通过联合方法验证白桦脂酸作为 SARS-CoV-2 主要蛋白酶潜在抑制剂的有效性。

IF 2.1 4区医学 Q4 BIOCHEMISTRY & MOLECULAR BIOLOGY Steroids Pub Date : 2024-10-17 DOI:10.1016/j.steroids.2024.109522

Jiankai Ye , Tao Xu , Rui Zhang, Xiaoping Liu, Chao Zhang, Yunyu Chen

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引用次数: 0

摘要

早先的一项研究报告称白桦脂酸是严重急性呼吸系统综合征冠状病毒 2（SARS-CoV-2）主蛋白酶（Mpro）的抑制剂，与此不同的是，我们通过荧光共振能量转移（FRET）测定、荧光偏振（FP）测定和蛋白酶生物传感器裂解测定等综合方法证明白桦脂酸不是潜在的 Mpro 抑制剂。我们的研究结果表明，在测定缓冲液中添加去垢剂对于评估天然产品作为 Mpro 抑制剂至关重要。在开发抗病毒药物时，有必要通过综合方法对 Mpro 抑制剂进行全面测试。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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Invalidating betulinic acid as a potential inhibitor against the main protease of SARS-CoV-2 via combined approaches

In contrast to an earlier study reporting that betulinic acid is an inhibitor of the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (Mpro), we demonstrated that beutilinic acid is not a potential Mpro inhibitor via combined approaches, including the fluorescence resonance energy transfer (FRET) assay, the fluorescence polarization (FP) assay, and the protease biosensor cleavage assay. Our results suggest that the addition of detergent to the assay buffers is essential for evaluating natural products as Mpro inhibitors. It is necessary to conduct comprehensive testing of Mpro inhibition via combined approaches for antiviral development.

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来源期刊

Steroids 医学-内分泌学与代谢

CiteScore

5.10

自引率

3.70%

发文量

120

审稿时长

73 days

期刊介绍： STEROIDS is an international research journal devoted to studies on all chemical and biological aspects of steroidal moieties. The journal focuses on both experimental and theoretical studies on the biology, chemistry, biosynthesis, metabolism, molecular biology, physiology and pharmacology of steroids and other molecules that target or regulate steroid receptors. Manuscripts presenting clinical research related to steroids, steroid drug development, comparative endocrinology of steroid hormones, investigations on the mechanism of steroid action and steroid chemistry are all appropriate for submission for peer review. STEROIDS publishes both original research and timely reviews. For details concerning the preparation of manuscripts see Instructions to Authors, which is published in each issue of the journal.