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Type: Artigo de periódico
Title: Comparison of the gastroprotective effect of a diterpene lactone isolated from Croton cajucara with its synthetic derivatives
Author: Melo, PS
Duran, N
Hiruma-Lima, CA
Souza-Brito, ARM
Haun, M
Abstract: The effect of three new derivatives from dehydrocrotonin (DHC-compound I) on gastric damage indifferent animal models including gastric ulceration induced by a necrotic agent and hypothermic restrained-stress was studied: compound 11 (produced by reducing the cyclohexenone moiety of DHC with NaBH4): compound III (produced by reducing the carbonyls with LiAlH4); and compound IV (produced by transforming the lactone moiety into an amide). Their structures were confirmed on the basis of chemical and physicochemical evidence. When previously administered (p.o.) at a dose of 100 mg/kg, compound II significantly (P < 0.01) reduced gastric injury induced by HCl/ethanol (78%) and indomethacin (88%) better than did reference compound 1 (48 and 43%, respectively). But the anti-ulcerogenic activity of compound II was completely abolished by the stress-induced ulcer. Reduction of carbonyls with LiAlH4 (compound 111) caused decreased activity, markedly when no protective effect in any of the models was applied (P > 0.05). However, compound IV, in which the lactone moiety was changed into an amide. when administered at the same dose (100 mg/kg, p.o.), was more effective. The presence of a lactone moiety or Michael acceptor is probably essential for the anti-ulcerogenic effect of these compounds. (C) 2003 Elsevier Science Ireland Ltd. All rights reserved.
Subject: gastroprotective activity
Croton cajucara
Country: Irlanda
Editor: Elsevier Sci Ireland Ltd
Rights: fechado
Identifier DOI: 10.1016/S0378-8741(03)00139-9
Date Issue: 2003
Appears in Collections:Artigos e Materiais de Revistas Científicas - Unicamp

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