Instituto Nacional de Psiquiatría Ramón de la Fuente Muñiz, Calz. México-Xochimilco No. 101 Col. Sn Lorenzo Huipulco 14370, México, D.F. México.
Pharmacol Biochem Behav. 2010 Mar;95(1):6-12. doi: 10.1016/j.pbb.2009.11.017. Epub 2009 Dec 5.
Annonas are consumed as fresh fruits, but are also widely used in folk medicine for treating pain and other ailments. Antinociceptive properties of the Annona diversifolia ethanol crude extract were tested using the pain-induced functional impairment model in rat (PIFIR) and the writhing test in mice. The ethanol extract caused a 25% recovery of limb function in rats; this response was significant and dose-dependent. Furthermore, this extract produced a similar antinociceptive response (ED(50)=15.35 mg/kg) to that of the reference drug tramadol (ED(50)=12.42 mg/kg) when evaluated in the writhing test in mice. Bio-guided fractionation yielded hexane and acetone active fractions from which the presence of palmitone and flavonoids was respectively detected. Palmitone produced an antinociceptive response with an ED(50)=19.57 mg/kg in the writhing test. Antinociceptive responses from ethanol extract and tramadol were inhibited in the presence of either naloxone (1mg/kg, s.c.)--an antagonist of endogenous opioids--or WAY100635 (0.8 mg/kg, s.c.)--a 5-HT(1A) serotonin receptor antagonist. These results provide evidence that A. diversifolia possesses antinociceptive activity, giving support to their traditional use for treatment of spasmodic and arthritic pain. In addition, our results suggest the participation of endogenous opioids and 5-HT(1A) receptors in this antinociceptive response.
番荔枝被当作新鲜水果食用，但也广泛应用于民间医学，用于治疗疼痛和其他疾病。本研究采用大鼠疼痛诱发功能障碍模型（PIFIR）和小鼠扭体试验测试番荔枝乙醇粗提物的镇痛作用。结果表明，乙醇提取物可使大鼠肢体功能恢复 25%，且呈剂量依赖性；此外，该提取物在扭体试验中的镇痛作用与曲马多（ED（50）=12.42mg/kg）相似（ED（50）=15.35mg/kg）。通过生物导向分离，从番荔枝的正己烷和丙酮活性部位中分别检测到了棕榈酮和黄酮类化合物。棕榈酮在扭体试验中产生的镇痛作用 ED（50）为 19.57mg/kg。在纳洛酮（1mg/kg，皮下注射）-内源性阿片类拮抗剂或 WAY100635（0.8mg/kg，皮下注射）-5-HT（1A）血清素受体拮抗剂存在的情况下，乙醇提取物和曲马多的镇痛反应被抑制。这些结果表明 A. diversifolia 具有镇痛活性，支持其用于治疗痉挛性和关节炎性疼痛的传统用途。此外，我们的结果表明内源性阿片类和 5-HT（1A）受体参与了这种镇痛反应。
