Ali Mumtaz, Rauf Abdur, Hadda Taibi Ben, Bawazeer Saud, Abu-Izneid Tareq, Khan Haroon, Raza Muslim, Khan Sher Ali, Shah S U A, Pervez Samreen, Patel Seema, Orhan Ilkay Erdogan
Geology Department, Univesity of Swabi, Anbar-23561, KPK, Pakistan.
Curr Top Med Chem. 2017;17(4):383-390. doi: 10.2174/1568026616666160824101429.
The present study was designed to evaluate the anti-hyperalgesic effect of kaempferol-3,7-di-O-α-L-rhamnopyranoside isolated from the ethyl acetate soluble part of Dryopteris cycadina. Pretreatment of the compound at the doses of 2.5, 5, and 10 mg/kg caused a significant reduction in abdominal constrictions in acetic acid-induced writhing test with maximum effect of 63.03% (P < 0.001) at 10 mg/kg i.p. When subjected in formalin test, it evoked a marked antinociceptive effect in both phases in a dose-dependent manner. The maximum (p < 0.01) pain-inhibiting effects were 61.36% and 65.89% in 1st and 2nd phases at 10 mg/kg i.p., respectively. Administration of atropine (non-selective cholinergic receptor antagonist) significantly (p < 0.05) antagonized the antihyperalgesic effect of the compound, while glibenclamide and naloxone did not alter the induced antinociceptive effect and thus, antinociceptive activity of the compound is mediated, at least in part, through cholinergic system antagonism; independent of calcium channel and opioidergic receptor participation. Furthermore, docking studies underlined strong COX-2 inhibitory activity of the compound.
Our data concluded that overall analgesic activity of the compound seems to involve COX-2 inhibition and activation of cholinergic receptors. However, further detailed studies are required in this direction to confirm the analgesic effect of the compound for its possible clinical utility.
本研究旨在评估从金毛狗脊乙酸乙酯可溶部分分离得到的山柰酚 -3,7 - 二 -O-α-L-鼠李糖苷的抗痛觉过敏作用。以2.5、5和10 mg/kg的剂量对该化合物进行预处理，在醋酸诱导的扭体试验中可显著减少腹部收缩次数，腹腔注射10 mg/kg时最大效应为63.03%（P < 0.001）。在福尔马林试验中，它在两个阶段均以剂量依赖性方式引起明显的抗伤害感受作用。腹腔注射10 mg/kg时，在第一阶段和第二阶段最大（p < 0.01）疼痛抑制作用分别为61.36%和65.89%。给予阿托品（非选择性胆碱能受体拮抗剂）可显著（p < 0.05）拮抗该化合物的抗痛觉过敏作用，而格列本脲和纳洛酮并未改变诱导的抗伤害感受作用，因此，该化合物的抗伤害感受活性至少部分是通过胆碱能系统拮抗介导的；与钙通道和阿片样物质受体参与无关。此外，对接研究强调了该化合物具有较强的COX - 2抑制活性。
我们的数据表明，该化合物的总体镇痛活性似乎涉及COX - 2抑制和胆碱能受体激活。然而，需要在这个方向上进行进一步详细研究，以确认该化合物的镇痛效果及其可能的临床应用价值。
