• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利：CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法，用中文像聊天一样搜索，搜遍4000万医学文献。AI智能推荐，让科研检索更轻松。

立即免费搜索

文件翻译

保留排版，准确专业，支持PDF/Word/PPT等文件格式，支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述，25分钟生成高质量综述，智能提取关键信息，辅助科研写作。

立即免费体验

二萜类化合物从Steud.的根部靶向严重急性呼吸综合征冠状病毒2（SARS-CoV-2）的RNA依赖性RNA聚合酶（RdRp）。

Diterpenoids target SARS-CoV-2 RdRp from the roots of Steud.

作者信息

Ruan Ting, Xiang Zheng-Rui, Zhang Yun-Wu, Fan Shi-Rui, Ren Juan, Zhao Qian, Sun Xiao-Long, Wu Shi-Li, Xu Li-Li, Qiao Miao, Jing Chen-Xu, Hao Xiao-Jiang, Chen Duo-Zhi

机构信息

State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, China.

Yunnan Characteristic Plant Extraction Laboratory, Kunming, China.

出版信息

Front Plant Sci. 2024 Jul 25;15:1425759. doi: 10.3389/fpls.2024.1425759. eCollection 2024.

DOI:10.3389/fpls.2024.1425759
PMID:39119497
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11306077/
Abstract

INTRODUCTION

Currently, the development of new antiviral drugs against COVID-19 remains of significant importance. In traditional Chinese medicine, the herb Steud is often used for antiviral treatment, yet its therapeutic effect against the COVID-19 has been scarcely studied. Therefore, this study focuses on the roots of Steud, exploring its chemical composition, antiviral activity against COVID-19, and the underlying basis of its antiviral activity.

METHODS

Isolation and purification of phytochemicals from Steud. The elucidation of their configurations was achieved through a comprehensive suite of 1D and 2D NMR spectroscopic analyses as well as X-ray diffraction. Performed cytopathic effect assays of SARS-CoV-2 using Vero E6 cells. Used molecular docking to screen for small molecule ligands with binding to SARS-CoV-2 RdRp. Microscale thermophoresis (MST) was used to determine the dissociation constant Kd.

RESULTS

Ultimately, nine new ent-atisane-type diterpenoid compounds were isolated from Steud, named Eupfisenoids A-I (compounds 1-9). The compound of 1 was established as a C-19-degraded ent-atisane-type diterpenoid. During the evaluation of these compounds for their antiviral activity against COVID-19, compound 1 exhibited significant antiviral activity. Furthermore, with the aid of computer virtual screening and microscale thermophoresis (MST) technology, it was found that this compound could directly bind to the RNA-dependent RNA polymerase (RdRp, NSP12) of the COVID-19, a key enzyme in virus replication. This suggests that the compound inhibits virus replication by targeting RdRp.

DISCUSSION

Through this research, not only has our understanding of the antiviral components and material basis of Steud been enriched, but also the potential of atisane-type diterpenoid compounds as antiviral agents against COVID-19 has been discovered. The findings mentioned above will provide valuable insights for the development of drugs against COVID-19.

摘要

引言

目前，开发针对新型冠状病毒肺炎（COVID-19）的新型抗病毒药物仍然至关重要。在传统中药中，“Steud”这种草药常被用于抗病毒治疗，但其对COVID-19的治疗效果鲜有研究。因此，本研究聚焦于“Steud”的根部，探索其化学成分、对COVID-19的抗病毒活性及其抗病毒活性的潜在基础。

方法

从“Steud”中分离和纯化植物化学物质。通过一系列一维和二维核磁共振光谱分析以及X射线衍射确定其构型。使用Vero E6细胞进行严重急性呼吸综合征冠状病毒2（SARS-CoV-2）的细胞病变效应测定。利用分子对接筛选与SARS-CoV-2 RNA依赖性RNA聚合酶（RdRp）结合的小分子配体。使用微量热泳动（MST）测定解离常数Kd。

结果

最终，从“Steud”中分离出9种新的对映-乌苏烷型二萜化合物，命名为优菲斯烷类化合物A-I（化合物1-9）。化合物1被确定为一种C-19降解的对映-乌苏烷型二萜。在评估这些化合物对COVID-19的抗病毒活性时，化合物1表现出显著的抗病毒活性。此外，借助计算机虚拟筛选和微量热泳动（MST）技术，发现该化合物可直接与COVID-19的RNA依赖性RNA聚合酶（RdRp，NSP12）结合，这是病毒复制中的关键酶。这表明该化合物通过靶向RdRp抑制病毒复制。

