Exploring Novel Vitamin K Derivatives with Anti-SARS-CoV-2 Activity

[23.11.07]

Almost four years have passed since the global pandemic of COVID-19 caused by SARS-CoV-2 infection. In the meantime, mRNA-derived vaccines have been developed, and several antiviral drugs targeting viral proteins have also been developed and clinically used. However, COVID-19 is still a serious problem because of various sequelae that can persist for several months or more after healing. Among them, neurological damage has been suggested as the cause of CNS disorder due to increased susceptibility to thrombosis and as non-transient taste and smell disorders. Therefore, it is extremely important to identify and develop drugs that have antiviral effects and also prevent these sequelae.

Professor Yoshitomo Suhara's research group at the Department of Bioscience and Engineering, College of Systems Engineering and Science, Shibaura Institute of Technology, has discovered "Vitamin K derivatives" as novel compounds that activate neural stem cells to differentiate into neurons. In collaboration with Specially Appointed Professor Mika Okamoto at the Division of Infection Control Research, Center for Advanced Science Research and Promotion, Kagoshima University, they found that some of the vitamin K derivatives selectively inhibited SARS-CoV-2 replication in cell culture. Furthermore, their mechanism of action was investigated and found that the compounds inhibited the activity of SARS-CoV-2 RNA polymerase.

Shibaura Institute of Technology and Kagoshima University have filed an international patent application for these research results and submitted them to ACS Omega (Impact Factor: 4.1, CiteScore: 5.9), a scientific journal of the American Chemical Society. The article has recently been accepted for publication. Since the anti-SARS-CoV-2 activity of the vitamin K derivatives identified in this study is not sufficient for clinical development as an anti-COVID-19 therapeutic agent, we continue to synthesize various new vitamin K derivatives at the Shibaura Institute of Technology and to evaluate their anti-SARS-CoV-2 activity at Kagoshima University. The collaborative research is currently in progress.

Exploring compounds with combined therapeutic effects against SARS-CoV-2 infection and cerebral infarction thrombosis, one of the sequelae.