Pertz, Heinz H. and Lehmann, Jochen and Roth-Ehrang, Rene and Elz, Sigurd (2011) Effects of Ginger Constituents on the Gastrointestinal Tract: Role of Cholinergic M-3 and Serotonergic 5-HT3 and 5-HT4 Receptors. PLANTA MEDICA, 77 (10). pp. 973-978. ISSN 0032-0943, 1439-0221
Full text not available from this repository. (Request a copy)Abstract
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-HT3 and 5-HT4 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-HT3 receptors, and rat 5-HT4 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 mu M. In the guinea pig myenteric plexus preparation (bioassay for contractile 5-HT3 receptors), 5-HT maximal responses were depressed by [10]-gingerol from 93 +/- 3% to 65 +/- 6% at an antagonist concentration of 3 mu M and to 48 +/- 3% at an antagonist concentration of 5 mu M following desensitization of 5-HT4 receptors and blockade of 5-HT1 and 5-HT2 receptors. [6]-Shogaol (3 mu M) induced depression to 61 +/- 3%. In rat esophageal tunica muscularis mucosae (bioassay for relaxant 5-HT4 receptors), [6]-gingerol, [8]-gingerol, [10]-gingerol, and [6]shogaol (2-6.3 mu M) 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-HT3 receptors. 5-HT4 receptors, which play a role in gastroduodenal motility, appear not to be involved in the action of these compounds.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | GUINEA-PIG ILEUM; ZINGIBER-OFFICINALE; MOTION SICKNESS; INDUCED EMESIS; EFFICACY; CHEMOTHERAPY; PHARMACOLOGY; PRINCIPLES; MOTILITY; THERAPY; ginger; Zingiber officinale Roscoe; Zingiberaceae; gastrointestinal diseases; cholinergic M-3 receptors; 5-HT3 receptors; 5-HT4 receptors |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry I (Prof. Elz) |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 09 Jun 2020 05:54 |
| Last Modified: | 09 Jun 2020 05:54 |
| URI: | https://pred.uni-regensburg.de/id/eprint/20625 |
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