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L提取物对SARS-CoV-2刺突蛋白与血管紧张素转换酶2相互作用的抑制作用。

Inhibitory Effect of L. Extracts on SARS-COV-2 Spike Protein-ACE2 Interaction.

作者信息

Ali Najma, Cyril Asha Caroline, Parambath Anagha, Vazhappilly Cijo George, Jan Reem Kais, Aburamadan Haneen, Akbarpoor Fatemeh, Shariar Islam S M, Nessa Fazilatun, Lozon Yosra, Karuvantevida Noushad, Radhakrishnan Rajan

机构信息

College of Medicine, Mohammed Bin Rashid University of Medicine and Health Sciences, Dubai, United Arab Emirates.

Department of Biotechnology, American University of Ras Al Khaimah, Ras Al Khaimah, United Arab Emirates.

出版信息

Curr Ther Res Clin Exp. 2024 Aug 31;101:100759. doi: 10.1016/j.curtheres.2024.100759. eCollection 2024.

DOI:10.1016/j.curtheres.2024.100759
PMID:39649409
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11625226/
Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

A catastrophic outbreak of severe acute respiratory syndrome (SARS-CoV-2; Coronavirus disease-19; COVID-19) was first detected in Wuhan, Hubei Province, China, in December 2019. Many experimental and clinical studies have focused on the effectiveness of medicinal plants such as (NS) in combating SARS-CoV-2. In this study, we aimed to evaluate the effect of NS seed extract on SARS-CoV-2 spike protein (S1)-angiotensin-converting enzyme 2 (S-ACE2) interaction.

MATERIALS AND METHODS

NS seed extracts used for the assay were prepared in chloroform, ethanol, and water by Soxhlet extraction and recovered by rotary evaporation. The inhibition percentage of S1-ACE2 interaction was analyzed using ELISA-SARS-CoV-2 S1 Protein-ACE2 Binding Inhibitor Screening Kit. Chemical finger-printing of the extracts was done using RP-HPLC.

RESULTS

Significant concentration-dependent inhibition of the S1-ACE2 interaction was observed with chloroform, ethanol, and water extracts, ranging from 0.01 to 10 mg/ml. The -values for the extracts were as follows: 0.0055, 0.0937, 0.0013, and 0.0003 for chloroform extract; 0.0876, 0.0703, 0.0183, and 0.0071 for ethanol extract; and 0.0915, 0.0312, 0.0006, and 0.0006 for water extract. The 50% inhibitory concentration (IC50) was determined to be 0.132 mg/ml, 0.288 mg/ml, and 4.06 mg/ml for chloroform, ethanol, and water extracts, respectively.

CONCLUSION

The analysis utilizing SARS-CoV2 spike (S1) and ACE2 proteins proved that NS seed extracts have the potential to inhibit the S-ACE2 interaction, which warrants further studies that could lead to potential drug discovery for SARS-CoV2 infection.

摘要

民族药理学相关性

2019年12月,在中国湖北省武汉市首次检测到严重急性呼吸综合征(SARS-CoV-2;冠状病毒病-19;COVID-19)的灾难性爆发。许多实验和临床研究都集中在药用植物如(NS)对抗SARS-CoV-2的有效性上。在本研究中,我们旨在评估NS种子提取物对SARS-CoV-2刺突蛋白(S1)-血管紧张素转换酶2(S-ACE2)相互作用的影响。

材料与方法

用于测定的NS种子提取物通过索氏提取法用氯仿、乙醇和水制备,并通过旋转蒸发回收。使用ELISA-SARS-CoV-2 S1蛋白-ACE2结合抑制剂筛选试剂盒分析S1-ACE2相互作用的抑制百分比。提取物的化学指纹图谱采用反相高效液相色谱法进行。

结果

氯仿、乙醇和水提取物在0.01至10mg/ml范围内观察到对S1-ACE2相互作用有显著的浓度依赖性抑制。提取物的-值如下:氯仿提取物为0.0055、0.0937、0.0013和0.0003;乙醇提取物为0.0876、0.0703、0.0183和0.0071;水提取物为0.0915、0.0312、0.0006和0.0006。氯仿、乙醇和水提取物的50%抑制浓度(IC50)分别确定为0.132mg/ml、0.288mg/ml和4.06mg/ml。

结论

利用SARS-CoV2刺突(S1)和ACE2蛋白进行的分析证明,NS种子提取物具有抑制S-ACE2相互作用的潜力,这值得进一步研究,可能会导致发现针对SARS-CoV2感染的潜在药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c486/11625226/fb8b0c522efd/gr4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c486/11625226/678c5dc3b6b2/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c486/11625226/dd3f6b1c6529/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c486/11625226/cb5af905e0df/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c486/11625226/fb8b0c522efd/gr4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c486/11625226/678c5dc3b6b2/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c486/11625226/dd3f6b1c6529/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c486/11625226/cb5af905e0df/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c486/11625226/fb8b0c522efd/gr4.jpg

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