Sapintoxin A. A fluorescent phorbol ester that is a potent activator of protein kinase C but is not a tumour promoter.

Abstract

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.

• Authors: G Brooks, A T Evans, A Aitken, F J Evans
• Journal: Cancer letters (Cancer Lett) Vol. 38 Issue 1-2 Pg. 165-70 (Dec 1987) ISSN: 0304-3835 [Print] Ireland
• PMID: 3690506 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Phorbol Esters
• sapintoxin A
• Protein Kinase C

Topics

• Animals
• Enzyme Activation (drug effects)
• Female
• Mice
• Neoplasms, Experimental (chemically induced)
• Phorbol Esters (pharmacology)
• Protein Kinase C (metabolism)