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Kretschmer, N; Rinner, B; Deutsch, AJ; Lohberger, B; Knausz, H; Kunert, O; Blunder, M; Boechzelt, H; Schaider, H; Bauer, R.
Naphthoquinones from Onosma paniculata induce cell-cycle arrest and apoptosis in melanoma Cells.
J Nat Prod. 2012; 75(5):865-869
Doi: 10.1021/np2006499
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- Führende Autor*innen der Med Uni Graz
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Kretschmer Nadine
- Co-Autor*innen der Med Uni Graz
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Deutsch Alexander
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Knausz Heike
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Lohberger Birgit
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Rinner Beate
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Schaider Helmut
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- Abstract:
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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.
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Antineoplastic Agents, Phytogenic - chemistry
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Antineoplastic Agents, Phytogenic - isolation & purification
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Antineoplastic Agents, Phytogenic - pharmacology
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Apoptosis - drug effects
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Boraginaceae - chemistry
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Caspase 3 - drug effects
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Caspase 3 - metabolism
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Caspase 7 - drug effects
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Caspase 7 - metabolism
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Cell Cycle - drug effects
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Drug Screening Assays, Antitumor -
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Drugs, Chinese Herbal - chemistry
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Drugs, Chinese Herbal - isolation & purification
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Drugs, Chinese Herbal - pharmacology
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Humans -
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Melanoma -
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Molecular Structure -
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Naphthoquinones - chemistry
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Naphthoquinones - isolation & purification
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Naphthoquinones - pharmacology
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Plant Roots - chemistry