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

IF 2 Q3 PHARMACOLOGY & PHARMACY Drug Target Insights Pub Date : 2024-06-18 eCollection Date: 2024-01-01 DOI:10.33393/dti.2024.2745
Abdur Rauf, Umer Rashid, Najla Al Masoud, Zuneera Akram, Anees Saeed, Naveed Muhammad, Taghrid S Alomar, Saima Naz, Marcello Iriti
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Abstract

Background: Pistacia chinensis is extensively employed in traditional medicine. This study aimed to isolate and evaluate the therapeutic effects of 3'4'78-tetrahydroxy-3-methoxyflavone from P. chinensis 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 Pistacia chinensis exhibits significant analgesic, anti-inflammatory, sedative, and muscle relaxing properties, with potential therapeutic applications by inhibiting COX and nociceptive pathways.

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从Pistacia chinensis 中分离的 3',4',7,8-四羟基-3-甲氧基黄酮的体内镇痛、抗炎、镇静和肌肉松弛活性及对接研究。
背景:Pistacia chinensis被广泛应用于传统医学中。本研究旨在从楷属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:研究采用柱层析法进行分离。材料和方法:研究采用柱层析法分离了植物提取物及其分离化合物,并对其体内镇痛(热板模型)、抗炎(角叉菜胶诱导的爪水肿)、镇静(开放场地模型)和肌肉松弛特性(斜面和牵引试验)进行了评估:在热诱导镇痛模型中,提取物(25、50 和 100 毫克/千克)和分离化合物(2.5、5、10 和 15 毫克/千克)在较高剂量下具有显著的镇痛效果。给药 120 分钟后,提取物(100 毫克/千克)明显延长了潜伏时间(21.98 秒)。分离出的化合物在 30 分钟后延长了潜伏时间(20.03 秒),在 120 分钟后仍有明显延长,潜伏时间为 24.11 秒。抗炎效果显示,治疗第五小时后,炎症反应减少了 50.23%(提取物)和 67.09%(化合物)。两种样品都表现出明显的镇静效果,与阴性对照组(180.99 条)相比,提取物阻碍运动的条数减少了 54.11 条。与阴性对照组(180.99 条横线)相比,分离化合物将横线数减少到 15.23±SEM。两种样品也都具有明显的肌肉松弛作用。Docking 研究表明,该化合物的治疗效果是由于抑制了 COX 和痛觉通路:从Pistacia chinensis 中分离出的化合物具有明显的镇痛、抗炎、镇静和肌肉松弛特性,通过抑制 COX 和痛觉通路具有潜在的治疗应用价值。
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来源期刊
Drug Target Insights
Drug Target Insights PHARMACOLOGY & PHARMACY-
CiteScore
2.70
自引率
0.00%
发文量
5
审稿时长
8 weeks
期刊最新文献
Cytotoxic activity, selectivity, and clonogenicity of fruits and resins of Saudi medicinal plants against human liver adenocarcinoma. Levofloxacin induces erythrocyte contraction leading to red cell death. Enhancement of apoptosis in Caco-2, Hep-G2, and HT29 cancer cell lines following exposure to Toxoplasma gondii peptides. Deciphering the molecular mechanisms underlying anti-pathogenic potential of a polyherbal formulation Enteropan® against multidrug-resistant Pseudomonas aeruginosa. In vivo analgesic, anti-inflammatory, sedative, muscle relaxant activities, and docking studies of 3',4',7,8-tetrahydroxy-3-methoxyflavone isolated from Pistacia chinensis.
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