期刊
NATURAL PRODUCT RESEARCH
卷 -, 期 -, 页码 -出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/14786419.2022.2138870
关键词
COVID-19; colchicine; magnolol; hybrid; 3-chymotrypsin-like protease; neutrophil elastase
资金
- Shenzhen Science and Technology Innovation Commission [JSGG20210901145539016, JCYJ20190812171005713, JCYJ20210324121611032, JCYJ20180227175929767, ZDSYS20190902093401689]
- Shenzhen Baoan Chinese Medicine Development Foundation [2020KJCX-KTYJ-215]
- Shenzhen excellent scientific and technological innovation talents training project-PhD Initiation Program [RCBS20210706092212002]
- GuangDong Basic and Applied Basic Research Foundation [2020A1515011427, 2022A1515011777, 2021A1515012474]
- Guangdong TCM Strong Provincial science and technology special key project [20215002]
- National Natural Science Foundation of China [81804145]
This study synthesized a series of novel colchicine-magnolol hybrids and found that they exhibited inhibitory effects on both the coronavirus 3CL(pro) and neutrophil elastase, which colchicine and magnolol alone did not possess.
Coronavirus disease 2019 (COVID-19), caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2 or 2019-nCoV), is a life-threatening infectious condition. Acute lung injury is a common complication in patients with COVID-19. 3-chymotrypsin-like protease (3CL(pro)) of 2019-nCoV and neutrophil elastase are critical targets of COVID-19 and acute lung injury, respectively. Colchicine and magnolol are reported to exert inhibitory effects on inflammatory response, the severe comorbidity in both COVID-19 and acute lung injury. We thus designed and synthesized a series of novel colchicine-magnolol hybrids based on a two-step synthetic sequence. It was found that these novel hybrids provided unexpected inhibition on 3CL(pro) and neutrophil elastase, a bioactivity that colchicine and magnolol did not possess. These findings not only provide perquisites for further in vitro and in vivo investigation to confirm the therapeutic potentiality of novel colchicine-magnolol hybrids, but also suggest that the concurrent inhibition of 3CL(pro) and neutrophil elastase may enable novel colchicine-magnolol hybrids as effective multi-target drug compounds.
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