demethylcantharidin and Colorectal-Neoplasms

demethylcantharidin has been researched along with Colorectal-Neoplasms* in 2 studies

Other Studies

2 other study(ies) available for demethylcantharidin and Colorectal-Neoplasms

ArticleYear
DNA damage induced by novel demethylcantharidin-integrated platinum anticancer complexes.
    Biochemical and biophysical research communications, 2007, Nov-09, Volume: 363, Issue:1

    Oxaliplatin is a third generation platinum (Pt) drug with a diaminocyclohexane (DACH) entity, which has recently obtained worldwide approval for the clinical treatment of colon cancer, and apparently operates by a different mechanism of action to the classical cisplatin or carboplatin. Introducing a novel dual mechanism of action is one approach in designing a new platinum-based anticancer agent, whereby an appropriate ligand, such as demethylcantharidin (DMC), is released from the parent compound to exert a cytotoxic effect, in addition to that of the DNA-alkylating function of the platinum moiety. To investigate the likelihood of a novel dual mechanism of anticancer action, demethylcantharidin-integrated Pt complexes: Pt(R,R-DACH)(DMC) with the same Pt-DACH moiety as oxaliplatin, and Pt(NH(3))(2)(DMC) akin to carboplatin; were studied for their ability to induce DNA damage in HCT116 colorectal cancer cells by an alkaline comet assay. The results showed that the DMC ligand released from the novel complexes caused additional DNA lesions when compared with oxaliplatin and carboplatin. The comet assay also revealed that the DNA-damaging behavior of cisplatin is characteristically different; and this study is the first to demonstrate the ability of DMC to induce DNA lesions, thus providing sufficient evidence to explain the superior antiproliferative effect of the novel DMC-integrated complexes.

    Topics: Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Cantharidin; Cell Line, Tumor; Colorectal Neoplasms; DNA Damage; DNA, Neoplasm; Humans; Platinum

2007
Anticancer activity of a series of platinum complexes integrating demethylcantharidin with isomers of 1,2-diaminocyclohexane.
    Bioorganic & medicinal chemistry letters, 2006, Mar-15, Volume: 16, Issue:6

    A series of platinum complexes derived from integrating demethylcantharidin (DMC) with different isomers of 1,2-diaminocyclohexane (DACH) has been synthesized and found to exhibit superior in vitro anticancer activity against colorectal and human hepatocellular cancer cell lines when compared with oxaliplatin, cisplatin, and carboplatin. Flow cytometric analysis revealed that the trans-DACH-Pt-DMC analogues showed similar behavior to oxaliplatin on affecting the cell cycle of the HCT116 colorectal cancer cell line, but distinct from that of cisplatin or carboplatin. The DACH component apparently dictates the trans-DACH-Pt-DMC complexes to behave mechanistically similar to oxaliplatin, whereas the DMC ligand appears to enhance the compounds' overall anticancer activity, probably by accelerating the cell cycle from G1 to S-phase with subsequent onset of G2/M arrest and accompanying apoptosis.

    Topics: Antineoplastic Agents; Apoptosis; Cantharidin; Carboplatin; Carcinoma, Hepatocellular; Cell Cycle; Cisplatin; Colorectal Neoplasms; Cyclohexylamines; Drug Resistance, Neoplasm; Drug Screening Assays, Antitumor; Flow Cytometry; Humans; Isomerism; Liver Neoplasms; Organoplatinum Compounds; Oxaliplatin; Platinum; Tumor Cells, Cultured

2006