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钙醇酮 B 的胃保护作用:与前列腺素、一氧化氮和巯基无关。

Gastroprotective effect of calealactone B: Lack of involvement of prostaglandins, nitric oxide and sulfhydryls.

机构信息

Escuela Superior de Medicina, Instituto Politécnico Nacional, Ciudad de México, México.

Departamento de Farmacia, Facultad de Química, Universidad Nacional Autónoma de México, Ciudad de México, 04510, México.

出版信息

Drug Dev Res. 2018 Feb;79(1):11-15. doi: 10.1002/ddr.21415. Epub 2017 Oct 26.

Abstract

Hit, Lead & Candidate Discovery The gastroprotective effect of calealactone B, isolated from Calea urticifolia was assessed in an ethanol-induced model of gastric lesioning. The possible involvement of prostaglandins, nitric oxide (NO) and sulfhydryl groups in the mechanism of action of calealactone B was also assessed. Calealactone B inhibited ethanol-induced gastric injuries with a maximal effect (95.3 ± 2.6%) at 30 mg kg . A similar value was obtained at 10 mg kg (83.5 ± 7.7%). Meanwhile, the reference anti-ulcer drug, carbenoxolone, an 11β-hydroxysteroid dehydrogenase (11β-HSD) inhibitor administered at 30 mg kg showed 63.5 ± 9.4% gastroprotection. Hence, calealactone B was more potent than carbenoxolone. Pretreatment with indomethacin, L-NAME or NEM did not reverse the effects of calealactone B, indicating that prostaglandins, NO and sulfhydryl compounds do not participate in its mechanism of action.

摘要

打击、领先和候选发现 从 Calea urticifolia 中分离出的 calalactone B 的胃保护作用在乙醇诱导的胃损伤模型中进行了评估。还评估了 calalactone B 的作用机制中前列腺素、一氧化氮 (NO) 和巯基的可能参与。calealactone B 抑制乙醇诱导的胃损伤,最大效应(95.3±2.6%)在 30 mg kg 时达到。在 10 mg kg 时也获得了类似的值(83.5±7.7%)。同时,参考抗溃疡药物 carbenoxolone,一种 11β-羟甾脱氢酶 (11β-HSD) 抑制剂,在 30 mg kg 时显示出 63.5±9.4%的胃保护作用。因此,calealactone B 比 carbenoxolone 更有效。预先用吲哚美辛、L-NAME 或 NEM 处理不能逆转 calalactone B 的作用,表明前列腺素、NO 和巯基化合物不参与其作用机制。

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