scholarly journals Discovery of a Small Molecule Inhibitor of Human Adenovirus Capable of Preventing Escape from the Endosome

2021 ◽  
Vol 22 (4) ◽  
pp. 1617
Author(s):  
Jimin Xu ◽  
Judith Berastegui-Cabrera ◽  
Marta Carretero-Ledesma ◽  
Haiying Chen ◽  
Yu Xue ◽  
...  
Keyword(s):  
Potent Inhibitor ◽  
Antiviral Drug ◽  
Human Adenovirus ◽  
Yield Reduction ◽  
Respiratory Illnesses ◽  
Molecule Inhibitor ◽  
Wide Range ◽  
Ic50 Values ◽  
Life Threatening ◽  
Salicylamide Derivatives

Human adenoviruses (HAdVs) display a wide range of tissue tropism and can cause an array of symptoms from mild respiratory illnesses to disseminated and life-threatening infections in immunocompromised individuals. However, no antiviral drug has been approved specifically for the treatment of HAdV infections. Herein, we report our continued efforts to optimize salicylamide derivatives and discover compound 16 (JMX0493) as a potent inhibitor of HAdV infection. Compound 16 displays submicromolar IC50 values, a higher selectivity index (SI > 100) and 2.5-fold virus yield reduction compared to our hit compound niclosamide. Moreover, unlike niclosamide, our mechanistic studies suggest that the antiviral activity of compound 16 against HAdV is achieved through the inhibition of viral particle escape from the endosome, which bars subsequent uncoating and the presentation of lytic protein VI.

scholarly journals SARS-CoV-2: An Update on Potential Antivirals in Light of SARS-CoV Antiviral Drug Discoveries

Vaccines ◽  
2020 ◽  
Vol 8 (2) ◽  
pp. 335 ◽  
Author(s):  
Hatem A. Elshabrawy
Keyword(s):  
Antiviral Drug ◽  
Severe Respiratory Distress ◽  
Respiratory Illnesses ◽  
High Fatality Rate ◽  
Causative Agents ◽  
Life Threatening ◽  
Current Outbreak ◽  
Severe Respiratory Distress Syndrome

Coronaviruses (CoVs) are a group of RNA viruses that are associated with different diseases in animals, birds, and humans. Human CoVs (HCoVs) have long been known to be the causative agents of mild respiratory illnesses. However, two HCoVs associated with severe respiratory diseases are Severe Acute Respiratory Syndrome-CoV (SARS-CoV) and Middle East Respiratory Syndrome-CoV (MERS-CoV). Both viruses resulted in hundreds of deaths after spreading to several countries. Most recently, SARS-CoV-2 has emerged as the third HCoV causing severe respiratory distress syndrome and viral pneumonia (known as COVID-19) in patients from Wuhan, China, in December 2019. Soon after its discovery, SARS-CoV-2 spread to all countries, resulting in millions of cases and thousands of deaths. Since the emergence of SARS-CoV, many research groups have dedicated their resources to discovering effective antivirals that can treat such life-threatening infections. The rapid spread and high fatality rate of SARS-CoV-2 necessitate the quick discovery of effective antivirals to control this outbreak. Since SARS-CoV-2 shares 79% sequence identity with SARS-CoV, several anti-SARS-CoV drugs have shown promise in limiting SARS-CoV-2 replication in vitro and in vivo. In this review, we discuss antivirals described for SARS-CoV and provide an update on therapeutic strategies and antivirals against SARS-CoV-2. The control of the current outbreak will strongly depend on the discovery of effective and safe anti-SARS-CoV-2 drugs.

Synthesis, Antioxidant and Antiurease Activities of Some New 5,6- dichloro-2-(4-fluorobenzyl)-1H-benzimidazole Derivatives Containing Furan, Oxadiazole, Triazole and Thiadiazole Moieties

2019 ◽  
Vol 16 (8) ◽  
pp. 939-947
Author(s):  
Hakan Bektas ◽  
Canan Albay ◽  
Emre Menteşe ◽  
Bahar Bilgin Sokmen ◽  
Zafer Kurt ◽  
...  
Keyword(s):  
Biological Activities ◽  
Benzimidazole Derivatives ◽  
Wide Range ◽  
Ic50 Values ◽  
Urease Inhibitory