讨论

通过本研究，不仅丰富了我们对“Steud”的抗病毒成分和物质基础的认识，还发现了乌苏烷型二萜化合物作为抗COVID-19抗病毒药物的潜力。上述发现将为开发抗COVID-19药物提供有价值的见解。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cdfe/11306077/af97726b947e/fpls-15-1425759-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cdfe/11306077/6c9a62c3e565/fpls-15-1425759-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cdfe/11306077/3e751a4bc65a/fpls-15-1425759-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cdfe/11306077/bff695e97630/fpls-15-1425759-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cdfe/11306077/a4a67f52387a/fpls-15-1425759-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cdfe/11306077/8cce5787d7c4/fpls-15-1425759-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cdfe/11306077/af97726b947e/fpls-15-1425759-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cdfe/11306077/6c9a62c3e565/fpls-15-1425759-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cdfe/11306077/3e751a4bc65a/fpls-15-1425759-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cdfe/11306077/bff695e97630/fpls-15-1425759-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cdfe/11306077/a4a67f52387a/fpls-15-1425759-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cdfe/11306077/8cce5787d7c4/fpls-15-1425759-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cdfe/11306077/af97726b947e/fpls-15-1425759-g006.jpg

相似文献

1
Diterpenoids target SARS-CoV-2 RdRp from the roots of Steud.二萜类化合物从Steud.的根部靶向严重急性呼吸综合征冠状病毒2（SARS-CoV-2）的RNA依赖性RNA聚合酶（RdRp）。
Front Plant Sci. 2024 Jul 25;15:1425759. doi: 10.3389/fpls.2024.1425759. eCollection 2024.
2
Structurally diverse diterpenoids from the roots of Euphorbia fischeriana Steud.瑞香狼毒根中的结构多样的二萜类化合物
Fitoterapia. 2022 Oct;162:105296. doi: 10.1016/j.fitote.2022.105296. Epub 2022 Sep 8.
3
Antiproliferative diterpenoids and acetophenone glycoside from the roots of Euphorbia fischeriana.瑞香狼毒根中的具有抗增殖作用的二萜类化合物和苯乙酮糖苷。
Phytochemistry. 2020 Sep;177:112437. doi: 10.1016/j.phytochem.2020.112437. Epub 2020 Jun 16.
4
Chemical Composition, Anti-Breast Cancer Activity and Extraction Techniques of Ent-Abietane Diterpenoids from Steud.葇荑花序式对叶兰中 Ent-Abietane 二萜的化学成分、抗乳腺癌活性及提取技术
Molecules. 2022 Jul 3;27(13):4282. doi: 10.3390/molecules27134282.
5
Existing knowledge on Euphorbia fischeriana Steud. (Euphorbiaceae): Traditional uses, clinical applications, phytochemistry, pharmacology and toxicology.关于大飞扬草（大戟科）的现有知识：传统用途、临床应用、植物化学、药理学和毒理学。
J Ethnopharmacol. 2021 Jul 15;275:114095. doi: 10.1016/j.jep.2021.114095. Epub 2021 Apr 2.
6
Structural Diversity and Biological Activities of Diterpenoids Derived from Steud.从 Steud. 中衍生的二萜类化合物的结构多样性和生物活性
Molecules. 2018 Apr 18;23(4):935. doi: 10.3390/molecules23040935.
7
Anti-Cancer Activities of Diterpenoids Derived from Euphorbia fischeriana Steud.瑞香狼毒中二萜的抗癌活性研究
Molecules. 2018 Feb 11;23(2):387. doi: 10.3390/molecules23020387.
8
Chemical profiling of Euphorbia fischeriana Steud. by UHPLC-Q/TOF-MS.利用 UHPLC-Q/TOF-MS 对大飞扬草进行化学特征分析。
J Pharm Biomed Anal. 2018 Mar 20;151:126-132. doi: 10.1016/j.jpba.2017.12.051. Epub 2017 Dec 26.
9
Two new ent-atisanes from the root of Euphorbia fischeriana Steud.从狼毒大戟根中分离得到的两种新的对映-贝壳杉烷型二萜
Nat Prod Res. 2016;30(2):144-9. doi: 10.1080/14786419.2015.1045904. Epub 2015 Jul 3.
10
Bisfischoids A and B, dimeric ent-abietane-type diterpenoids with anti-inflammatory potential from Euphorbia fischeriana Steud.双贝壳杉烷 A 和 B，来自大戟属植物 Euphorbia fischeriana Steud 的具有潜在抗炎作用的二聚型贝壳杉烷型二萜。
Bioorg Chem. 2021 Nov;116:105356. doi: 10.1016/j.bioorg.2021.105356. Epub 2021 Sep 15.

