Sapintoxin A. A fluorescent phorbol ester that is a potent activator of protein kinase C but is not a tumour promoter.
In this communication we report on the activity of the naturally occurring, highly fluorescent phorbol ester Sapintoxin A (12-o-[2-methylaminobenzoate]-4-deoxyphorbol 13-acetate). This compound potently activates the enzyme protein kinase C (PKC) (Ka 76 nM) but is neither a complete nor second-stage tumour promoter in traditional Berenblum tests. Sapintoxin A has properties in common with promoters such as 12-o-tetradecanoylphorbol 13-acetate (TPA) in that it will induce erythema in vivo, induce lymphocyte mitogenesis in vitro and cause aggregation of human and rabbit platelets. Accordingly, Sapintoxin A is a suitable negative control compound for biochemical studies concerning the involvement of PKC in tumour promotion and cell proliferation.
Department of Pharmacognosy, School of Pharmacy, University of London, U.K.
G
G
Brooks
A T
AT
Evans
A
A
Aitken
F J
FJ
Evans
D000818:Animals; D004789:Enzyme Activation / Q000187:drug effects; D005260:Female; D051379:Mice; D009374:Neoplasms, Experimental / Q000139:chemically induced*; D010703:Phorbol Esters / Q000494:pharmacology*; D011493:Protein Kinase C / Q000378:metabolism*
D010703:Phorbol Esters; C032016:sapintoxin A; D011493:Protein Kinase C