Background:Benzimidazoles and its derivatives have been attracting interest for many years because of their biological activities. Benzimidazoles containing different heterocyclic moieties have wide range of biological activities such as antimicrobial, antioxidant, anticancer, antiviral, etc.Methods:In this study, some benzimidazole derivatives containing furan, oxadiazole, triazole and thiadiazole moieties have been synthesized and then evaluated for their antioxidant and antiurease activities.Results:The results showed that all the tested benzimidazoles indicated remarkable urease inhibitory potentials with IC50 values ranging between 0.303±0.03 to 0.591±0.08 µM.Conclusion:In conclusion, synthesized benzimidazole derivatives showed good antioxidant and antiurease activities. Heterocyclic groups on benzimidazole nucleus enhance the activities.

scholarly journals Beehive Products as Antibacterial Agents: A Review

Antibiotics ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 717
Author(s):  
Rita Abou Nader ◽  
Rawan Mackieh ◽  
Rim Wehbe ◽  
Dany El El Obeid ◽  
Jean Marc Sabatier ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Honey Bee ◽  
Antibacterial Agents ◽  
Royal Jelly ◽  
Biological Activities ◽  
Vital Role ◽  
Bee Venom ◽  
Bacterial Strains ◽  
Wide Range ◽  
Life Threatening

Honeybees are one of the most marvelous and economically beneficial insects. As pollinators, they play a vital role in every aspect of the ecosystem. Beehive products have been used for thousands of years in many cultures for the treatment of various diseases. Their healing properties have been documented in many religious texts like the Noble Quran and the Holy Bible. Honey, bee venom, propolis, pollen and royal jelly all demonstrated a richness in their bioactive compounds which make them effective against a variety of bacterial strains. Furthermore, many studies showed that honey and bee venom work as powerful antibacterial agents against a wide range of bacteria including life-threatening bacteria. Several reports documented the biological activities of honeybee products but none of them emphasized on the antibacterial activity of all beehive products. Therefore, this review aims to highlight the antibacterial activity of honey, bee venom, propolis, pollen and royal jelly, that are produced by honeybees.

scholarly journals Human adenovirus species in children with acute respiratory illnesses

2021 ◽  
Vol 134 ◽  
pp. 104716
Author(s):  
Varvara Probst ◽  
Emily K. Datyner ◽  
Zaid Haddadin ◽  
Danielle A. Rankin ◽  
Lubna Hamdan ◽  
...  
Keyword(s):  
Human Adenovirus ◽  
Respiratory Illnesses

scholarly journals Could metabolomics drive the fate of COVID-19 pandemic? A narrative review on lights and shadows

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Michele Mussap ◽  
Vassilios Fanos
Keyword(s):  
Molecular Mechanisms ◽  
Vascular Dysfunction ◽  
Asymptomatic Infection ◽  
Multiple Organ ◽  
Therapeutic Interventions ◽  
Patient Specific ◽  
Wide Range ◽  
Life Threatening ◽  
The Individual ◽  
Host Metabolism

Abstract Human Severe Acute Respiratory Syndrome CoronaVirus 2 (SARS-CoV-2) infection activates a complex interaction host/virus, leading to the reprogramming of the host metabolism aimed at the energy supply for viral replication. Alterations of the host metabolic homeostasis strongly influence the immune response to SARS-CoV-2, forming the basis of a wide range of outcomes, from the asymptomatic infection to the onset of COVID-19 and up to life-threatening acute respiratory distress syndrome, vascular dysfunction, multiple organ failure, and death. Deciphering the molecular mechanisms associated with the individual susceptibility to SARS-CoV-2 infection calls for a system biology approach; this strategy can address multiple goals, including which patients will respond effectively to the therapeutic treatment. The power of metabolomics lies in the ability to recognize endogenous and exogenous metabolites within a biological sample, measuring their concentration, and identifying perturbations of biochemical pathways associated with qualitative and quantitative metabolic changes. Over the last year, a limited number of metabolomics- and lipidomics-based clinical studies in COVID-19 patients have been published and are discussed in this review. Remarkable alterations in the lipid and amino acid metabolism depict the molecular phenotype of subjects infected by SARS-CoV-2; notably, structural and functional data on the lipids-virus interaction may open new perspectives on targeted therapeutic interventions. Several limitations affect most metabolomics-based studies, slowing the routine application of metabolomics. However, moving metabolomics from bench to bedside cannot imply the mere determination of a given metabolite panel; rather, slotting metabolomics into clinical practice requires the conversion of metabolic patient-specific data into actionable clinical applications.