引用本文的文献

1
3CL of SARS-CoV-2 as a new target for bufadienolides: in silico and in vitro study.严重急性呼吸综合征冠状病毒2型的3CL作为蟾蜍二烯内酯的新靶点：计算机模拟和体外研究
J Comput Aided Mol Des. 2025 Jul 5;39(1):41. doi: 10.1007/s10822-025-00623-2.

本文引用的文献

1
Ent-atisane diterpenoids from Euphorbia wallichii and their anti-influenza A virus activity.来自大戟科大戟的对映贝壳杉烷二萜类化合物及其抗甲型流感病毒活性。
Phytochemistry. 2024 Apr;220:113996. doi: 10.1016/j.phytochem.2024.113996. Epub 2024 Feb 3.
2
Development of a robust UPLC-MS/MS method for the quantification of riluzole in human plasma and its application in pharmacokinetics.开发一种用于定量测定人血浆中利鲁唑的稳健超高效液相色谱-串联质谱法及其在药代动力学中的应用。
Front Pharmacol. 2023 Aug 9;14:1227354. doi: 10.3389/fphar.2023.1227354. eCollection 2023.
3
Orally administered BZL-sRNA-20 oligonucleotide targeting TLR4 effectively ameliorates acute lung injury in mice.
口服 BZL-sRNA-20 寡核苷酸靶向 TLR4 可有效改善小鼠急性肺损伤。
Sci China Life Sci. 2023 Jul;66(7):1589-1599. doi: 10.1007/s11427-022-2219-0. Epub 2023 Feb 13.
4
Gossypol Broadly Inhibits Coronaviruses by Targeting RNA-Dependent RNA Polymerases.棉酚通过靶向 RNA 依赖性 RNA 聚合酶广泛抑制冠状病毒。
Adv Sci (Weinh). 2022 Dec;9(35):e2203499. doi: 10.1002/advs.202203499. Epub 2022 Oct 20.
5
Integrated network pharmacology analysis, molecular docking, LC-MS analysis and bioassays revealed the potential active ingredients and underlying mechanism of for COVID-19.综合网络药理学分析、分子对接、液相色谱-质谱联用分析和生物测定揭示了[药物名称]对2019冠状病毒病的潜在活性成分和潜在作用机制。 （原文中“for COVID-19”前缺少具体药物名称，翻译时补充为“[药物名称]对2019冠状病毒病” ）
Front Plant Sci. 2022 Sep 15;13:988655. doi: 10.3389/fpls.2022.988655. eCollection 2022.
6
Quercetin and luteolin are single-digit micromolar inhibitors of the SARS-CoV-2 RNA-dependent RNA polymerase.槲皮素和木犀草素是 SARS-CoV-2 依赖 RNA 的 RNA 聚合酶的个位数微摩尔抑制剂。
Sci Rep. 2022 Jun 22;12(1):10571. doi: 10.1038/s41598-022-14664-2.
7
Natural Polyphenols, 1,2,3,4,6-O-Pentagalloyglucose and Proanthocyanidins, as Broad-Spectrum Anticoronaviral Inhibitors Targeting Mpro and RdRp of SARS-CoV-2.天然多酚、1,2,3,4,6 - 五没食子酰葡萄糖和原花青素作为靶向SARS-CoV-2的Mpro和RdRp的广谱抗冠状病毒抑制剂。
Biomedicines. 2022 May 18;10(5):1170. doi: 10.3390/biomedicines10051170.
8
Duration of effectiveness of vaccines against SARS-CoV-2 infection and COVID-19 disease: results of a systematic review and meta-regression.疫苗预防严重急性呼吸综合征冠状病毒 2 型（SARS-CoV-2）感染和 COVID-19 疾病有效性的持续时间：系统评价和荟萃回归的结果。
Lancet. 2022 Mar 5;399(10328):924-944. doi: 10.1016/S0140-6736(22)00152-0. Epub 2022 Feb 23.
9
Antibodies elicited by SARS-CoV-2 infection or mRNA vaccines have reduced neutralizing activity against Beta and Omicron pseudoviruses.由 SARS-CoV-2 感染或 mRNA 疫苗引发的抗体对 Beta 和奥密克戎假病毒的中和活性降低。
Sci Transl Med. 2022 Mar 2;14(634):eabn7842. doi: 10.1126/scitranslmed.abn7842.
10
Existing knowledge on Euphorbia fischeriana Steud. (Euphorbiaceae): Traditional uses, clinical applications, phytochemistry, pharmacology and toxicology.关于大飞扬草（大戟科）的现有知识：传统用途、临床应用、植物化学、药理学和毒理学。
J Ethnopharmacol. 2021 Jul 15;275:114095. doi: 10.1016/j.jep.2021.114095. Epub 2021 Apr 2.