ArticleFrontiers in pharmacology2015
Identification of Glycyrrhiza as the rikkunshito constituent with the highest antagonistic potential on heterologously expressed 5-HT3A receptors due to the action of flavonoids.
Article in Frontiers in pharmacology, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers, 1 of them a synthesis that pooled it.
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Who cites it
14 citing papers in PubMed, 1 synthesis or guideline pooled it, 23 citations in OpenAlex.
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- Medicinal Plants for Chemotherapy-Induced Nausea and Vomiting: A Systematic Review of Antiemetic, Chemosensitizing, and Immunomodulatory Mechanisms.Therapeutics and clinical risk management · 2025Review
- Bioelectric medicine: unveiling the therapeutic potential of micro-current stimulation.Biomedical engineering letters · 2024Review
- Research Progress on the Pharmacodynamic Mechanisms of Sini Powder against Depression from the Perspective of the Central Nervous System.Medicina (Kaunas, Lithuania) · 2023Review
- Review on the Diverse Biological Effects of Glabridin.Drug design, development and therapy · 2023Review
- Treatment of Gastrointestinal Disorders-Plants and Potential Mechanisms of Action of Their Constituents.Molecules (Basel, Switzerland) · 2022Review
- Role of Licochalcone A in Potential Pharmacological Therapy: A Review.Frontiers in pharmacology · 2022Review
- The Calcium-Activated Chloride Channel TMEM16A is Inhibitied by Liquiritigenin.Frontiers in pharmacology · 2021Article
- Effect of 158 herbal remedies on human TRPV1 and the two-pore domain potassium channels KCNK2, 3 and 9.Journal of traditional and complementary medicine · 2020Article
- Article
- Hwangryunhaedok-tang induces the depolarization of pacemaker potentials through 5-HTWorld journal of gastroenterology · 2017Article
- Potentiating effect of glabridin fromBiochemistry and biophysics reports · 2016Article
- Kampo Medicine: Evaluation of the Pharmacological Activity of 121 Herbal Drugs on GABAA and 5-HT3A Receptors.Frontiers in pharmacology · 2016Article
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Authors and funding
6 authors at 1 institution in 1 country.
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No grant is acknowledged in the PubMed record.
Abstract
The traditional Japanese phytomedicine rikkunshito is traditionally used for the treatment of gastrointestinal motility disorders, cachexia and nausea. These effects indicate 5-HT3 receptor antagonism, due to the involvement of these receptors in such pathophysiological processes. E.g., setrons, specific 5-HT3 receptor antagonists are the strongest antiemetics, developed so far. Therefore, the antagonistic effects of the eight rikkunshito constituents at heterologously expressed 5-HT3Areceptors were analyzed using the two-electrode voltage-clamp technique. The results indicate that tinctures from Aurantii, Ginseng, Zingiberis, Atractylodis and Glycyrrhiza inhibited the 5-HT3A receptor response, whereas the tinctures of Poria cocos, Jujubae and Pinellia exhibited no effect. Surprisingly, the strongest antagonism was found for Glycyrrhiza, whereas the Zingiberis tincture, which is considered to be primarily responsible for the effect of rikkunshito, exhibited the weakest antagonism of 5-HT3A receptors. Rikkunshito contains various vanilloids, ginsenosides and flavonoids, a portion of which show an antagonistic effect on 5-HT3 receptors. A screening of the established ingredients of the active rikkunshito constituents and related substances lead to the identification of new antagonists within the class of flavonoids. The flavonoids (-)-liquiritigenin, glabridin and licochalcone A from Glycyrrhiza species were found to be the most effective inhibitors of the 5-HT-induced currents in the screening. The flavonoids (-)-liquiritigenin and hesperetin from Aurantii inhibited the receptor response in a non-competitive manner, whereas glabridin and licochalcone A exhibited a potential competitive antagonism. Furthermore, licochalcone A acts as a partial antagonist of 5-HT3A receptors. Thus, this study reveals new 5-HT3A receptor antagonists with the aid of increasing the comprehension of the complex effects of rikkunshito.
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