Abstract
A combination of demethylcantharidin, a modified component of a traditional Chinese medicine (TCM), with a platinum moiety has produced a series of TCM-based platinum compounds [Pt(C(8)H(8)O(5))(NH(2)R)(2)] 1-5, which demonstrate selective cytotoxicity toward SK-Hep-1 (human liver) cell line, and circumvention of cross-resistance. The inclusion of demethylcantharidin rendered the compounds highly active as protein phosphatase (PP2A) inhibitors. The new TCM-Pt compounds may possess a novel dual mechanism of antitumor action: inhibition of PP2A and platination of DNA.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antineoplastic Agents, Phytogenic / chemistry*
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Antineoplastic Agents, Phytogenic / therapeutic use
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Bridged Bicyclo Compounds, Heterocyclic / chemical synthesis*
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Bridged Bicyclo Compounds, Heterocyclic / pharmacology*
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Carcinoma, Non-Small-Cell Lung / drug therapy
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Cell Division / drug effects
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DNA, Neoplasm / drug effects
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Enzyme Inhibitors / pharmacology
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Humans
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Leukemia L1210 / drug therapy
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Liver Neoplasms, Experimental / drug therapy
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Liver Neoplasms, Experimental / pathology
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Lung Neoplasms / drug therapy
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Medicine, Chinese Traditional
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Mice
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Mice, Inbred ICR
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Mice, Nude
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Neoplasm Transplantation
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Organoplatinum Compounds / chemistry*
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Organoplatinum Compounds / therapeutic use
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Phosphoprotein Phosphatases / antagonists & inhibitors
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Phytotherapy
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Plants, Medicinal / chemistry
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Tumor Cells, Cultured
Substances
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Antineoplastic Agents, Phytogenic
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Bridged Bicyclo Compounds, Heterocyclic
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DNA, Neoplasm
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Enzyme Inhibitors
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Organoplatinum Compounds
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norcantharidin
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Phosphoprotein Phosphatases