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标题：Natural trans-Crotonin: The Antiulcerogenic Effect of Another Diterpene Isolated from the Bark of Croton cajucara BENTH.
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作者：Clélia Akiko Hiruma-Lima ; Walber Toma ; Juliano de Souza Gracioso 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2002
卷号：25
期号：4
页码：452-456
DOI：10.1248/bpb.25.452
出版社：The Pharmaceutical Society of Japan
摘要：The nor-clerodane diterpene trans -crotonin isolated from the bark of Croton cajucara B ENTH . was investigated for its ability to prevent the formation of gastric-mucosa ulceration in different experimental models in mice. The results obtained from crotonin were compared with those obtained with another diterpene, DHC ( trans -dehydrocrotonin) in the same models. When previously administered ( p.o. ) at the dose of 100 mg/kg, crotonin, as well as DHC, significantly reduced ( p <0.05) gastric injury induced by stress (72, 67%), indomethacin/bethanechol (78, 29%) and pylorus ligature (35, 30%). In the HCl/ethanol-induced gastric ulcer model, at oral doses of 100 and 250 mg/kg, crotonin significantly prevented ( p <0.05) the formation of gastric lesions by 51 and 56%, respectively, when compared to the control group. Gastric injury was also of significantly less magnitude in the DHC treatment group ( p <0.05). In the pylorus-ligature model, crotonin ( p.o. ), like cimetidine, increased the volume of gastric juice when compared to the control group ( p <0.05). No significant modifications where found in gastric parameters such as pH or total acid content after oral crotonin treatment. However, systemic alterations were observed when crotonin (100 mg/kg) was previously administered intraduodenally to mice. We observed significant changes ( p <0.001) in gastric-juice parameters such as an increase in volume and a decrease in gastric acidity. Those pre-treated with crotonin as well as with DHC did not increase free mucus production ( p >0.05). The results suggest that crotonin presents a significant anti-ulcer effect when assessed in these ulcer-induced models. As with DHC, the antiulcerogenic effects of crotonin are probably related to anti-secretory or/and gastroprotective properties of this substance. In light of results obtained with DHC and natural trans -crotonin in the present study, we concluded that the A-ring of both diterpenes is not directly involved in the antiulcerogenic activity.
关键词：crotonin;DHC;gastroprotective activity;Croton cajucara;diterpene;Euphorbiaceae