Suppr超能文献

解释葫芦素作为抗2019冠状病毒潜在治疗药物作用的合理机制。

Plausible mechanisms explaining the role of cucurbitacins as potential therapeutic drugs against coronavirus 2019.

作者信息

Kapoor Neha, Ghorai Soma Mondal, Kushwaha Prem Kumar, Shukla Richa, Aggarwal Charu, Bandichhor Rakeshwar

机构信息

Department of Chemistry, Hindu College, University of Delhi, Delhi, 110007, India.

Department of Zoology, Hindu College, University of Delhi, Delhi, 110007, India.

出版信息

Inform Med Unlocked. 2020;21:100484. doi: 10.1016/j.imu.2020.100484. Epub 2020 Nov 25.

Abstract

In the year 2019, the potent zoonotic virus, severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) began to rage globally, which resulted in the World Health Organization (WHO) declaring it as a pandemic on March 11th, 2020. Although extensive research is currently ongoing worldwide to understand the molecular mechanism and disease pathogenicity of SARS-CoV-2, there are still many nuances to elucidate. Therefore, developing an appropriate vaccine or therapeutic drug to combat coronavirus 2019 (COVID-19) is exceedingly challenging. Such scenarios require multifaceted approaches to identify suitable contenders for drugs against COVID-19. In this context, investigating natural compounds found in food, spices, and beverages can lead to the discovery of lead molecules that could be repurposed to treat COVID-19. Sixteen cucurbitacin analogues were investigated for activity against the SARS-CoV-2 main protease protein (Mpro), angiotensin-converting enzyme 2 (ACE2) binding receptor, nonstructural protein 12 (NSP12) RNA-dependent RNA polymerase (RdRp), NSP13 helicase, and Janus kinase 2 (JAK2)/signal transducer and activator of transcription 3 (STAT3) pathway using several relevant tools and simulated screening methods. All key proteins were found to bind efficiently only with cucurbitacin G 2-glucoside and cucurbitacin H with the lowest global energy. Further, the absorption, distribution, metabolism, and excretion (ADME) of all the cucurbitacins were analysed to explore their drug profiles. Cucurbitacin G 2-glucoside and H showed the best hits and all the analogues showed no adverse properties that would diminish their drug-likeness abilities. The encouraging results of the current study may lay the foundation for future research and development of effective measures and preventive medications against SARS-CoV-2.

摘要

2019年,烈性人畜共患病毒严重急性呼吸综合征冠状病毒2(SARS-CoV-2)开始在全球肆虐,这导致世界卫生组织(WHO)于2020年3月11日宣布其为大流行病。尽管目前全球正在进行广泛研究以了解SARS-CoV-2的分子机制和疾病致病性,但仍有许多细微之处有待阐明。因此,开发一种合适的疫苗或治疗药物来对抗2019冠状病毒病(COVID-19)极具挑战性。这种情况需要多方面的方法来确定对抗COVID-19的合适药物候选物。在此背景下,研究食品、香料和饮料中发现的天然化合物可能会发现可重新用于治疗COVID-19的先导分子。使用几种相关工具和模拟筛选方法,研究了16种葫芦素类似物对SARS-CoV-2主要蛋白酶蛋白(Mpro)、血管紧张素转换酶2(ACE2)结合受体、非结构蛋白12(NSP12)RNA依赖性RNA聚合酶(RdRp)、NSP13解旋酶以及Janus激酶2(JAK2)/信号转导和转录激活因子3(STAT3)途径的活性。发现所有关键蛋白仅与葫芦素G 2-葡萄糖苷和葫芦素H以最低的全局能量有效结合。此外,分析了所有葫芦素的吸收、分布、代谢和排泄(ADME)以探索它们的药物特性。葫芦素G 2-葡萄糖苷和H显示出最佳结果,并且所有类似物均未显示出会削弱其类药能力的不良特性。当前研究的令人鼓舞的结果可能为未来针对SARS-CoV-2的有效措施和预防药物的研发奠定基础。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f3cd/7685940/ee40643c158b/fx1_lrg.jpg

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验