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© 1983 Oxford University Press

research-article

Inhibition of specific binding of [3H]phorbol-12,13-dipropionate to an epidermal fraction by certain irritants and irritant promoters of mouse skin

R. Schmidt 1, W. Adolf 1, A. Mareton 1, H. Roeser 1, B. Sorg 1, H. Fujiki 2, T. Sugimura 2, R.E. Moore 3 and E. Hecker 1

1Institute of Biochemistry, German Cancer Research Center Im Neuenheimer Feld 280, D-6900 Heidelberg, FRG
2National Cancer Center Research Institute 5-1-1, Tsukiji, Chuo-ku, Tokyo 104, Japan
3Department of Chemistry, University of Hawaii Honolulu, HI 96822, USA

Specific binding of [3H]phorbol-12,13-dipropionate ([3H]PDPr) to a participate fraction of mouse skin is demonstrated (KD = 35 nM; Rt = 1.2 pmol/mg protein). A series of compounds of the diterpene ester, indole akaloid and polyacetate types with different degrees of activity as skin tumor promoters and/or irritants have been tested for their capacity to inhibit specific [3H]PDPr binding. Three main categories are found: (i) compounds which exhibit a positive correlation between their potency as irritants and promoters in vivo and their inhibition of specific binding in vitro: 12-O-tetradecanoyiphorbol-13-acetate, 3-O-tetradecanoylingenol, pimelea factor P2, ‘teleocidin’, dihydroteleocidin B, and iyngbyatoxin are active in vivo and in vitro, whereas phorbol and ingenol are inactive and 4-O-methyl-12-C)-tetradecanoyl-phorbol-13-acetate is weakly active; (ii) compounds which are strong irritants and inhibitors of binding but are weak or practically non-promoters: mezerein, 12-O-retinoylphorbol-13-acetate and milliamine C; (iii) strong irritants which are weak or marginally active inhibitors of binding: debromoaplysiatoxin and resiniferatoxin. Some consequences of these findings with respect to interpretations of the biochemical mechanism(s) of tumor promotion are discussed.


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Home page
 Toxicol PatholHome page
E. Hecker
Three Stage Carcinogenesis in Mouse Skin--Recent Results and Present Status of an Advanced Model System of Chemical Carcinogenesis
Toxicol Pathol, February 1, 1987; 15(2): 245 - 258.
[Abstract] [PDF]


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