1. Griseolic acid, an inhibitor of cyclic adenosine 3',5'-monophosphate phosphodiesterase. I. Taxonomy, isolation and characterization
- Author
-
Takao Okazaki, Atsushi Naito, Mitsuo Yamazaki, Fumio Nakagawa, and Yasuteru Iijima
- Subjects
Adenosine ,Chemical Phenomena ,Stereochemistry ,Griseolic acid ,In Vitro Techniques ,chemistry.chemical_compound ,Streptomyces griseoaurantiacus ,Drug Discovery ,Cyclic AMP ,medicine ,Animals ,Moiety ,Aorta ,Pharmacology ,chemistry.chemical_classification ,Phosphodiesterase ,Phosphate ,Streptomyces ,Rats ,Chemistry ,Enzyme ,Adenosine 3 5 monophosphate ,chemistry ,Biochemistry ,3',5'-Cyclic-AMP Phosphodiesterases ,medicine.drug - Abstract
Griseolic acid, a potent inhibitor of cyclic adenosine 3',5'-monophosphate (cyclic AMP) phosphodiesterase (EC 3.1.4.17) was isolated from the cultured broth of Streptomyces griseoaurantiacus SANK 63479. Griseolic acid has an adenine moiety and two carboxyl groups and possesses the molecular formula C14H13N5O8. Griseolic acid inhibited cyclic AMP phosphodiesterase competitively with regard to cyclic AMP, the substrate and the resulting Ki value was 0.26 microM. Griseolic acid showed the most potent inhibitory effect on rat aorta cyclic AMP phosphodiesterase among the enzymes of several rat organs tested. The plasma level of cyclic AMP was increased when griseolic acid was subcutaneously injected rats.
- Published
- 1985
- Full Text
- View/download PDF