15 research outputs found
Naphthoquinones from Onosma paniculata induce cell-cycle arrest and apoptosis in melanoma cells
Activity-guided fractionation of a petroleum ether-soluble extract of the roots of Onosma paniculata, which has been shown to affect the cell cycle and to induce apoptosis in melanoma cells, led to the isolation of several shikonin derivatives, namely, β-hydroxyisovalerylshikonin (1), acetylshikonin (2), dimethylacrylshikonin (3), and a mixture of α-methylbutyrylshikonin and isovalerylshikonin (4+5). All compounds exhibited strong cytotoxicity against eight cancer cell lines and MRC-5 lung fibroblasts, with 3 found to possess the most potent cytotoxicity toward four melanoma cell lines (SBcl2, WM35, WM9, and WM164). Furthermore, 3 and the mixture of 4+5 were found to interfere with cell-cycle progression in these cell lines and led to an increasing number of cells in the subG1 region as well as to caspase-3/7 activation, indicating apoptotic cell death
Synthesis of the NK1 Receptor Antagonist GW597599. Part 3: Development of a Scalable Route to a Key Chirally Pure Arylpiperazine Urea, A Happy End
Naphthoquinones from <i>Onosma paniculata</i> Induce Cell-Cycle Arrest and Apoptosis in Melanoma Cells
Activity-guided fractionation of a petroleum ether-soluble
extract of the roots of <i>Onosma paniculata</i>, which
has been shown to affect the cell cycle and to induce apoptosis in
melanoma cells, led to the isolation of several shikonin derivatives,
namely, β-hydroxyisovalerylshikonin (<b>1</b>), acetylshikonin
(<b>2</b>), dimethylacrylshikonin (<b>3</b>), and a mixture
of α-methylbutyrylshikonin and isovalerylshikonin (<b>4</b>+<b>5</b>). All compounds exhibited strong cytotoxicity against
eight cancer cell lines and MRC-5 lung fibroblasts, with <b>3</b> found to possess the most potent cytotoxicity toward four melanoma cell lines (SBcl2, WM35, WM9, and WM164). Furthermore, <b>3</b> and the mixture of <b>4</b>+<b>5</b> were found
to interfere with cell-cycle progression in these cell lines and led
to an increasing number of cells in the subG1 region as well as to
caspase-3/7 activation, indicating apoptotic cell death