Muscarinic-dependent inhibition of gastric emptying and intestinal motility by fractions of Maytenus ilicifolia Mart ex. Reissek

J Ethnopharmacol. 2009 Jun 25;123(3):385-91. doi: 10.1016/j.jep.2009.03.037. Epub 2009 Apr 5.

Abstract

Ethnopharmacological relevance: Maytenus ilicifolia Mart. ex. Reissek (Celastraceae) is widely used in Brazilian folk medicine to treat gastric disturbances.

Aim of the study: This work intended to characterize the effects of Maytenus ilicifolia on gastrointestinal motility.

Materials and methods: Gastric emptying and intestinal transit were measured in the same animal. Mice received a semisolid marked with phenol red, half an hour after treatment with extracts. The amount of marker in the stomach and the distance reached in the intestine after 15 min were measured as index of gastrointestinal emptying and intestinal transit, respectively.

Results: Intraperitoneal administration of a flavonoid-rich extract potently reduced the gastric emptying (ED(50)=89 mg/kg) and the intestinal transit (ED(50)=31 mg/kg) of mice. Bio-guided purification of the flavonoid-rich extract by chemical partition with solvents of decreasing polarity yielded fraction insF with about 12-14 times higher activity than the initial flavonoid extract in both the gastric emptying and the intestinal transit. The inhibitory effects of the insF (9.7 mg/kg, i.p.) on gastric emptying and intestinal transit were reversed by co-administration of bethanechol (10 mg/kg, s.c.) but not by co-administration of metoclopramide (30 mg/kg, p.o.) indicating muscarinic but not dopaminergic interaction of the compounds of Maytenus. Chemical investigation of the insF fraction by HPLC-MS allowed the identification of 4 free flavonoids (catechin, epicatechin, quercetin and kaempferol), 29 flavonol glycosides and 8 tannins. The flavonol glycosides ranged from 1 to 4 monosaccharide units, having mainly quercetin and kaempferol as aglycone moieties, and the tannins were composed by catechin/epicatechin and/or afzelechin/epiafzelechin.

Conclusions: Overall, the results indicate that the components of Maytenus ilicifolia have a potential use in the treatment of gastrointestinal motility disturbances such as diarrhea.

MeSH terms

  • Animals
  • Bethanechol / pharmacology
  • Cholinergic Agents / administration & dosage
  • Cholinergic Agents / chemistry
  • Cholinergic Agents / pharmacology*
  • Female
  • Flavonoids / pharmacology
  • Flavonols / pharmacology
  • Gastric Emptying / drug effects*
  • Gastrointestinal Motility / drug effects*
  • Glycosides / pharmacology
  • Injections, Intraperitoneal
  • Maytenus* / chemistry
  • Mice
  • Plant Extracts / administration & dosage
  • Plant Extracts / chemistry
  • Plant Extracts / isolation & purification
  • Plant Extracts / pharmacology*
  • Plants, Medicinal
  • Tannins / pharmacology

Substances

  • Cholinergic Agents
  • Flavonoids
  • Flavonols
  • Glycosides
  • Plant Extracts
  • Tannins
  • Bethanechol