Evaluation of Betulin Derivatives Against the COVID-19 Virus

University of Minnesota Background
Natural triterpenoids, including betulin, and derivatives thereof have been found to have anti-viral activity (Amiri et al. 2020, Hordyjewska et al. 2019, Santos da Silva et al. 2018, Kazakova et al. 2018, Wang et al 2015). Furthermore, a simple derivative, 2,28-diacetylbetulin, proved effective against respiratory syncytial virus (Santos da Silva et al. 2018). Betulin and triterpenoid derivatives have been in various clinical trials (Amiri et al. 2020) but bioavailability can be an issue. However, multiple solutions to this bioavailability problem have been forthcoming (Grymel et al. 2019, Ali-Seyed et al. 2016). In addition, triterpenoid derivatives appear to be nontoxic (Ali-Seyed et al. 2016).
Technology Overview
The University’s hypothesis is that one or more triterpenoid derivatives will be effective against the COVID-19 virus, based upon this literature background. NRRI has an existing library of over 1,100 betulin derivatives and a staff of chemists who have synthesized many of these derivatives. The University of Minnesota propose working with collaborators who can evaluate the effectiveness of selected members of the NRRI library. Once lead compounds are identified, further analogs can be synthesized for testing. The goal will be to find a triterpenoid analog that is highly effective against COVID-19 proliferation, is non-toxic, and can be delivered with reasonable bioavailability. While use of betulin derivatives as anti-viral agents is not novel, the use of these agents against the specific COVID-19 virus is novel.
The University will provide selected compounds from the University of Minnesota’s library to laboratories who are capable of testing these compounds for anti-COVID-19 activity. Once lead compounds are identified, the University is capable of synthesizing additional analog for optimization.
Further Details:

Amiri, S.; et al. Biotechnology Advances 2020, 38.
Grymel, M. et al. , Journal of Natural Products 2019, 82 (6), 1719-1730.
Hordyjewska, A. et al. Phytochemistry Reviews 2019, 18 (3), 929-951.
Kazakova, O. B. et al. Russ. J. Bioorg. Chem. 2018, 44 (6), 740-744.
Santos da Silva, G. N et al. Archiv der Pharmazie (Weinheim, Germany) 2018, 351 (8), n/a.
Ali-Seyed, M. et al. Chemical biology & drug design 2016, 87 (4), 517-36.
Wang, D et al. Acta Pharm Sin B 2015, 5 (6), 493-9.

Stage of Development
The University of Minnesota have compounds ready for screening against the COVID-19 virus
Opportunity
The University of Minnesota will provide selected compounds from their library to laboratories who are capable of testing these compounds for anti-COVID-19 activity. Once lead compounds are identified, they are capable of synthesizing additional analog for optimization.

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