Researchers from the Higher Council for Scientific Research (CSIC in Spanish) have identified and characterized a new class of antivirals against SARS-CoV-2 that act by blocking the entry of the virus into the host cell through its interaction with the ‘spike’ protein (S protein).

The work has been carried out by researchers from the Higher Council for Scientific Research at the Institute of Medicinal Chemistry (IQM-CSIC), the Institute of Integrative Systems Biology (I2SysBio-CSIC-UV) and the Institute of Biomedicine of Valencia (IBV -CSIC), members of the Interdisciplinary Thematic Platform (PTI) Global Health, and has been the result of the interdisciplinary collaboration of the authors within the framework of the ‘PTI+ Global Health’, which has been published in the Journal of Medicinal Chemistry.

In the initial stages of the replication cycle of SARS-CoV-2, the causative agent of Covid-19, interaction occurs between the viral S protein and the primary receptor of the host cell, angiotensin-converting enzyme 2 (ACE2), followed by internalization of the virus.

According to the CSIC, these initial stages of the infection are especially attractive in the search for antivirals, since compounds that act at this level could be used both therapeutically and prophylaxis.

Previous studies carried out by IQM-CSIC researchers indicated that tryptophan derivatives (an essential amino acid) are good candidates for use as antivirals, since they have the ability to inhibit the entry of different viruses and have low cytotoxicity.

In this study, screening tests have been carried out from a collection of different multivalent derivatives of tryptophan, with possible antiviral activity. By using VSV (vesicular stomatitis virus) pseudoparticles, capable of expressing the S protein of SARS-CoV-2, the interaction of the compounds in the collection with the viral ‘spike’ protein was evaluated.

After this screening process, the scientists have identified a hit compound, a molecule with the sought-after pharmacological activity, which has been studied and optimized, obtaining a thiophenyltryptophan C-2 trimer, active and useful for more advanced clinical studies.

Among the studies to which this compound has been subjected, the validation of the antiviral activity against genuine SARS-CoV-2 is included. In addition, other analyzes with Thermofluor and microscale thermophoresis demonstrate the interaction of these compounds with the RBD receptor binding domain of the S protein, preventing the interaction with ACE2.

Finally, the researchers used high-resolution cryoelectronic microscopy to characterize the structure of the S protein in the presence and absence of the hit compound tested, which has contributed to clarifying the mechanism of action of this new class of antiviral compounds.

Source: dpa

(Reference image source: Unsplash, in collaboration with Getty Images)

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The company Bioinicia and the Higher Council for Scientific Research (CSIC) launched the Bio Hygienic mask with EPI-type fit. It is the first compostable nanofiber mask in the world, which has a filtration superior to 98 % against aerosols and compost in twenty-two days.

According to the information outlined, it is the “most sustainable option to avoid the accumulation of masks in the environment.” It also indicates that the most respectful aspect “is to produce them using raw materials derived from biomass or waste and their subsequent organic recycling in the form of industrial composting, so that the carbon returns to the earth.”

As explained by José María Lagarón, CSIC researcher and leader of the group of researchers who, together with Bioinicia, creators of the mask, at this time almost all masks are made of a plastic derived from petroleum that does not biodegrade.

The new Proveil EPI mask is made with natural raw material and with 30% less plastics in its constitution. Its components will become water and CO2 over time, preventing millions of tons of plastics from reaching the oceans.

Respecting the environment

The use of the mask, as protection from Covid-19, has become an imminent risk for the environment because the mere fact of throwing them in the toilet or on the ground, and not doing it in the recommended places is a serious problem, since it causes the same damage as throwing wipes and plastics.

It takes many years to disintegrate thus becoming a pollutant of the environment. And also, its fragments will form microplastics that will be consumed by living organisms.

M. Rodríguez

With information from international agencies and news media

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