The Croton oil ear test revisited

Tubaro, Aurelia; Dri, Pietro; Delbello, Giorgio; Zilli, Chiara; Loggia, R. Della

doi:10.1007/bf01982641

Cited by 217 publications

(202 citation statements)

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“…Oedema was quantified by the difference in weight between the samples taken from the right treated and left untreated ears. The antioedema activity was expressed as percent inhibition of oedema in mice treated with the test substances with respect to oedema of animals treated with the irritant alone (Tubaro et al, 1985).Evaluation of the granulocyte infiltrate. The cellular infiltrate was quantified in the treated ears measuring the myeloperoxidase activity, as index of the presence of neutrophilic granulocytes, in the same ear samples as used to determine oedema (Tubaro et al, 1985).…”

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confidence: 99%

Rimonabant reduces keratinocyte viability by induction of apoptosis and exerts topical anti‐inflammatory activity in mice

Malfitano

Sosa

Laezza

et al. 2010

British J Pharmacology

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There is growing evidence that the cannabinoid CB1 receptor antagonist, rimonabant (SR141716) exerts potential anti-proliferative and anti-inflammatory actions. Here, we have assessed the effects of rimonabant in vitro in murine immortalized keratinocytes and in vivo by assaying the topical anti-inflammatory activity. EXPERIMENTAL APPROACHCell viability and death in a keratinocyte cell line (C5N cells) were measured by Trypan blue exclusion assay and cytotoxicity by sulphorhodamine B test. Cell cycle progression was assessed by flow cytometry and the expression of apoptotic and anti-apoptotic markers, cyclins, pathways of signal transduction and CB1 receptor levels were evaluated by Western blot. The topical anti-inflammatory properties of rimonabant were analysed by inhibition of croton oil-induced ear dermatitis in mice. KEY RESULTSRimonabant reduced cell viability and induced apoptosis as shown by the enhanced number of cells in the subG0 phase of the cell cycle, the expression of Bax and reduced levels of Bcl-2 and X-inhibitor of apoptosis protein. In addition, reduced levels of phosphorylated serine/threonine protein kinase Akt and nuclear factor-kappa B were detected associated with regulation of total nuclear factor-kappa B and inhibitor of kappa B-a, phosphorylated inhibitor of kappa B-a, cyclins D1, E and A. In croton oil-induced ear dermatitis, rimonabant significantly reduced oedema and leukocyte infiltrate. CONCLUSIONS AND IMPLICATIONSRimonabant reduced cell viability, inducing cell death in keratinocytes and decreased croton oil-induced ear dermatitis. Our findings suggest a potential application of rimonabant as a topical anti-inflammatory drug. We did not assess the involvement of CB1 receptors in these effects of rimonabant. AbbreviationsFBS, fetal bovine serum; NSAID, non-steroidal anti-inflammatory drug; TMB, tetramethylbenzidine; TRPV1, vanilloid receptor BJP British Journal of Pharmacology DOI:10.1111DOI:10. /j.1476DOI:10. -5381.2010 84 British Journal of Pharmacology (2011) Introduction Rimonabant (SR141716) [N-piperidino-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4methyl pyrazole-3-carboxamide] is a potent and selective cannabinoid CB1 receptor antagonist (receptor nomenclature follows Alexander et al., 2009), inhibiting food intake and exhibiting anti-obesity activity (RinaldiCarmona et al., 1994;1995;Colombo et al., 1998;Simiand et al., 1998;Ravinet Trillou et al., 2003;Carai et al., 2005;Jbilo et al., 2005). It is widely used as a tool to investigate mechanisms by which cannabinoid agonists produce their pharmacological effects and may exert several of its actions by blocking the activation of CB1 receptors, thus modulating the endocannabinoid system, which is tonically activated under certain pathophysiological conditions (Di Marzo and Matias, 2005;Engeli et al., 2005;Matias et al., 2006;Jhaveri et al., 2007;Pertwee, 2009). Anti-tumour properties have been attributed to rimonabant by our group in several cancer cell lines in vitro and in vivo (Sarnataro et al., 2006;Santoro et al., 200...

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confidence: 99%

Rimonabant reduces keratinocyte viability by induction of apoptosis and exerts topical anti‐inflammatory activity in mice

Malfitano

Sosa

Laezza

et al. 2010

British J Pharmacology

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“…27,28 The previous administration (60 min) of the crude oil from stem barks from D. brasiliensis at 200 mg kg -1 , showed an oedema reduction similar to the positive control indomethacin at 10 mg kg -1 but superior to that observed to pure polygodial at same concentration (200 mg kg -1 ) before 60 min of carrageenan administration (Figure 3). This result indicated that the volatile derivatives from stem bark showed antiedematogenic/anti-inflammatory proprieties due to reduction of acute oedema.…”

Section: Resultsmentioning

confidence: 81%

Chemical composition and anti-inflammatory evaluation of essential oils from leaves and stem barks from Drimys brasiliensis Miers (Winteraceae)

