Efficient synthesis of novel colchicine-magnolol hybrids and evaluation of their inhibitory activity on key proteases of 2019-nCoV replication and acute lung injury

Article Integrative & Complementary Medicine

Inhibitory effect of honokiol on furin-like activity and SARS-CoV-2 infection

Takashi Tanikawa et al.

Summary: This study found that honokiol has a remarkable inhibitory effect on SARS-CoV-2 infection, suggesting that honokiol and related traditional Chinese medicine may be potential therapeutic agents for treating SARS-CoV-2.

JOURNAL OF TRADITIONAL AND COMPLEMENTARY MEDICINE (2022)

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Article Immunology

Combined administration of inhaled DNase, baricitinib and tocilizumab as rescue treatment in COVID-19 patients with severe respiratory failure

Efstratios Gavriilidis et al.

Summary: A combined rescue treatment consisting of inhaled DNase, anti-IL-6-receptor tocilizumab, and JAK1/2 inhibitor baricitinib, administered on top of standard-of-care, significantly reduces mortality and intubation rate in COVID-19 patients with severe respiratory failure. This treatment targets multiple interconnected pathways of immunothrombosis, providing a mechanistic explanation for its clinical effectiveness.

CLINICAL IMMUNOLOGY (2022)

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Article Chemistry, Applied

Inhibition of the SARS-CoV-2 3CLpro main protease by plant polyphenols

Miha Bahun et al.

Summary: Research has shown the potential of various plant polyphenols in inhibiting the SARS-CoV-2 virus, such as quercetin and curcumin. Through in-vitro assays and molecular dynamics simulations, stable interactions between these polyphenols and the virus's crucial enzyme 3CL(pro) have been revealed, laying the foundation for further development of these inhibitors.

FOOD CHEMISTRY (2022)

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Article Biochemistry & Molecular Biology

Repurposing Multiple-Molecule Drugs for COVID-19-Associated Acute Respiratory Distress Syndrome and Non-Viral Acute Respiratory Distress Syndrome via a Systems Biology Approach and a DNN-DTI Model Based on Five Drug Design Specifications

Ching-Tse Ting et al.

Summary: The study focused on investigating the pathogenic mechanisms of COVID-19-associated ARDS and non-viral ARDS by constructing a candidate host-pathogen interspecies genome-wide genetic and epigenetic network. By comparing core signal pathways, essential biomarkers were identified as drug targets, and potential multiple-molecule drugs were repurposed for therapeutic options in treating the two types of ARDS.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2022)

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Article Multidisciplinary Sciences

A TMPRSS2 inhibitor acts as a pan-SARS-CoV-2 prophylactic and therapeutic

Tirosh Shapira et al.

Summary: The COVID-19 pandemic caused by the SARS-CoV-2 virus is still a global public health crisis, with reduced efficacy of vaccination campaigns due to emerging variants of concern. Development of host-directed therapeutics and prophylactics can limit resistance and provide urgently needed protection against these variants.

NATURE (2022)

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Review Multidisciplinary Sciences

Safety and efficacy of colchicine in COVID-19 patients: A systematic review and meta-analysis of randomized control trials

Farah Yasmin et al.

Summary: Colchicine treatment reduces COVID-19 severity and CRP levels, but has no significant impact on D-dimer levels, all-cause mortality, and mechanical ventilation.

PLOS ONE (2022)

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Article Multidisciplinary Sciences

Structural basis for replicase polyprotein cleavage and substrate specificity of main protease from SARS-CoV-2

Yao Zhao et al.

Summary: This study determines the high-resolution structures of SARS-CoV-2 M-Pro in different states, revealing the conformational changes that occur during substrate processing. The study also demonstrates the enzyme's specificity for certain sequences and provides a foundation for the development of new anti-SARS-CoV-2 drugs.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2022)

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Article Multidisciplinary Sciences

Covalent narlaprevir- and boceprevir-derived hybrid inhibitors of SARS-CoV-2 main protease

Daniel W. Kneller et al.

Summary: The study designed three covalent hybrid inhibitors that showed comparable antiviral activity to a known drug in vitro. The binding mechanism of these inhibitors to the viral main protease was also analyzed, providing important atomic and thermodynamic details.

