Bronchodilator activity of Phymatodes scolopendria (Burm.) Ching and its bioactive constituent

Phymatodes scolopendria (Burm.) Ching (Polypodiaceae) is widely used in the Eastern coast of Madagascar to treat respiratory disorders. Bioassay-guided fractionation using guinea pig trachea pre-contracted with histamine to monitor the activity led to the isolation of 1,2-benzopyrone (coumarin) as t...

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Published inJournal of ethnopharmacology Vol. 102; no. 3; pp. 400 - 407
Main Authors Ramanitrahasimbola, D., Rakotondramanana, D.A., Rasoanaivo, P., Randriantsoa, A., Ratsimamanga, S., Palazzino, G., Galeffi, C., Nicoletti, M.
Format Journal Article
LanguageEnglish
Published Shannon Elsevier Ireland Ltd 01.12.2005
Elsevier
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Summary:Phymatodes scolopendria (Burm.) Ching (Polypodiaceae) is widely used in the Eastern coast of Madagascar to treat respiratory disorders. Bioassay-guided fractionation using guinea pig trachea pre-contracted with histamine to monitor the activity led to the isolation of 1,2-benzopyrone (coumarin) as the main active constituent. Effectively, it induced a concentration-dependent relaxation of the histamine with a median effective concentration (EC 50) of 35.03 μg/ml, or carbachol (EC 50 = 33.41 μg/ml) pre-contracted guinea pig trachea, and also provoked 100% relaxation at 72.10 μg/ml. It was less active either on KCl pre-contracted trachea (EC 50 = 130.78 μg/ml) or endothelium denuded trachea (153.4 ± 22 μg/ml). It inhibited, in a non-competitive manner, the histamine and the external calcium spasm effect on the isolated trachea but it did not significantly modify the broncho-constrictive activity of KCl. When combined with theophylline, coumarin produced a significant additive relaxing effect on pre-contracted trachea. Furthermore, its bronchodilator effect was not blocked by propranolol. In vivo, pre-treated guinea pig with coumarin showed significant resistance to histamine inhalation, with an adequate dose protecting 50% of the tested animals (AD 50) of 75 mg/kg. These results indicate that the bronchodilator effect of coumarin is partly due to the endothelium-dependent tracheal relaxation, and may be mediated through a non-specific tracheal relaxation.
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ISSN:0378-8741
1872-7573
DOI:10.1016/j.jep.2005.06.037