Department of Pharmacognosy, Faculty of Pharmacy, Ain-Shams University, Cairo, 11566, Egypt.
Department of Pharmacology, Faculty of Veterinary Medicine, Suez Canal University, Ismailia, 41522, Egypt.
Drug Dev Res. 2018 Jun;79(4):157-164. doi: 10.1002/ddr.21430. Epub 2018 May 6.
Hit, Lead & Candidate Discovery The acetic acid-induced writhing and hot plate models in mice were utilized to determine the analgesic effect of epicatechin gallate (ECG) isolated from Bauhinia hookeri. The anti-inflammatory activity of ECG was determined using carrageenan-induced paw edema model. The pro-inflammatory mediators (PGE , TNF-α, IL-1β, and IL-6) were estimated in the plasma of different treatment groups. ECG was tested at doses of 100, 200, and 400 mg/kg p.o. and diclofenac sodium was used as a standard drug (100 mg/kg) in all experiments. ECG significantly (p < .001) suppressed the writhing response in mice. The inhibition percentages were 32, 52, and 62%, at the tested doses of ECG, respectively as compared to the positive control group receiving acetic acid only. Furthermore, ECG significantly (p < .001) increased the reaction time in hot plate model. The maximum analgesic effect was evident after 120 min. ECG demonstrated a significant anti-inflammatory activity as evidenced by the inhibition of carrageenan-induced paw edema (46, 50, and 58%, at the tested doses, respectively). This effect was persistent all over the experimental period. ECG produced a significant (p < .001) reduction in plasma PGE (by 27, 38, and 50%), TNF-α (15, 33, and 41%), IL-1β (17, 25, and 33%), and IL-6 (22, 32, and 43%), at the tested doses, respectively. This study supports the use of ECG as both analgesic and anti-inflammatory agent.
镇痛和抗炎作用 从白花油麻藤中分离得到的表儿茶素没食子酸酯(ECG),通过醋酸诱导的扭体和热板模型来评估其镇痛作用,通过角叉菜胶诱导的足肿胀模型来评估其抗炎活性。在不同治疗组的血浆中评估促炎介质(PGE 、TNF-α、IL-1β和 IL-6)。ECG 在 100、200 和 400mg/kg 剂量下进行测试,双氯芬酸钠(100mg/kg)在所有实验中用作标准药物。 ECG 显著(p < .001)抑制了小鼠的扭体反应。与仅接受醋酸的阳性对照组相比,ECG 在测试剂量下的抑制率分别为 32%、52%和 62%。此外,ECG 显著(p < .001)增加了热板模型中的反应时间。最大镇痛作用在 120 分钟后显现。 ECG 表现出显著的抗炎活性,表现为抑制角叉菜胶诱导的足肿胀(在测试剂量下分别为 46%、50%和 58%)。这种作用在整个实验期间持续存在。 ECG 显著降低了血浆 PGE(降低 27%、38%和 50%)、TNF-α(降低 15%、33%和 41%)、IL-1β(降低 17%、25%和 33%)和 IL-6(降低 22%、32%和 43%),在测试剂量下,分别。这项研究支持 ECG 作为镇痛和抗炎药物的应用。