• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利：CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法，用中文像聊天一样搜索，搜遍4000万医学文献。AI智能推荐，让科研检索更轻松。

立即免费搜索

文件翻译

保留排版，准确专业，支持PDF/Word/PPT等文件格式，支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述，25分钟生成高质量综述，智能提取关键信息，辅助科研写作。

立即免费体验

通过酵母诱导发热模型和分子对接研究评估粘菌素作为一种有效且安全的解热剂

Viscosine as a Potent and Safe Antipyretic Agent Evaluated by Yeast-Induced Pyrexia Model and Molecular Docking Studies.

作者信息

Muhammad Akhtar, Khan Behramand, Iqbal Zafar, Khan Amir Zada, Khan Inamullah, Khan Kashif, Alamzeb Muhammad, Ahmad Nasir, Khan Khalid, Lal Badshah Syed, Ullah Asad, Muhammad Sayyar, Jan Muhammad Tariq, Nadeem Said, Kabir Nurul

机构信息

Department of Chemistry, Islamia College University, Peshawar, KPK 25120, Pakistan.

Department of Pharmacy, University of Peshawar, Peshawar 25120, Pakistan.

出版信息

ACS Omega. 2019 Aug 21;4(10):14188-14192. doi: 10.1021/acsomega.9b01041. eCollection 2019 Sep 3.

DOI:10.1021/acsomega.9b01041
PMID:31508540
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6732982/
Abstract

The antipyretic potential of viscosine, a natural product isolated from the medicinal plant , was investigated using yeast-induced pyrexia rat model, and its structure-activity relationship was investigated through molecular docking analyses with the target enzymes cyclooxygenase-1 (COX-1), cyclooxygenase-2 (COX-2), and microsomal prostaglandin E synthase-1 (mPGES-1). The in vivo antipyretic experiments showed a progressive dose-dependent reduction in body temperatures of the hyperthermic test animals when injected with viscosine. Comparison of docking analyses with target enzymes showed strongest bonding interactions (binding energy -17.34 kcal/mol) of viscosine with the active-site pocket of mPGES-1. These findings suggest that viscosine shows antipyretic properties by reducing the concentration of prostaglandin E in brain through its mPGES-1 inhibitory action and make it a potential lead compound for developing effective and safer antipyretic drugs for treating fever and related pathological conditions.

摘要

使用酵母诱导发热大鼠模型研究了从药用植物中分离出的天然产物粘菌素的解热潜力，并通过与靶酶环氧合酶-1（COX-1）、环氧合酶-2（COX-2）和微粒体前列腺素E合酶-1（mPGES-1）进行分子对接分析来研究其构效关系。体内解热实验表明，给发热实验动物注射粘菌素后，其体温呈剂量依赖性逐渐降低。与靶酶的对接分析比较显示，粘菌素与mPGES-1的活性位点口袋具有最强的结合相互作用（结合能-17.34 kcal/mol）。这些发现表明，粘菌素通过其对mPGES-1的抑制作用降低脑中前列腺素E的浓度而表现出解热特性，使其成为开发治疗发热及相关病理状况的有效且更安全的解热药物的潜在先导化合物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/71a6/6732982/7ad965c1e565/ao9b01041_0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/71a6/6732982/b3de4f1d7a42/ao9b01041_0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/71a6/6732982/623786dacc3d/ao9b01041_0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/71a6/6732982/e7615c51087f/ao9b01041_0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/71a6/6732982/da0ad4789758/ao9b01041_0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/71a6/6732982/7ad965c1e565/ao9b01041_0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/71a6/6732982/b3de4f1d7a42/ao9b01041_0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/71a6/6732982/623786dacc3d/ao9b01041_0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/71a6/6732982/e7615c51087f/ao9b01041_0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/71a6/6732982/da0ad4789758/ao9b01041_0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/71a6/6732982/7ad965c1e565/ao9b01041_0005.jpg

