Boldine is the main alkaloid of Peumus boldus Molina, widely used in the traditional medicine for the treatment of digestive disorders. It is a compound with excellent antioxidant and anti-inflammatory properties already described. Despite the widespread use of P. boldus for digestive disorders treatment, the gastroprotective effect of Boldine remains unknown. Considering the need for new approaches to treat gastric ulcers with fewer side effects than current therapy, this study aimed to investigate the gastroprotective effect of Boldine in mice, as well as the mechanisms underlying this effect. The gastroprotective effect of Boldine was evaluated on gastric ulcer induced by 60% ethanol/0.3 M HCl or indomethacin (100 mg/kg) in mice. Histological analysis and the mucin-like glycoprotein content were evaluated in ethanol-ulcerated tissue, as well as, oxidative stress and inflammatory parameters. The mechanisms involved in the effect of Boldine were evaluated by pretreating mice with NEM (a sulfhydryl group chelator, 10 mg/kg, i.p.), l-NAME (a non-selective nitric oxide synthase inhibitor, 70 mg/kg, i.p.), yohimbine (an alpha-adrenergic receptor antagonist, 2 mg/kg, i.p.) and indomethacin (a cyclooxygenase inhibitor, 10 mg/kg, i.p.). In addition, the in vitro effect of Boldine on H⁺/K⁺-ATPase activity was determined. Boldine was able to protect gastric mucosa against the damage induced by ethanol/HCl and indomethacin, as evidenced by reduced lesion area and histological analysis. Moreover, the alkaloid reduced oxidative stress and inflammatory mediators in ethanol-ulcerated tissue, beyond has increased mucin-like glycoprotein amount. Finally, Boldine effect is dependent on non-protein sulfhydryl groups and prostanoids but does not involve the inhibition of H+/K + -ATPase activity, being a promising natural resource for gastric ulcer treatment.

Boldine是Peumus boldus Molina的主要生物碱，广泛用于治疗消化系统疾病的传统医学中。它是一种具有出色抗氧化和抗炎特性的化合物。尽管广泛使用了P. boldus对于消化系统疾病的治疗，Boldine的胃保护作用仍然未知。考虑到需要一种新的方法来治疗胃溃疡，其副作用要比目前的治疗方法少，因此本研究旨在研究Boldine对小鼠的胃保护作用，以及该作用的潜在机制。评价了鲍丁对小鼠60％乙醇/0.3M HCl或消炎痛（100mg / kg）诱导的胃溃疡的胃保护作用。组织学分析和粘液样糖蛋白含量在乙醇溃疡组织中进行了评估，以及氧化应激和炎症参数。参与Boldine的作用机制通过用NEM（巯基螯合剂，10毫克/千克，腹膜内），预处理的小鼠进行评价升-NAME（一种非选择性一氧化氮合酶抑制剂，70 mg / kg，ip），育亨宾（一种α-肾上腺素受体拮抗剂，2 mg / kg，ip）和消炎痛（一种环加氧酶抑制剂，10 mg / kg，ip） 。此外，Boldine对H ⁺ / K ^+的体外作用确定了ATP酶活性。病灶面积减少和组织学分析证明，Boldine能够保护胃粘膜免受乙醇/ HCl和消炎痛诱导的损害。此外，生物碱减少了乙醇溃疡组织中的氧化应激和炎症介质，增加了粘蛋白样糖蛋白的含量。最后，Boldine效应取决于非蛋白质巯基和类前列腺素，但不涉及抑制H + / K + -ATPase活性，这是治疗胃溃疡的有希望的天然资源。