Bilobalide, a unique constituent of Ginkgo biloba, inhibits inflammatory pain in rats
Bilobalide, a unique constituent of Ginkgo biloba, inhibits inflammatory pain in rats
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DOI：
10.1097/fbp.0b013e32836360ab
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发表时间：
2013-08-01
影响因子：
1.6
通讯作者：
Dolan, Sharron
中科院分区：
文献类型：
--
作者：
Goldie, Michelle;Dolan, Sharron
标准化银杏叶提取物EGb 761已被证明可抑制大鼠的炎性痛觉过敏;然而，其作用机制尚不清楚。本研究旨在探讨银杏内酯的抗炎镇痛作用。biloba成分，在三个充分表征的急性炎症性疼痛模型。口服、足底或鞘内给予白果内酯或药物-载体的作用在成年雄性Wistar大鼠皮内后爪注射角叉菜胶之前和之后，评估了0.25%琼脂; 10%乙醇水溶液）对后爪有害热和机械刺激的反应以及爪水肿的影响（3%; 50 L）或辣椒素（10 g; 50 L）或后爪切开后（n=6-8/组）。白果内酯（10-30 mg/kg）经口给药可显著抑制角叉菜胶、辣椒素和爪切口引起的热痛觉过敏，与剂量无关，其疗效与双氯芬酸相似。在角叉菜胶模型中，银杏内酯（10-30 mg/kg）治疗后，机械超敏反应和爪水肿也显著减少。鞘内注射白果内酯（0.5-1 g）可抑制角叉菜胶诱导的热痛觉过敏，但对机械超敏反应或爪水肿没有影响（应用2 g可诱导不良反应，排除更高剂量的试验）。足底注射白果内酯（30-100 g）没有效果。这些数据表明，白果内酯是一种有效的抗炎和抗痛觉过敏剂，其治疗作用部分是通过作用的中心部位介导的，并且可以解释整个提取物G的治疗作用。biloba.
Standardized Ginkgo biloba extract EGb 761 has been shown to inhibit inflammatory hyperalgesia in rats; however, the mechanism of action is not known. This study set out to investigate the anti-inflammatory and analgesic potential of bilobalide, a unique G. biloba constituent, in three well-characterized models of acute inflammatory pain. The effect of oral, intraplantar or intrathecal administration of bilobalide or drug-vehicle (0.25% agar; 10% ethanol in H2O) on responses to noxious thermal and mechanical stimulation of the hindpaw, and paw oedema were assessed in adult male Wistar rats before and after intradermal hindpaw injection of carrageenan (3%; 50 l) or capsaicin (10 g; 50 l) or after hindpaw incision (n=6-8/group). Oral administration of bilobalide (10-30 mg/kg) significantly inhibited thermal hyperalgesia in response to carrageenan, capsaicin and paw incision, independent of dose, with an efficacy similar to that of diclofenac. In the carrageenan model, mechanical hypersensitivity and paw oedema were also significantly reduced after treatment with bilobalide (10-30 mg/kg). Intrathecal administration of bilobalide (0.5-1 g) inhibited carrageenan-induced thermal hyperalgesia, but had no effect on mechanical hypersensitivity or paw oedema (application2 g induced adverse effects, precluding testing of higher doses). Intraplantar administration of bilobalide (30-100 g) had no effect. These data show that bilobalide is a potent anti-inflammatory and antihyperalgesic agent, the therapeutic effects of which are mediated in part through a central site of action, and may account for the therapeutic action of the whole extract G. biloba.