Jahan Nishat, Mandal Manoj, Rakib Imam Hossen, Al Hasan Md Sakib, Mia Emon, Yana Noshin Tasnim, Alfaifi Mohammed, Altemani Faisal H, Hossan Rakib, Sumaya Umme Habiba, Hasan Ali Mohamod Wasaf, Sayeed Md Abu, Mou Moushumi Afroza, Islam Muhammad Torequl, Bhuia Md Shimul
Department of Biochemistry and Molecular Biology, Gopalganj Science and Technology University, Gopalganj, 8100, Bangladesh.
Department of Pharmacy, Gopalganj Science and Technology University, Gopalganj, 8100, Bangladesh.
Naunyn Schmiedebergs Arch Pharmacol. 2025 May 30. doi: 10.1007/s00210-025-04309-2.
Oleuropein (OLP), a bioactive compound mainly found in olive leaves, is recognized for its wide range of biological effects, such as antioxidant, anti-inflammatory, and antimicrobial activities. This study aimed to assess the anti-inflammatory effects of OLP in an in vivo model and explore its molecular interactions through in silico docking studies. We investigated the individual and combined effects of OLP (10 and 20 mg/kg) alongside standard anti-inflammatory drugs, celecoxib (CXB) and ketoprofen (KPN), at 42 mg/kg (p.o.) in a formalin-induced inflammatory chick model. In addition, an in silico analysis was conducted to examine how OLP and the standard drugs interact with cyclooxygenase (COX)-1 and COX-2 enzymes. The results indicated that OLP exhibited a dose-dependent anti-inflammatory effect in chicks, with OLP-20 mg/kg significantly reducing paw-licking frequency and paw edema diameters. Furthermore, the combination of OLP-20 mg/kg with CXB-42 mg/kg and KPN-42 mg/kg showed enhanced anti-inflammatory efficacy. In the molecular docking analysis, OLP demonstrated comparable binding interactions with both COX-1 (‒7.6 kcal/mol) and COX-2 (‒7.7 kcal/mol) enzymes, similar to the standard drugs. Pharmacokinetic (PK) analysis revealed that OLP has favorable properties and a safe toxicity profile, with an LD of 2000 mg/kg. In conclusion, OLP effectively and dose-dependently reduced paw licks and edema in animals, suggesting that its anti-inflammatory effects are mediated through interactions with COX-1 and COX-2 enzymes. Additional research is essential to comprehensively uncover the underlying mechanisms of its action and evaluate its potential for clinical use.
橄榄苦苷（OLP）是一种主要存在于橄榄叶中的生物活性化合物，因其具有抗氧化、抗炎和抗菌等广泛的生物学效应而被人们所熟知。本研究旨在评估OLP在体内模型中的抗炎作用，并通过计算机对接研究探索其分子相互作用。我们在福尔马林诱导的炎症雏鸡模型中，研究了OLP（10和20毫克/千克）与标准抗炎药物塞来昔布（CXB）和酮洛芬（KPN）（均为42毫克/千克，口服）的单独及联合作用。此外，还进行了计算机分析，以研究OLP和标准药物如何与环氧化酶（COX）-1和COX-2酶相互作用。结果表明，OLP在雏鸡中呈现出剂量依赖性抗炎作用，20毫克/千克的OLP能显著降低舔爪频率和爪部水肿直径。此外，20毫克/千克的OLP与42毫克/千克的CXB和42毫克/千克的KPN联合使用时，显示出增强的抗炎效果。在分子对接分析中，OLP与COX-1（-7.6千卡/摩尔）和COX-2（-7.7千卡/摩尔）酶的结合相互作用与标准药物相似。药代动力学（PK）分析显示，OLP具有良好的性质和安全的毒性特征，其半数致死量为2000毫克/千克。总之，OLP能有效且剂量依赖性地减少动物的舔爪行为和水肿，表明其抗炎作用是通过与COX-1和COX-2酶的相互作用介导的。进一步的研究对于全面揭示其作用的潜在机制和评估其临床应用潜力至关重要。
