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abril 30, 2021

Metabolic Basis of Creatine in Health and Disease: A Bioinformatics-Assisted Review

Creatine (Cr) is a ubiquitous molecule that is synthesized mainly in the liver, kidneys, and pancreas. Most of the Cr pool is found in tissues with high-energy demands. Cr enters target cells through a specific symporter called Na^(+)/Cl^(-)-dependent Cr transporter (CRT). Once within cells, creatine kinase (CK) catalyzes the reversible transphosphorylation reaction between [Mg^(2+):ATP^(4-)]^(2-) and Cr to produce phosphocreatine (PCr) and [Mg^(2+):ADP^(3-)]^(-). We aimed to perform a…

Computer-aided search for 5-arylideneimidazolone anticancer agents able to overcome ABCB1-based multidrug resistance

ABCB1 modulation is an interesting strategy in search for new anticancer agents overcoming multidrug resistance (MDR). Hence, 17 new 5-arylideneimidazolones containing amine moiety, as potential ABCB1 inhibitors was designed, synthesized, and investigated. The series was tested in both, parental (PAR) and multidrug resistant (MDR) overproducing ABCB1, T-lymphoma cancer cells using cytotoxicity assay. The ABCB1 modulating activity was examined in the rhodamine 123 accumulation test, followed by…

Microbial Genomics as a Catalyst for Targeted Antivirulence Therapeutics

Virulence arresting drugs (VAD) are an expanding class of antimicrobial treatment that act to «disarm» rather than kill bacteria. Despite an increasing number of VAD being registered for clinical use, uptake is hampered by the lack of methods that can identify patients who are most likely to benefit from these new agents. The application of pathogen genomics can facilitate the rational utilization of advanced therapeutics for infectious diseases. The development of genomic assessment of VAD…

A New Chalcone Derivative C49 Reverses Doxorubicin Resistance in MCF-7/DOX Cells by Inhibiting P-Glycoprotein Expression

Objective: C49 is a chalcone derivative. The aim of the current study is to illuminate the efficacy of C49 in reversing multidrug resistance (MDR) in MCF-7/DOX cells and its underlying molecular mechanism. Methods: The cytotoxic effects of C49 on MCF-7/DOX cells were evaluated by MTT assay using different concentration (0-250 μmol/L) of C49. Cell proliferation was evaluated by colony formation assay. Cell death was examined by morphological analysis using Hoechst 33,258 staining. Flow cytometry…

Impact of Sodium Alginate Packaging Film Synthesized Using <em>Syzygium cumini</em> Seed Extract on Multi Drug Resistant <em>Escherichia coli</em> Isolated from Raw Buffalo Meat

A total of 50 Escherichia coli were isolated from buffalo meat and their antibiotic profiling was carried out. 90% E. coli isolates showed resistant to two or more classes of 21 commonly used antibiotics. Moreover, there was also variation in resistance/sensitivity behavior towards antibiotics. Highest resistance was found to be against methicillin (84%) in the isolates followed by vancomicin (70%), sulphadiazine (68%) and cefaclor (66%), whereas, resistance was less common for kanamycin (8%)…

The role of chemotaxis and efflux pumps on nitrate reduction in the toxic regions of a ciprofloxacin concentration gradient

Spatial concentration gradients of antibiotics are prevalent in the natural environment. Yet, the microbial response in these heterogeneous systems remains poorly understood. We used a microfluidic reactor to create an artificial microscopic ecosystem that generates diffusive gradients of solutes across interconnected microenvironments. With this reactor, we showed that chemotaxis toward a soluble electron acceptor (nitrate) allowed Shewanella oneidensis MR-1 to inhabit and sustain metabolic…

Design, synthesis and antibacterial evaluation of ocotillol derivatives with polycyclic nitrogen-containing groups

Aim: With the increasing abuse of antibacterial drugs, multidrug-resistant bacteria have become a burden on human health and the healthcare system. To find alternative compounds effective against hospital-acquired methicillin-resistant Staphylococcus aureus (HA-MRSA), novel derivatives of ocotillol were synthesized. Methods & Results: Ocotillol derivatives with polycyclic nitrogen-containing groups were synthesized and evaluated for in vitro antibacterial activity. Compounds 36-39 exhibited…

Exploring combined herbal extract-loaded phytoniosomes for antimalarial and antibacterial activity against methicillin-resistant Staphylococcus aureus

Antibiotic resistance in the context of treating malarial infections is a major challenge in India. Home remedies such as thulasi leaves (Ocimum tenuiflorum), black pepper seeds (Piper nigrum), clove buds (Syzygium aromaticum), cinnamon bark (Cinnamomum verum), and nilavembu whole plant powder (Andrographis paniculata) were taken to explore antimalarial and methicillin-resistant Staphylococcus aureus (MRSA) activity. Among the five extracts, the best two extracts, C. verum and P. nigrum extract,…

The Antibacterial Properties of 4, 8, 4′, 8′-Tetramethoxy (1,1′-biphenanthrene) -2,7,2′,7′-Tetrol from Fibrous Roots of <em>Bletilla striata</em>

Biphenanthrene compound, 4, 8, 4′, 8′-tetramethoxy (1, 1′-biphenanthrene)-2, 7, 2′, 7′-tetrol (LF05), recently isolated from fibrous roots of Bletilla striata, exhibits antibacterial activity against several Gram-positive bacteria. In this study, we investigated the antibacterial properties, potential mode of action and cytotoxicity. Minimum inhibitory concentrations (MICs) tests showed LF05 was active against all tested Gram-positive strains, including methicillin-resistant Staphylococcus…