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Distinct effects of novel naphtoquinone-based triazoles in human leukaemic cell lines
Tangbadioa H Coulidiati1, Bruna B Dantas1, Glaucia V Faheina-Martins1
1Departamento de Biotecnologia, Centro de Biotecnologia, Universidade Federal da Paraíba, João Pessoa, Brazil.
Objectives:
The aim of this study was to investigate the cytotoxic effect of new 1,4-naphthoquinone- 1,2,3-triazoles, named C2 to C8 triazole derivatives, towards human cancer cell lines.
Methods:
The effect on cell viability was assessed by MTT and propidium iodide assays. The cytotoxic effect of C2 and C3 in K562 and HL-60 cells were analyzed by flow cytometry, DNA fragmentation and reactive oxygen species (ROS) production. Western blot and q-PCR procedures were also performed.
Key Findings:
C2 and C3 inhibited both K562 and HL-60 cells growth in a concentration-dependent manner. C2 presented the highest cytotoxic activity with an IC50 of approximately 14 μm and 41 μm for HL-60 and K562 cells, respectively, while being less toxic to normal peripheral blood monocyte cells. Both derivatives induced cellular changes in HL-60 cells, characteristic of apoptosis, such as mitochondrial membrane depolarization, phosphatidylserine externalization, increasing sub-G1 phase, DNA fragmentation, downregulating Bcl-2 protein and upregulating Bax protein. In K562 cells, C2 and C3 induced S-phase arrest of cell cycle, which was associated with upregulation of p21. The effect of these derivatives in HL-60 cells can be related to the ROS intracellular level.
Conclusion:
Taken together our results showed that C2 and C3 triazole derivatives presented the best potential for drug design.
Insights
New triazole derivatives, C2 and C3, show potent anticancer activity against human cancer cell lines. These compounds effectively inhibit cancer cell growth and induce apoptosis, offering promising potential for drug design.
Area of Science:
- Medicinal Chemistry
- Cancer Biology
- Pharmacology
Background:
- 1,4-naphthoquinone derivatives are recognized for their diverse biological activities.
- Triazole moieties are frequently incorporated into drug candidates to enhance pharmacological properties.
Purpose of the Study:
- To evaluate the cytotoxic effects of novel 1,4-naphthoquinone-1,2,3-triazole derivatives (C2-C8) on human cancer cell lines.
- To identify specific derivatives with significant anticancer potential and elucidate their mechanisms of action.
Main Methods:
- MTT and propidium iodide assays for cell viability assessment.
- Flow cytometry, DNA fragmentation, and reactive oxygen species (ROS) production analysis for C2 and C3.
- Western blot and quantitative PCR (q-PCR) for molecular target investigation.
Main Results:
- C2 and C3 demonstrated concentration-dependent inhibition of K562 and HL-60 cell growth.
- C2 exhibited potent cytotoxicity (IC50 ~14 μm for HL-60, ~41 μm for K562) with lower toxicity to normal cells.
- Apoptosis induction in HL-60 cells (via ROS, Bcl-2/Bax modulation) and S-phase arrest in K562 cells (via p21 upregulation) were observed.
Conclusions:
- The triazole derivatives C2 and C3 show significant potential as anticancer agents.
- These compounds represent promising scaffolds for future drug design and development in oncology.
