Synthesis, Structure, DNA/BSA Binding, DNA Cleaving, Cytotoxic and SOD Mimetic Activities of Copper(II) Complexes Derived from Methoxybenzylamine Schiff Base Ligands
Year: 2025
Type: article
Abstract: Schiff base ligands prepared from salicylaldehyde and 2-, 3- and 4-methoxybenzylamine were used to prepare copper(II) complexes, characterized by spectral methods, elemental analysis and X-ray crystallography in the case of complex 4a derived from 2-methoxybenzylamine. The DNA cleavage activity of the prepared complexes was exceptional, with best activities of over 95% one-strand cleavage for 4c at 3 mM and full double-strand cleavage for complex 4a at 5 mM. Absorption titration studies with ct-DNA revealed good binding constants (at 105 M−1) with a decrease of up to 56% light absorption. Meanwhile, the EB–DNA displacement method and viscosity studies revealed groove binding as a possible binding mode. For BSA binding studies, all three complexes showed KBSA values in the optimal range for reversible BSA binding (104 M−1). The copper(II) complexes showed significant cytotoxic effects (67–96% at 1 mM) in mitochondrial activity monitoring assays. Cytotoxicity was confirmed against cancer cell lines (A549 and HepG2) and HEL cells. The complexes 4a and 4c exhibited high activity against HepG2 cancer cells (IC50 < 22 μM), comparable to cisplatin. The radical scavenging activity was determined by the INT method with the best IC50 for 4c (189 ± 11 μM). Overall, complexes 4a and 4c with a methoxy group in the ortho and para positions show high potential in most determined activities, but mainly as DNA cleavers and as cytotoxic agents with selectivity against HepG2 cells.
Source: Molecules
Language: English
Subfield: Oncology
Field: Medicine
Domain: Health Sciences
Open Access status: gold
Estimated APC paid: $3,258
Awards: G1099935310, G1110178404, G1201009108, G1273147647, G1367439234, G1692994730, G1816820439, G1944792718, G2638621483, G3953621384, G4081715406, G485291616, G4962319149, G5290585320, G5529322123, G6299241118, G6463683671, G7272359787, G7813630204, G7900386159, G8480092605, G8496417212, Štúdium rozdielov medzi elektrónovou štruktúrou v kryštáli a v izolovanej molekule, ich vplyv na zmenu chemických a fyzikálnochemických vlastností základného a excitovaného stavu., G881382632, Potenciálne mimetiká a kancerostatika na báze komplexov prechodných kovov, G8945127882, G937320723
OpenAlex ID: W4413412393