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天然产物作为新型神经保护剂;分子靶点、药物代谢动力学性质及安全性的计算预测

Natural Products as Novel Neuroprotective Agents; Computational Predictions of the Molecular Targets, ADME Properties, and Safety Profile.

作者信息

Alghamdi Sahar Saleh, Suliman Rasha Saad, Aljammaz Norah Abdulaziz, Kahtani Khawla Mohammed, Aljatli Dimah Abdulqader, Albadrani Ghadeer M

机构信息

College of Pharmacy, King Saud bin Abdulaziz University for Health Sciences, Riyadh 11481, Saudi Arabia.

King Abdullah International Medical Research Centre (KAIMRC), Ministry of National Guard Health Affairs, Riyadh 11481, Saudi Arabia.

出版信息

Plants (Basel). 2022 Feb 18;11(4):549. doi: 10.3390/plants11040549.

Abstract

Neurodegenerative diseases (NDs) are one of the most challenging public health issues. Despite tremendous advances in our understanding of NDs, little progress has been made in establishing effective treatments. Natural products may have enormous potential in preventing and treating NDs by targeting microglia; yet, there have been several clinical concerns about their usage, primarily due to a lack of scientific evidence for their efficacy, molecular targets, physicochemical properties, and safety. To solve this problem, the secondary bioactive metabolites derived from neuroprotective medicinal plants were identified and selected for computational predictions for anti-inflammatory activity, possible molecular targets, physicochemical properties, and safety evaluation using PASS online, Molinspiration, SwissADME, and ProTox-II, respectively. Most of the phytochemicals were active as anti-inflammatory agents as predicted using the PASS online webserver. Moreover, the molecular target predictions for some phytochemicals were similar to the reported experimental targets. Moreover, the phytochemicals that did not violate important physicochemical properties, including blood-brain barrier penetration, GI absorption, molecular weight, and lipophilicity, were selected for further safety evaluation. After screening 54 neuroprotective phytochemicals, our findings suggest that Aromatic-turmerone, Apocynin, and Matrine are the most promising compounds that could be considered when designing novel neuroprotective agents to treat neurodegenerative diseases via modulating microglial polarization.

摘要

神经退行性疾病(NDs)是最具挑战性的公共卫生问题之一。尽管我们对NDs的理解有了巨大进展,但在建立有效治疗方法方面进展甚微。天然产物可能通过靶向小胶质细胞在预防和治疗NDs方面具有巨大潜力;然而,关于其使用存在一些临床担忧,主要是由于缺乏关于其疗效、分子靶点、物理化学性质和安全性的科学证据。为了解决这个问题,分别使用在线PASS、Molinspiration、SwissADME和ProTox-II对源自神经保护药用植物的次生生物活性代谢产物进行了鉴定和选择,以进行抗炎活性、可能的分子靶点、物理化学性质和安全性评估的计算预测。使用在线PASS网络服务器预测,大多数植物化学物质具有抗炎活性。此外,一些植物化学物质的分子靶点预测与报道的实验靶点相似。此外,选择了不违反包括血脑屏障穿透、胃肠道吸收、分子量和亲脂性在内的重要物理化学性质的植物化学物质进行进一步的安全性评估。在筛选了54种神经保护植物化学物质后,我们的研究结果表明,芳香姜黄酮、阿朴吗啡和苦参碱是最有前景的化合物,在设计通过调节小胶质细胞极化来治疗神经退行性疾病的新型神经保护剂时可以考虑。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2bc9/8878483/4961376ef420/plants-11-00549-g001.jpg

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