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  • Title: Growth inhibitory effects on human colon adenocarcinoma-derived Caco-2 cells and calcemic potential of 1 alpha,25-dihydroxyvitamin D3 analogs: structure-function relationships.
    Author: Bischof MG, Redlich K, Schiller C, Chirayath MV, Uskokovic M, Peterlik M, Cross HS.
    Journal: J Pharmacol Exp Ther; 1995 Dec; 275(3):1254-60. PubMed ID: 8531089.
    Abstract:
    A panel of synthetic analogs of 1 alpha,25-dihydroxyvitamin D3 [1 alpha,25(OH)2D3] bearing one or multiple structural modifications at functionally or metabolically sensitive positions of the molecule, i.e., C-1, 16, 23, 26 and 27, were tested for their growth inhibitory and prodifferentiating potency in human colon adenocarcinoma-derived Caco-2 cells. With respect to the peak response elicited at 10(-8) M, 1 alpha,25-dihydroxy-16-ene-vitamin D3, 1 alpha,25-dihydroxy-23-yne-vitamin D3 and 1 alpha,25-dihydroxy-16,23Z-diene-vitamin D3 suppressed [3H]thymidine incorporation in confluent Caco-2 cells less than 1 alpha,25(OH)2D3. 1 alpha,25-dihydroxy-16,23e-diene-vitamin D3 was at least equipotent to the parent compound, whereas 1 alpha,25-dihydroxy-16-ene-23-yne-vitamin D3 and most conspicuously 1 alpha,25-dihydroxy-26,27-hexafluoro-16-ene-23-yne- vitamin D3 reduced growth of Caco-2 cells to significantly (P < .05) lower levels than 1 alpha,25(OH)2D3. The same rank order was obtained for the ability of the vitamin D compounds to induce activity of the differentiation marker enzyme, alkaline phosphatase, in quiescent Caco-2 cells. Whereas the effect of the synthetic analogs on calcium uptake by cultured embryonic chick duodenum in general was less pronounced than that of 1 alpha,25(OH)2D3, the two most potent antimitogenic compounds, 1 alpha,25-dihydroxy-16-ene-23-yne-vitamin D3 and 1 alpha,25-dihydroxy-26,27-hexafluoro-16-ene-23-yne-vitamin D3, elicited calcium mobilization from cultured neonatal mouse calvaria at a 10-fold lower concentration than the parent compound.(ABSTRACT TRUNCATED AT 250 WORDS)
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