相似文献

1
Viscosine as a Potent and Safe Antipyretic Agent Evaluated by Yeast-Induced Pyrexia Model and Molecular Docking Studies.通过酵母诱导发热模型和分子对接研究评估粘菌素作为一种有效且安全的解热剂
ACS Omega. 2019 Aug 21;4(10):14188-14192. doi: 10.1021/acsomega.9b01041. eCollection 2019 Sep 3.
2
Rutin hydrate and extract from Castanopsis tribuloides reduces pyrexia via inhibiting microsomal prostaglandin E synthase-1.从柯属植物中提取的芦丁水合物通过抑制微粒体前列腺素 E 合酶-1 来降低发热。
Biomed Pharmacother. 2022 Apr;148:112774. doi: 10.1016/j.biopha.2022.112774. Epub 2022 Feb 28.
3
Antipyretic activity of (Rottl.) leaves extract along with phytoconstituent's binding affinity to COX-1, COX-2, and mPGES-1 receptors: and approaches.（Rottl.）叶提取物的解热活性以及植物成分与COX-1、COX-2和mPGES-1受体的结合亲和力： 以及 方法。
Saudi J Biol Sci. 2021 Sep;28(9):5302-5309. doi: 10.1016/j.sjbs.2021.05.050. Epub 2021 May 24.
4
Molecular Docking Analysis of Phytic Acid and 4-hydroxyisoleucine as Cyclooxygenase-2, Microsomal Prostaglandin E Synthase-2, Tyrosinase, Human Neutrophil Elastase, Matrix Metalloproteinase-2 and -9, Xanthine Oxidase, Squalene Synthase, Nitric Oxide Synthase, Human Aldose Reductase, and Lipoxygenase Inhibitors.植酸和4-羟基异亮氨酸作为环氧化酶-2、微粒体前列腺素E合酶-2、酪氨酸酶、人中性粒细胞弹性蛋白酶、基质金属蛋白酶-2和-9、黄嘌呤氧化酶、角鲨烯合酶、一氧化氮合酶、人醛糖还原酶和脂氧合酶抑制剂的分子对接分析
Pharmacogn Mag. 2017 Oct;13(Suppl 3):S512-S518. doi: 10.4103/pm.pm_195_16. Epub 2017 Oct 11.
5
GABA(A) receptor modulation and neuropharmacological activities of viscosine isolated from Dodonaea viscosa (Linn).从坡柳（Dodonaea viscosa (Linn)）中分离得到的粘胶素的GABA(A)受体调节作用及神经药理活性
Pharmacol Biochem Behav. 2015 Sep;136:64-72. doi: 10.1016/j.pbb.2015.07.006. Epub 2015 Jul 14.
6
Hepatoprotective activity of viscosine is mediated by attenuation of hepatic macrophages and iNOS expression in CCl-intoxicated rats.粘丝菌素的肝脏保护活性是通过减轻四氯化碳中毒大鼠肝脏巨噬细胞和诱导型一氧化氮合酶的表达来介导的。
Toxicol Res (Camb). 2016 Sep 13;5(6):1688-1698. doi: 10.1039/c6tx00165c. eCollection 2016 Nov 1.
7
Potent inhibition of human 5-lipoxygenase and microsomal prostaglandin E₂ synthase-1 by the anti-carcinogenic and anti-inflammatory agent embelin.抑癌抗炎剂 Embelin 对人 5-脂氧合酶和微粒体前列腺素 E₂ 合酶-1 的强效抑制作用。
Biochem Pharmacol. 2013 Aug 15;86(4):476-86. doi: 10.1016/j.bcp.2013.04.015. Epub 2013 Apr 24.
8
Identification of the two-phase mechanism of arachidonic acid regulating inflammatory prostaglandin E2 biosynthesis by targeting COX-2 and mPGES-1.通过靶向COX-2和mPGES-1鉴定花生四烯酸调节炎症性前列腺素E2生物合成的双相机制。
Arch Biochem Biophys. 2016 Aug 1;603:29-37. doi: 10.1016/j.abb.2016.04.011. Epub 2016 May 10.
9
MF63 [2-(6-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)-isophthalonitrile], a selective microsomal prostaglandin E synthase-1 inhibitor, relieves pyresis and pain in preclinical models of inflammation.MF63 [2-(6-氯-1H-菲并[9,10-d]咪唑-2-基)-间苯二甲腈]，一种选择性微粒体前列腺素E合酶-1抑制剂，可缓解炎症临床前模型中的发热和疼痛。
J Pharmacol Exp Ther. 2008 Sep;326(3):754-63. doi: 10.1124/jpet.108.138776. Epub 2008 Jun 4.
10
Acetaminophen reduces lipopolysaccharide-induced fever by inhibiting cyclooxygenase-2.对乙酰氨基酚通过抑制环氧化酶-2 减少脂多糖诱导的发热。
Neuropharmacology. 2013 Aug;71:124-9. doi: 10.1016/j.neuropharm.2013.03.012. Epub 2013 Mar 29.

