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2000

Brazilian Siparuna Species as a Source of Antiviral Agents

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Influenza is an acute viral infection of the respiratory tract caused by the Alphainfluenzavirus whose subtypes were responsible for historical pandemics. Recently, the coronavirus SARS-CoV-2 has also affected the world, causing acute respiratory syndrome, thus rendering the search for anti-influenza and anti-SARS-CoV-2 compounds an urgent task. Plants of the genus Siparuna are used in Brazilian folk medicine for treating colds, fever, headaches, and rheumatic pain as well as gastrointestinal disorders. S. apiosyce ("Limão Bravo") is mentioned in the first Brazilian Pharmacopeia due to its importance as an ingredient in syrup and cough drops. Alkaloids, methylated and glycosylated flavonoids stand out as secondary metabolites described for these species, being also well described in the literature for their antiviral activity. During our investigation of Brazilian plants active against viral infections, the anti-influenza activity of five Amazonian Siparuna (S. cristata, S. decipiens, S. glycycarpa, S. reginae and S. sarmentosa) were investigated, showing the n-butanol extracts of S. glycycarpa and S. sarmentosa as the most active. Dereplication of these extracts pointed alkaloids, O- and C-glycosylated flavonoids as well as dihydrochalcones and a procyanidin dimer as potential active metabolites. On the other hand, the dichloromethane extract from S. cristata containing methylated flavonoids was able to inhibit the in vitro replication of SARS-CoV-2, where it was shown that retusin and kumatakenin presented a higher selectivity index than lopinavir/ritonavir and chloroquine controls. Further in-silico studies showed the potential interaction between these flavonoids and the virus proteases 3CLpro and PLpro. Here we highlight the possible application of compounds isolated from Siparuna species as antiviral agents.

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