New Sesquiterpenes with Intestinal Relaxant Effect from Celastrus paniculatus

Abstract

The seed oil obtained from Celastrus paniculatus has been used in Ayurvedic medicine for the treatment of several complaints including intestinal disorders. The muscle relaxing activity of C. paniculatus has been studied in vitro on isolated preparations of rat intestine. C. paniculatus seeds extract (0.001 - 100 μg/mL) produced a concentration-related relaxation of the rat ileum [IC₅₀ (95 % c. l.) 0.24 (0.13 - 0.45) μg/mL]. Among the four fractions (n-hexane, CCl₄, CHCl₃, n-BuOH) obtained from the methanolic extract of C. paniculatus, only the carbon tetrachloride fraction (0.01 - 10 000 ng/mL) induced a significant relaxation of the intestinal muscle [IC₅₀ (95 % c. l.): 1.9 (1.38 - 2.87) ng/mL]. Three new sesquiterpene polyol esters have been isolated from the carbon tetrachloride fraction. These new metabolites, characterised as 1α,8β,14-triacetoxy-9β-furoyloxydihydro-β-agarofuran (1), 1α, 6β,8β,14-tetraacetoxy-9β-benzoyloxydihydro-β-agarofuran (2) and 1α,8β-diacetoxy-9β-benzoyloxydihydro-β-agarofuran (3), at the concentration of 1 μg/mL produced a relaxant effect of 30.6 ± 12.2 %, 26.9 ± 4.7 % and 7.27 ± 1.7 %, respectively.

Key words

Celastrus paniculatus - Celastraceae - sesquiterpenes - dihydro-β-agarofurans - intestinal motility - muscle-relaxant activity

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