• 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

基于计算机模拟发现并评估植物化学物质与人类儿茶酚-O-甲基转移酶的结合机制,作为帕金森病左旋多巴治疗的潜在生物增强剂。

In silico discovery and evaluation of phytochemicals binding mechanism against human catechol-O-methyltransferase as a putative bioenhancer of L-DOPA therapy in Parkinson disease.

作者信息

Rath Surya Narayan, Jena Lingaraja, Bhuyan Rajabrata, Mahanandia Nimai Charan, Patri Manorama

机构信息

Department of Bioinformatics, Odisha University of Agriculture and Technology, Bhubaneswar 751003, India.

Neurobiology Laboratory, Department of Zoology, School of Life Sciences, Ravenshaw University, Cuttack 753003, India.

出版信息

Genomics Inform. 2021 Mar;19(1):e7. doi: 10.5808/gi.20061. Epub 2021 Feb 26.

DOI:10.5808/gi.20061
PMID:33840171
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8042297/
Abstract

Levodopa (L-DOPA) therapy is normally practised to treat motor pattern associated with Parkinson disease (PD). Additionally, several inhibitory drugs such as Entacapone and Opicapone are also cosupplemented to protect peripheral inactivation of exogenous L-DOPA (~80%) that occurs due to metabolic activity of the enzyme catechol-O-methyltransferase (COMT). Although, both Entacapone and Opicapone have U.S. Food and Drug Administration approval but regular use of these drugs is associated with high risk of side effects. Thus, authors have focused on in silico discovery of phytochemicals and evaluation of their effectiveness against human soluble COMT using virtual screening, molecular docking, drug-like property prediction, generation of pharmacophoric property, and molecular dynamics simulation. Overall, study proposed, nine phytochemicals (withaphysalin D, withaphysalin N, withaferin A, withacnistin, withaphysalin C, withaphysalin O, withanolide B, withasomnine, and withaphysalin F) of plant Withania somnifera have strong binding efficiency against human COMT in comparison to both of the drugs i.e., Opicapone and Entacapone, thus may be used as putative bioenhancer in L-DOPA therapy. The present study needs further experimental validation to be used as an adjuvant in PD treatment.

摘要

左旋多巴(L-DOPA)疗法通常用于治疗与帕金森病(PD)相关的运动模式。此外,还会联合使用几种抑制药物,如恩他卡朋和奥匹卡朋,以保护外源性L-DOPA因儿茶酚-O-甲基转移酶(COMT)的代谢活性而发生的外周失活(约80%)。尽管恩他卡朋和奥匹卡朋均已获得美国食品药品监督管理局的批准,但长期使用这些药物会带来较高的副作用风险。因此,作者致力于通过虚拟筛选、分子对接、类药性质预测、药效团性质生成和分子动力学模拟,在计算机上发现植物化学物质并评估它们对人可溶性COMT的有效性。总体而言,该研究提出,与奥匹卡朋和恩他卡朋这两种药物相比,印度人参的九种植物化学物质(睡茄素D、睡茄素N、睡茄素A、睡茄新苷、睡茄素C、睡茄素O、睡茄内酯B、睡茄胺和睡茄素F)对人COMT具有更强的结合效率,因此可作为L-DOPA疗法中假定的生物增强剂。本研究需要进一步的实验验证,才能用作PD治疗的辅助药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/04dc/8042297/b93e6f9d8e21/gi-20061f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/04dc/8042297/739345af8aa5/gi-20061f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/04dc/8042297/12d357222277/gi-20061f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/04dc/8042297/9ac249ab8246/gi-20061f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/04dc/8042297/432c05bfe723/gi-20061f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/04dc/8042297/a3569fbdc75b/gi-20061f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/04dc/8042297/b93e6f9d8e21/gi-20061f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/04dc/8042297/739345af8aa5/gi-20061f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/04dc/8042297/12d357222277/gi-20061f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/04dc/8042297/9ac249ab8246/gi-20061f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/04dc/8042297/432c05bfe723/gi-20061f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/04dc/8042297/a3569fbdc75b/gi-20061f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/04dc/8042297/b93e6f9d8e21/gi-20061f6.jpg

