Málstofa Lífvísindaseturs - Development of new antileukemic and antimicrobial phenazines

Málstofa Lífvísindaseturs fimmtudaginn 10. apríl kl. 12:30-13:10 í Öskju, stofu N-132

Fyrirlesari: Dr. Elvar Örn Viktorsson, lektor við Lyfjafræðideild Háskóla Íslands

Titill: Development of new antileukemic and antimicrobial phenazines derived from the natural products iodinin and myxin 

Ágrip: Phenazines are a large class of colorful, tricyclic aromatic natural compounds derived from the shikimic acid biosynthetic pathway in bacteria. Their bioactivity is largely associated with antimicrobial and antineoplastic effects in vitro. This work highlights our recent efforts to develop novel antineoplastic and antimicrobial agents based on the phenazine 5,10-dioxide antibiotics iodinin and myxin, with a particular focus on acute myeloid leukemia (AML) and tuberculosis.

Iodinin, myxin, and a range of structurally related analogs were synthesized from commercially available reagents. Structure–activity relationship (SAR) studies were performed to evaluate the cytotoxic potential of these compounds against both leukemic and non-malignant mammalian cell lines. Cell viability was assessed using the WST-1 cell proliferation assay, while antimycobacterial activity was evaluated against a virulent strain of Mycobacterium tuberculosis (H37Rv) using the Resazurin Microtiter Assay (REMA).

Several carbamate analogs of iodinin and myxin demonstrated potent cytotoxicity toward acute myeloid leukemia (AML) cells (MOLM-13), while exhibiting significantly reduced effects on non-malignant cell lines (NRK: Normal Rat Kidney and H9c2: Rat Cardiomyoblast). In parallel, selected regioisomers of iodinin and myxin showed strong and selective inhibitory activity against M. tuberculosis in vitro, while maintaining low cytotoxicity in mammalian cells.

Heimild: https://www.sciencedirect.com/science/article/pii/S0223523425000091?via%...