5-HT 3 and 5-HT 4 receptors contribute to the anti-motility effects of Garcinia buchananii bark extract in the guinea-pig distal colon

P. A. Boakye, C. Stenkamp-Strahm, Y. Bhattarai, M. D. Heckman, Stuart Brierley, S. P. Pasilis, O. B. Balemba

    Research output: Contribution to journalArticle

    15 Citations (Scopus)

    Abstract

    Background Garcinia buchananii bark extract is an anti-motility diarrhea remedy. We investigated whether G. buchananii bark extract has components that reduce gastrointestinal peristaltic activity via 5-HT 3 and 5-HT 4 receptors. Methods Aqueous G. buchananii extract was separated into fractions using preparative thin layer chromatography (PTLC), and major chemical components were identified using standard tests. The anti-motility effects of the extract and its fractions (PTLC1-5) were studied through pellet propulsion assays using isolated guinea-pig distal colons. Key Results Anti-motility (PTLC1 & PTLC5) and pro-motility (PTLC2) fractions were isolated from the extract. Flavonoids, steroids, alkaloids, tannins, and phenols were identified in the extract and PTLC1&5. The potency of the extract applied via the mucosal surface was reduced by 5-HT, 5-HT 3 receptor agonist RS-56812, 5-HT 4 receptor agonists cisapride and CJ-033466, 5-HT 3 receptor antagonist granisetron, and 5-HT 4 receptor antagonist GR-113808. The anti-motility effects of the aqueous extract and PTLC1&5 when applied serosally were reversed by RS-56812, cisapride, and CJ-033466. The 5-HT 3 receptor antagonists, granisetron and ondansetron, reduced the effects of the extract to an extent and completely reversed the anti-motility effects of PTLC1&5. GR-113808 inhibited the actions of the extract during the initial 10min, but enhanced the extracts' anti-motility effects after 15min. GR-113808 augmented the anti-motility activities of PTLC1 and PTLC5 by 30%. Conclusions & Inferences These results indicate that the anti-motility effects of G. buchananii aqueous extract are potentially mediated by compounds that affect 5-HT 3 and 5-HT 4 receptors. Identification and characterization of the bioactive compounds within G. buchananii could lead to the discovery of new non-opiate anti-diarrhea formulations.

    Original languageEnglish
    Pages (from-to)e27-e40
    Number of pages14
    JournalNeurogastroenterology and Motility
    Volume24
    Issue number1
    DOIs
    Publication statusPublished - Jan 2012

    Keywords

    • Diarrhea
    • Garcinia
    • Herbal remedy
    • Intestinal motility
    • Serotonin and 5-hydroxytryptamine

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