Planta Med 2001; 67(8): 726-731
DOI: 10.1055/s-2001-18342
Original Paper
Pharmacology
© Georg Thieme Verlag Stuttgart · New York

 A Mechanistic Approach to the In Vivo Anti-Inflammatory Activity of Sesquiterpenoid Compounds Isolated from Inula viscosa

Victoriano Hernández, María del Carmen Recio, Salvador Máñez, José María Prieto, Rosa María Giner, José Luis Ríos*
  • Departament de Farmacologia, Facultat de Farmàcia, Universitat de València, Burjassot, Spain
Weitere Informationen

Publikationsverlauf

October 20, 2000

January 28, 2001

Publikationsdatum:
09. November 2001 (online)

Abstract

The present study was designed to examine the anti-inflammatory activity of the sesquiterpenoids ilicic acid and inuviscolide, isolated from Inula viscosa, on cell degranulation, leukotriene biosynthesis, neurogenic drive and glucocorticoid-like interactions. Swiss female mice were used to measure the ear oedema induced by phorbol esters or ethyl phenylpropiolate (EPP), and the paw oedema induced by phospholipase A2 (PLA2) or serotonin. Drug treatment consisted of one topically-applied dose in the ear models and a subcutaneous or intraperitoneal injection in the paw models. Quantitative analysis of leukotriene B4 (LTB4) formation was performed on rat peritoneal neutrophils by high performance liquid chromatography (HPLC). The lactone inuviscolide reduced the PLA2-induced oedema (ID50: 98 μmol/kg). The effect on serotonin-induced oedema was not changed by modifiers of the glucocorticoid response. Ilicic acid showed minor in vivo effects, but was slightly more potent than inuviscolide on the 12-O-tetradecanoylphorbol 13-acetate (TPA) acute oedema test (ID50: 0.650 μmol per ear). Inuviscolide reduced LTB4 generation in intact cells, with an IC50 value of 94 μM. On the basis of the reported results, inuviscolide is the main anti-inflammatory sesquiterpenoid from Inula viscosa, and may act by interfering with leukotriene synthesis and PLA2-induced mastocyte release of inflammatory mediators.

Abbreviations

COX:cyclooxygenase

DMSO:dimethyl sulphoxide

DPP:12-deoxyphorbol 13-phenylacetate

EPP:ethyl phenylpropiolate

HPLC:high performance liquid chromatography

ID50:50 % inhibitory dose

5-HT:serotonin

LOX:lipoxygenase

LTB4:leukotriene B4

MTT:3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl-tetrazolium

PGB2:prostaglandin B2

PKC:protein kinase C

PLA2:phospholipase A2

TPA:12-O-tetradecanoylphorbol 13-acetate

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Prof. Dr. J. L. Ríos

Departament de Farmacologia

Facultat de Farmàcia

Universitat de València

Av. Vicent Andrés Estellés sn

46100 Burjassot

Spain

eMail: riosjl@uv.es

Fax: + 34-963 - 864 973