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对从Wall. ex Benth.中分离出的纯化合物的抗伤害感受、抗炎潜力及药物代谢动力学/药物毒性学研究

Investigation of anti-nociceptive, anti-inflammatory potential and ADMET studies of pure compounds isolated from Wall. ex Benth.

作者信息

Alshehri Osama M, Zeb Anwar, Mukarram Shah Syed Muhammad, Mahnashi Mater H, Asiri Saeed Ahmed, Alqahtani Omaish, Sadiq Abdul, Ibrar Muhammad, Alshamrani Saleh, Jan Muhammad Saeed

机构信息

Department of Clinical Laboratory Sciences, College of Applied Medical Sciences, Najran University, Najran, Saudi Arabia.

Department of Pharmacy, University of Swabi, Swabi, Pakistan.

出版信息

Front Pharmacol. 2024 Feb 13;15:1328128. doi: 10.3389/fphar.2024.1328128. eCollection 2024.

Abstract

The strong ethnopharmacological utilization of Wall. Ex. Benth is evident in the treatment of several types of pain and inflammation, including toothache, earache, abdominal pain, gastric pain, and generalized body pain and inflammation. Based on this background, the antinociceptive effects of the crude extract, various fractions, and essential oil have been reported previously. In this research work, we isolate and characterize pure bioactive compounds from and evaluate possible mechanisms using various and models. The pure compounds were analyzed for analgesic and anti-inflammatory activities through various assays. The column chromatography of the chloroform fraction of led to the identification of two pure compounds, i.e., 1 and 2. Compound 1 demonstrated notable inhibition (62% writhing inhibition, 72.77% COX-2 inhibition, and 76.97% 5-LOX inhibition) and anti-inflammatory potential (>50% paw edema inhibition at various intervals). The possible mechanism involved in antinociception was considered primarily, a concept that has already been elucidated through the application of naloxone (an antagonist of opioid receptors). The involvement of adrenergic receptors was investigated using a hot plate model (an adrenergic receptor antagonist). The strong ethnomedicinal analgesic background of , supported by previous reports and current observations, leads to the conclusion that is a potential source of antinociceptive and anti-inflammatory bioactive compounds. It may be concluded from the results that the isolated analgesic compounds of may be a possible alternative remedy for pain and inflammation management with admirable efficacy and safety profiles.

摘要

Wall. Ex. Benth在多种疼痛和炎症治疗中的强大民族药理学应用十分明显,包括牙痛、耳痛、腹痛、胃痛以及全身性疼痛和炎症。基于此背景,先前已有关于粗提物、各种馏分和精油的抗伤害感受作用的报道。在本研究工作中,我们从[植物名称]中分离并鉴定了纯生物活性化合物,并使用各种[动物模型名称1]和[动物模型名称2]模型评估了可能的作用机制。通过各种测定方法分析了这些纯化合物的镇痛和抗炎活性。对[植物名称]氯仿馏分进行柱色谱分离后,鉴定出两种纯化合物,即化合物1和化合物2。化合物1表现出显著的抑制作用(扭体抑制率62%,COX - 2抑制率72.77%,5 - LOX抑制率76.97%)和抗炎潜力(在不同时间间隔对爪肿胀的抑制率>50%)。抗伤害感受作用涉及的可能机制主要被考虑,这一概念已通过应用纳洛酮(阿片受体拮抗剂)得以阐明。使用热板模型(一种肾上腺素能受体拮抗剂)研究了肾上腺素能受体参与情况。先前的报道和当前的观察结果都支持[植物名称]强大的民族医学镇痛背景,由此得出结论,[植物名称]是抗伤害感受和抗炎生物活性化合物的潜在来源。从结果可以推断,[植物名称]中分离出的镇痛化合物可能是用于疼痛和炎症管理的一种可行替代疗法,具有令人满意的疗效和安全性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6573/10897015/8c5eb871ecbc/fphar-15-1328128-g001.jpg

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