CJ-12,373, A NOVEL TOPOISOMERASE-II INHIBITOR - FERMENTATION, ISOLATION, STRUCTURE ELUCIDATION AND BIOLOGICAL-ACTIVITIES

A novel isochroman carboxylic acid CJ-12,373 was isolated from Penicil lium sp. CL22557. CJ-12,373 inhibits both DNA gyrase-mediated supercoi ling and relaxation without the formation of a cleavage intermediate, suggesting that CJ-12,373 inhibits DNA gyrase at a stage distinct from the religation step. CJ-12,373 is not selective for procaryotic DNA g yrase as it also inhibits relaxation mediated by eukaryotic topoisomer ase II. The antimicrobial potency of CJ-12,373, however, is largely at tributed to its inhibition of DNA gyrase.