J Med Chem. 2001 Jun; 44(13): 2065-8.

Potential new antitumor agents from an innovative combination of demethylcantharidin, a modified traditional Chinese medicine, with a platinum moiety.

Ho YP, To KK, Au-Yeung SC, Wang X, Lin G, Han X.

School of Pharmacy, Department of Pharmacology, The Chinese University of Hong Kong, Shatin, New Territories, Hong Kong, The People's Republic of China. [email protected]

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.