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

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.

Gastroprotective Effect of Juanislamin on Ethanol-Induced Gastric Lesions in Rats: Role of Prostaglandins, Nitric Oxide and Sulfhydryl Groups in the Mechanism of Action

“…Consequently, the mechanism of action of the test compound is not related to nitric oxide. For carbenoxolone, however, gastroprotection was notably decreased by l-NAME pretreatment, as previously reported [8].…”

“…Since indomethacin pretreatment did not diminish the gastroprotection provided by juanislamin (Figure 4a), prostaglandins do not take part in its mechanism of action. Contrarily, indomethacin sharply reduced the gastroprotection of the reference drug, as observed in other studies [8].…”

“…In general, medicinal plants are an attractive source of new drugs. A plant with known gastroprotective activity, C. urticifolia [7][8][9], was herein processed to isolate juanislamin, which was evaluated for gastroprotection in a model of ethanol-induced gastric lesions. Assays were carried out to explore the possible contributions of prostaglandins, nitric oxide and sulfhydryl groups in the mechanism of action of the compound under study.…”

“…Contrarily, the effect of carbenoxolone was reversed by NEM pretreatment, coinciding with published results. None of the three gastroprotective factors examined herein take part in the mechanism of action of juanislamin or the other three compounds isolated from C. urticifolia that have shown gastroprotective activity [7][8][9].…”

“…Medicinal plants are often the source of new drugs. From one such plant, Calea urticifolia, three compounds with gastroprotective activity have been isolated and previously reported [7][8][9]. The aim of the present study was to evaluate the gastroprotective effect of juanislamin (PubChem CID 6440536), isolated from C. urticifolia, in a rat model of ethanol-induced gastric lesions.…”