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Marine-Derived Compounds Targeting Topoisomerase II in Cancer Cells: A Review
Giulia Greco1, Valentina Pellicioni1, Ivan Cruz-Chamorro1,2,3
1Department for Life Quality Studies, University of Bologna, Corso d'Augusto 237, 47921 Rimini, Italy.
Abstract:
Cancer affects more than 19 million people and is the second leading cause of death in the world. One of the principal strategies used in cancer therapy is the inhibition of topoisomerase II, involved in the survival of cells. Side effects and adverse reactions limit the use of topoisomerase II inhibitors; hence, research is focused on discovering novel compounds that can inhibit topoisomerase II and have a safer toxicological profile. Marine organisms are a source of secondary metabolites with different pharmacological properties including anticancer activity. The objective of this review is to present and discuss the pharmacological potential of marine-derived compounds whose antitumor activity is mediated by topoisomerase II inhibition. Several compounds derived from sponges, fungi, bacteria, ascidians, and other marine sources have been demonstrated to inhibit topoisomerase II. However, some studies only report docking interactions, whereas others do not fully explain the mechanisms of topoisomerase II inhibition. Further in vitro and in vivo studies are needed, as well as a careful toxicological profile evaluation with a focus on cancer cell selectivity.
Insights
Marine compounds show promise for cancer therapy by inhibiting topoisomerase II (an enzyme crucial for cell survival). Further research is needed to confirm their efficacy and safety as novel anticancer agents.
Area of Science:
- Marine Biology
- Pharmacology
- Oncology
Background:
- Cancer is a leading cause of death globally, affecting millions.
- Topoisomerase II (an enzyme vital for cell survival) inhibition is a key cancer therapy strategy.
- Current topoisomerase II inhibitors have limitations due to side effects, driving the search for safer alternatives.
Purpose of the Study:
- To review marine-derived compounds with anticancer activity mediated by topoisomerase II inhibition.
- To discuss the pharmacological potential of these natural products.
- To identify research gaps and future directions.
Main Methods:
- Literature review of studies on marine-derived compounds and topoisomerase II inhibition.
- Analysis of reported mechanisms of action and pharmacological properties.
- Evaluation of existing data on anticancer activity.
Main Results:
- Numerous marine organisms (sponges, fungi, bacteria, ascidians) yield compounds that inhibit topoisomerase II.
- Some compounds show promising anticancer activity through this mechanism.
- Evidence for inhibition mechanisms varies, with some studies relying on docking interactions.
Conclusions:
- Marine natural products represent a valuable resource for developing novel topoisomerase II inhibitors.
- Further in vitro and in vivo studies are essential to validate efficacy and selectivity.
- Comprehensive toxicological profiling is crucial for clinical translation of these marine compounds.
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