NATURE COMMUNICATIONS (2022)

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Article Multidisciplinary Sciences

Development of optimized drug-like small molecule inhibitors of the SARS-CoV-2 3CL protease for treatment of COVID-19

Hengrui Liu et al.

Summary: The authors have described small molecule inhibitors of the SARS-CoV-2 3CL protease for potential treatment of COVID-19. These inhibitors have shown promising antiviral activity and could serve as valuable tools in controlling the ongoing pandemic.

NATURE COMMUNICATIONS (2022)

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Article Pharmacology & Pharmacy

Efficacy and Outcome of Remdesivir and Tocilizumab Combination Against Dexamethasone for the Treatment of Severe COVID-19: A Randomized Controlled Trial

Abu Taiub Mohammed Mohiuddin Chowdhury et al.

Summary: The study demonstrated that combination therapy with remdesivir and tocilizumab was more effective and safer than dexamethasone therapy for severe COVID-19 patients in terms of clinical improvement, mortality rate, duration of ICU stay, and total period of hospitalization.

FRONTIERS IN PHARMACOLOGY (2022)

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Article Infectious Diseases

A Multicenter Phase 2 Randomized Controlled Study on the Efficacy and Safety of Reparixin in the Treatment of Hospitalized Patients with COVID-19 Pneumonia

Giovanni Landoni et al.

Summary: In patients with severe COVID-19, treatment with reparixin resulted in improved clinical outcomes compared to standard of care. Larger phase 3 clinical studies are required to validate these findings.

INFECTIOUS DISEASES AND THERAPY (2022)

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Article Engineering, Biomedical

ROS-responsive polymer nanoparticles with enhanced loading of dexamethasone effectively modulate the lung injury microenvironment

Wali Muhammad et al.

Summary: Acute lung injury (ALI) is an inflammatory disorder associated with cytokine storm, and there is an urgent need for medication and effective drug delivery to reduce inflammation. The study found that PFTU@DEX NPs can effectively suppress inflammatory cells, ROS signaling pathways, and cell apoptosis to ameliorate ALI.

ACTA BIOMATERIALIA (2022)

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Article Biochemistry & Molecular Biology

Magnolol and Honokiol Inhibited the Function and Expression of BCRP with Mechanism Exploration

Chung-Ping Yu et al.

Summary: The study showed that the active compounds magnolol (MN) and honokiol (HK) from Magnolia officinalis can decrease the function and expression of breast cancer resistance protein (BCRP), and overcome chemotherapy resistance by inhibiting the EGFR/PI3K signaling pathway. Both MN and HK are promising candidates for reversing multidrug resistance in chemotherapy.

MOLECULES (2021)

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Article Medicine, General & Internal

Magnolol protects against acute gastrointestinal injury in sepsis by down-regulating regulated on activation, normal T-cell expressed and secreted

Shi-Hao Mao et al.

Summary: The study evaluated the protective effect of magnolol on intestinal mucosal epithelial cells in sepsis, showing that magnolol down-regulates RANTES levels by inhibiting the LPS/NF-kappa B signaling pathways, thereby suppressing IL-1 beta, IL-6, and TNF-alpha expression.

WORLD JOURNAL OF CLINICAL CASES (2021)

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Article Toxicology

Investigation of molecular mechanisms underlying the antiproliferative effects of colchicine against PC3 prostate cancer cells

Mustafa Ergul et al.

Summary: Colchicine exerts significant cytotoxicity on PC3 cells through mechanisms involving oxidative stress induction, reduction of mitochondrial membrane potential, increased DNA damage, and promotion of apoptosis. Further research is needed to evaluate its potential as an anticancer drug for prostate cancer treatment.

TOXICOLOGY IN VITRO (2021)

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Article Chemistry, Medicinal

dIdentification of Inhibitors of SARS-CoV-2 3CL-Pro Enzymatic Activity Using a Small Molecule in Vitro Repurposing Screen

Maria Kuzikov et al.

Summary: Compound repurposing is a crucial strategy for identifying effective treatments against SARS-CoV-2 infection and COVID-19. The SARS-CoV-2 main protease, 3CL-Pro, is a promising drug target due to its central role in viral replication. This study identified multiple compounds with potential inhibitory effects on 3CL-Pro, including the compound myricetin which was found to covalently bind to the enzyme and inhibit its activity.

ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE (2021)

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Review Chemistry, Medicinal