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[Cancer Research 66, 412-418, January 1, 2006]
© 2006 American Association for Cancer Research

Experimental Therapeutics, Molecular Targets, and Chemical Biology

Inhibition of Bladder Tumor Growth by 1,1-Bis(3'-Indolyl)-1-(p-Substitutedphenyl)Methanes: A New Class of Peroxisome Proliferator-Activated Receptor {gamma} Agonists

Wassim Kassouf1, Sudhakar Chintharlapalli4, Maen Abdelrahim3, Gina Nelkin1, Stephen Safe3,4 and Ashish M. Kamat1,2

Departments of 1 Urology and 2 Cancer Biology, The University of Texas M.D. Anderson Cancer Center; 3 Institute of Biosciences and Technology, Texas A&M University System Health Science Center, Houston, Texas; and 4 Department of Biochemistry and Biophysics, Texas A&M University, College Station, Texas

Requests for reprints: Ashish M. Kamat, Department of Urology, The University of Texas M.D. Anderson Cancer Center, Unit 1373, 1515 Holcombe Boulevard, Houston, TX 77030. Phone: 713-792-3250; Fax: 713-794-4824; E-mail: akamat{at}mdanderson.org.

1,1-Bis(3'-indolyl)-1-(p-substitutedphenyl)methanes containing p-trifluoromethyl (DIM-C-pPhCF3), p-t-butyl (DIM-C-pPhtBu), and phenyl (DIM-C-pPhC6H5) substituents have been identified as a new class of peroxisome proliferator-activated receptor {gamma} (PPAR{gamma}) agonists that exhibit antitumorigenic activity. The PPAR{gamma}-active C-DIMs have not previously been studied against bladder cancer. We investigated the effects of the PPAR{gamma}-active C-DIMs on bladder cancer cells in vitro and bladder tumors in vivo. In this study, the PPAR{gamma}-active compounds inhibited the proliferation of KU7 and 253J-BV bladder cancer cells, and the corresponding IC50 values were 5 to 10 and 1 to 5 µmol/L, respectively. In the less responsive KU7 cells, the PPAR{gamma} agonists induced caveolin-1 and p21 expression but no changes in cyclin D1 or p27; in 253J-BV cells, the PPAR{gamma} agonists did not affect caveolin-1, cyclin D1, or p27 expression but induced p21 protein. In KU7 cells, induction of caveolin-1 by each of the PPAR{gamma} agonists was significantly down-regulated after cotreatment with the PPAR{gamma} antagonist GW9662. DIM-C-pPhCF3 (60 mg/kg thrice a week for 4 weeks) inhibited the growth of implanted KU7 orthotopic and s.c. tumors by 32% and 60%, respectively, and produced a corresponding decrease in proliferation index. Treatment of KU7 cells with DIM-C-pPhCF3 also elevated caveolin-1 expression by 25% to 30%, suggesting a role for this protein in mediating the antitumorigenic activity of DIM-C-pPhCF3 in bladder cancer. (Cancer Res 2006; 66(1): 412-8)




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