引用本文的文献

1
Galegine, a Bioprivileged Alkaloid from : Antipyretic Activity Insights.加勒金，一种来自[具体来源未给出]的具有生物特权的生物碱：解热活性见解。
Curr Top Med Chem. 2025;25(8):943-954. doi: 10.2174/0115680266333237241212071912.
2
The protective effects of Zingiber zerumbet rhizome against fevers in rats.菖蒲根茎防治大鼠发热的保护作用。
Naturwissenschaften. 2024 Apr 1;111(2):20. doi: 10.1007/s00114-024-01907-7.
3
Polyphenols and extracts from (Roxb.) Roscoe leaf mitigate pain, inflammation and pyrexia by inhibiting cyclooxygenase-2: an and studies.

本文引用的文献

1
Hepatoprotective activity of viscosine is mediated by attenuation of hepatic macrophages and iNOS expression in CCl-intoxicated rats.粘丝菌素的肝脏保护活性是通过减轻四氯化碳中毒大鼠肝脏巨噬细胞和诱导型一氧化氮合酶的表达来介导的。
Toxicol Res (Camb). 2016 Sep 13;5(6):1688-1698. doi: 10.1039/c6tx00165c. eCollection 2016 Nov 1.
2
Receptor-ligand molecular docking.受体-配体分子对接
Biophys Rev. 2014 Mar;6(1):75-87. doi: 10.1007/s12551-013-0130-2. Epub 2013 Dec 21.
3
Identification of novel microsomal prostaglandin E synthase-1 (mPGES-1) lead inhibitors from Fragment Virtual Screening.
（罗克斯伯）罗斯科叶中的多酚和提取物通过抑制环氧化酶-2减轻疼痛、炎症和发热：一项体外和体内研究。
Front Pharmacol. 2024 Feb 14;15:1344123. doi: 10.3389/fphar.2024.1344123. eCollection 2024.
4
Pharmacological Effects and Underlying Mechanisms of Licorice-Derived Flavonoids.甘草源黄酮类化合物的药理作用及潜在机制
Evid Based Complement Alternat Med. 2022 Jan 17;2022:9523071. doi: 10.1155/2022/9523071. eCollection 2022.
5
Computational Study of SARS-CoV-2 RNA Dependent RNA Polymerase Allosteric Site Inhibition.SARS-CoV-2 依赖 RNA 的 RNA 聚合酶变构位点抑制的计算研究。
Molecules. 2021 Dec 30;27(1):223. doi: 10.3390/molecules27010223.
6
Antipyretic activity of (Rottl.) leaves extract along with phytoconstituent's binding affinity to COX-1, COX-2, and mPGES-1 receptors: and approaches.（Rottl.）叶提取物的解热活性以及植物成分与COX-1、COX-2和mPGES-1受体的结合亲和力： 以及 方法。
Saudi J Biol Sci. 2021 Sep;28(9):5302-5309. doi: 10.1016/j.sjbs.2021.05.050. Epub 2021 May 24.
7
Antidepressant, anxiolytic, antipyretic, and thrombolytic profiling of methanol extract of the aerial part of : In vivo, in vitro, and in silico approaches.某植物地上部分甲醇提取物的抗抑郁、抗焦虑、解热和溶栓特性分析：体内、体外及计算机模拟方法
Food Sci Nutr. 2021 Jan 5;9(2):833-846. doi: 10.1002/fsn3.2047. eCollection 2021 Feb.
