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胡椒碱具有抗炎作用,并拮抗塞来昔布和酮洛芬的特性:以及分子对接研究。

Piperine exerts anti-inflammatory effects and antagonises the properties of celecoxib and ketoprofen: and molecular docking studies.

作者信息

Hasan Rubel, Bhuia Md Shimul, Chowdhury Raihan, Khan Muhammad Ali, Mazumder Modhurima, Yana Noshin Tasnim, Alencar Marcus Vinícius Oliveira Barros de, Ansari Siddique Akber, Ansari Irfan Aamer, Islam Muhammad Torequl

机构信息

Department of Pharmacy, Bangabandhu Sheikh Mujibur Rahman Science and Technology University, Gopalganj, Bangladesh.

Bioinformatics and Drug Innovation Laboratory, BioLuster Research Center Ltd, Gopalganj, Bangladesh.

出版信息

Nat Prod Res. 2024 Oct 11:1-16. doi: 10.1080/14786419.2024.2413039.

DOI:10.1080/14786419.2024.2413039
PMID:39390887
Abstract

This study evaluates the anti-inflammatory effects of a natural product, piperine (PPN), using and methodologies. In the segment, inflammation was induced in the right hind paw of young chicks a formalin (50 μL) injection. PPN was orally administered at doses of 25 and 50 mg/kg with or without celecoxib (CXB) and/or ketoprofen (KPN) (42 mg/kg). The vehicle acted as the negative control group (NC). The analysis predicted the drug-likeness, pharmacokinetics, and toxicity profile of PPN, along with evaluating its binding affinity and ligand-receptor interactions. Results indicate that PPN significantly ( < 0.05) reduced licking frequency and paw edoema in a dose-dependent manner. However, in combination therapy, PPN diminished the effects of both CXB and KPN. PPN showed high affinity (-8.6 kcal/mol) towards the COX-2 enzyme. Therefore, PPN exerts anti-inflammatory effects in chicks through COX-2 inhibition pathways and antagonises CXB and KPN activities.

摘要

本研究采用[具体方法1]和[具体方法2]评估天然产物胡椒碱(PPN)的抗炎作用。在[具体实验阶段],通过向幼雏右后爪注射50μL福尔马林诱导炎症。PPN以25和50mg/kg的剂量口服给药,同时或不同时给予塞来昔布(CXB)和/或酮洛芬(KPN)(42mg/kg)。赋形剂作为阴性对照组(NC)。[具体分析方法]分析预测了PPN的类药性质、药代动力学和毒性概况,同时评估了其结合亲和力和配体 - 受体相互作用。结果表明,PPN以剂量依赖性方式显著(P < 0.05)降低舔舐频率和爪部水肿。然而,在联合治疗中,PPN减弱了CXB和KPN的作用。PPN对COX - 2酶表现出高亲和力(-8.6kcal/mol)。因此,PPN通过抑制COX - 2途径在雏鸡中发挥抗炎作用,并拮抗CXB和KPN的活性。

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