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
Kaempferol: an encouraging flavonoid for COVID-19.

file:///C:/Users/User/Downloads/33-Texto%20del%20art%C3%ADculo-53-1-10-20200817.pdf
Rutin A Potential Antiviral for Repurposing as a SARS-CoV-2 Main Protease (Mpro) Inhibitor
also called sophorin, rutoside, and quercetin-3-rutinoside, is a polyphenolic flavonoid, abundantly present in various dietary sources such as buckwheat, onions, oranges, lemons, grapes,
limes, berries, peaches, plums, apples, and tomatoes, as well as in drinks such as wine and black tea. Two of the benefits are ancillary therapeutic agent for snakebites and cognitive impairment prevention. 6/n
Rutin, along with other flavonoid glycosides present in the ethanolic extract of Ficus benjamina L. (weeping fig), exhibited activity against HSV-1 and HSV2. Rutin from plum (Prunus domestica L.) was suggested as a strong inhibitor of hepatitis C virus (HCV) entry by
7/n
inhibiting the early entry stage of the HCV lifecycle. Sulfated rutin was revealed in vitro to possess an antiviral effect against HIV-1 × 4 virus IIIB, and HIV-1 R5 isolates Ada-M and Ba-L strains by blocking viral entry and virus-cell fusion through interacting with
8/n
the HIV-1 envelope glycoprotein. 9/n
journals.sagepub.com/doi/full/10.11…
Quercetin (1) and 8-(p-tolylselenyl)quercetin (2d) block SC2 replication in infected cells at non-toxic concentrations, with an IC50 of 192 μM and 8 μM, respectively. Based on docking experiments driven by experimental evidence,a non-covalent mechanism for Mpro inhibition in 11/n
which a hydrogen bond between the selenium atom and Gln189 residue in the catalytic pocket could explain the higher Mpro activity of 2d and, as a result, its better antiviral profile. 12/end.
pubmed.ncbi.nlm.nih.gov/34208928/

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More from @mega_pindang71

9 Nov
Road to #Paxlovid #Pfizer #COVID19 new drug. pubmed.ncbi.nlm.nih.gov/34029993/
3CLpro inhibitors commonly target host proteases, which presents a potential liability for unexpected side effects.
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
Read 8 tweets
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A thread. #paxlovid #protease #inhibitors #ivermectin #COVID19
Dr. John Campbell: Paxlovid vs Ivermectin
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
Read 22 tweets
9 Nov
February 15 and August 15, 2021 C19 Vaccination during Pregnancy & First-Trimester Miscarriage
compares to
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#percentage doesn't fit. #covid & #COVIDVaccination era has more miscarriages.

March 2019 Norway study: Image
March 2019 norway study
file:///C:/Users/User/Downloads/Role_of_maternal_age_and_pregnancy_history_in_risk.pdf
#covid #Covidvaccine era in Norway Feb 2021-Aug 2021
nejm.org/doi/full/10.10…
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eventiavversinews.it/2-433-decessi-…
ImageImageImage
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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…
Read 6 tweets
8 Nov
In silico identification of natural products from Centella asiatica as SARS-COV-2 main protease (M pro) inhibitor. 1/n

❌❌❌ #ritonavir #molnupiravir in #COVID19
No more #tryglyceride #mutagenesis

pubmed.ncbi.nlm.nih.gov/34345605/
2/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

hindawi.com/journals/ecam/…
Read 8 tweets

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