Sección de Estudios de Posgrado e Investigación, Escuela Superior de Medicina, Instituto Politécnico Nacional, Col. Santo Tomás, 11340 México, México.
Planta Med. 2010 May;76(7):665-70. doi: 10.1055/s-0029-1240658. Epub 2009 Nov 30.
Heliopsis longipes is used as analgesic in Mexican traditional medicine. The present study assesses the possible antinociceptive effect of Heliopsis longipes and describes the pharmacological mechanism of action of the antinociceptive effect of affinin, identified as the one active principle in Heliopsis longipes acetone extract. Intraperitoneal administration of H. longipes extract and affinin produced a dose-dependent antinociceptive effect when assessed in mice submitted to acetic acid and capsaicin tests. Affinin-induced antinociception (30 mg/kg, I. P.) was blocked by naltrexone (1 mg/kg, S. C.), P-chlorophenylalanine (80 mg/kg, I. P.) and flumazenil (5 mg/kg, S. C.) suggesting that its pharmacological effect could be due to the activation of opiodergic, serotoninergic and GABAergic systems. In addition, the antinociceptive effect of affinin was attenuated by pretreatment with 1 H-[1,2,4]oxadiazolo[1,2- A]quinoxalin-1-one (1 mg/kg, S. C.) and glibenclamide (10 mg/kg, S. C.) suggesting that the nitric oxide-K (+) channels pathway could be involved in its mechanism of action. These results suggest that affinin itself or its derivatives may have potential antinociceptive effects.
山蚂蝗被墨西哥传统医学用作镇痛药。本研究评估了山蚂蝗可能的镇痛作用，并描述了鉴定为山蚂蝗丙酮提取物中一种活性成分的 affinin 的镇痛作用的药理作用机制。在对乙酸和辣椒素试验的小鼠中，腹腔给予山蚂蝗提取物和 affinin 均产生剂量依赖性的镇痛作用。阿非宁诱导的镇痛作用（30mg/kg，腹腔注射）被纳曲酮（1mg/kg，皮下注射）、对氯苯丙氨酸（80mg/kg，腹腔注射）和氟马西尼（5mg/kg，皮下注射）阻断，表明其药理作用可能是由于阿非宁激活了阿片能、5-羟色胺能和 GABA 能系统。此外，预处理 1 H-[1,2,4]恶二唑并[1,2-a]喹喔啉-1-酮（1mg/kg，皮下注射）和格列本脲（10mg/kg，皮下注射）可减弱 affinin 的镇痛作用，表明一氧化氮-K（+）通道途径可能参与其作用机制。这些结果表明 affinin 本身或其衍生物可能具有潜在的镇痛作用。
