Comparative anti-inflammatory and antinociceptive effects of terpenoids and an aqueous extract obtained from Croton cajucara Benth

Abstract

RESUMO: "Avaliação comparativa dos efeitos anti-infl amatório e antinociceptivo de terpenóides e de extrato aquoso obtidos de Croton cajucara Benth". O 19-nor-clerodano trans-crotonina (CTN) e o triterpeno ácido acetil aleuritólico (AAA), isolados das cascas do caule de Croton cajucara Benth (Euphorbiaceae), uma planta tradicional da Região Amazônica do Brasil, bem como o extrato aquoso (EA) das cascas do caule deste Croton, foram submetidos a experimentos farmacológicos utilizando animais, para avaliação das atividades anti-infl amatória e antinociceptiva. A administração oral de AAA (50 mg/kg), CTN (50 mg/kg) ou AE (300 mg/ kg) inibiram as contorções em ratos, induzidas por ácido acético. Os terpenóides AAA e CTN, bem como o extrato polar EA, inibiram signifi cativamente o edema de pata em ratos, induzido por carragenina. As inibições foram observadas em todos os intervalos de medições, tendo sido evidenciado melhores inibições para os terpenóides AAA (47,7%, após a primeira hora) e CTN (54,4%, após a segunda hora). Evidenciou-se ainda, após 90 minutos do estímulo, signifi cante inibição no edema induzido por dextrana (31,9% para CTN e 28,5% para AAA) e por histamina (43,2% para CTN e 40,5% para AAA). Estes resultados confi rmam o uso popular de Croton cajucara na região Amazônica do Brasil, no combate a infl amações. Unitermos:Croton cajucara, ácido acetil aleuritólico, trans-crotonina, anti-infl amatório, antinociceptivo. ABSTRACT:The 19-nor-clerodane trans-crotonin (CTN) and the triterpene acetyl aleuritolic acid (AAA), isolated from the stem bark of Croton cajucara Benth (Euphorbiaceae), a traditional medicinal plant from Amazon region of Brazil, as well as the aqueous extract (AE) from its stem bark, were submitted to pharmacological screening for anti-infl ammatory and antinociceptive activities in animal models. The oral administration of AAA (50 mg/kg), CTN (50 mg/kg) or AE (300 mg/kg) inhibited the acetic acid-induced writhing in mice. The AE, CTN and AAA had shown signifi cant inhibition of carrageenin-induced edema in rats, in all time intervals measured after the injection of the stimulus, with the greatest inhibition at the fi rst hour for AAA (47.7%) and the second hour for CTN (54.4%). They have also exhibited signifi cant inhibition in the dextran-induced edema 90 minutes after the stimulus: 31.9% for CTN and 28.5% for AAA. In the histamine-induced edema, the inhibition showed by CTN and AAA were 43.2% and 40.5%, respectively, 90 minutes after the injection of stimulus. This study extends and supports the popular medicine and folkloric uses of Croton cajucara in the Amazon region of Brazil.

Terpenóides com atividade sobre o Sistema Nervoso Central (SNC)

“…Compostos como linalool, limoneno e citronelol possuem ação anticonvulsivante, enquanto mentol e mirceno, atividade analgésica. Muitos derivados monoterpênicos têm demonstrado atividades sobre o SNC, incluindo sedativa, antinociceptiva e antidepressiva (Pergentino de Souza et al, 2007;Sousa et al, 2007;Perazzo et al, 2007Perazzo et al, , 2008Leite et al, 2008). O presente trabalho propõe uma revisão sobre terpenos com ações descritas no SNC, enfocando principalmente os sistemas neurotransmissores relacionados a estas.…”

Evaluation of antinociceptive and antiinflammatory effects of Croton pullei var. glabrior Lanj. (Euphorbiaceae)

“…In this context, a genus with several species used in the folk medicine to treat different disorders is the genus Croton. Some of Croton species have been exhaustively studied with their medicinal and toxicological properties being scientifi cally proven (Souza et al, 2006;Costa et al, 2007;Perazzo et al, 2007;Salatino et al, 2007;Torrico et al, 2007). Other species of this genus were poorly studied, and their pharmacological properties and collateral effects are still unknown.…”

Terpenoids as Source of Anti-Inflammatory Compounds

“…Compound showed exhibited significant inhibition in the dextran-induced edema 90 minutes after the stimulus: 31.9% for CTN and 28.5% for AAA. In the histamine-induced edema, the inhibition showed by CTN and AAA were 43.2% and 40.5%, respectively [40]. Acetyl-11-keto--boswellic acid (AKBA) (21), a component of an Ayurvedic therapeutic plant Boswellia serrata, is a pentacyclic terpenoid active against a large number of inflammatory diseases AKBA inhibited the NF-B-dependent reporter gene expression activated by TNFR type 1, TNFR-associated death domain protein, TNFR-associated factor 2, NF-B-inducing kinase, and IKK [41].…”