Effect of Ginseng Saponins on the Recombinant Serotonin Type 3A Receptor Expressed in Xenopus Oocytes: Implication of Possible Application as an Antiemetic

Min, Kyungha; Koo, Bon‐Nyeo; Kang, Jeong Wan; Bai, Sun Joon; Ko, Sung Ryong; Cho, Zang-Hee

doi:10.1089/107555303322284794

Cited by 23 publications

(9 citation statements)

References 21 publications

(22 reference statements)

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“…Ginsenosides (Rg 1 , Re or Rg 2 ) have been acknowledged as key regulators of the 5HT3A receptor during emesis. Another study reports that Rb 1 and Rg 1 exert a similar degree of inhibitory activity on the 5HT3A receptor in Xenopus laevis oocytes Min et al, 2003). The HPLC analysis of RG in this study revealed relatively high and moderate concentrations of the protopanaxadiol ginsenosides Rb 1 , Rg 3, Rc, Rb 2 , Rg 2 and other protopanaxatriol (Table 1).…”

Section: Discussionsupporting

confidence: 63%

Saponin and non-saponin fractions of red ginseng ameliorate cisplatin-induced pica in rats

Sathyanath

Rao

Kim

et al. 2013

Pharmaceutical Biology

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Context: Nausea and vomiting are considered as the foremost unpleasant side effects of chemotherapy experienced by 20-90% of cancer patients. Objective: In the present study, the effects of Korean Panax ginseng C.A. Meyer (Araliaceae) (RG), ginseng saponin (GS) and non-saponin (GNS) on cisplatin (CP)-induced pica and gastric damage in rats were investigated. Material and methods: Rats were treated with RG (25, 50, 100 mg/kg b.wt.), GS (5 and 10 mg/kg 100 mg/kg b.wt.) and GNS (50 and 100 mg/kg b.wt.) before or after a single intraperitoneal injection of CP (6 mg/kg b.wt.). Kaolin together with normal food intake, normal food alone, body weight, histological examination of stomach and small intestine were used as indices of CP-induced pica in rats. Results: Pre-treatment with RG (50 and 100 mg/kg b.wt.) attenuated CP-induced kaolin intake at 24 h. CP-induced kaolin intake decreased upon post-treatment of rats with RG (50 and 100 mg/ kg b.wt.) at 48 h. The incidence of body weight reduction at 48 and 72 h diminished in rats posttreated with RG (50 mg/kg b.wt.). Pre-treatment with GS (5 and 10 mg/kg b.wt.) and GNS (50 and 100 mg/kg b.wt.) attenuated CP-induced kaolin intake while normal food intake was not improved in 24 and 48 h. Discussion and conclusion: The gastro-protective effects of RG, GS and GNS were further confirmed by histopathological (damage in glandular portion and villi with dilated appearance) findings. The study indicates that both the red GS and GNS improve feeding behavior against CP-induced pica in rats.

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Section: Discussionsupporting

confidence: 63%

Saponin and non-saponin fractions of red ginseng ameliorate cisplatin-induced pica in rats

Sathyanath

Rao

Kim

et al. 2013

Pharmaceutical Biology

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“…1), and thus Rg1 and Rb1 would be thought of as active compounds in our experimental model. However, our previous study indicated that nonginsenoside fractions of P. ginseng also exerted protective effects, comparable with the ginsenoside fraction, on cisplatin-induced gastric damage in a rat model [51], and others also showed similar effects using nonsaponin fractions [52]. Moreover, the general formula of P. ginseng traditionally comprises the whole fraction, as the PGE used in our current study.…”

Section: Discussionsupporting

confidence: 49%

Panax ginseng Meyer prevents radiation-induced liver injury via modulation of oxidative stress and apoptosis

Kim

Jang

Lee

et al. 2017

Journal of Ginseng Research

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BackgroundRadiotherapy is one of the most important modalities in cancer treatment; however, normal tissue damage is a serious concern. Drug development for the protection or reduction of normal tissue damage is therefore a clinical issue. Herein, we evaluated the protective properties of Panax ginseng Meyer and its corresponding mechanisms.MethodsC56BL/6 mice were orally pretreated with P. ginseng water extract (PGE; 25 mg/kg, 50 mg/kg, or 100 mg/kg) or intraperitoneally injected melatonin (20 mg/kg) for 4 d consecutively, then exposed to 15-Gy X-ray radiation 1 h after the last administration. After 10 d of irradiation, the biological properties of hematoxicity, fat accumulation, histopathology, oxidative stress, antioxidant activity, pro-inflammatory cytokines, and apoptosis signals were examined in the hepatic tissue.ResultsThe irradiation markedly induced myelosuppression as determined by hematological analysis of the peripheral blood. Steatohepatitis was induced by X-ray irradiations, whereas pretreatment with PGE significantly attenuated it. Oxidative stress was drastically increased, whereas antioxidant components were depleted by irradiation. Irradiation also notably increased serum liver enzymes and hepatic protein levels of pro-inflammatory cytokines. Those alterations were markedly normalized by pretreatment with PGE. The degree of irradiation-induced hepatic tissue apoptosis was also attenuated by pretreatment with PGE, which was evidenced by a terminal deoxynucleotidyl transferase 2′-deoxyuridine 5′-triphosphate nick-end labeling assay, western blotting, and gene expressions analysis, particularly of apoptotic molecules.ConclusionWe suggest that PGE could be applicable for use against radiation-induced liver injury, and its corresponding mechanisms involve the modulation of oxidative stress, inflammatory reactions, and apoptosis.

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“…Kim et al showed that Ginseng extracts reduce cisplatin-induced nausea in ferrets (Kim et al, 2005 ). Steroid glycosides, called ginsenosides, are accountable for the observed 5-HT 3A receptor antagonism (Min et al, 2003 ; Lee et al, 2007 ), and their binding site in the pore region of 5-HT 3A receptors has been identified (Lee et al, 2007 ).…”

Section: Discussionmentioning

confidence: 99%

Identification of Glycyrrhiza as the rikkunshito constituent with the highest antagonistic potential on heterologously expressed 5-HT3A receptors due to the action of flavonoids

et al. 2015

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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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Effect of Ginseng Saponins on the Recombinant Serotonin Type 3A Receptor Expressed in Xenopus Oocytes: Implication of Possible Application as an Antiemetic

Cited by 23 publications

References 21 publications

Saponin and non-saponin fractions of red ginseng ameliorate cisplatin-induced pica in rats

Saponin and non-saponin fractions of red ginseng ameliorate cisplatin-induced pica in rats

Panax ginseng Meyer prevents radiation-induced liver injury via modulation of oxidative stress and apoptosis

Identification of Glycyrrhiza as the rikkunshito constituent with the highest antagonistic potential on heterologously expressed 5-HT3A receptors due to the action of flavonoids

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