Action of 50 synthetic compounds will be tested against novel coronavirus

In a project supported by FAPESP, researchers at São Paulo State University (UNESP) will assess the potential of peptides and other bioactive molecules to inhibit the infection of cultured cells.

By José Tadeu Arantes  |  Agência FAPESP – In Brazil, researchers at São Paulo State University’s Araraquara Institute of Chemistry (IQA-UNESP), in collaboration with colleagues at the university’s Institute of Biosciences, Letters and Exact Sciences (IBILCE-UNESP), are testing a library of dozens of bioactive peptides to find out if they are active against the novel coronavirus SARS-CoV-2.

The study is supported by FAPESP and led by Eduardo Maffud Cilli, Director of IQA-UNESP.

“The aim is to identify and investigate the potential of peptides and bioconjugates [two bioactive molecules coupled together] to inhibit infection by SARS-CoV-2. We’ll evaluate the toxicity and antiviral activity of these molecules in a series of trials that will provide information on their inhibitory potential in the various stages of the virus’s lifecycle, such as cell entry and multiplication in cytoplasm,” Paulo Ricardo da Silva Sanches, a researcher on the IQA-UNESP team, told Agência FAPESP. “Trials have begun with human lung cells and monkey kidney cells. The toxicity of the compounds has been shown to be low. The next step is to analyze their action in cells infected by SARS-CoV-2.”

One of the compounds with significant potential, Sanches explained, is the bioconjugate gallic acid-hecate (GA-hecate), which displays low toxicity in healthy cells and has been shown to act powerfully against Zika virus (ZIKV) and hepatitis C virus (HCV) as well as to attack bacteria, fungi and cancer cells. The properties of this compound, synthesized at IQA-UNESP, were previously reported in a paper published in Scientific Reports (read more at: agencia.fapesp.br/29470).

“GA-hecate is a bioconjugate synthesized from the natural compound gallic acid and the peptide hecate, Sanches said. “One of the targets proposed for the bioconjugate is the viral envelope [the layer of lipids that encloses the genetic material of some viruses]. Like ZIKV and HCV, SARS-CoV-2 also has this lipidic envelope. It could also be a target for GA-hecate.”

“Screening of commercial antiinflammatory drugs in conjunction with antiviral compounds will point to a possible combined treatment with the aim of reducing viral load and controlling the inflammation frequently seen in severe cases of the disease,” Cilli said.

In addition to Cilli and Sanches, the project team includes Paula Rahal, a professor at IBILCE-UNESP, and Cintia Bittar and Marília Calmon, researchers at the same institution.