Activity-directed Isolation of Spasmolytic (anti-cholinergic) Alkaloids from Brugmansia arborea (L.) Lagerheim

Abstract

This paper examined the effects of the extracts MeOH and H 2 O, chromatographic fractions and three pure alkaloids from Brugmansia arborea (L.) Lagerheim (Solanaceae) on the electrically-and acetylcholine (Ach)-induced contractions of isolated guinea-pig ileum. The results indicate that both MeOH and H 2 O extracts dose-dependently reduced the electrical contractions of guinea-pig ileum. Furthermore, the partially purified fractions 2 and 3 from MeOH extract and three pure compounds obtained from the fraction 2 of MeOH extract significantly and dose-dependently reduced the electrical and the Ach-induced contractions of the ileum. The chemical identification, performed by spectroscopic methods, indicate that the three active substances -atropine, scopolamine, norhyoscine -were tropane alkaloids.

A Methanol Extract ofBrugmansia arboreaAffects the Reinforcing and Motor Effects of Morphine and Cocaine in Mice

“…This is in accordance with the literature, in which there are reports that the genus Brugmansia contains this class of alkaloids [9, 19]. …”

“…Drug addiction can be considered as a disorder of DA-dependent associative learning [24], and the fact that CPP and the hyperactivity induced by morphine are blocked by B. arborea extract suggests that this plant undermines the development of opiate addiction. Another possible explanation for the results obtained is the strong anticholinergic activity reported for a methanol extract of B. arborea [9]. Recent evidence implicates muscarinic acetylcholine receptors in the behavioral effects of drugs of abuse such as morphine and cocaine.…”

“…In one report, extracts, chromatographic fractions, and pure alkaloids from the species exerted an inhibitory activity on the contraction of isolated guinea pig ileum induced both electrically and by acetylcholine and on spasmolytic activity in vitro [9], thus indicating an anticholinergic activity. The three pure tropane alkaloids obtained from B. arborea were found to undermine symptoms in a concentration-dependent manner in an in vitro model of morphine withdrawal [10].…”

Effects ofBrugmansia arboreaExtract and Its Secondary Metabolites on Morphine Tolerance and Dependence in Mice

“…This result agrees with the available literature that reports that the genus Brugmansia contains this class of alkaloids [3]. …”

Medicinal Potentials and Toxicity Concerns of Bioactive Principles

“…Moreover, recent review showed that certain alkaloids are medicinally applied as local anesthetic [70], stimulants -(caffeine, nicotine, threobromine, methylated derivatives of xanthine, methylated uric acids such as theacrine, methylliberine and libertine [7]), psychedelics, analgesics -(morphine [72,73], codeine [41], N-methyl-N-deethylaconitine [74]), bactericidal-(piperidine [75], harmandiamines A-C [76]), anti-cancer drugs -(camptothecin, vinblastine, vincristine [7,77]), anti-hypertensive agents -(serpentine [78][79][80][81]), cholinomimerics -(aceclidine [41]), spasmolysis agents - [82], vasodilators -(rutaecarpine [83]), anti-arrhythmia, anti-asthma [41], anti-malarials (quinine and artemisinin [7]) etc.…”