title: 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 microg/mL) produced a concentration-related relaxation of the rat ileum [IC (50) (95 % c. l.) 0.24 (0.13 - 0.45) microg/mL]. Among the four fractions ( n-hexane, CCl (4), CHCl (3), 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 [IC (50) (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 1alpha,8beta,14-triacetoxy-9beta-furoyloxydihydro-beta-agarofuran ( 1), 1alpha, 6beta,8beta,14-tetraacetoxy-9beta-benzoyloxydihydro-beta-agarofuran ( 2) and 1alpha,8beta-diacetoxy-9beta-benzoyloxydihydro-beta-agarofuran ( 3), at the concentration of 1 microg/mL produced a relaxant effect of 30.6 +/- 12.2 %, 26.9 +/- 4.7 % and 7.27 +/- 1.7 %, respectively.
authors.affiliation: Dipartimento di Farmacologia Sperimentale, Università degli Studi di Napoli Federico II, Via D. Montesano 49, 80131 Naples, Italy. franborr@unina.it
authors.forename: Francesca
authors.initials: F
authors.lastname: Borrelli
authors.forename: Nicola
authors.initials: N
authors.lastname: Borbone
authors.forename: Raffaele
authors.initials: R
authors.lastname: Capasso
authors.forename: Domenico
authors.initials: D
authors.lastname: Montesano
authors.forename: Angelo A
authors.initials: AA
authors.lastname: Izzo
authors.forename: Simona
authors.initials: S
authors.lastname: De Marino
authors.forename: Francesco
authors.initials: F
authors.lastname: Capasso
authors.forename: Lydia
authors.initials: L
authors.lastname: Ferrara
authors.forename: Rocco
authors.initials: R
authors.lastname: Longo
authors.forename: Franco
authors.initials: F
authors.lastname: Zollo
mesh_terms: D000818:Animals; D031247:Celastrus; D004305:Dose-Response Relationship, Drug; D007082:Ileum / Q000187:drug effects*; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects*; D008517:Phytotherapy; D010938:Plant Oils / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D012639:Seeds; D012717:Sesquiterpenes / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology
chemical_list: D010938:Plant Oils; D012717:Sesquiterpenes