相似文献

1
In silico discovery and evaluation of phytochemicals binding mechanism against human catechol-O-methyltransferase as a putative bioenhancer of L-DOPA therapy in Parkinson disease.基于计算机模拟发现并评估植物化学物质与人类儿茶酚-O-甲基转移酶的结合机制,作为帕金森病左旋多巴治疗的潜在生物增强剂。
Genomics Inform. 2021 Mar;19(1):e7. doi: 10.5808/gi.20061. Epub 2021 Feb 26.
2
Simultaneous MAO-B and COMT inhibition in L-Dopa-treated patients with Parkinson's disease.左旋多巴治疗的帕金森病患者中同时抑制单胺氧化酶B和儿茶酚-O-甲基转移酶
Mov Disord. 1997 Jul;12(4):497-505. doi: 10.1002/mds.870120404.
3
Opicapone: A Review in Parkinson's Disease.阿扑吗啡酮:治疗帕金森病的一种药物。
Drugs. 2016 Sep;76(13):1293-1300. doi: 10.1007/s40265-016-0623-y.
4
The effect of catechol-O-methyltransferase inhibition with entacapone on cardiovascular autonomic responses in L-Dopa-treated patients with Parkinson's disease.恩他卡朋抑制儿茶酚-O-甲基转移酶对左旋多巴治疗的帕金森病患者心血管自主神经反应的影响。
Clin Neuropharmacol. 2001 Jan-Feb;24(1):50-7. doi: 10.1097/00002826-200101000-00009.
5
Pharmacokinetic drug evaluation of opicapone for the treatment of Parkinson's disease.opicapone治疗帕金森病的药代动力学药物评价
Expert Opin Drug Metab Toxicol. 2018 Mar;14(3):353-360. doi: 10.1080/17425255.2018.1430138. Epub 2018 Jan 24.
6
Effects of peripheral and central catechol-O-methyltransferase inhibition on striatal extracellular levels of dopamine: a microdialysis study in freely moving rats.外周和中枢儿茶酚-O-甲基转移酶抑制对纹状体细胞外多巴胺水平的影响:一项对自由活动大鼠的微透析研究
Parkinsonism Relat Disord. 2003 Jan;9(3):145-50. doi: 10.1016/s1353-8020(02)00016-0.
7
The effects of different repeated doses of entacapone on the pharmacokinetics of L-Dopa and on the clinical response to L-Dopa in Parkinson's disease.不同重复剂量的恩他卡朋对帕金森病患者左旋多巴药代动力学及左旋多巴临床反应的影响。
Clin Neuropharmacol. 2001 May-Jun;24(3):150-7. doi: 10.1097/00002826-200105000-00006.
8
The preclinical discovery and development of opicapone for the treatment of Parkinson's disease.opicapone用于治疗帕金森病的临床前发现与开发。
Expert Opin Drug Discov. 2020 Sep;15(9):993-1004. doi: 10.1080/17460441.2020.1767580. Epub 2020 May 26.
9
Opicapone for the management of end-of-dose motor fluctuations in patients with Parkinson's disease treated with L-DOPA.奥匹卡朋治疗左旋多巴治疗的帕金森病患者的剂末运动波动。
Expert Rev Neurother. 2017 Jul;17(7):649-659. doi: 10.1080/14737175.2017.1336086. Epub 2017 Jun 5.
10
Nitrocatechol Derivatives of Chalcone as Inhibitors of Monoamine Oxidase and Catechol-O-Methyltransferase.查尔酮的硝基邻苯二酚衍生物作为单胺氧化酶和儿茶酚-O-甲基转移酶的抑制剂
Cent Nerv Syst Agents Med Chem. 2018;18(2):115-127. doi: 10.2174/1871524918666180426125714.

