2. Academic Validation
  3. An ascidian Polycarpa aurata-derived pan-inhibitor against coronaviruses targeting Mpro

An ascidian Polycarpa aurata-derived pan-inhibitor against coronaviruses targeting Mpro

  • Bioorg Med Chem Lett. 2024 May 1:103:129706. doi: 10.1016/j.bmcl.2024.129706.
Jing Zhang 1,  Lili Zhao 2,  Yuxin Bai 3,  Shanshan Li 1,  Meifang Zhang 1,  Bo Wei 1,  Xianyang Wang 4,  Yan Xue 5,  Li Li 6,  Guiliang Ma 7,  Yu Tang 8,  Xin Wang 9
Affiliations

Affiliations

  • 1 Key Laboratory of Marine Drugs of Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China; Center for Innovation Marine Drug Screening & Evaluation of Pilot National Laboratory for Marine Science and Technology (Qingdao), Qingdao 266237, China.
  • 2 Key Laboratory of Marine Drugs of Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China; Center for Innovation Marine Drug Screening & Evaluation of Pilot National Laboratory for Marine Science and Technology (Qingdao), Qingdao 266237, China; Marine Biomedical Research Institute of Qingdao, Qingdao 266003, China. Electronic address: zhaolili@ouc.edu.cn.
  • 3 Key Laboratory of Marine Drugs of Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China; Marine Biomedical Research Institute of Qingdao, Qingdao 266003, China.
  • 4 Key Laboratory of Marine Drugs of Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China.
  • 5 Department of Physiology, School of Basic Medicine, Qingdao University, Qingdao 266000, China.
  • 6 Key Laboratory of Marine Drugs of Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China; Center for Innovation Marine Drug Screening & Evaluation of Pilot National Laboratory for Marine Science and Technology (Qingdao), Qingdao 266237, China; Marine Biomedical Research Institute of Qingdao, Qingdao 266003, China.
  • 7 Department of General Surgery, Qingdao Municipal Hospital, No. 5, Donghaizhong Road, Qingdao 266071, China. Electronic address: mgl-8568097@163.com.
  • 8 Key Laboratory of Marine Drugs of Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China; Marine Biomedical Research Institute of Qingdao, Qingdao 266003, China. Electronic address: tangyu@ouc.edu.cn.
  • 9 Key Laboratory of Marine Drugs of Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China; Center for Innovation Marine Drug Screening & Evaluation of Pilot National Laboratory for Marine Science and Technology (Qingdao), Qingdao 266237, China; Marine Biomedical Research Institute of Qingdao, Qingdao 266003, China. Electronic address: wx8399@ouc.edu.cn.
PMID: 38508325 DOI: 10.1016/j.bmcl.2024.129706
Abstract

Coronaviruses (CoVs) are responsible for a wide range of illnesses in both Animals and human. The main Protease (Mpro) of CoVs is an attractive drug target, owing its critical and highly conserved role in viral replication. Here, we developed and refined an enzymatic technique to identify putative Mpro inhibitors from 189 marine chemicals and 46 terrestrial Natural Products. The IC50 values of Polycarpine (1a), a marine natural substance we studied and synthesized, are 30.0 ± 2.5 nM for SARS-CoV-2 Mpro and 0.12 ± 0.05 μM for PEDV Mpro. Our research further demonstrated that pretreatment with Polycarpine (1a) inhibited the betacoronavirus SARS-CoV-2 and alphacoronavirus PEDV multiplication in Vero-E6 cells. As a result, Polycarpine (1a), a pan-inhibitor of Mpro, will function as an effective and promising Antiviral option to combat CoVs Infection and as a foundation for further therapeutic research.

Keywords

Antiviral agents; M(pro); Marine natural products; Pan-inhibitors; SARS-CoV-2.

Figures
Products
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z