SARS-CoV-2 PL-Pro (Nsp3) Inhibitors. #nature#plantbased
Salvia miltiorrhiza.
PLpro has an implication in viral invasion by shutting down the viral-induced host innate immune response. Dihydrotanshinone I appears to be the strongest inhibitor amongst the tanshinone ..1/n
derivatives. It is a natural compound isolated from lipophilic fraction of Salvia miltiorrhiza, which has a long history in traditional Chinese medicine. Several derivatives of tanshinones were previously reported to be inhibitors for SARS-CoV-1 PLpro and to a lesser extent ..2/n
in 3CLpro. Dihydrotanshinone I is the best inhibitor of SARS-CoV-2 PLpro and did not inhibit 3CLpro. 3/n portlandpress.com/biochemj/artic…
Overview of Salvia miltiorrhiza as a Potential Therapeutic Agent for Various Diseases: An Update on Efficacy and Mechanisms of Action 4/n mdpi.com/2076-3921/9/9/…
Challenges : enzyme inhibition was only achieved in the absence of physiologically relevant reducing agents, and the reported antiviral effect in cells infected with SARS-CoV-2 could not be reproduced and was therefore suspected to be an indirect consequence of cell death.
Additional challenges in assessing 3CLpro inhibition potency in infected cells arose from the role of host proteases in virus entry. SARSCoV-2 uses human ACE2 as its entry receptor and human proteases as entry activators including cell surface transmembrane protease/serine
New Pfizer antiviral and ivermectin, a pharmacodynamic analysis. Paxlovid (PF-07321332), C₂₃H₃₂F₃N₅O₄
Paxlovid is designed to block the activity of the SARS-CoV-2-3CL protease, an enzyme that the coronavirus needs to replicate. Co-administration with a low dose of
ritonavir helps slow the metabolism, or breakdown, of Paxlovid in order for it to remain active in the body for longer periods of time at higher concentrations to help combat the virus. Paxlovid inhibits viral replication at a stage known as proteolysis, which occurs before
SC2 MPro inhibitors alternatives, plant flavonoids. 1/n #MPro#SARSCoV2#inhibitor
Kaempferol, Quercetin, and Rutin
were able to bind at the substrate binding pocket of 3CLpro with high affinity and interact with the active site residues .. chemrxiv.org/engage/chemrxi…
such as His41 and Cys145 through hydrogen bonding and hydrophobic interactions. In fact, the binding affinity of Rutin was much higher than Chloroquine (1000 times) and Hydroxychloroquine (100 times) and was comparable to that of the reference drug Remdesivir. 2/n
The results suggest that natural compounds such as flavonoids have the potential to be developed as novel inhibitors of SARS-CoV-2. 3/n
Anti-Inflammatory and anti-vascular leakage effects by combination of Centella asiatica and Vitis vinifera L. (Grapevine) leaf extracts. #antiinflammatory qualities #anti#vascular#leakage effect