GROWTH-INHIBITION OF HUMAN-MELANOMA CELLS BY VITAMIN-D ANALOGS
- RV BRENNER
- M SHABAHANG
- AM HOUGHTON
- RJ NAUTA
- MR USKOKOVIC
- LM SCHUMAKER
- RR BURAS
- SRT EVANS
Affiliations: GEORGETOWN UNIV,MED CTR,VINCENT T LOMBARDI CANC RES CTR,DEPT SURG,WASHINGTON,DC 20007. HOFFMANN LA ROCHE INC,NUTLEY,NJ 07110.
- Published online on: November 1, 1995 https://doi.org/10.3892/or.2.6.1157
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The antiproliferative activity of 1,25(OH)(2)-vitamin D-3, and four vitamin D analogs was assessed in RPMI-7951, a human melanoma cell line which expresses the vitamin D receptor. Proliferation assays consisted of a [H-3]-thymidine incorporation assay, and a 6-day growth study. The affinity of vitamin D analogs for vitamin D receptor relative to 125(OH)(2)-vitamin D-3 was determined with a hydroxyapatite-based competitive binding assay. For the proliferation assays, cells were treated with 10(-8) M 1,25(OH)(2)-vitamin D-3, 1,25(OH)(2)-16-ene-23-yne-vitamin D-3 (Ro 23-7553), 1,25(OH)(2)-16-ene-23-yne-26,27-hexafluoro-vitamin D-3 (Ro 24-5531), 1,25(OH),-16,23Z-diene-26,27-hexafluoro-vitamin D-3 (Ro 25-5317), and 1 alpha-fluoro-25(OH)- 16-ene-23-yne-hexafluoro-vitamin D-3 (Ro 24-5583). 1,25(OH)(2)-vitamin D-3 and the four analogs all significantly inhibited melanoma cell growth (P<0.05). Competitive binding of the vitamin D analogs to vitamin D receptor ranged from 51% to 72% that of 1,25(OH)(2)-vitamin D-3, suggesting a receptor-mediated response. These results demonstrate that analogs of 1,25(OH)(2)-vitamin D-3 are potent antiproliferative agents in human melanoma cells in vitro.