shogaol and Vomiting

Despite advances in antiemetic therapy, chemotherapy-induced nausea and vomiting (CINV) still poses a significant burden to patients undergoing chemotherapy. Nausea, in particular, is still highly prevalent in this population. Ginger has been traditionally used as a folk remedy for gastrointestinal complaints and has been suggested as a viable adjuvant treatment for nausea and vomiting in the cancer context. Substantial research has revealed ginger to possess properties that could exert multiple beneficial effects on chemotherapy patients who experience nausea and vomiting. Bioactive compounds within the rhizome of ginger, particularly the gingerol and shogaol class of compounds, interact with several pathways that are directly implicated in CINV in addition to pathways that could play secondary roles by exacerbating symptoms. These properties include 5-HT

Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Antiemetics; Antineoplastic Agents; Antioxidants; Catechols; Ethnopharmacology; Fatty Alcohols; Humans; Models, Biological; Nausea; Rhizome; Vomiting; Zingiber officinale

To investigate the antiemetic effect of the active extract (ginger ether extract, GEE) and its bioactive compounds in ginger, the pica vomiting model in rats and the gastric emptying model in mice were used to observe the antiemetic effect of GEE in cisplatin-induced pica and gastric emptying, and the main components in GEE were detected by RP-HPLC; in vitro, the antagonist effect of GEE and the four components in it were explored by the contraction of guinea-pig ileum induced by SR57227A and carbachol. The results showed that the amount of Kaolin ingested by rats were declined significantly in all the three groups of GEE (25,50,100 mg•kg⁻¹) (P<0.01), while cisplatin-induced gastric emptying in mice was also suppressed in all the three groups (P<0.01), and 6-gingerol, 8-gingerol,10-gingerol and 6-shogaol were found mainly in GEE by RP-HPLC; the maximum contraction of isolated guinea-pig ileum could be reduced by addition of GEE (2.3, 4.6, 11.5 mg•L⁻¹), 6-gingerol,8-gingerol,10-gingerol or 6-shogaol (1, 2, 5 μmol•L⁻¹) when the concentration of SR5727A was 1×10⁻⁵ mol•L⁻¹ and that of carbachol was 1×10⁻⁴ mol•L⁻¹ (P<0.05, P<0.01). In conclusion, 5-HT3 and M3 receptors could be antagonized by GEE and its bioactive compounds 6-gingerol, 8-gingerol, 10-gingerol and 6-shogaol, which may be correlated with the antiemetic mechanism of ginger maybe related to it.

Topics: Animals; Antiemetics; Catechols; Fatty Alcohols; Guinea Pigs; Male; Mice; Mice, Inbred ICR; Plant Extracts; Rats; Rats, Sprague-Dawley; Vomiting; Zingiber officinale

The herbal drug ginger (Zingiber officinale Roscoe) may be effective for treating nausea, vomiting, and gastric hypomotility. In these conditions, cholinergic M (3) receptors and serotonergic 5-HT (3) and 5-HT (4) receptors are involved. The major chemical constituents of ginger are [6]-gingerol, [8]-gingerol, [10]-gingerol, and [6]-shogaol. We studied the interaction of [6]-gingerol, [8]-gingerol, [10]-gingerol (racemates), and [6]-shogaol with guinea pig M (3) receptors, guinea pig 5-HT (3) receptors, and rat 5-HT (4) receptors. In whole segments of guinea pig ileum (bioassay for contractile M (3) receptors), [6]-gingerol, [8]-gingerol, [10]-gingerol, and [6]-shogaol slightly but significantly depressed the maximal carbachol response at an antagonist concentration of 10 µM. In the guinea pig myenteric plexus preparation (bioassay for contractile 5-HT (3) receptors), 5-HT maximal responses were depressed by [10]-gingerol from 93 ± 3 % to 65 ± 6 % at an antagonist concentration of 3 µM and to 48 ± 3 % at an antagonist concentration of 5 µM following desensitization of 5-HT (4) receptors and blockade of 5-HT (1) and 5-HT (2) receptors. [6]-Shogaol (3 µM) induced depression to 61 ± 3 %. In rat esophageal tunica muscularis mucosae (bioassay for relaxant 5-HT (4) receptors), [6]-gingerol, [8]-gingerol, [10]-gingerol, and [6]-shogaol (2-6.3 µM) showed no agonist effects. The maximal 5-HT response remained unaffected in the presence of the compounds. It is concluded that the efficiency of ginger in reducing nausea and vomiting may be based on a weak inhibitory effect of gingerols and shogaols at M (3) and 5-HT (3) receptors. 5-HT (4) receptors, which play a role in gastroduodenal motility, appear not to be involved in the action of these compounds.

Topics: Animals; Antiemetics; Catechols; Dose-Response Relationship, Drug; Drug Evaluation, Preclinical; Esophagus; Fatty Alcohols; Gastrointestinal Tract; Guinea Pigs; Ileum; In Vitro Techniques; Male; Muscle Contraction; Muscle Relaxation; Myenteric Plexus; Nausea; Phytotherapy; Plants, Medicinal; Rats; Rats, Wistar; Receptor, Muscarinic M3; Receptors, G-Protein-Coupled; Receptors, Serotonin, 5-HT3; Receptors, Serotonin, 5-HT4; Serotonin Antagonists; Vomiting; Zingiber officinale

The structure-activity relationship of diarylheptanoids and their analogues inhibitory of emesis induced by copper sulfate in young chicks was investigated by testing 19 compounds. The compounds are 5 diarylheptanoids isolated from Alpinia katsumadai (Zingiberacea), 5 chemical derivatives of them, 6 analogues isolated from Zingiber officinale rhizome (Zingiberaceae), and 3 analogues available on the market. Among them, two types of essential functional structure of diarylheptanoids and their analogues showed the inhibitory effects against emesis.

Topics: Animals; Antiemetics; Catechols; Chickens; Copper Sulfate; Fatty Alcohols; Heptanes; Magnetic Resonance Spectroscopy; Male; Molecular Structure; Phytotherapy; Plant Extracts; Structure-Activity Relationship; Vomiting; Zingiber officinale; Zingiberaceae