Lago¹,

Carvalho²,

Silva³

et al. 2010

J. Braz. Chem. Soc.

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Os óleos essenciais das folhas e das cascas do tronco de Drimys brasiliensis Miers (Winteraceae) foram obtidos individualmente por hidrodestilação e suas composições químicas foram determinadas através de análise por CG/DIC e CG/EM. Os principais constituintes identificados foram monoterpenos (folhas 4,31% e cascas do tronco 90,02%) e sesquiterpenos (folhas 52,31% e cascas do tronco 6,35%). Adicionalmente, o sesquiterpeno poligodial foi isolado do extrato em hexano das cascas do tronco de D. brasiliensis após fracionamento cromatográfico e caracterizado por métodos espectroscópicos. Visando a avaliação do potencial anti-inflamatório, os óleos essenciais brutos e o sesquiterpeno poligodial foram submetidos à bioensaios para avaliação da toxicidade aguda destes compostos bem como das atividades anti-inflamatória e antinociceptiva induzidas por carragenina e formalina em ratos. Nossos resultados mostraram que o óleo essencial bruto obtido das cascas do tronco reduziu significativamente o edema induzido por carragenina. O efeito anti-inflamatório induzido pelo óleo das cascas do tronco (a 200 mg kg -1 ) foi similar ao observado para indometacina (a 10 mg kg -1 ) e superior ao poligodial (a 200 mg kg -1 ) em 30 e em 60 min após administração. A resposta inflamatória induzida pela formalina foi efetiva para o óleo das cascas do tronco (62,5%) em comparação ao poligodial (50,0%).The essential oils from leaves and stem barks from Drimys brasiliensis Miers (Winteraceae) were individually obtained by hydrodistillation and their compounds characterized by use of GC/FID and GC/MS. The main identified derivatives were monoterpenes (leaves 4.31% and stem barks 90.02%) and sesquiterpenes (leaves 52.31% and stem barks 6.35%). Additionally, the sesquiterpene polygodial was isolated from hexane extract from stem barks of D. brasiliensis after chromatographic steps and characterized by spectroscopic means, mainly NMR. Aiming the evaluation of anti-inflammatory potential, the crude essential oils and the sesquiterpene polygodial were subjected to bioassays to evaluate the acute toxicity of these compounds as well as the anti-inflammatory and antinociceptive activities induced by carrageenan and formalin in mices. Ours results showed that essential oil obtained from the stem barks significantly reduced the oedema induced by carrageenan. The anti-inflammatory effect induced by stem barks oil (at 200 mg kg -1 ) was similar to observed for indomethacin (at 10 mg kg -1 ) and superior for polygodial (at 200 mg kg -1 ) in 30 and 60 min after the administration of essential oils. The inflammatory response induced by formalin was effective to the stem barks oil (62.5%) in comparison to polygodial (50.0%).Keywords: Drimys brasiliensis Miers, essential oil composition, antinociceptive, antiinflammatory, acute toxicity IntroductionDrimys brasiliensis Miers belongs to Winteraceae family, whose occurrence is restrict to South America. This species is known in Brazil with a vernacular name "cascad'anta" and has been used in folk medicine as analg...

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“…TKI did not in¯uence the cutaneous in¯ammation induced by croton oil, a model strongly inhibited by steroid antiin¯ammatory agents (Tubaro et al, 1985), excluding once more a possible drug in¯uence on the endogenous corticosteroids system. In contrast, TKI reduced the ear oedema induced by capsaicin in mice, a model of neurogenic in¯ammation reported to involve primarily the release of neuropeptides through activation of sensory nerves (Inoue et al, 1993), suggesting implication of tissue kallikrein also in this model.…”

Section: Discussionmentioning

confidence: 83%

Evidence for activation of the tissue kallikrein‐kinin system in nociceptive transmission and inflammatory responses of mice using a specific enzyme inhibitor

Emim¹,

Souccar²,

Castro³

et al. 2000

British J Pharmacology

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1 The pharmacological activity of phenylacetyl-Phe-Ser-Arg-N-(2,4-dinitrophenyl)-ethylenediamine (TKI), a tissue kallikrein speci®c inhibitor, was assessed using models of nociception and in¯ammation in mice. 2 Injection of TKI (13.6 ± 136 mmol kg 71 , i.p. or 41 ± 410 mmol kg 71 , s.c.) produced a dose-related inhibition of the acetic acid-induced writhes (by 37 to 85% or 34 to 80%, respectively). The antinociceptive activity of TKI (41 mmol kg 71 , i.p.) was maximal after 30 min injection and lasted for 120 min. The e ect was unaltered by pretreatment with naloxone (8.2 mmol kg 71 , s.c.) or bilateral adrenalectomy. 3 TKI (41 and 136 mmol kg 71 , i.p.) produced a dose-related decrease of the late phase of formalininduced nociception by 79 and 98%, respectively. At 136 mmol kg 71 , i.p., TKI also shortened the duration of paw licking in the early phase by 69%. TKI (41 and 136 mmol kg 71 , i.p.) also reduced the capsaicin-induced nociceptive response (by 51 to 79%). 4 TKI (41 mmol kg 71 , i.p. or 410 mmol kg 71 , s.c.) reduced the oedematogenic response, from the second to the ®fth hour after carrageenin injection by 36 to 30% or by 47 to 39%, respectively. 5 Pretreatment with TKI (41 mmol kg 71 , i.p.) reduced the capsaicin-induced neurogenic in¯ammation in the mouse ear by 54%. 6 It is concluded that TKI presents antinociceptive and antiin¯ammatory activities mediated by inhibition of kinin formation by tissue kallikrein in mice. The results also indicate that the tissue kallikrein-dependent pathway contributes to kinin generation in nociceptive and in¯ammatory processes in mice.

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The Croton oil ear test revisited

Cited by 217 publications

References 4 publications

Rimonabant reduces keratinocyte viability by induction of apoptosis and exerts topical anti‐inflammatory activity in mice

Rimonabant reduces keratinocyte viability by induction of apoptosis and exerts topical anti‐inflammatory activity in mice

Chemical composition and anti-inflammatory evaluation of essential oils from leaves and stem barks from Drimys brasiliensis Miers (Winteraceae)

Evidence for activation of the tissue kallikrein‐kinin system in nociceptive transmission and inflammatory responses of mice using a specific enzyme inhibitor

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