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. Copyright
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. Copyright
Authors: Suryatheja Ananthula; Parash Parajuli; Fathy A Behery; Alaadin Y Alayoubi; Sami Nazzal; Khalid El Sayed; Paul W Sylvester Journal: Biomed Res Int Date: 2014-07-22 Impact factor: 3.411
Authors: Chakrabhavi Dhananjaya Mohan; Hanumantharayappa Bharathkumar; Shobith Rangappa; Muthu K Shanmugam; Arunachalam Chinnathambi; Sulaiman Ali Alharbi; Tahani Awad Alahmadi; Atanu Bhattacharjee; Peter E Lobie; Amudha Deivasigamani; Kam Man Hui; Gautam Sethi; Kanchugarakoppal S Rangappa; Alan Prem Kumar Journal: Front Pharmacol Date: 2018-11-05 Impact factor: 5.810