficial in neurodegeneration. Clinical studies in mentally retarded children have also shown that it enhances the Intelligence quotient. CP also ameliorates stress associated cognitive dysfunctions. The herb possesses antioxidant, free radical scavenging and neuroprotective activity. This manuscript reviews current information on the neuropharmacological effects of Celastrus paniculatus (CP) in different neuropsychiatric conditions.

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Extraoral Taste Receptor Discovery: New Light on Ayurvedic Pharmacology

Cited by 28 publications

References 358 publications

Functionally expressed bitter taste receptor TAS2R14 in human epidermal keratinocytes serves as a chemosensory receptor

Functionally expressed bitter taste receptor TAS2R14 in human epidermal keratinocytes serves as a chemosensory receptor

Toward the Identification of Extra-Oral TAS2R Agonists as Drug Agents for Muscle Relaxation Therapies via Bioinformatics-Aided Screening of Bitter Compounds in Traditional Chinese Medicine

Neuropharmacological and Cognitive Effects of Celastrus paniculatus – A Comprehensive Review

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