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. yeepingho@cuhk.edu.hk

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.