Novel 20-epi-vitamin D3 analog combined with 9-cis-retinoic acid markedly inhibits colony growth of prostate cancer cells

Prostate. 1999 Aug 1;40(3):141-9. doi: 10.1002/(sici)1097-0045(19990801)40:3<141::aid-pros1>3.0.co;2-c.

Abstract

Background: 1,25 dihydroxyvitamin D3 (1,25D) and retinoids may play an important role in preventing progression of prostate cancer.

Methods: We examined the ability of four novel 20-epi-vitamin D3 analogs (CB1093, KH1060, KH1266, and CB1267), either alone or in combination with 9-cis retinoic acid (RA) to inhibit colony growth of a human prostate cancer cell line, LNCaP, using soft agar as well as bone marrow stroma. Also, the effect of these analogs on the cell cycle and expression of Ki-67, p21(waf-1), and p27(kip1) in LNCaP cells was examined.

Results: The analog CB1267 was the most potent, with 8 x 10(-10) M of the analog inhibiting 50% colony growth (ED50) of LNCaP. 9-cis-RA also inhibited colony growth of LNCaP (ED50, 5 x 10(-7) M). Combined, CB1267 and 9-cis-RA synergistically inhibited colony growth and significantly increased the number of LNCaP cells in G0/G1 phase. Cell cycle arrest was associated with increased levels of p21(waf-1) and p27(kip1) and decreased expression of Ki-67 protein. Pulse-exposure to this combination (5 x 10(-8) M) irreversibly inhibited colony growth, both in soft agar and on normal human bone marrow stroma.

Conclusions: Combination of a new vitamin D3 analog (CB1267) and a retinoid (9-cis-RA) potently inhibited colony formation of LNCaP prostate cancer cells in vitro, suggesting further studies in animal models. This combination may afford an interesting therapeutic approach to low-burden prostate cancer.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Alitretinoin
  • Antineoplastic Agents / toxicity*
  • Bone Marrow Cells / cytology
  • Calcitriol / analogs & derivatives*
  • Calcitriol / toxicity*
  • Cell Cycle / drug effects*
  • Cell Cycle Proteins*
  • Cell Division / drug effects
  • Cell Survival / drug effects
  • Cyclin-Dependent Kinase Inhibitor p21
  • Cyclin-Dependent Kinase Inhibitor p27
  • Cyclins / metabolism
  • Drug Synergism
  • Humans
  • Male
  • Microtubule-Associated Proteins / metabolism
  • Prostatic Neoplasms
  • Stromal Cells / cytology
  • Stromal Cells / drug effects
  • Tretinoin / toxicity*
  • Tumor Cells, Cultured
  • Tumor Suppressor Proteins*

Substances

  • Antineoplastic Agents
  • CB 1093
  • CB 1267
  • CDKN1A protein, human
  • Cell Cycle Proteins
  • Cyclin-Dependent Kinase Inhibitor p21
  • Cyclins
  • KH 1266
  • Microtubule-Associated Proteins
  • Tumor Suppressor Proteins
  • KH 1060
  • Cyclin-Dependent Kinase Inhibitor p27
  • Alitretinoin
  • Tretinoin
  • Calcitriol