TY - JOUR
T1 - 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
AU - Boakye, P. A.
AU - Stenkamp-Strahm, C.
AU - Bhattarai, Y.
AU - Heckman, M. D.
AU - Brierley, S. M.
AU - Pasilis, S. P.
AU - Balemba, O. B.
PY - 2012/1
Y1 - 2012/1
N2 - 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.
AB - 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.
KW - Diarrhea
KW - Garcinia
KW - Herbal remedy
KW - Intestinal motility
KW - Serotonin and 5-hydroxytryptamine
UR - http://www.scopus.com/inward/record.url?scp=84155186397&partnerID=8YFLogxK
U2 - 10.1111/j.1365-2982.2011.01807.x
DO - 10.1111/j.1365-2982.2011.01807.x
M3 - Article
C2 - 22074563
AN - SCOPUS:84155186397
SN - 1350-1925
VL - 24
SP - e27-e40
JO - Neurogastroenterology and Motility
JF - Neurogastroenterology and Motility
IS - 1
ER -