Stricto Sensu Postgraduate Program in Environmental Sciences, Community University of Chapeco Region (Unochapeco), Chapeco, Brazil.
Health Sciences Area, Community University of Chapeco Region (Unochapeco), Chapeco, Brazil.
Biomed J. 2021 Dec;44(6 Suppl 1):S63-S72. doi: 10.1016/j.bj.2020.06.009. Epub 2020 Jul 2.
A. gratissima is a shrub used in folk medicine as analgesic and sedative. However, studies on its antinociceptive activity are scarce. This research aimed to evaluate the antinociceptive effect of a supercritical carbon dioxide (SCCO) extract of A. gratissima leaves (EAG) in mice.
A. gratissima leaves were subjected to extraction with supercritical CO (60 °C, 200 bar). The chemical composition of EAG was determined by gas chromatography-mass spectrometry (GC-MS). The antinociceptive profile of the extract (1, 10 and 30 mg/kg, p.o.) was established using acetic acid-induced abdominal contraction tests and formalin-induced paw-licking tests. The open field and rota-rod tests were used to evaluate a possible interference of EAG on mice motor performance. The contribution of the opioid system and adenosine triphosphate (ATP) sensitive K channels in the mechanism(s) of EAG action was evaluated by specific receptor blockers. EAG's acute toxicity was investigated using OECD 423 guideline.
The GC-MS revealed the presence of sesquiterpenes (guaiol and pinocamphone) in the EAG. Doses of 10 mg/kg and 30 mg/kg significantly reduced the number of abdominal writhes and paw licking time in mice in the formalin test. The EAG did not affect the locomotor activity and motor coordination of the mice. The antinociceptive effect of the EAG was prevented by glibenclamide in the mice formalin test, unlike naloxone pre-treatment. The acute administration of EAG caused no mortality.
A. gratissima leaves possess antinociceptive effect, mediated by K channels sensitive to ATP.
A. gratissima 是一种灌木,在民间医学中被用作镇痛药和镇静剂。然而,关于其镇痛活性的研究很少。本研究旨在评估 A. gratissima 叶的超临界二氧化碳(SCCO)提取物(EAG)在小鼠中的镇痛作用。
用超临界 CO(60°C,200 巴)对 A. gratissima 叶进行提取。通过气相色谱-质谱联用(GC-MS)测定 EAG 的化学成分。采用醋酸诱导的腹部收缩试验和福尔马林诱导的舔爪试验确定提取物(1、10 和 30mg/kg,po)的镇痛谱。使用旷场和转棒试验评估 EAG 对小鼠运动性能的可能干扰。通过特定的受体阻滞剂评估阿片系统和三磷酸腺苷(ATP)敏感的 K 通道在 EAG 作用机制中的作用。按照 OECD 423 指南研究 EAG 的急性毒性。
GC-MS 显示 EAG 中存在倍半萜(愈创木醇和胡椒酮)。10mg/kg 和 30mg/kg 的剂量可显著减少福尔马林试验中小鼠的腹部扭动次数和舔爪时间。EAG 不影响小鼠的运动活动和运动协调能力。EAG 在小鼠福尔马林试验中的镇痛作用被 glibenclamide 阻止,而不像纳洛酮预处理。EAG 的急性给药未引起死亡。
A. gratissima 叶具有镇痛作用,由对 ATP 敏感的 K 通道介导。