Department of Pharmacology, College of Pharmacy, University of Sargodha, Sargodha, 40100, Pakistan.
Department of Pharmacology, Institute of Pharmacy, Faculty of Pharmaceutical and Allied Health Sciences, Lahore College for Women University, Jail Road, Lahore, 54000, Pakistan.
Inflammopharmacology. 2024 Aug;32(4):2377-2394. doi: 10.1007/s10787-024-01480-5. Epub 2024 May 15.
Arbutin, a naturally soluble glycosylated phenol has antioxidant, antimicrobial, antitumor and anti-inflammatory properties. The current exploration appraises the treatment of arthritis by use of Arbutin (25, 50 and 100 mg/kg) orally in CFA-induced rat arthritis model. Body weight changes, paw size, and joint diameter were recorded till the 28th day in the arthritic-induced rats. Hematological, biochemical, oxidative and inflammatory biomarkers were measured through the blood samples of anesthetized rats. Arbutin markedly decreased paw volume, PGE-2, anti-CCP and 5-LOX levels, however, maintained metabolic and hematological balance and prevented weight loss. Radiology and histology changes improved significantly in the ankle joints of rats. Moreover, Arbutin increased gene pointers such as IL-10 and IL-4 while significantly reducing the levels of CRP and WBCs, whereas Hb, platelets and RBCs count markedly raised in post-treatments. Antioxidant levels of SOD, CAT and GSH were improved and MDA level was reduced in treated groups. Rt-PCR investigation showed a significant reduction of the interleukin-1β, TNF-α, interleukin-6, cyclooxygenase-2, NF-κB and IL-17 and increased expression of gene pointers like IL-4, and IL-10 in treated groups. Assessment of molecular docking revealed a strong binding interaction of Arbutin against 5-LOX, IL-17, TNF-alpha and interleukin-6, cyclooxygenase-2, nuclear factor-κB, IL-4 and iNOS providing a strong association between experimental and theoretical results. As a result, Arbutin has significantly reduced CFA-induced arthritis by modulation of anti-inflammatory cytokines, i.e., IL-10 and IL-4, the pro-inflammatory cytokines panel such as NF-κB, TNF-alpha, IL-1β, IL-6, PGE-2, 5-LOX and COX-2 and oxidative biomarkers.
熊果苷,一种天然可溶性糖基化酚,具有抗氧化、抗菌、抗肿瘤和抗炎特性。目前的研究探索了熊果苷(25、50 和 100mg/kg)口服治疗 CFA 诱导的大鼠关节炎模型中的关节炎的治疗效果。在诱导关节炎的大鼠中,直至第 28 天记录体重变化、爪子大小和关节直径。通过麻醉大鼠的血液样本测量血液学、生化、氧化和炎症生物标志物。熊果苷显著降低了爪子体积、PGE-2、抗 CCP 和 5-LOX 水平,然而,维持了代谢和血液学平衡并防止了体重减轻。大鼠踝关节的放射学和组织学变化明显改善。此外,熊果苷增加了 IL-10 和 IL-4 等基因指针,同时显著降低了 CRP 和白细胞计数,而治疗后 Hb、血小板和 RBC 计数明显升高。SOD、CAT 和 GSH 的抗氧化水平提高,MDA 水平降低。RT-PCR 研究表明,治疗组白细胞介素-1β、TNF-α、白细胞介素-6、环氧化酶-2、NF-κB 和白细胞介素-17 的表达显著降低,而基因指针如 IL-4 和 IL-10 的表达增加。分子对接评估表明,熊果苷对 5-LOX、IL-17、TNF-α和白细胞介素-6、环氧化酶-2、核因子-κB、白细胞介素-4 和 iNOS 具有很强的结合相互作用,为实验结果和理论结果之间提供了很强的关联。结果表明,熊果苷通过调节抗炎细胞因子,即白细胞介素-10 和白细胞介素-4,以及促炎细胞因子谱,如 NF-κB、TNF-α、白细胞介素-1β、白细胞介素-6、PGE-2、5-LOX 和 COX-2,以及氧化生物标志物,显著减轻了 CFA 诱导的关节炎。