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(Wall.)的生物活性及对环氧化酶的抑制作用研究。

Bioactivities of (Wall.) and Study against Cyclooxygenase Enzymes.

机构信息

Department of Pharmacy, Faculty of Biological Science and Technology, Jashore University of Science and Technology, Jashore 7408, Bangladesh.

出版信息

Biomed Res Int. 2022 Apr 28;2022:1331758. doi: 10.1155/2022/1331758. eCollection 2022.

Abstract

(Wall.) is extensively used in traditional medicine for the treatment of various diseases including rheumatism, kidney problems, jaundice, urinary tract disorders, fever, and pain. The present study was designed to explore new lead compound(s) to alleviate pain, pyresis, and diarrhea from methanol, ethyl acetate, and n-hexane extracts of (Wall.) leaves (MHP, EAHP, and NHP, respectively). Analgesic activity of the extracts was assessed through acetic acid induced writhing, tail immersion, and hot plate tests while brewer's yeast-induced pyrexia test was employed for the assessment of antipyretic activity. Besides, castor oil and magnesium sulfate induced diarrheal tests were utilized for the evaluation of antidiarrheal properties. Moreover, study of the isolated compounds was undertaken to seek out best-fit phytoconstituent(s) against cyclooxygenase enzymes. MHP revealed substantial antioxidant activities in different assays compared to EAHP and NHP. In the acetic acid-induced writhing test, among the extracts, MHP (400 mg/kg) revealed maximum 74.15 ± 1% inhibition of writhing comparable to that of standard (85.77 ± 1.39%). Again, in tail immersion and hot plate tests, higher doses of all the test samples exhibited a significant increase of latent period in a time-dependent manner. In brewer yeast-induced pyrexia test, at 3 and 4 hour of treatment, significant ( < 0.05) antipyretic action was found in the test samples. In both castor oil and magnesium induced diarrheal tests, MHP at 400 mg/kg showed the highest percent inhibition of diarrhea (68.62 ± 4.74 and 64.99 ± 2.90, respectively). Moreover, molecular docking analysis corroborated the results of the present study. The findings of the present study supported the traditional uses of this plant for the alleviation of pain and fever. Furthermore, hoyasterone was found to be the most effective lead compound as cyclooxygenase enzyme inhibitor.

摘要

(Wall.)在传统医学中被广泛用于治疗各种疾病,包括风湿、肾脏问题、黄疸、尿路疾病、发热和疼痛。本研究旨在探索新的先导化合物,以缓解甲醇、乙酸乙酯和正己烷提取物(MHP、EAHP 和 NHP)对(Wall.)叶的疼痛、发热和腹泻。通过醋酸诱导的扭体、尾部浸入和热板试验评估提取物的镇痛活性,而利用啤酒酵母诱导的发热试验评估解热活性。此外,还利用蓖麻油和硫酸镁诱导的腹泻试验评估抗腹泻特性。此外,还进行了分离化合物的研究,以寻找最适合的植物成分对抗环氧化酶。与 EAHP 和 NHP 相比,MHP 在不同的抗氧化试验中表现出显著的抗氧化活性。在醋酸诱导的扭体试验中,在提取物中,MHP(400mg/kg)对扭体的抑制作用最大,达到 74.15%±1%,与标准品(85.77%±1.39%)相当。同样,在尾部浸入和热板试验中,所有测试样品的较高剂量均表现出明显的潜伏期随时间的依赖性增加。在啤酒酵母诱导的发热试验中,在治疗 3 和 4 小时时,测试样品显示出显著的(<0.05)解热作用。在蓖麻油和硫酸镁诱导的腹泻试验中,MHP 在 400mg/kg 时显示出最高的腹泻抑制率(分别为 68.62%±4.74%和 64.99%±2.90%)。此外,分子对接分析证实了本研究的结果。本研究的结果支持该植物用于缓解疼痛和发热的传统用途。此外,发现霍氏海胆甾酮是最有效的环氧化酶抑制剂先导化合物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c919/9071894/74c751d6da1b/BMRI2022-1331758.001.jpg

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