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抗冠状病毒的抗菌二萜评估:新型土木香醇类似物的应用。

Anticoronavirus Evaluation of Antimicrobial Diterpenoids: Application of New Ferruginol Analogues.

机构信息

Université de Lorraine, CNRS, L2CM, F-54000 Nancy, France.

Laboratoire de Virologie, CHRU de Nancy Brabois, 54500 Vandoeuvre-lès-Nancy, France.

出版信息

Viruses. 2023 Jun 9;15(6):1342. doi: 10.3390/v15061342.

Abstract

The abietane diterpene (+)-ferruginol (), like other natural and semisynthetic abietanes, is distinguished for its interesting pharmacological properties such as antimicrobial activity, including antiviral. In this study, selected C18-functionalized semisynthetic abietanes prepared from the commercially available (+)-dehydroabietylamine or methyl dehydroabietate were tested in vitro against human coronavirus 229E (HCoV-229E). As a result, a new ferruginol analogue caused a relevant reduction in virus titer as well as the inhibition of a cytopathic effect. A toxicity prediction based on in silico analysis was also performed as well as an estimation of bioavailability. This work demonstrates the antimicrobial and specifically antiviral activity of two tested compounds, making these molecules interesting for the development of new antivirals.

摘要

松香二萜(+)-去铁杉醇()与其他天然和半合成松香烷一样,以其有趣的药理特性而著称,如抗菌活性,包括抗病毒活性。在这项研究中,从市售的(+)-脱氢枞胺或甲基脱氢枞酸制备的选定的 C18 功能化半合成松香烷在体外针对人冠状病毒 229E(HCoV-229E)进行了测试。结果,一种新型的去铁杉醇类似物导致病毒滴度显著降低,并抑制细胞病变效应。还进行了基于计算机分析的毒性预测以及生物利用度的估算。这项工作证明了两种测试化合物的抗菌和特定的抗病毒活性,使这些分子成为开发新型抗病毒药物的有前途的候选物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/41be/10301393/c0a048bb26c0/viruses-15-01342-g001.jpg

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