Phenacein--an angiotensin-converting enzyme inhibitor produced by a streptomycete. I. Taxonomy, fermentation and biological properties.

Phanacein, 3,6-dihydroxy-1-phenazinecarboxylic acid, was a specific angiotensin-converting enzyme (ACE) inhibitor isolated from a member of the Streptomyces tanashiensis-zaomyceticus group. Phenacein acted as a pure competitive inhibitor with a Ki of 0.58 microM. ACE inhibition could be reversed by Zn++, but not by Co++, Ca++, or Mg++; therefore, phenacein may chelate the active site zinc of ACE. However, other zinc-containing enzymes were not inhibited at high phenacein concentrations. Phenacein exhibited weak activity against Gram-positive bacteria, but was not active against Candida sp. or Gram-negative organisms.