Isolation and chemical and pharmacological characterization of potential trace amine-associated receptor antagonist from plant sources

Natividad, Gaudencio M. 2010. Isolation and chemical and pharmacological characterization of potential trace amine-associated receptor antagonist from plant sources. PhD Thesis, Cardiff University.

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Abstract

The present study describes the preliminary evaluation of Philippine medicinal plants Artemisia vulgaris, Chrysanthemum coronarium, Moringa oleifera, Sesbania grandiflora and Vitex negundo for their antagonistic activity at selected biogenic amine receptors on smooth muscle of the airways, gastrointestinal tract and vascular system. The antagonistic activity of these plants were studied against dose-response curves for contractions of the guinea pig ileum, trachea and aorta to 5-hydroxytryptamine (5-HT2 receptors), methacholine (M3 muscarinic receptors), histamine (Hi receptors), phenylephrine (d -adrenoceptors) and P-phenylethylamine (trace amine-associated receptors, TAARi). The methanolic extracts of S. grandiflora (flowers and leaves) revealed the presence of histamine Hi receptor and muscarinic M3 receptor antagonist in the ileum. The A. vulgaris chloroform (AV-CHC13) and methanol (AV-MeOH) extracts, and the acid-base extract of V. negundo (VN-E) showed histamine Hi antagonism in the ileum and trachea. Further analysis of AV-CHCI3 isolated two major components yomogin and l,2,3,4-diepoxy-ll(13)-eudesmen-12,8-olide. Yomogin a sesquiterpene lactone exhibited a novel histamine Hi receptor antagonism in the ileum. Repeated exposure of aortic rings to phenylephrine and (3-PEA CRCs produced significant increases in maximum vascular tension due to enhanced intracellular Ca2+ mobilization. Both the AV-CHCI3 and VN-E inhibited this enhanced response. Further analysis of AV-CHCI3 revealed that it is probably inhibiting the increase of vascular tone mediated via intracellular Ca2+ release regulated by ryanodine. This study further validates the traditional use of S. grandiflora, A. vulgaris and V. negundo in the treatment of hyperactive gut, asthma and hypertension.

Item Type:	Thesis (PhD)
Status:	Unpublished
Schools:	Pharmacy
Subjects:	R Medicine > RM Therapeutics. Pharmacology
ISBN:	9781303195808
Funders:	Ford Foundation - International Fellowship Program
Date of First Compliant Deposit:	30 March 2016
Last Modified:	19 Mar 2016 23:29
URI:	https://orca.cardiff.ac.uk/id/eprint/54392

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