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Can J Physiol Pharmacol ; 81(4): 387-96, 2003 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-12769230

RESUMO

The effects of beta-cyclodextrin (betaCD) inclusion complexation on the ability of violacein to prevent gastric ulceration in mice were studied. Violacein-betaCD inclusion complexes were prepared in 1:1 and 1:2 molar ratios and analysed by differential scanning calorimetry and powder X-ray diffractometry. Violacein previously administered orally at 10 mg/kg significantly reduced indomethacin-induced gastric lesions, as well as 100 mg/kg of cimetidine (positive control). However, betaCD complexation in both molar ratios significantly potentiated the protective action of violacein. In the HCl--ethanol-induced gastric ulcer model, violacein and the 1:2 inclusion complex (10 mg/kg, p.o.) inhibited gastric damage by almost 85%, whereas a 63% reduction was observed for the positive control, lansoprazole, at 30 mg/kg. In contrast, treatment with the 1:1 inclusion complex resulted in almost total disappearance of the antiulcer activity in this model. No significant changes in stress-induced gastric injury were found. In addition, the 1:2 inclusion complex improved the antilipoperoxidant activity of violacein in rat liver cells exposed to t-butyl hydroperoxide, whereas the 1:1 complex was less active than violacein. In summary, the 1:2 betaCD inclusion complex has gastroprotective properties similar to or higher than that of violacein. An increase in mucosal defensive mechanisms and protection against peroxidative damage might be involved.


Assuntos
Antiulcerosos/farmacologia , Ciclodextrinas/farmacologia , Indóis/farmacologia , Animais , Células Cultivadas , Química Farmacêutica , Cimetidina/farmacologia , Modelos Animais de Doenças , Etanol/efeitos adversos , Hepatócitos/efeitos dos fármacos , Ácido Clorídrico/efeitos adversos , Indometacina/efeitos adversos , Indometacina/antagonistas & inibidores , Peroxidação de Lipídeos/efeitos dos fármacos , Masculino , Malondialdeído/metabolismo , Camundongos , Ratos , Ratos Wistar , Úlcera Gástrica/induzido quimicamente , Úlcera Gástrica/tratamento farmacológico , Úlcera Gástrica/prevenção & controle , Estresse Fisiológico/fisiopatologia , terc-Butil Hidroperóxido/efeitos adversos
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