Abstract

Present study investigated triterpene profile, antihyperalgesic and antiedematous activities of Hieracium scheppigianum flowering aerial parts dichloromethane extract (SCH), and antihyperalgesic and antiedematous activities of previously chemically characterised polyphenol-rich H. glabratum and H. calophyllum flowering aerial parts methanol extracts (GLA and CAL, respectively). α- and β-Amyrin and their acetates, and lupeol acetate were identified and quantified in SCH by GC-FID and GC-MS. In carrageenan-induced localised inflammation model in rats, SCH and GLA (50–200 mg/kg, p.o.) produced significant and dose-dependent antihyperalgesic effect of 26.9%–56.2% (ED₅₀=163.0 ± 26.5 mg/kg) and 25.3%–51.6% (ED₅₀=211.6 ± 70.6 mg/kg), respectively, and CAL (200 mg/kg, p.o.) exhibited effect of 38.1%. Extracts did not significantly reduce paw edema. SCH and GLA, which demonstrated higher (over 50%) antihyperalgesic efficacy, were tested in a rotarod test (200 mg/kg, p.o.) and no alteration of motor coordination was observed. Also, acute administration of SCH and GLA in mice (2000 mg/kg, p.o.) caused neither mortality nor toxicity.

摘要

目前的研究调查了三萜类成分、山楂开花地上部分二氯甲烷提取物 (SCH) 的抗痛觉过敏和抗水肿活性，以及​​先前化学表征的富含多酚的H. glabratum和H 的抗痛觉过敏和抗水肿活性。calophyllum开花地上部分甲醇提取物（分别为 GLA 和 CAL）。通过 GC-FID 和 GC-MS 在 SCH 中鉴定和定量α - 和β -香树脂素及其乙酸盐和羽扇豆醇乙酸酯。在角叉菜胶诱导的大鼠局部炎症模型中，SCH 和 GLA（50–200 mg/kg，po）产生 26.9%–56.2%（ED ₅₀=163.0 ± 26.5 mg/kg) 和 25.3%–51.6% (ED ₅₀ =211.6 ± 70.6 mg/kg) 和 CAL (200 mg/kg, po) 表现出 38.1% 的效果。提取物没有显着减轻爪水肿。SCH 和 GLA 表现出更高（超过 50%）的抗痛觉过敏功效，在旋转棒试验（200 毫克/千克，口服）中进行了测试，没有观察到运动协调的改变。此外，在小鼠中急性施用 SCH 和 GLA (2000 mg/kg, po) 既不会导致死亡也不会引起毒性。