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Published on: June 26, 2018
Comparative investigation into the anticancer activity of analogs of marine coelenterazine and coelenteramine
Carla M Magalhães1, Renato B Pereira2, El Hadi Erbiai1
1Centro de Investigação em Química (CIQUP), Instituto de Ciências Moleculares (IMS), Departamento de Geociências, Ambiente e Ordenamento do Território, Faculdade de Ciências, Universidade do Porto, Rua do Campo Alegre s/n, 4169-007 Porto, Portugal.
Abstract:
Cancer is still one of the most challenging diseases to treat, making the pursuit for novel molecules with potential anticancer activity an important research topic. Herein, we have performed a comparative investigation into the anticancer activity of analogs of marine coelenterazine and coelenteramine. The former is a well-known bioluminescent substrate, while the latter is a metabolic product of the resulting bioluminescent reaction. While both types of analogs showed anticancer activity toward lung and gastric cancer cell lines, we have obtained data that highlight relevant differences between the activity of these two types of compounds. More specifically, we observed relevant differences in structure-activity relationships between these types of compounds. Also, coelenteramine analogs showed time-dependent activity, while coelenterazine-based compounds usually present time-independent activity. Coelenterazine analogs also appear to be relatively safer toward noncancer cells than coelenteramine analogs. There was also seen a correlation between the activity of the coelenterazine-based compounds and their light-emission properties. Thus, these results further indicate the potential of the marine coelenterazine chemi-/bioluminescent system as a source of new molecules with anticancer activity, while providing more insight into their modes of action.
Insights
Marine coelenterazine and coelenteramine analogs show anticancer effects on lung and gastric cancer cells. Coelenterazine analogs exhibit safer profiles and linked light-emission activity, suggesting potential for novel cancer therapeutics.
Area of Science:
- Marine natural products chemistry
- Medicinal chemistry
- Cancer biology
Background:
- Cancer remains a significant global health challenge, necessitating the discovery of novel therapeutic agents.
- Marine organisms, such as those producing coelenterazine, are a rich source of bioactive compounds.
- Coelenterazine and its metabolite coelenteramine are key components of marine bioluminescent systems.
Purpose of the Study:
- To comparatively investigate the anticancer activity of marine coelenterazine and coelenteramine analogs.
- To elucidate structure-activity relationships and differences in the mode of action between these analog classes.
- To assess the safety profile of these analogs on noncancerous cells.
Main Methods:
- Synthesis and characterization of coelenterazine and coelenteramine analogs.
- In vitro evaluation of anticancer activity against lung and gastric cancer cell lines.
- Assessment of time-dependent activity and structure-activity relationships.
- Evaluation of cytotoxicity against noncancerous cell lines.
- Correlation analysis between anticancer activity and light-emission properties.
Main Results:
- Both coelenterazine and coelenteramine analogs demonstrated significant anticancer activity against tested cancer cell lines.
- Distinct structure-activity relationships were observed between the two analog classes.
- Coelenteramine analogs exhibited time-dependent activity, whereas coelenterazine analogs showed time-independent effects.
- Coelenterazine analogs displayed a more favorable safety profile toward noncancer cells compared to coelenteramine analogs.
- A correlation was identified between the anticancer efficacy of coelenterazine analogs and their light-emission characteristics.
Conclusions:
- Marine coelenterazine and coelenteramine analogs represent promising candidates for anticancer drug development.
- Coelenterazine analogs, with their favorable safety and linked luminescence, warrant further investigation as potential cancer therapeutics.
- Understanding the distinct mechanisms of action and structure-activity relationships can guide the design of more effective anticancer agents from this marine system.
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