Postgraduate Program in Pharmaceutical Sciences, State University of Paraíba, Campina Grande, PB 58429-500, Brazil.
Department of Pharmacy, State University of Paraíba, Campina Grande, PB 58429-500, Brazil.
Molecules. 2021 Mar 12;26(6):1581. doi: 10.3390/molecules26061581.
L. (Anacardiaceae) has a worldwide distribution and is present in all regions of Brazil. Its leaves, flowers and bark are used as teas in folk medicine to treat diseases of the digestive system. This study aimed to evaluate the acute non-clinical toxicity, gastroprotective activity, and the related mechanisms of action of nebulized extract and tablets based on dried (SmNE). SmNE screening showed the presence of flavonoids (0.65%), polyphenols (25.50%), where the major compound is gallic acid. In the acute oral toxicity assay, a dose of 2000 mg/kg of SmNE administered orally in Swiss mice did not induce any behavioral changes. SmNE (250 or 500 mg/kg p.o) significantly reduced the ulcerative lesion area when compared to the control group in ethanol and non-steroidal anti-inflammatory drug (NSAIDs) models. Results showed that treatment with SmNE (250 mg/kg) reduced acid secretion and gastric content, accompanied with an increase in pH. Previous administration of indomethacin and glibenclamide reversed the protection provided by SmNE, confirming the participation of prostaglandins (PGs) and ATP-sensitive potassium channels (KATP) in its gastroprotective effect. The SmNE tablets met the pharmacopeial quality requirements with gastroprotective activity and similar protection in comparison to the isolated extract administrated. In conclusion, SmNe has a gastroprotective activity related to cytoprotective mechanisms, such as the participation of endogenous prostaglandins and KATP channels, having an anti-secretory effect with systemic action. The formulation obtained presented gastroprotective effects similar to the administration of the extract, the tablets showed favorable compression characteristics by the direct route and met the pharmacopeial quality requirements.
（漆树科）分布于世界各地，存在于巴西的所有地区。其叶、花和树皮被民间医学用作茶，用于治疗消化系统疾病。本研究旨在评估雾化提取物和干制剂片（SmNE）的急性非临床毒性、胃保护活性和相关作用机制。SmNE 筛选显示存在黄酮类化合物（0.65%）和多酚（25.50%），其中主要化合物是没食子酸。在急性口服毒性试验中，SmNE（2000mg/kg）口服给予瑞士小鼠后，未引起任何行为改变。SmNE（250 或 500mg/kg，po）与对照组相比，在乙醇和非甾体抗炎药（NSAIDs）模型中显著减少溃疡病变面积。结果表明，SmNE（250mg/kg）治疗可减少胃酸分泌和胃内容物，同时 pH 值升高。预先给予吲哚美辛和格列本脲可逆转 SmNE 提供的保护，证实前列腺素（PGs）和 ATP 敏感性钾通道（KATP）参与其胃保护作用。SmNE 片剂符合药典质量要求，具有胃保护活性，与单独给予提取物的活性相当。总之，SmNe 具有与细胞保护机制相关的胃保护活性，例如内源性前列腺素和 KATP 通道的参与，具有全身作用的抗分泌作用。所获得的配方具有与给予提取物相似的胃保护作用，片剂通过直接途径显示出良好的压缩特性，并符合药典质量要求。