8
Important Flavonoids and Their Role as a Therapeutic Agent.重要类黄酮及其作为治疗剂的作用。
Molecules. 2020 Nov 11;25(22):5243. doi: 10.3390/molecules25225243.
9
Genomics approaches to synthesize plant-based biomolecules for therapeutic applications to combat SARS-CoV-2.利用基因组学方法合成基于植物的生物分子，用于治疗 SARS-CoV-2 的应用。
Genomics. 2020 Nov;112(6):4322-4331. doi: 10.1016/j.ygeno.2020.07.033. Epub 2020 Jul 25.
通过片段虚拟筛选鉴定新型微粒体前列腺素E合酶-1（mPGES-1）先导抑制剂。
Eur J Med Chem. 2017 Jan 5;125:278-287. doi: 10.1016/j.ejmech.2016.09.042. Epub 2016 Sep 14.
4
GABA(A) receptor modulation and neuropharmacological activities of viscosine isolated from Dodonaea viscosa (Linn).从坡柳（Dodonaea viscosa (Linn)）中分离得到的粘胶素的GABA(A)受体调节作用及神经药理活性
Pharmacol Biochem Behav. 2015 Sep;136:64-72. doi: 10.1016/j.pbb.2015.07.006. Epub 2015 Jul 14.
5
Perspective of microsomal prostaglandin E2 synthase-1 as drug target in inflammation-related disorders.微粒体前列腺素 E2 合酶-1 作为炎症相关疾病的药物靶点的展望。
Biochem Pharmacol. 2015 Nov 1;98(1):1-15. doi: 10.1016/j.bcp.2015.06.022. Epub 2015 Jun 27.
6
Crystal Structures of mPGES-1 Inhibitor Complexes Form a Basis for the Rational Design of Potent Analgesic and Anti-Inflammatory Therapeutics.mPGES-1抑制剂复合物的晶体结构为强效镇痛和抗炎治疗药物的合理设计奠定了基础。
J Med Chem. 2015 Jun 11;58(11):4727-37. doi: 10.1021/acs.jmedchem.5b00330. Epub 2015 May 20.
7
Fever management in intensive care patients with infections.重症监护病房感染患者的发热管理
Crit Care. 2014 Mar 18;18(2):206. doi: 10.1186/cc13773.
8
Structure-activity relationship of nonacidic quinazolinone inhibitors of human microsomal prostaglandin synthase 1 (mPGES 1).非酸性喹唑啉酮类人微粒体前列腺素合酶 1（mPGES-1）抑制剂的构效关系。
J Med Chem. 2012 Apr 26;55(8):3792-803. doi: 10.1021/jm201687d. Epub 2012 Apr 11.
9
Observation of two modes of inhibition of human microsomal prostaglandin E synthase 1 by the cyclopentenone 15-deoxy-Δ(12,14)-prostaglandin J(2).观察环戊烯酮 15-脱氧-Δ(12,14)-前列腺素 J(2)对人微粒体前列腺素 E 合酶 1 的两种抑制模式。
Biochemistry. 2012 Mar 20;51(11):2348-56. doi: 10.1021/bi2019332. Epub 2012 Mar 8.
10
Design, synthesis, and pharmacological activity of nonallergenic pyrazolone-type antipyretic analgesics.非变应原吡唑酮类解热镇痛药的设计、合成及药理活性。
J Med Chem. 2010 Dec 23;53(24):8727-33. doi: 10.1021/jm101208x. Epub 2010 Dec 1.