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. 2024 Jun 4;7(6):1694–1710. doi: 10.1021/acsptsci.4c00084

Table 2. In Vitro Studies: Effect of Various Phytochemicals on 5-HT3R.

S. No. Plant Name Chemical Constituents/Extracts Class In Vitro Model Concentration (IC50) Binding Site Reference
1. Panax ginseng (radix) (Araliaceae) Ginsenoside Steroid glycoside Xenopus laevis oocytes 27.6 ± 4.3 μM Antagonism of 5-HT3AR (22, 138)
2. Syzygium aromaticum (flos) (Myrtaceae) Tannic acid Polyphenol Xenopus laevis oocytes 48.2 ± 4.1 μM Antagonism of 5-HT3AR (22)
3. Lindera aggregate (radix) (Lauraceae) and Peumus boldus (Monimiaceae) Boldine Aporphine alkaloid Xenopus laevis oocytes 0.53 ± 0.15 μM Antagonism of 5-HT3AR (22, 139, 140)
4. Leonurus japonicas (herba) (Lamiaceae) Leonurine Alkaloid Xenopus laevis oocytes 2.17 ± 0.15 μM Antagonism of 5-HT3AR (22)
5. Schisandra chinesis (fructus) (Schisandraceae) Schizandrin Dibenzocyclooctadiene Xenopus laevis oocytes 48.2 ± 4.1 μM Antagonism of 5-HT3AR (22)
6. Zingiber officinale Roscoe (Zingiberaceae) Galanolactone Diterpene Guinea pig ileum 4.93 μM Contractile inhibition of ileum via 5-HT3R (27)
7. Rosa damascene (Rosaceae) Citronellol Monoterpenes Xenopus laevis oocyte 64 μM Competitively inhibits 5-HT3AR (40)
8. Cannabis sativa (Cannabaceae) Cannabinoid cannabidiol Alkaloids Xenopus laevis oocyte 121 nM to 29 μM Noncompetitively inhibits 5-HT3AR (41, 42)
9. Syzygium aromaticum (Myrtaceae) Eugenol vanillin Benzaldehyde Xenopus laevis oocytes 1159 μM eugenol and 4744 μM vanillin Noncompetitive antagonist at 5-HT3AR (40)
10. Zingiber officinale (Zingiberaceae) 6-Shogaol Polyphenol Xenopus laevis oocytes 30.6 ± 0.54 μM Noncompetitive antagonist at 5-HT3AR (40)
11. Zingiber officinale (Zingiberaceae) 6-Gingerol Polyphenol Xenopus laevis oocytes 46.6 ± 0.64 μM Noncompetitive antagonist at 5-HT3AR (40)
12. Hypericum perforatum (Hypericaceae) Hyperforin Terpene Peritoneal cells 3.4 μg/mL Inhibiting serotonin uptake via 5-HT3R antagonism (84)
13. Uncaria hook (Rubiaceae) Hirsutine Indole alkaloid Xenopus laevis oocytes 22.12 μM Antagonism of 5-HT3R and 5-HT3ABR (141)
14. Eucalyptus globulus (Myrtaceae) Eucalyptol Monoterpene Xenopus laevis oocytes 258 μM Antagonism of 5-HT3R (142)
15. Lippia alba (Varbenaceae) Citral Monoterpene Xenopus laevis oocytes 120 μM Antagonism of 5-HT3R (142)
16. Gingko biloba (Ginkgoaceae) Bilobalide, ginkgolides B Sesquiterpenoid Xenopus laevis oocytes Bilobalide 470 μM, Ginkgolide B730 μM Antagonism of 5-HT3R (110)
17. Cudrania tricuspidata (Moraceae) Kaempferol Flavonoid Xenopus laevis oocytes 12.8 ± 2.0 μM Antagonism of 5-HT3R (103)
18. Chili peppers (Solanaceae) Capsaicin Alkaloid Xenopus laevis oocytes 62 μM Antagonism of 5-HT3R (143)
19. Chili peppers (Solanaceae) Capsaicin Alkaloid HEK-293 cells 54 μM Antagonism of 5-HT3R (143)
20. Schisandra chinensis (Schisandraceae) Schisandrin C Lignan Xenopus laevis oocytes 27.0 μM Competitively antagonized 5-HT3R (144)
21. Xanthium spinosum (Asteraceae)     HEK-293 cells 4.6 ± 0.8 μg/mL Antagonism of 5-HT3R (23)
22. Senecio mathewsii (Asteraceae)     HEK-293 cells 5.0 ± 1.0 μg/mL Antagonism of 5-HT3R (23)