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Updated: Apr 28, 2026
Preclinical Assessment of the Bioactivity of the Anticancer Coumarin OT48 by Spheroids, Colony Formation Assays, and Zebrafish Xenografts
Published on: June 26, 2018
Oxazine derivatives of γ- and δ-tocotrienol display enhanced anticancer activity in vivo
Suryatheja Ananthula1, Parash Parajuli1, Fathy A Behery1
1School of Pharmacy, University of Louisiana at Monroe, Monroe, LA, U.S.A.
Background:
Oxazine derivatives of tocotrienols display enhanced anticancer activity. Studies were conducted to further characterize these effects in vivo.
Materials And Methods:
Tetrazolium assay was used to determine the inhibitory effects of oxazine derivatives of γ-tocotrienol and δ-tocotrienol in vitro. These compounds were further formulated as lipid nanoemulsions and intralesional administration was used to examine their anticancer activity in vivo.
Results:
Tocotrienol oxazine derivatives significantly inhibited +SA mammary tumor growth in syngeneic mice as compared to their respective parent compound, and these effects were associated with a reduction in cell proliferation and survival (phosphorylated protein kinase B (AKT) and nuclear factor kappa-light-chain-enhancer of activated B cells (NFκB), and cyclooxygenase-2 (COX2) and cell-cycle progression (cyclin D1, cyclin-dependent kinase 2 (CDK2), CDK4 and CDK6) markers, and increase in cell-cycle arrest proteins (p21 and p27).
Conclusion:
Tocotrienol oxazine derivatives may provide benefit as therapeutic agents against breast cancer.
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