Planta Med 2004; 70(7): 652-656
DOI: 10.1055/s-2004-827190
Original Paper
Natural Product Chemistry
© Georg Thieme Verlag KG Stuttgart · New York

New Sesquiterpenes with Intestinal Relaxant Effect from Celastrus paniculatus

Francesca Borrelli1 , Nicola Borbone2 , Raffaele Capasso1 , Domenico Montesano3 , Angelo A. Izzo1 , Simona De Marino2 , Francesco Capasso1 , Lydia Ferrara3 , Rocco Longo4 , Franco Zollo2
  • 1Dipartimento di Farmacologia Sperimentale, Università degli Studi di Napoli ”Federico II”, Napoli, Italy
  • 2Dipartimento di Chimica delle Sostanze Naturali, Università degli Studi di Napoli ”Federico II”, Napoli, Italy
  • 3Dipartimento di Chimica Farmaceutica e Tossicologica, Università degli Studi di Napoli ”Federico II”, Napoli, Italy
  • 4Carlo Sessa SpA Laboratori Farmaceutici, Sesto S.G., Milano, Italy
Further Information

Publication History

Received: November 26, 2003

Accepted: March 21, 2004

Publication Date:
15 July 2004 (online)

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.

References

Francesca Borrelli

Dipartimento di Farmacologia Sperimentale

Università degli Studi di Napoli ”Federico II”

Via D. Montesano 49

80131 Napoli

Italy

Phone: +39-81-678-436

Fax: +39-81-678-403

Email: franborr@unina.it