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Mechanisms of anti-cancer agents: emphasis on oxidative stress and electron transfer
1Department of Chemistry, San Diego State University, San Diego, CA 92182-1030, USA. jgenoves@sundown.sdsu.edu
Abstract:
A large body of evidence has accumulated indicating involvement of oxidative stress (OS) in the mode of action of various bioactive substances, including those of the immune system. The data for anticancer drugs (main and miscellaneous) are summarized herein. Although diverse origins pertain, reactive oxygen species (ROS) are frequently generated by redox cycling via electron transfer (ET) groups, such as quinones (or phenolic precursors), metal complexes (or complexors), aromatic nitro compounds (or reduced products) and conjugated imines (or iminium species). We believe it is not coincidental that these functionalities are frequently found in anticancer agents or their metabolites. Generally, the ET moieties display reduction potentials in the physiologically active range. Often ROS are also implicated in more traditional rationales, namely, enzyme inhibition, membrane or DNA insult, and interference with DNA or protein synthesis. A multi-faceted approach to mechanism appears to be the most logical. Significantly, the unifying theme of ET-OS also applies to other drug categories, as well as to toxins, carcinogens, hormones, and enzymes. Since this theoretical framework aids in our understanding of drug action, it can serve as a useful tool in the design of more active and safer pharmaceuticals.
Insights
Oxidative stress (OS) is crucial for many bioactive substances, including anticancer drugs. Electron transfer (ET) groups in these drugs generate reactive oxygen species (ROS), a unifying mechanism for drug action.
Area of Science:
- Pharmacology
- Biochemistry
- Toxicology
Background:
- Oxidative stress (OS) plays a significant role in the action of bioactive compounds.
- Anticancer drugs often involve complex mechanisms of action.
Purpose of the Study:
- To summarize evidence linking oxidative stress to anticancer drug efficacy.
- To explore the role of electron transfer (ET) groups in generating reactive oxygen species (ROS).
Main Methods:
- Review and synthesis of existing data on anticancer drugs and oxidative stress.
- Analysis of the chemical functionalities responsible for ET and ROS generation.
Main Results:
- ET groups like quinones and metal complexes are frequently found in anticancer agents.
- These groups generate ROS via redox cycling, contributing to drug action.
- ROS generation is implicated in enzyme inhibition and DNA/protein synthesis interference.
Conclusions:
- Electron transfer-mediated oxidative stress (ET-OS) is a unifying mechanism for anticancer drugs.
- This framework extends to other bioactive substances, toxins, and hormones.
- Understanding ET-OS can guide the design of safer and more effective pharmaceuticals.