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Related Concept Videos

Extraction: Advanced Methods00:56

Extraction: Advanced Methods

Metal ions can be separated from one another by complexation with organic ligands–the chelating agent– to form uncharged chelates. Here, the chelating agent must contain hydrophobic groups and behave as a weak acid, losing a proton to bind with the metal. Since most organic ligands used in this process are insoluble or undergo oxidation in the aqueous phase, the chelating agent is initially added to the organic phase and extracted into the aqueous phase. The metal-ligand complex is formed in...
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Bioactivation and Tissue Toxicity

Bioactivation is a metabolic process that transforms less reactive substances into highly reactive metabolites, initiating tissue toxicity. This transformation can lead to various toxic effects, including carcinogenesis and teratogenesis. Reactive metabolites are classified into two main types: electrophiles and free radicals.Electrophiles are electron-deficient species and are produced primarily by the enzyme cytochrome P-450 during the metabolism of compounds containing carbon, nitrogen, or...
Electron Transport Chain: Complex I and II01:46

Electron Transport Chain: Complex I and II

The mitochondrial electron transport chain (ETC) is the main energy generation system in the eukaryotic cells. However, mitochondria also produce cytotoxic reactive oxygen species (ROS) due to the large electron flow during oxidative phosphorylation. While Complex I is one of the primary sources of superoxide radicals, ROS production by Complex II is uncommon and may only be observed in cancer cells with mutated complexes.
ROS generation is regulated and maintained at moderate levels necessary...

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Anticancer Metal Complexes: Synthesis and Cytotoxicity Evaluation by the MTT Assay
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Macrocyclic copper(II) complexes: superoxide scavenging activity, structural studies and cytotoxicity evaluation.

Ana S Fernandes1, Jorge Gaspar, M Fátima Cabral

  • 1CECF, Faculty of Pharmacy, University of Lisbon, Av. Prof. Gama Pinto, 1649-003 Lisboa, Portugal.

Journal of Inorganic Biochemistry
|March 23, 2007
PubMed
Summary

Synthetic copper(II) complexes show promise as superoxide dismutase mimetics for treating oxidative stress. Four of five macrocyclic complexes effectively scavenged superoxide anions with low toxicity.

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Area of Science:

  • Medicinal Chemistry
  • Biochemistry
  • Inorganic Chemistry

Background:

  • Oxidative stress is implicated in various diseases.
  • Superoxide dismutase (SOD) enzymes protect against oxidative damage.
  • Synthetic SOD mimetics, particularly metal complexes, are explored as therapeutic agents.

Purpose of the Study:

  • To synthesize and evaluate novel macrocyclic copper(II) complexes as superoxide anion scavengers.
  • To assess the structure-activity relationship of these complexes.
  • To determine the cytotoxicity of the synthesized complexes.

Main Methods:

  • Synthesis of five macrocyclic copper(II) complexes.
  • Evaluation of superoxide scavenging activity using nitro blue tetrazolium (NBT) and dihydroethidium (DHE) assays.
  • Spectroscopic and electrochemical characterization.
  • Cytotoxicity assessment using the MTT assay in V79 cells.

Main Results:

  • Four out of five complexes demonstrated effective superoxide scavenging with IC(50) values in the low micromolar range.
  • DHE assay yielded approximately threefold lower IC(50) values compared to the NBT assay.
  • Complexes showed minimal toxicity to V79 cells at effective scavenging concentrations.
  • Structural and electrochemical properties correlated with scavenging activity.

Conclusions:

  • Macrocyclic copper(II) complexes are potent superoxide scavengers.
  • Complexes with high stability and low IC(50) are promising candidates for further investigation.
  • These compounds represent a potential new class of drugs for oxidative stress-related diseases.