Programa de Pós-Graduação em Ciências Veterinárias, Núcleo de Pesquisa em Sanidade Animal, Universidade Estadual do Ceará, Brazil; Laboratório de Química de Produtos Naturais (LQPN), Universidade Estadual do Ceará, Fortaleza, Ceará, Brazil; Instituto Federal do Ceará, Campus Itapipoca, Ceará, Brazil.
Programa de Pós-Graduação em Ciências Veterinárias, Núcleo de Pesquisa em Sanidade Animal, Universidade Estadual do Ceará, Brazil; Laboratório de Química de Produtos Naturais (LQPN), Universidade Estadual do Ceará, Fortaleza, Ceará, Brazil.
Biomed Pharmacother. 2018 Nov;107:1030-1036. doi: 10.1016/j.biopha.2018.08.089. Epub 2018 Aug 24.
The aim of this study was to evaluate the antinociceptive effect of Kaempferol-3-O-rutinoside (KR), isolated from the plant Ouratea fieldingiana, on the orofacial nociception and possible mechanisms of action. Adult zebrafish (Danio rerio) were tested as a behavioral model to study formalin, glutamate, capsaicin, cinnamaldehyde and acidic saline-induced orofacial nociception, using as parameter the number of times the fish crossed the lines between the quadrants of a glass Petri dish during a specific time. Morphine was used as positive control. The effect of KR was tested for modulation by opioid (naloxone), nitrergic (L-NAME), TRPV1 (ruthenium red), TRPA1 (camphor) or ASIC (amiloride) antagonists. The effect of KR on zebrafish locomotor behavior was evaluated with the open field test. KR did not alter the fish's locomotor system and significantly reduced the orofacial nociceptive behavior induced by all noxious agents compared to the control group. The antinociceptive effect of KR was similar to morphine. All antagonists inhibited the antinociceptive effect of KR. KR has pharmacological potential for the treatment of acute orofacial pain and this effect is modulated by the opioid and nitrergic systems as well as TRPV1, TRPA1 and ASIC channels. These results can lead to the development of a new natural product for the treatment of orofacial pain and confirm the popular use of O. fieldingiana leaf for pain relief.
本研究旨在评估来自植物 Ouratea fieldingiana 的山奈酚-3-O-芸香糖苷(KR)对口腔疼痛的抗伤害作用及其可能的作用机制。成年斑马鱼(Danio rerio)被用作行为模型,以研究福尔马林、谷氨酸、辣椒素、肉桂醛和酸性盐水引起的口腔疼痛,参数为在特定时间内鱼穿过玻璃培养皿象限之间的线的次数。吗啡用作阳性对照。测试了 KR 对阿片类(纳洛酮)、硝化(L-NAME)、TRPV1(钌红)、TRPA1(樟脑)或 ASIC(阿米洛利)拮抗剂的调制作用。用旷场试验评估了 KR 对斑马鱼运动行为的影响。与对照组相比,KR 不改变鱼的运动系统,并且显著减少了所有有害剂诱导的口腔疼痛行为。KR 的镇痛作用与吗啡相似。所有拮抗剂均抑制 KR 的镇痛作用。KR 具有治疗急性口腔疼痛的药理学潜力,这种作用受阿片类和硝化系统以及 TRPV1、TRPA1 和 ASIC 通道的调节。这些结果可以导致开发一种用于治疗口腔疼痛的新型天然产物,并证实了 O. fieldingiana 叶用于缓解疼痛的广泛使用。