Valério Daniel A R, Cunha Thiago M, Arakawa Nilton S, Lemos Henrique P, Da Costa Fernando B, Parada Carlos A, Ferreira Sergio H, Cunha Fernando Q, Verri Waldiceu A
Department of Pharmacology, School of Medicine of Ribeirão Preto, University of São Paulo, São Paulo, Avenida Bandeirantes, 3900, 14049-900-Ribeirão Preto, São Paulo, Brazil.
Eur J Pharmacol. 2007 May 7;562(1-2):155-63. doi: 10.1016/j.ejphar.2007.01.029. Epub 2007 Feb 1.
The anti-inflammatory activities of some medicinal plants are attributed to their contents of sesquiterpene lactones. In the present study, the anti-inflammatory and anti-nociceptive activity of a sesquiterpene lactone isolated from Viguiera robusta, budlein A in mice was investigated. The treatment with budlein A dose--(1.0-10.0 mg/kg, p.o., respectively) dependently inhibited the carrageenan-induced: i. neutrophil migration to the peritoneal cavity (2-52%), ii. neutrophil migration to the paw skin tissue (32-74%), iii. paw oedema (13-74%) and iv. mechanical hypernociception (2-58%) as well as the acetic acid-induced writhings (0-66%). Additionally, budlein A (10.0 mg/kg) treatment inhibited the mechanical hypernociception-induced by tumour necrosis factor (TNF-alpha, 36%), Keratinocyte-derived chemokine (KC, 37%) and Interleukin-1beta (IL-1beta, 28%), but not of prostaglandin E(2) or dopamine. Budlein A also inhibited the carrageenan-induced release of TNF-alpha (52%), KC (70%) and IL-1beta (59%). Furthermore, an 8 days treatment with budlein A inhibited Complete Freund's adjuvant (10 microl/paw)-induced hypernociception, paw oedema and paw skin myeloperoxidase activity increase while not affecting the motor performance or myeloperoxidase activity in the stomach. Concluding, the present data suggest that budlein A presents anti-inflammatory and antinociceptive property in mice by a mechanism dependent on inhibition of cytokines production. It supports the potential beneficial effect of orally administered budlein A in inflammatory diseases involving cytokine-mediated nociception, oedema and neutrophil migration.
一些药用植物的抗炎活性归因于其倍半萜内酯含量。在本研究中,对从粗壮沼菊中分离出的一种倍半萜内酯——布德林A在小鼠体内的抗炎和抗伤害感受活性进行了研究。布德林A(分别为1.0 - 10.0毫克/千克,口服)剂量依赖性地抑制了角叉菜胶诱导的:i. 中性粒细胞向腹腔的迁移(2 - 52%),ii. 中性粒细胞向爪皮肤组织的迁移(32 - 74%),iii. 爪水肿(13 - 74%)和iv. 机械性痛觉过敏(2 - 58%)以及乙酸诱导的扭体反应(0 - 66%)。此外,布德林A(10.0毫克/千克)处理抑制了由肿瘤坏死因子(TNF-α,36%)、角质形成细胞衍生趋化因子(KC,37%)和白细胞介素-1β(IL-1β,28%)诱导的机械性痛觉过敏,但对前列腺素E(2)或多巴胺诱导的无效。布德林A还抑制了角叉菜胶诱导的TNF-α(52%)、KC(70%)和IL-1β(59%)的释放。此外,布德林A进行8天的处理抑制了完全弗氏佐剂(10微升/爪)诱导的痛觉过敏、爪水肿和爪皮肤髓过氧化物酶活性增加,同时不影响运动性能或胃中的髓过氧化物酶活性。总之,目前的数据表明布德林A通过依赖于抑制细胞因子产生的机制在小鼠中呈现抗炎和抗伤害感受特性。它支持口服布德林A在涉及细胞因子介导的痛觉过敏、水肿和中性粒细胞迁移的炎症性疾病中的潜在有益作用。