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从……中分离得到的3',4',7,8-四羟基-3-甲氧基黄酮的体内镇痛、抗炎、镇静、肌肉松弛活性及对接研究

In vivo analgesic, anti-inflammatory, sedative, muscle relaxant activities, and docking studies of 3',4',7,8-tetrahydroxy-3-methoxyflavone isolated from .

作者信息

Rauf Abdur, Rashid Umer, Masoud Najla Al, Akram Zuneera, Saeed Anees, Muhammad Naveed, Alomar Taghrid S, Naz Saima, Iriti Marcello

机构信息

Department of Chemistry, University of Swabi, Anbar, Khyber Pakhtunkhwa - Pakistan.

Department of Chemistry, COMSATS University Islamabad, Abbottabad Campus, Abbottabad - Pakistan.

出版信息

Drug Target Insights. 2024 Jun 18;18:47-53. doi: 10.33393/dti.2024.2745. eCollection 2024 Jan-Dec.

Abstract

BACKGROUND

is extensively employed in traditional medicine. This study aimed to isolate and evaluate the therapeutic effects of 3'4'78-tetrahydroxy-3-methoxyflavone from crude extract.

MATERIALS AND METHODS

The study utilized column chromatography for isolation. The plant extract and its isolated compound were assessed for in vivo analgesic (hot plate model), anti-inflammatory (carrageenan-induced paw edema), sedative (open field model), and muscle relaxing properties (inclined plane and traction test).

RESULTS

In the thermal-induced analgesic model, a significant analgesic effect was observed for the extract (25, 50, and 100 mg/kg) and the isolated compound (2.5, 5, 10, and 15 mg/kg) at higher doses. The extract (100 mg/kg) significantly prolonged latency time (21.98 seconds) after 120 minutes of administration. The isolated compound elevated the latency time (20.03 seconds) after 30 minutes, remaining significant up to 120 minutes with a latency time of 24.11 seconds. The anti-inflammatory effect showed a reduction in inflammatory reactions by 50.23% (extract) and 67.09% (compound) after the fifth hour of treatment. Both samples demonstrated significant sedative effects, with the extract hindering movement by 54.11 lines crossed compared to the negative control (180.99 lines). The isolated compound reduced the number of lines crossed to 15.23±SEM compared to the negative control. Both samples were also significant muscle relaxants. Docking studies indicated that the compound's therapeutic effect is due to inhibiting COX and nociceptive pathways.

CONCLUSION

The isolated compound from exhibits significant analgesic, anti-inflammatory, sedative, and muscle relaxing properties, with potential therapeutic applications by inhibiting COX and nociceptive pathways.

摘要

背景

在传统医学中被广泛应用。本研究旨在从粗提取物中分离并评估3'4'78 - 四羟基 - 3 - 甲氧基黄酮的治疗效果。

材料与方法

本研究采用柱色谱法进行分离。对植物提取物及其分离出的化合物进行了体内镇痛(热板模型)、抗炎(角叉菜胶诱导的爪肿胀)、镇静(旷场模型)和肌肉松弛特性(斜面和牵引试验)的评估。

结果

在热诱导镇痛模型中,提取物(25、50和100 mg/kg)和分离出的化合物(2.5、5、10和15 mg/kg)在较高剂量时显示出显著的镇痛效果。提取物(100 mg/kg)在给药120分钟后显著延长潜伏期(21.98秒)。分离出的化合物在30分钟后延长潜伏期(20.03秒),直至120分钟仍保持显著,潜伏期为24.11秒。抗炎作用显示,治疗第五小时后,炎症反应分别降低了50.23%(提取物)和67.09%(化合物)。两个样品均显示出显著的镇静作用,与阴性对照(180.99条)相比,提取物使穿过的线条数减少了54.11条。分离出的化合物与阴性对照相比,使穿过的线条数减少至15.23±标准误。两个样品也是显著的肌肉松弛剂。对接研究表明,该化合物的治疗效果是由于抑制了COX和伤害感受途径。

结论

从[植物名称未给出]中分离出的化合物具有显著的镇痛、抗炎、镇静和肌肉松弛特性,通过抑制COX和伤害感受途径具有潜在的治疗应用价值。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/36de/11188735/e90f39090ccc/dti-18-47_g001.jpg

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