Toxins, anticancer agents, and tumor promoters from marine prokaryotes

Abstract

Marine prokaryotic organisms, in particular blue–green algae belonging to the Oscillatoriaceae, are potentially good sources of new antineoplastic agents. The dermatitis–producing substances in the blue–green alga Lyngbya majuscula, however, which exhibit marginal anticancer activities, are powerful tumor promoters. The potencies and modes of action of two of these tumor promoters, aplysiatoxin and lyngbyatoxin A, are essentially identical with the potency and mode of action of the well known tumor promoter from Croton oil, 12–0–tetradecanoylphorbol 13–acetate (TPA). Structure–activity relationships are presented for aplysiatoxin, lyngbyatoxin A, TPA, and related compounds. The absolute stereochemistries of the aplysiatoxin and lyngbyatoxin A are discussed. © 1982, Walter de Gruyter. All rights reserved.