ANTIBIOTIC SUSCEPTIBILITY PATTERN OF STAPHYLOCOCCOUS AUREUS ISOLATED FROM VARIOUS CLINICAL SPECIMENS OF TERTIARY CARE HOSPITAL IN TIRUPATI.

2021 ◽  
pp. 14-15
Author(s):  
Indira Ananthapadmanab asamy ◽  
V. Pavani Sai Mounika ◽  
K. Vijayakumar ◽  
C.H. Srinivasa Rao
Keyword(s):  
Antimicrobial Susceptibility ◽  
Tertiary Care ◽  
Care Hospital ◽  
Susceptibility Pattern ◽  
Clinical Specimens ◽  
Antimicrobial Susceptibility Pattern ◽  
Wide Range ◽  
Life Threatening ◽  
Mrsa Infection ◽  
Systemic Infections

INTRODUCTION: Staphylococcus aureus causes a wide range of infections including skin and soft tissue infections to life-threatening systemic infections like sepsis, endocarditis. This study ais to evaluate the antimicrobial susceptibility pattern of S.aurues among various clinical specimens. METHODS: The study included 326 S.aurues, isolated from various clinical specimens which were subjected to antimicrobial susceptibility testing as per CLSI guidelines. RESULTS: Among the 326 isolates, the highest were from pus specimens (47.85%), and was from Orthopaedics department (28.53%). Among the isolates, 219 (67.17%) were Methicilin resistant. All isolates were sensitive to Vancomycin, and all urine isolates were sensitive to Nitrofurantoin. The highest resistance was towards Penicillin (87.42%), Erythromycin (85.28), and Ciprooxacin (83.13%). CONCLUSION: The most effective way to prevent MRSA infection in every hospital is by performing continuous surveillance of antibiotic resistance and by following an effetive antibiotic policy.

Updates and Advances: Pediatric Musculoskeletal Infection Imaging Made Easier for Radiologists and Clinicians

2021 ◽  
Vol 25 (01) ◽  
pp. 167-175
Author(s):  
Michael S. Furman ◽  
Ricardo Restrepo ◽  
Supika Kritsaneepaiboon ◽  
Bernard F. Laya ◽  
Domen Plut ◽  
...  
Keyword(s):  
Clinical Practice ◽  
Imaging Techniques ◽  
Daily Clinical Practice ◽  
Infants And Children ◽  
Imaging Evaluation ◽  
Musculoskeletal Infection ◽  
Wide Range ◽  
Life Threatening ◽  
Optimal Patient Management

AbstractInfants and children often present with a wide range of musculoskeletal (MSK) infections in daily clinical practice. This can vary from relatively benign superficial infections such as cellulitis to destructive osseous and articular infections and life-threatening deep soft tissue processes such as necrotizing fasciitis. Imaging evaluation plays an essential role for initial detection and follow-up evaluation of pediatric MSK infections. Therefore, a clear and up-to-date knowledge of imaging manifestations in MSK infections in infants and children is imperative for timely and accurate diagnosis that, in turn, can result in optimal patient management. This article reviews an up-to-date practical imaging techniques, the differences between pediatric and adult MSK infections, the spectrum of pediatric MSK infections, and mimics of pediatric MSK infections encountered in daily clinical practice by radiologists and clinicians.

scholarly journals A new lead to NLRP3 inhibition

2017 ◽  
Vol 214 (11) ◽  
pp. 3147-3149 ◽  
Author(s):  
Mohamed Lamkanfi ◽  
Vishva M. Dixit
Keyword(s):  
Small Molecule ◽  
Small Molecule Inhibitor ◽  
Therapeutic Benefit ◽  
Human Diseases ◽  
Molecule Inhibitor ◽  
Wide Range ◽  
Potential Therapeutic Benefit

The discovery of a small molecule inhibitor that targets the inflammasome sensor NLRP3 offers a new path for the development of selective inflammasome blockers with potential therapeutic benefit in a wide range of human diseases (in this issue, see Jiang et al., https://doi.org/10.1084/jem.20171419).

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