2. Academic Validation
  3. Antiviral Activity of Cannabidiolic Acid and Its Methyl Ester against SARS-CoV-2

Antiviral Activity of Cannabidiolic Acid and Its Methyl Ester against SARS-CoV-2

  • J Nat Prod. 2023 Jul 28;86(7):1698-1707. doi: 10.1021/acs.jnatprod.3c00111.
Martina Tamburello 1,  Stefano Salamone 2 3,  Lisa Anceschi 4 5,  Paolo Governa 6,  Virginia Brighenti 4,  Alice Morellini 1,  Giada Rossini 7,  Fabrizio Manetti 6,  Giorgio Gallinella 8,  Federica Pollastro 2 3,  Federica Pellati 4
Affiliations

Affiliations

  • 1 Section of Microbiology, Department of Medical and Surgical Sciences (DIMEC), Alma Mater Studiorum University of Bologna, Via Massarenti 9, 40138 Bologna, Italy.
  • 2 Department of Pharmaceutical Sciences, University of Eastern Piedmont, Largo Donegani 2, 28100 Novara, Italy.
  • 3 PlantaChem srls, Via A. Canobio 4/6, 28100 Novara, Italy.
  • 4 Department of Life Sciences, University of Modena and Reggio Emilia, Via Giuseppe Campi 103, 41125 Modena, Italy.
  • 5 Clinical and Experimental Medicine PhD Program, University of Modena and Reggio, Via Giuseppe Campi 287, 41125 Modena, Italy.
  • 6 Department of Biotechnology, Chemistry and Pharmacy, University of Siena, Via Aldo Moro 2, 53100 Siena, Italy.
  • 7 Microbiology Unit, IRCCS Azienda Ospedaliero-Universitaria di Bologna, Via Massarenti 9, 40138 Bologna, Italy.
  • 8 Department of Pharmacy and Biotechnology, Alma Mater Studiorum University of Bologna, Via Massarenti 9, 40138 Bologna, Italy.
PMID: 37402317 DOI: 10.1021/acs.jnatprod.3c00111
Abstract

In the present study, the Antiviral activity of cannabinoids isolated from Cannabis sativa L. was assessed in vitro against a panel of SARS-CoV-2 variants, indicating cannabidiolic acid (CBDA) was the most active. To overcome the instability issue of CBDA, its methyl ester was synthesized and tested for the first time for its Antiviral activity. CBDA methyl ester showed a neutralizing effect on all the SARS-CoV-2 variants tested with greater activity than the parent compound. Its stability in vitro was confirmed by ultra-high-performance liquid chromatography (UHPLC) analysis coupled with high-resolution mass spectrometry (HRMS). In addition, the capacity of both CBDA and its derivative to interact with the virus spike protein was assessed in silico. These results showed that CBDA methyl ester can be considered as a lead compound to be further developed as a new effective drug against COVID-19 Infection.

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