De Souza M M, Pereira M A, Ardenghi J V, Mora T C, Bresciani L F, Yunes R A, Delle Monache F, Cechinel-Filho V
Programa de Mestrado em Ciências Farmacêuticas e Núcleo de Investigações Químico-Farmacêuticas (NIQFAR), Universidade do Vale do Itajaí (UNIVALI), 88302-202, Itajaí, SC, Brazil.
Pharmacol Biochem Behav. 2009 Jul;93(1):40-6. doi: 10.1016/j.pbb.2009.04.004. Epub 2009 Apr 16.
In the present study, we describe the antinociceptive effect of filicene, a triterpene isolated from Adiantum cuneatum (Adiantaceae) leaves, in several models of pain in mice. When evaluated against acetic acid-induced abdominal constrictions, filicene (10, 30 and 60 mg/kg, i.p.) produced dose-related inhibition of the number of constrictions, being several times more potent [ID(50)=9.17 (6.27-13.18) mg/kg] than acetaminophen [ID(50)=18.8 (15.7-22.6) mg/kg], diclofenac [ID(50)=12.1(9.40-15.6) mg/kg] and acetylsalicylic acid [ID(50)=24.0(13.1-43.8) mg/kg] in the same doses as those used for the standard drugs. Filicene also produced dose-related inhibition of the pain caused by capsaicin and glutamate, with mean ID(50) values of 11.7 (8.51-16.0) mg/kg and <10 mg/kg, respectively. Its antinociceptive action was significantly reversed by atropine, haloperidol, GABA(A) and GABA(B) antagonists (bicuculline and phaclofen, respectively), but was not affected by L-arginine-nitric oxide, serotonin, adrenergic and the opioid systems. Together, these results indicate that the mechanisms involved in its action are not completely understood, but seem to involve interaction with the cholinergic, dopaminergic, glutamatergic, GABAergic and tachykinergic systems.
在本研究中,我们描述了从楔叶铁线蕨(铁线蕨科)叶片中分离出的三萜类化合物——绵马素,在几种小鼠疼痛模型中的镇痛作用。当针对乙酸诱导的腹部收缩进行评估时,绵马素(10、30和60mg/kg,腹腔注射)对收缩次数产生剂量相关的抑制作用,其效力比对乙酰氨基酚[半数抑制剂量(ID50)=18.8(15.7 - 22.6)mg/kg]、双氯芬酸[ID50=12.1(9.40 - 15.6)mg/kg]和乙酰水杨酸[ID50=24.0(13.1 - 43.8)mg/kg]高出数倍,且使用的剂量与标准药物相同。绵马素还对辣椒素和谷氨酸引起的疼痛产生剂量相关的抑制作用,平均ID50值分别为11.7(8.51 - 16.0)mg/kg和<10mg/kg。其镇痛作用被阿托品、氟哌啶醇、GABA(A)和GABA(B)拮抗剂(分别为荷包牡丹碱和法氯芬)显著逆转,但不受L - 精氨酸 - 一氧化氮、5 - 羟色胺、肾上腺素能和阿片系统的影响。总之,这些结果表明其作用机制尚未完全明确,但似乎涉及与胆碱能、多巴胺能、谷氨酸能、GABA能和速激肽能系统的相互作用。