Multiuser Health Center Facility (CMulti-Saúde), Federal University of Sergipe, São Cristóvão, SE, Brazil; Health Sciences Graduate Program (PPGCS), Federal University of Sergipe, São Cristóvão, SE, Brazil; Laboratory of Neurosciences and Pharmacological Assays (LANEF), Department of Physiology, Federal University of Sergipe, São Cristóvão, Brazil.
Laboratory of Neurosciences and Pharmacological Assays (LANEF), Department of Physiology, Federal University of Sergipe, São Cristóvão, Brazil.
Biomed Pharmacother. 2022 Jul;151:113142. doi: 10.1016/j.biopha.2022.113142. Epub 2022 May 25.
Inflammatory arthritis is the most prevalent chronic inflammatory disease worldwide. The pathology of the disease is characterized by increased inflammation and oxidative stress, which leads to chronic pain and functional loss in the joints. Conventional anti-arthritic drugs used to relieve pain and other arthritic symptoms often cause severe side effects. α-bisabolol (BIS) is a sesquiterpene that exhibits high anti-inflammatory potential and a significant antinociceptive effect. This study evaluates the anti-arthritic, anti-inflammatory and antihyperalgesic effects of BIS alone and in a β-cyclodextrin (βCD/BIS) inclusion complex in a CFA-induced arthritis model. Following the intra-articular administration of CFA, male mice were treated with vehicle, BIS and βCD/BIS (50 mg/kg, p.o.) or a positive control and pain-related behaviors, knee edema and inflammatory and oxidative parameters were evaluated on days 4, 11, 18 and/or 25. Ours findings shows that the oral administration of BIS and βCD/BIS significantly attenuated spontaneous pain-like behaviors, mechanical hyperalgesia, grip strength deficit and knee edema induced by repeated injections of CFA, reducing the joint pain and functional disability associated with arthritis. BIS and βCD/BIS also inhibited the generation of inflammatory and oxidative markers in the knee and blocked MAPK in the spinal cord. In addition, ours results also showed that the incorporation of BIS in cyclodextrin as a drug delivery system improved the pharmacological profile of this substance. Therefore, these results contribute to the pharmacological knowledge of BIS and demonstrated that this terpene appears to be able to mitigate deleterious symptoms of arthritis.
炎症性关节炎是全球最常见的慢性炎症性疾病。该疾病的病理学特征为炎症和氧化应激增加,导致关节慢性疼痛和功能丧失。用于缓解疼痛和其他关节炎症状的传统抗关节炎药物通常会引起严重的副作用。α- 姜烯醇(BIS)是一种具有高抗炎潜力和显著镇痛作用的倍半萜烯。本研究评估了 BIS 单独以及在 CFA 诱导的关节炎模型中与β-环糊精(βCD/BIS)包合物联合使用时的抗关节炎、抗炎和抗痛觉过敏作用。在关节内注射 CFA 后,雄性小鼠用载体、BIS 和βCD/BIS(50mg/kg,po)或阳性对照物处理,并在第 4、11、18 和/或 25 天评估与疼痛相关的行为、膝关节肿胀和炎症及氧化参数。我们的研究结果表明,BIS 和βCD/BIS 的口服给药显著减轻了由重复注射 CFA 引起的自发性疼痛样行为、机械性痛觉过敏、握力下降和膝关节肿胀,减轻了与关节炎相关的关节疼痛和功能障碍。BIS 和βCD/BIS 还抑制了膝关节中炎症和氧化标志物的产生,并阻断了脊髓中的 MAPK。此外,我们的结果还表明,将 BIS 纳入环糊精作为药物传递系统改善了该物质的药理学特性。因此,这些结果有助于了解 BIS 的药理学知识,并表明这种萜烯似乎能够减轻关节炎的有害症状。