Read & Download your Issue of Thursday – February 25 FNN News

A new class of α-ketoamide derivatives with potent anticancer and anti-SARS-CoV-2 activities

• Inhibitors of the proteasome have been extensively studied for their applications in the treatment of human diseases such as hematologic malignancies, autoimmune disorders, and viral infections.
• Many derivatives displayed highly potent biological activities in proteasome inhibition and anticancer activity against a panel of six cancer cell lines, which were further rationalized by molecular modeling analyses.
• Furthermore, a representative α-ketoamide derivative was tested and found to be active in inhibiting the cellular infection of SARS-CoV-2 which causes the COVID-19 pandemic.

Source: ScienceDirect

Essential oils as an effective alternative for the treatment of COVID-19

• The current health concern to the entire world is the chronic respiratory disease caused by coronavirus 2 (COVID-19).
• The Coronavirus replication takes place by the conversion of the polypeptide into functional protein and this occurs due to the key enzyme Main protease (Mpro).
• Therefore, identification of natural and effective Mpro inhibitors could be a safe and promising approach for COVID-19 control.
• The outcome of this study reported that the essential oil of Eucalyptus and Corymbia species, mainly eucalyptol can be utilized as a potential inhibitor against COVID-19 and also it can be used in its treatment.

Source: ScienceDirect

Antibacterial activity of new substituted 4-N-alkylated-2-trifluoromethyl-quinoline analogues against sensitive and resistant Mycobacterium tuberculosis strains

• The emergence of resistant strain has aggravated the tuberculosis situation in the world, running out of control and hard to fight.
• This study evaluates forty new quinoline analogues against sensitive and resistant Mycobacterium tuberculosis (Mtb).
• Twenty-nine compounds displayed activity against sensitive strain, and thirteen were active against resistant strains.
• Against sensitive strain, the most promising compounds were 4c and 4d.

Source: ScienceDirect

Artemisinin and artemisinin derivatives as anti-fibrotic therapeutics

• Fibrosis is a pathological reparative process that can occur in most organs and is responsible for nearly half of deaths in the developed world.
• Artemisinin compounds are best known as antimalarial therapeutics, but they also demonstrate antiparasitic, antibacterial, anticancer, and anti-fibrotic effects.
• Here they summarize literature describing anti-fibrotic effects of artemisinin compounds in in vivo and in vitro models of tissue fibrosis, and describe the likely mechanisms by which artemisinin compounds appear to inhibit cellular and tissue processes that lead to fibrosis

Source: ScienceDirect

Tocilizumab reduces deaths in patients hospitalised with COVID-19

• The ‘RECOVERY’ trial has found that an anti-inflammatory treatment, tocilizumab, reduces the risk of death when given to hospitalised patients with severe COVID-19.
• The ‘RECOVERY’ trial has found that an anti-inflammatory treatment, tocilizumab, reduces the risk of death when given to hospitalised patients with severe COVID-19.
• The preliminary results from the study also showed that tocilizumab shortens the time until patients are successfully discharged from hospital and reduces the need for a mechanical ventilator.

Source: UKRI

Corilagin inhibits SARS-CoV-2 replication by targeting viral RNA-dependent RNA polymerase

• Severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) has become one major threat to human population health.
• Herein, they report that corilagin effectively inhibits the polymerase activity in both cell-free and cell-based assays and fully resists the proofreading activity and potently inhibits SARS-CoV-2 infection.
• Together with the current data available on the safety and pharmacokinetics of corilagin as a medicinal herbal agent, these results demonstrate the potential of being developed into one of the much-needed SARS-CoV-2 therapeutics.

Source: ScienceDirect

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