Stabilization of c-myc G-Quadruplex DNA, inhibition of telomerase activity, disruption of mitochondrial functions and tumor cell apoptosis by platinum(II) complex with 9-amino-oxoisoaporphine

Oxoaporphine Metal Complexes (CoII, NiII, ZnII) with High Antitumor Activity by Inducing Mitochondria-Mediated Apoptosis and S-phase Arrest in HepG2

“…The DCFH-DA method was used to determined the effects of 1–3 on ROS generation as reported68. In this method, the stable non-fluorescent DCFH-DA was hydrolyzed by esterases in cells to non-fluorescent DCFH, which was rapidly oxidized by ROS to highly fluorescent 2′,7′-dichlorofluorescein (DCF).…”

Oxoisoaporphine Alkaloids: Prospective Anti‐Alzheimer's Disease, Anticancer, and Antidepressant Agents

“…By considering the effectso fc omplexes of Group 10 metals (nickel,p latinum, and palladium), such as stabilizing G-tetrameric DNA, regulating gene expression, and controlling telomerase, two complexesc ombining [Pd(L)(dmso)Cl 2 ]a nd [Pt(L)(dmso)Cl 2 ]w ith 9-aminooxoisoaporphine (L) were synthesized ( Figure 8) by Qin et al [41] The cytotoxicities toward seven tumorc ell lines, HepG2, SK-OV-3, SK-VO-3/DDP,B EL-7402, A549/DDP,N CI-H460, and HCT-8, as well as normalh epatocyte HL-7702c ells, were determined. The results indicated that the complexes had higherc ytotoxic activities, and their selectivity to Hep-G2c ells was stronger than that of normall iver cells (HL-7702).…”

“…Chemical structureso f29 [40]. Chemical structures of 30 [41]. ChemMedChem 2018, 13,1262 -1274 www.chemmedchem.org of up to 4.8 mm,w hereas 31 b showedt he best IC 50 values against SK-OV-3/DDP up to 4.5 mm.C ytotoxic mechanistic studies demonstrated that both 31 a and 31 b could inhibitt elomerase and affect the expression of bcl-2 and caspase-3 by acting on G-quadruplex (G4) DNA, which played ar ole in inducing cell apoptosis.…”

Three novel transition metal complexes of 6-methyl-2-oxo-quinoline-3-carbaldehyde thiosemicarbazone: synthesis, crystal structure, cytotoxicity, and mechanism of action

“…Therefore, the copper complex 1 could induce cell apoptosis by triggering the caspase-3/9 activity in MGC80-3 cells. [62][63][64][65][66] Taken together, the copper complex 1 most likely induced apoptosis in MGC80-3 cells by disrupting mitochondrial function, which led to signicantly decreased level of the bcl-2 protein and the loss of Dj, as well as the signicant increase in the ROS level, intracellular Ca 2+ , cytochrome c, apaf-1, activated caspase-3, and activated caspase-9 in MGC80-3 cells.…”