New sesquiterpenes with intestinal relaxant effect from Celastrus paniculatus.
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.
Borrelli
Francesca
F
Dipartimento di Farmacologia Sperimentale, Università degli Studi di Napoli Federico II, Via D. Montesano 49, 80131 Naples, Italy. franborr@unina.it
Borbone
Nicola
N
Capasso
Raffaele
R
Montesano
Domenico
D
Izzo
Angelo A
AA
De Marino
Simona
S
Capasso
Francesco
F
Ferrara
Lydia
L
Longo
Rocco
R
Zollo
Franco
F
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
D010938:Plant Oils; D012717:Sesquiterpenes