Discovery of an angiotensin II binding inhibitor from a Cytospora sp. using semi-automated screening procedures

S Stevens-Miles; M A Goetz; G F Bills; R A Giacobbe; J S Tkacz; R S Chang; M Mojena; I Martin; M T Diez; F Pelaez; O D Hensens; T Jones; R W Burg; Y L Kong; L Huang

doi:10.7164/antibiotics.49.119

Discovery of an angiotensin II binding inhibitor from a Cytospora sp. using semi-automated screening procedures

J Antibiot (Tokyo). 1996 Feb;49(2):119-23. doi: 10.7164/antibiotics.49.119.

Authors

S Stevens-Miles¹, M A Goetz, G F Bills, R A Giacobbe, J S Tkacz, R S Chang, M Mojena, I Martin, M T Diez, F Pelaez, O D Hensens, T Jones, R W Burg, Y L Kong, L Huang

Affiliation

¹ Merck Research Laboratories, Rahway, New Jersey 07065, USA.

PMID: 8621349
DOI: 10.7164/antibiotics.49.119

Abstract

Cytosporin A, B and C, three antagonists of [125I]-angiotensin II binding to rat adrenal glands were discovered in fermentations of an endophytic Cytospora sp. during routine screening using semi-automated procedures. The most potent of these displayed an IC50 of 1.5-3 microM and was specific for angiotensin II AT2.

MeSH terms

Adrenal Glands / metabolism
Angiotensin II / antagonists & inhibitors*
Angiotensin II / metabolism
Animals
Benzopyrans / chemistry
Benzopyrans / pharmacology*
Fermentation
Mass Spectrometry
Mitosporic Fungi / chemistry*
Rats

Substances

Benzopyrans
cytosporin A
cytosporin B
cytosporin C
Angiotensin II