Laboratório de Farmacologia da Inflamação e do Oxido Nítrico, Instituto de Ciências Biomédicas, Universidade Federal do Rio de Janeiro, Brazil.
J Ethnopharmacol. 2010 Mar 2;128(1):177-83. doi: 10.1016/j.jep.2010.01.005. Epub 2010 Jan 12.
Copaifera multijuga Hayne (Leguminosae) is a tree that produces an oleoresin, which is extensively commercialized in Brazil as capsules or crude oil for the treatment of several disorders. Ethnopharmacological studies show a diversity of indications such as anti-inflammatory and epidermal wound cicatrization.
In the present work three fractions obtained from Copaifera multijuga oleoresin (hexane (HF), chloroform (CF), and methanol (MF) from a KOH impregnated silica gel column chromatography, representing the three main classes of compounds in the Copaifera genus (hydrocarbon sesquiterpenes, oxygenated sesquiterpenes and acidic diterpenes), were evaluated using antinociceptive and anti-inflammatory models.
HF, CF, and MF (doses ranging between 1 and 150 mg/kg, depending on the model used), Copaifera multijuga oleoresin (CMO, 100mg/kg, p.o.) and the reference drug morphine (5mg/kg, p.o.) were evaluated using models for analgesia (acetic acid-induced contortions and tail flick) or inflammation (rat paw oedema and increase in vascular permeability). To elucidate the mechanism of action from the fractions, animals were pre-treated with naloxone (opioid receptor antagonist, 5mg/kg, i.p.).
Fractions significantly inhibited (in a concentration-dependant way) the number of contortions induced by acetic acid and the second phase of formalin-induced licking response. Similar results were observed in the tail flick model. The central antinociceptive effect for HF and CF at the doses of 50 and 100mg/kg was higher than the one observed for morphine (1mg/kg). Administration of naloxone inhibited the antinociceptive effect of fractions indicating that HF, CF, and MF may be acting on opioid receptors. All three fractions also inhibited rat paw oedema and the increase in vascular permeability induced by several phlogistic agents (carrageenan, histamine, and serotonin).
Our results indicate that fractions obtained from Copaifera multijuga Hayne demonstrate an antinociceptive effect probably mediated by opioid receptors, and anti-inflammatory activity through inhibition of histaminergic and serotoninergic pathways.
Copaifera multijuga Hayne（豆科）是一种产生油树脂的树，在巴西被广泛商业化，作为胶囊或粗油用于治疗多种疾病。民族药理学研究表明，它具有多种适应症，如抗炎和表皮伤口愈合。
在本工作中，从 Copaifera multijuga 油树脂中获得的三个馏分（正己烷（HF）、氯仿（CF）和甲醇（MF），通过 KOH 浸渍硅胶柱色谱分离，代表 Copaifera 属的三种主要化合物类（碳氢化合物倍半萜烯、含氧倍半萜烯和酸性二萜烯），在镇痛和抗炎模型中进行了评估。
HF、CF 和 MF（剂量范围为 1 至 150mg/kg，取决于所用模型）、Copaifera multijuga 油树脂（CMO，100mg/kg，po）和参考药物吗啡（5mg/kg，po）用于镇痛模型（乙酸诱导的扭曲和尾巴拍打）或炎症（大鼠足肿胀和血管通透性增加）。为了阐明馏分的作用机制，动物用纳洛酮（阿片受体拮抗剂，5mg/kg，ip）预处理。
馏分显著抑制（浓度依赖性）乙酸诱导的扭曲次数和福尔马林诱导的舔舐反应的第二阶段。尾巴拍打模型也观察到类似的结果。HF 和 CF 在 50 和 100mg/kg 剂量下的中枢镇痛作用高于吗啡（1mg/kg）。纳洛酮的给药抑制了馏分的镇痛作用，表明 HF、CF 和 MF 可能作用于阿片受体。所有三个馏分还抑制了几种炎症介质（角叉菜胶、组胺和 5-羟色胺）诱导的大鼠足肿胀和血管通透性增加。
我们的结果表明，从 Copaifera multijuga Hayne 获得的馏分表现出镇痛作用，可能通过阿片受体介导，以及通过抑制组胺能和 5-羟色胺能途径的抗炎活性。
