Development of new chemotherapeutic agents to treat microbial infections and recurrent cancers is of pivotal importance. Metal based drugs particularly ruthenium complexes have the uniqueness and desired properties that make them suitable candidates for the search of potential chemotherapeutic agents. In this study, two mixed ligand Ru(III) complexes [Ru(Cl)(SB)(Phen] (RC-1) and [Ru(Cl)(SB)(Bipy)] (RC-2) were synthesised and characterized by elemental analysis, IR, UV-Vis, H, C NMR spectroscopic techniques and their molecular structure was confirmed by X-ray crystallography. Antibacterial activity evaluation against two Gram-positive (S. pneumonia and E. faecalis) and four Gram-negative strains (P. aurogenosa, K. pneumoniae, S. enterica, and E. coli) revealed their moderate antibacterial activity with MIC value of ≥250 μg/mL. Anticancer activity evaluation against a non-small lung cancer cell line (H1299) revealed the tremendous anticancer activity of these complexes which was further validated by DNA binding and docking results. DNA binding profile of the complexes studied by UV-Visible and fluorescence spectroscopy showed an intercalative binding mode with CT-DNA and an intrinsic binding constant in the range of 3.481-1.015× 10 M. Both the complexes were also found to exert weak toxicity to human erythrocytes by haemolytic assay compared to cisplatin. Potential of these complexes as anticancer agents will be further delineated by in vivo studies.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1016/j.bioorg.2019.03.080 | DOI Listing |
Biochemistry
January 2025
Department of Chemistry, Washington University in St. Louis, One Brookings Drive, St. Louis, Missouri 63130, United States.
Branch-point syntheses in nonribosomal peptide assembly are rare but useful strategies to generate tripodal peptides with advantageous hexadentate iron-chelating capabilities, as seen in siderophores. However, the chemical logic underlying the peptide branching by nonribosomal peptide synthetase (NRPS) often remains complex and elusive. Here, we review the common strategies for the biosynthesis of branched nonribosomal peptides (NRPs) and present our biochemical investigation on the NRPS-catalyzed assembly of fimsbactin A, a branched mixed-ligand siderophore produced by the human pathogenic strain .
View Article and Find Full Text PDFJ Fluoresc
January 2025
Infectious Disease Department, Hangzhou First People's Hospital Tonglu Hospital, Hangzhou, Zhejiang, China.
This study synthesizes a novel three-dimensional (3D) porous coordination polymer (CP), {[Co(L)₀.₅(H₂O)]·NMP·H₂O} (1), via a solvothermal method in a mixed solvent of water and NMP (1-methyl-2-pyrrolidinone), reacting Co(II) ions with H₄L (1,4-bis(5,6-carboxybenzimidazolylmethyl)benzene). The CP exhibits unique fluorescence properties, emitting at 420 nm under UV light excitation at 350 nm, and serves as a carrier for Mesalazine (MSZ) in therapeutic applications.
View Article and Find Full Text PDFMikrochim Acta
January 2025
Key Laboratory of Optoelectronic Chemical Materials and Devices of Ministry of Education, College of Optoelectronic Materials and Technology, Jianghan University, Wuhan, 430056, China.
An electrochemical sensor is presented for the detection of the chloramphenicol (CAP) based on a bimetallic MIL-101(Fe/Co) MOF electrocatalyst. The MIL-101(Fe/Co) was prepared by utilizing mixed-valence Fe (III) and Co (II) as metal nodes and terephthalic acid as ligands with a simple hydrothermal method and characterized by SEM, TEM, XRD, FTIR, and XPS. Electrochemical measurements such as electrochemical impedance spectroscopy (EIS), cyclic voltammetry (CV), and differential pulse voltammetry (DPV) showed that bimetallic MIL-101(Fe/Co) had the faster electron transfer, larger electroactive area, and higher electrocatalytic activity compared with their monometallic counterparts due to the strong synergistic effect between bimetals.
View Article and Find Full Text PDFMalar J
January 2025
West African Centre for Cell Biology of Infectious Pathogens, Accra University of Ghana, Volta Rd, Accra, Ghana.
Background: Malaria remains a leading cause of death worldwide, claiming over 600,000 lives each year. Over 90% of these deaths, mostly among children under 5 years, occur in sub-Saharan Africa and are caused by Plasmodium falciparum. The merozoites stage of the parasite, crucial for asexual development invade erythrocytes through ligand-receptor interactions.
View Article and Find Full Text PDFCell Commun Signal
January 2025
Department of Life Sciences, Institute of Genome Sciences, National Yang Ming Chiao Tung University, 155 Li-Nong Street, Section 2, Beitou, Taipei, 112, Taiwan.
Background: TGF-β1 is the most abundant cytokine in bone, in which it serves as a vital factor to interdict adipogenesis and osteogenesis of bone marrow-derived mesenchymal stem cells (BM-MSCs). However, how TGF-β1 concurrently manipulates differentiation into these two distinct lineages remains elusive.
Methods: Treatments with ligands or inhibitors followed by biochemical characterization, reporter assay, quantitative PCR and induced differentiation were applied to MSC line or primary BM-MSCs for signaling dissection.
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!