Lima J A, Oliveira A S, de Miranda A L P, Rezende C M, Pinto A C
Departamento de Química Orgânica, Instituto de Química, Universidade Federal do Rio de Janeiro, RJ, Brasil.
Braz J Med Biol Res. 2005 Jul;38(7):1095-103. doi: 10.1590/s0100-879x2005000700013. Epub 2005 Jul 4.
Carpotroche brasiliensis is a native Brazilian tree belonging to the Oncobeae tribe of Flacourtiaceae. The oil extracted from its seeds contains as major constituents the same cyclopentenyl fatty acids hydnocarpic (40.5%), chaulmoogric (14.0%) and gorlic (16.1%) acids found in the better known chaulmoogra oil prepared from the seeds of various species of Hydnocarpus (Flacourtiaceae). These acids are known to be related to the pharmacological activities of these plants and to their use as anti-leprotic agents. Although C. brasiliensis oil has been used in the treatment of leprosy, a disease that elicits inflammatory responses, the anti-inflammatory and analgesic activities of the oil and its constituents have never been characterized. We describe the anti-inflammatory and antinociceptive activities of C. brasiliensis seed oil in acute and chronic models of inflammation and in peripheral and central nociception. The mixture of acids from C. brasiliensis administered orally by gavage showed dose-dependent (10-500 mg/kg) anti-inflammatory activity in carrageenan-induced rat paw edema, inhibiting both the edema by 30-40% and the associated hyperalgesia. The acid fraction (200 mg/kg) also showed significant antinociceptive activity in acetic acid-induced constrictions (57% inhibition) and formalin-induced pain (55% inhibition of the second phase) in Swiss mice. No effects were observed in the hot-plate (100 mg/kg; N = 10), rota-road (200 mg/kg; N = 9) or adjuvant-induced arthritis (50 mg/kg daily for 7 days; N = 5) tests, the latter a chronic model of inflammation. The acid fraction of the seeds of C. brasiliensis which contains cyclopentenyl fatty acids is now shown to have significant oral anti-inflammatory and peripheral antinociceptive effects.
巴西角果木是一种原产于巴西的树木，隶属于大风子科的刺篱木族。从其种子中提取的油主要成分包含与从大风子属（大风子科）不同物种种子制备的、更为人熟知的大风子油中相同的环戊烯基脂肪酸，即氢化大风子酸（40.5%）、晁模酸（14.0%）和戈里酸（16.1%）。已知这些酸与这些植物的药理活性及其作为抗麻风病药物的用途有关。尽管巴西角果木油已被用于治疗麻风病（一种引发炎症反应的疾病），但其油及其成分的抗炎和镇痛活性从未得到过表征。我们描述了巴西角果木种子油在急性和慢性炎症模型以及外周和中枢伤害感受中的抗炎和抗伤害感受活性。通过灌胃口服给予的巴西角果木酸混合物在角叉菜胶诱导的大鼠足爪水肿中显示出剂量依赖性（10 - 500毫克/千克）的抗炎活性，抑制水肿达30 - 40%以及相关的痛觉过敏。酸组分（200毫克/千克）在瑞士小鼠的醋酸诱导的扭体反应（抑制57%）和福尔马林诱导的疼痛（抑制第二阶段的55%）中也显示出显著的抗伤害感受活性。在热板试验（100毫克/千克；n = 10）、转棒试验（200毫克/千克；n = 9）或佐剂诱导的关节炎试验（连续7天每天50毫克/千克；n = 5）中未观察到效果，后者是一种慢性炎症模型。现已表明，含有环戊烯基脂肪酸的巴西角果木种子的酸组分具有显著的口服抗炎和外周抗伤害感受作用。
