Effects of Ginger Constituents on the Gastrointestinal Tract: Role of Cholinergic M3 and Serotonergic 5-HT3 and 5-HT4 Receptors (original) (raw)

Planta Med 2011; 77(10): 973-978
DOI: 10.1055/s-0030-1270747

Biological and Pharmacological Activity

Original Papers
© Georg Thieme Verlag KG Stuttgart · New York

Heinz H. Pertz1 , Jochen Lehmann2 , 3 , René Roth-Ehrang2 , Sigurd Elz4

• 1Institut für Pharmazie, Freie Universität Berlin, Berlin (Dahlem), Germany
• 2Institut für Pharmazie, Friedrich-Schiller-Universität Jena, Jena, Germany
• 3College of Pharmacy, King Saud University, Riyadh, Saudi Arabia
• 4Institut für Pharmazie, Universität Regensburg, Regensburg, Germany

Further Information

Publication History

received October 18, 2010 revised January 10, 2011

accepted January 14, 2011

Publication Date:
08 February 2011 (online)

Abstract

The herbal drug ginger (Zingiber officinale Roscoe) may be effective for treating nausea, vomiting, and gastric hypomotility. In these conditions, cholinergic M3 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 M3 receptors, guinea pig 5-HT3 receptors, and rat 5-HT4 receptors. In whole segments of guinea pig ileum (bioassay for contractile M3 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-HT3 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-HT4 receptors and blockade of 5-HT1 and 5-HT2 receptors. [6]-Shogaol (3 µM) 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 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 M3 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.

Key words

ginger - Zingiber officinale Roscoe - Zingiberaceae - gastrointestinal diseases - cholinergic M3 receptors - 5‐HT3 receptors - 5‐HT4 receptors

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Prof. Dr. Heinz H. Pertz

Institut für Pharmazie
Freie Universität Berlin

Königin-Luise-Straße 2 + 4

14195 Berlin (Dahlem)

Germany

Phone: +49 30 83 85 31 35

Fax: +49 30 83 85 55 76

Email: hpertz@zedat.fu-berlin.de