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Alpha-Terpineol as Antitumor Candidate in Pre-Clinical Studies
Helber A Negreiros1, Kariely Gonçalves de Moura2, Maria L L Barreto do Nascimento1
1Toxicological Genetics Research Laboratory (LAPGENIC), Postgraduate Program in Pharmaceutical Sciences, Federal University of Piaui, Teresina, Piaui, Brazil.
Background:
Alpha-terpineol is monoterpene alcohol with anti-tumor activity against different tumor cell lines (lung, breast, leukemias and colorectal) through blockage of NF-kB expression, which play an important role in tumor cells growth.
Objective:
Evaluate the antitumor activity of alpha-terpineol in murine Sarcoma 180 cell line.
Methods:
For the tests, different cytotoxic and genotoxic assays were used, including Trypan blue, cytokinesis- blocked micronucleus assay, comet assay, agarose gel DNA fragmentation, flow cytometry and cell viability using fluorescence. Ascitic fluid cells from sarcoma 180 were obtained from Mus musculus peritoneal cavity and Alpha-terpineol was tested at 100, 250 and 500 μg/mL. Doxorubicin and Cisplatin were used as positive controls.
Results:
Cytotoxic effects of alpha-terpineol were found in all concentrations tested, reducing cell viability in 50.9; 38.53; 30.82% at 100, 250 and 500 μg/mL, respectively. Alpha-terpineol induced genotoxic effects due to DNA fragmentation (increased frequency and index of damage), and was clastogenic by increased micronuclei formation, nucleoplasmic bridges and nuclear buds. DNA fragmentation and increased cell death indicated that alpha-terpineol can cause early, late, and necrotic apoptosis.
Conclusion:
Our data indicate that alpha-terpineol has antitumor activity revealed by cytogenetic mechanisms and / or loss of cell membrane integrity.
Insights
Alpha-terpineol demonstrates antitumor properties by inducing cell death and DNA damage in cancer cells. This monoterpene alcohol shows potential as a therapeutic agent against various tumor types.
Area of Science:
- Pharmacology
- Oncology
- Natural Products
Background:
- Alpha-terpineol, a monoterpene alcohol, exhibits known anti-tumor activity.
- It functions by inhibiting NF-kB expression, crucial for tumor cell proliferation.
Purpose of the Study:
- To investigate the anti-tumor effects of alpha-terpineol.
- To evaluate its efficacy against the murine Sarcoma 180 cell line.
Main Methods:
- Cytotoxic and genotoxic assays were employed, including Trypan blue, micronucleus assay, comet assay, and DNA fragmentation analysis.
- Alpha-terpineol was tested at concentrations of 100, 250, and 500 μg/mL on Sarcoma 180 cells.
- Doxorubicin and Cisplatin served as positive controls.
Main Results:
- Alpha-terpineol significantly reduced cell viability across all tested concentrations.
- Genotoxic effects were observed, including DNA fragmentation and increased micronuclei formation, indicating clastogenic activity.
- Apoptosis, including early, late, and necrotic forms, was induced by alpha-terpineol.
Conclusions:
- Alpha-terpineol possesses significant anti-tumor activity.
- The anti-tumor effects are mediated through cytogenetic mechanisms and disruption of cell membrane integrity.
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