UCE6, a new antitumor antibiotic with topoisomerase I-mediated DNA cleavage activity produced by actinomycetes: producing organism, fermentation, isolation and biological activity.
A novel antitumor antibiotic, UCE6 (1,3,8,10,11-pentahydroxy-2-methyl-10-(2-oxo-4-hydroxypentyl)na phthacene-5, 12-dione) with topoisomerase I-mediated DNA cleavage activity, was isolated from the culture broth of actinomycetes strain UOE6. Addition of silicone oil antifoam agent, KS69 (2%), to the fermentation enhanced the production of UCE6 by approximately 3 fold. A total of 1.15 g of UCE6 was recovered as reddish orange crystals from a 100 liter fermentation supplemented with 2% KS69. UCE6 exhibited growth inhibitory activity against HeLa S3, HCT116 and Lu-65 cells comparable to that of camptothecin.
Fujii
N
N
Kyowa Hakko Kogyo Co. Ltd., Technical Research Laboratories, Hofu, Yamaguchi, Japan.
Tanaka
F
F
Yamashita
Y
Y
Ashizawa
T
T
Chiba
S
S
Nakano
H
H
D000190:Actinomyces / Q000737:chemistry / Q000378:metabolism*; D000903:Antibiotics, Antineoplastic / Q000096:biosynthesis* / Q000302:isolation & purification / Q000494:pharmacology*; D004264:DNA Topoisomerases, Type I / Q000378:metabolism*; D004273:DNA, Neoplasm / Q000187:drug effects* / Q000378:metabolism*; D005285:Fermentation; D006367:HeLa Cells; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy; D011809:Quinones / Q000302:isolation & purification / Q000378:metabolism / Q000494:pharmacology; D014407:Tumor Cells, Cultured
D000903:Antibiotics, Antineoplastic; D004273:DNA, Neoplasm; D011809:Quinones; C082796:UCE6; D004264:DNA Topoisomerases, Type I