本文引用的文献

1
Understanding ligands driven mechanism of wild and mutant aryl hydrocarbon receptor in presence of phytochemicals combating Parkinson's disease: an and study.理解在对抗帕金森病的植物化学物质存在下,野生型和突变型芳香烃受体的配体驱动机制:一项和研究。
J Biomol Struct Dyn. 2020 Feb;38(3):807-826. doi: 10.1080/07391102.2019.1590240. Epub 2019 Apr 2.
2
discovery of potential drug molecules to improve the treatment of isoniazid-resistant .发现潜在的药物分子以改善耐异烟肼的治疗。
J Biomol Struct Dyn. 2019 Aug;37(13):3388-3398. doi: 10.1080/07391102.2018.1515116. Epub 2018 Nov 4.
3
Computational discovery of potent drugs to improve the treatment of pyrazinamide resistant Mycobacterium tuberculosis mutants.
计算发现强效药物,改善耐吡嗪酰胺结核分枝杆菌突变体的治疗效果。
J Cell Biochem. 2018 Sep;119(9):7328-7338. doi: 10.1002/jcb.27033. Epub 2018 May 15.
4
Modulation of Benzo[a]Pyrene Induced Anxiolytic-Like Behavior by Retinoic Acid in Zebrafish: Involvement of Oxidative Stress and Antioxidant Defense System.视黄酸对斑马鱼中苯并[a]芘诱导的抗焦虑样行为的调节作用:氧化应激和抗氧化防御系统的参与
Neurotox Res. 2017 May;31(4):493-504. doi: 10.1007/s12640-016-9694-5. Epub 2017 Jan 6.
5
Virtual Screening for Potential Inhibitors of NS3 Protein of Zika Virus.寨卡病毒NS3蛋白潜在抑制剂的虚拟筛选
Genomics Inform. 2016 Sep;14(3):104-111. doi: 10.5808/GI.2016.14.3.104. Epub 2016 Sep 30.
6
Clinical pharmacology review of opicapone for the treatment of Parkinson's disease.奥匹卡朋治疗帕金森病的临床药理学综述
Neurodegener Dis Manag. 2016 Oct;6(5):349-62. doi: 10.2217/nmt-2016-0022. Epub 2016 Sep 7.
7
Exploring neuroprotective potential of Withania somnifera phytochemicals by inhibition of GluN2B-containing NMDA receptors: An in silico study.通过抑制含GluN2B的NMDA受体探索睡茄植物化学物质的神经保护潜力:一项计算机模拟研究。
Med Hypotheses. 2016 Jul;92:35-43. doi: 10.1016/j.mehy.2016.04.034. Epub 2016 Apr 20.
8
Withania somnifera Leaf Extract Ameliorates Benzo[a]pyrene-Induced Behavioral and Neuromorphological Alterations by Improving Brain Antioxidant Status in Zebrafish (Danio rerio).印度人参叶提取物通过改善斑马鱼(Danio rerio)的脑抗氧化状态减轻苯并[a]芘诱导的行为和神经形态学改变。
Zebrafish. 2016 Jun;13(3):188-96. doi: 10.1089/zeb.2015.1215. Epub 2016 Mar 29.
9
Opicapone as an adjunct to levodopa in patients with Parkinson's disease and end-of-dose motor fluctuations: a randomised, double-blind, controlled trial.奥匹卡朋作为帕金森病患者左旋多巴辅助治疗药物,用于治疗剂末运动波动:一项随机、双盲、对照试验。
Lancet Neurol. 2016 Feb;15(2):154-165. doi: 10.1016/S1474-4422(15)00336-1. Epub 2015 Dec 23.
10
Small-molecule library screening by docking with PyRx.使用PyRx进行对接的小分子文库筛选。
Methods Mol Biol. 2015;1263:243-50. doi: 10.1007/978-1-4939-2269-7_19.