Estimation of tumor promoting activity and structure-function relationships of aplysiatoxins

1 January 1984

journal article
research article
Published by Oxford University Press (OUP) in Carcinogenesis: Integrative Cancer Research

Vol. 5 (3) , 315-318
https://doi.org/10.1093/carcin/5.3.315

Abstract

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.

Keywords

TETRADECANOYLPHORBOL ACETATE

This publication has 1 reference indexed in Scilit:

Direct measurment of specific binding of highly lipophilic phorbol diester to mouse epidermal membranes using cold acetone
Biochemical and Biophysical Research Communications, 1981