Spasmolytic Effects Of Kauranoid And Ester Of Linear Alkaloid From The Aerial Part Of Croton Borarium (Euphorbiaceae) Endemic In South Part Of Madagascar

Abstract

The aerial part of the plant known under the vernacular name Somorombohitse (Malagasy name) and scientifically named Croton Borarium (Euphorbiaceae) endemic in the South part of Madagascar, is used by the local communities to treat asthma and hypertension. The biologic test result riddling of the isolated trachea of guinea pig stimulated by the acetylcholine in 210^-2M showed antiasthmatic activity with the CE50= 0.85±0.001µg/ml (n=6). Effet concentration of carbachol from 10^-9M to 10^-3M have been realized in absence and in presence of the hydro-ethanolic extract of Cr. Borarium to 0.1mg/ml, verapamil to 10µM and atropine to 10nM. The relaxing activity of hydro-ethanolic extract from 0.1 to 3 mg/ml has been executed on the isolated aorta and jejunum of rabbit stimulated with the KCl to 50nM. White the using of the extract technic by partitioned liquid-liquid to permitted localizing the active fraction (Hex/DCM: 3/1) with CI50= 0.275±0.003µg/ml (n=6).

The bioassay-guided fractionation of the active fraction using repeated silica gel column chromatography resulted in the isolation of two pure compounds active as evidenced by analytical TLC and HPLC analysis. The elucidation of pharmacologic mechanism of these active principles has showed that, to first and active principle bring into play the calcic movement through the cellular membrane of vascular and polished muscle and the second is the by way of NO intermediate. Their chemical structures of two pure compounds were determined by 1D and 2D NMR spectroscopy and spectroscopy High-resolution MS.