Copper(II) pyrithione

Copper (II) pyrithione is an inhibitor of New Delhi metallo-β-lactamase 1 (NDM-1). It functions by transmetalation, substituting its zinc (II) cofactor with copper (II), and exhibits cytotoxic effects on pancreatic cancer cells and osteosarcoma cells. Additionally, Copper (II) pyrithione has antimicrobial properties against gram-positive bacteria and certain gram-negative bacteria. It can enhance the efficacy of β-lactam antibiotics against β-lactam-resistant bacteria synergistically. This compound can be utilized in research related to pancreatic cancer, osteosarcoma, and bacterial infections.

Copper (II) pyrithione, when incubated for 24 hours, inhibits the proliferation of MIA PaCa-2 pancreatic cancer cells, 143B osteosarcoma cells, and ARPE-19 normal retinal epithelial cells with respective IC50 values of 0.15 μM, 0.20 μM, and 0.22 μM. Following a 4-hour incubation with 1 μM concentration, the uptake by 143B osteosarcoma cells is 16 ng Cu per 10^6 cells. This compound inhibits the growth of Staphylococcus aureus ATCC 29213 with a MIC of 0.4 μM; Escherichia coli ATCC 25922 with a MIC of 6.4 μM; Klebsi pneumoniae BAA 1705 and Acinetobacter baumannii BAA 1605, both with a MIC of 12.8 μM, while showing no activity against Pseudomonas aeruginosa ATCC 27853 even at concentrations up to 100 μM. At a concentration of 25 μM, Copper (II) pyrithione enhances the efficacy of meropenem and ertapenem against NDM-1 producing β-lactam-resistant E. coli by reducing their MIC tenfold.