Unraveling the therapeutic potential of Tephrosia linearis: Anti-inflammatory, analgesic activity, and molecular docking approaches

Moses Opio , Kenedy Kiyimba , Catherine Nabitandikwa , Richard Maseruka , Tony Lukwago Wotoyitidde , Moses Andima , Mercy Chebijira , Sharon Tracy Edeya , Alice Nabatanzi , Yahaya Gavamukulya , Dan Kibuule , Paul Waako , Richard Oriko Owor , Samuel Baker Obakiro
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Abstract

Background

Inflammatory diseases such as arthritis affect over 300 million people globally. The current treatment mainly involves the use of Non-Steroidal Anti-inflammatory drugs (NSAIDS) which possess several adverse drug reactions that are sometimes life threatening. This has prompted many patients to gain interest in plant-based remedies. Tephrosia linearis (Willd.) Pers (Fabaceae) is widely used in Uganda to manage symptoms of inflammation. However, there was a paucity of information concerning its analgesic and anti-inflammatory activities. This study investigated the anti-inflammatory, analgesic, and acute toxicity effects of ethanolic extracts from the aerial parts of Tephrosia linearis in Wistar albino rats.

Methods

Plant samples were collected from Katakwi District, Eastern Uganda and extracted using 70 % ethanol. Quantitative phytochemical analysis was conducted using UV/Vis spectroscopy. Acute toxicity was assessed using Lorke’s method, while analgesic and anti-inflammatory activities were evaluated through Complete Freud’s Adjuvant-induced arthritis model. Three doses of T. linearis (200, 400, and 800 mg/kg) were compared with a control group receiving 20 mg/kg of diclofenac. Three marker compounds were assessed using in silico modeling to predict their pharmacokinetic properties, organ toxicity, and binding energy against selected protein targets involved in inflammation.

Results

The ethanolic extract contained significant concentrations of flavonoids (82.9 ± 0.1 mg/g), tannins (140.2 ± 0.9 mg/g), alkaloids (93.4 ± 1.0 mg/g), and triterpenoids (76.1 ± 1.5 mg/g). No toxic effects were observed at doses below 2000 mg/kg, with an estimated LD50 of 2692 mg/kg. The extract exhibited a non-dose dependent analgesic and anti-inflammatory activities that were significantly lower than that of diclofenac (p < 0.05). Molecular docking revealed strong binding affinities for apigenin, luteolin, and velutin with COX2, PLA2, and TNFα.

Conclusion

This study supports T. linearis as a safe herbal remedy for managing inflammation, suggesting further optimization through active ingredient isolation for enhanced therapeutic outcomes.
揭示毛茛的治疗潜力:抗炎、镇痛活性和分子对接方法
关节炎等炎性疾病影响着全球超过3亿人。目前的治疗主要包括使用非甾体抗炎药(NSAIDS),这些药物有几种不良反应,有时会危及生命。这促使许多患者对植物性疗法产生了兴趣。毛茛(野生)豆科植物在乌干达广泛用于治疗炎症症状。然而,关于其镇痛和抗炎活性的信息缺乏。本研究探讨了灰参地上部乙醇提取物对Wistar白化大鼠的抗炎、镇痛和急性毒性作用。方法采自乌干达东部Katakwi地区的植物样品,用70% %乙醇提取。采用紫外/可见光谱法进行植物化学定量分析。采用Lorke的方法评估急性毒性,而通过完全弗洛伊德佐剂诱导关节炎模型评估镇痛和抗炎活性。将三种剂量(200,400和800 mg/kg)的线性弓形虫与接受20 mg/kg双氯芬酸的对照组进行比较。使用计算机模型评估了三种标记化合物,以预测它们的药代动力学特性、器官毒性和针对炎症中选定的蛋白质靶点的结合能。ResultsThe ethanolic提取中类黄酮的含量显著(82.9 ±0.1  毫克/ g),单宁(140.2 ±0.9  毫克/克)、生物碱(93.4 ±1.0  毫克/ g),和常用药用(76.1 ±1.5  毫克/克)。剂量低于2000 mg/kg时未观察到毒性作用,估计LD50为2692 mg/kg。该提取物具有非剂量依赖性的镇痛和抗炎活性,显著低于双氯芬酸(p <; 0.05)。分子对接发现,芹菜素、木犀草素和鹿皮素与COX2、PLA2和TNFα具有较强的结合亲和力。结论:本研究支持T. linear是一种安全的治疗炎症的草药,建议通过分离活性成分进一步优化,以提高治疗效果。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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