Estimation of tumor promoting activity and structure-function relationships of aplysiatoxins.
Twelve aplysiatoxin compounds have been evaluated as possible tumor promoters in vivo by means of three biological tests: viz. irritation of mouse ear, induction of ornithine decarboxylase in dorsal skin of mice, and inhibition of specific binding of [3H]12-O-tetradecanoylphorbol-13-acetate (TPA) to an epidermal particulate fraction. The potencies of these three biological activities correlate well for each derivative. Bromoaplysiatoxin shows biological activities that are similar to those of the strong tumor promoter, aplysiatoxin. The present studies suggest that the C-3, C-20 and C-30 hydroxyl groups of the aplysiatoxins are involved in binding to the specific receptor of TPA.
D000818:Animals; D029742:Caenorhabditis elegans Proteins; D002273:Carcinogens; D002352:Carrier Proteins; D004790:Enzyme Induction; D005260:Female; D007783:Lactones / Q000633:toxicity*; D008235:Lyngbya Toxins; D051379:Mice; D008978:Mollusk Venoms / Q000633:toxicity*; D009955:Ornithine Decarboxylase / Q000096:biosynthesis; D011493:Protein Kinase C; D011956:Receptors, Cell Surface / Q000378:metabolism; D011955:Receptors, Drug; D012867:Skin / Q000187:drug effects / Q000201:enzymology; D013329:Structure-Activity Relationship; D013755:Tetradecanoylphorbol Acetate / Q000378:metabolism
D029742:Caenorhabditis elegans Proteins; D002273:Carcinogens; D002352:Carrier Proteins; D007783:Lactones; D008235:Lyngbya Toxins; D008978:Mollusk Venoms; D011956:Receptors, Cell Surface; D011955:Receptors, Drug; C083141:phorbol ester binding protein; C027776:phorbol ester receptor; C006610:aplysiatoxin; D011493:Protein Kinase C; D009955:Ornithine Decarboxylase; D013755:Tetradecanoylphorbol Acetate