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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.

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/8042297/739345af8aa5/gi-20061f1.jpg

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