Abstract
We have efficiently synthesized albiziabioside A (1) together with its six disaccharide analogues through a linear synthesis, and evaluated their cytotoxicity against six different skin cancer cells. All of the analogues showed weak cytotoxicity, with the exception of compound 1, which exhibited strong cytotoxicity against A375 cells. Albiziabioside A can induce cell cycle arrest in both the S and G2/M phases. Moreover, albiziabioside A can induce A375 cell apoptosis via mitochondrial pathways involving a caspase cascade. These results provide for the first time a basic mechanism for the anticancer activity of 1.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Amino Acid Chloromethyl Ketones / pharmacology
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology*
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Apoptosis / drug effects*
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Apoptosis / genetics
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Cell Cycle Checkpoints / drug effects
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Cell Cycle Checkpoints / genetics
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Drug Screening Assays, Antitumor
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Gene Expression Regulation, Neoplastic / drug effects
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Humans
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Melanoma / genetics
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Melanoma / pathology*
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Membrane Potential, Mitochondrial / drug effects
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Mitochondria / drug effects
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Mitochondria / metabolism
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Saponins / chemical synthesis*
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Saponins / chemistry
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Saponins / pharmacology*
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Signal Transduction / drug effects
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Signal Transduction / genetics
Substances
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Amino Acid Chloromethyl Ketones
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Antineoplastic Agents
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Saponins
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albiziabioside A
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benzyloxycarbonylvalyl-alanyl-aspartyl fluoromethyl ketone