2070-DTI, a topoisomerase inhibitor produced by Streptomyces sp. strain No. 2070.
A novel inhibitor of topoisomerase II designated as 2070-DTI was isolated from the culture filtrate of Streptomyces sp. strain No. 2070. The structure was determined to be that of the known soyasaponin I on the basis of spectroscopic methods (NMR and MS). 2070-DTI strongly inhibited the decatenation activity of human placenta topoisomerase II in a noncompetitive manner, and weakly inhibited or was inert towards the relaxation activities of various topoisomerase I's and DNA-related enzymes. 2070-DTI is an inhibitor belonging to the cleavable complex-nonforming type without DNA intercalation.
Department of Pharmaceutical Microbiology, Faculty of Medical and Pharmaceutical Sciences, Kumamoto University, Kumamoto 862-0973, Japan.
Keitarou
K
Suzuki
Satoru
S
Doi
Shoji
S
Yahara
Masaru
M
Uyeda
D000818:Animals; D002166:Camptothecin / Q000378:metabolism / Q000494:pharmacology; D002240:Carbohydrate Sequence; D002417:Cattle; D002453:Cell Cycle / Q000187:drug effects; D002522:Chlorocebus aethiops; D004247:DNA / Q000187:drug effects; D004264:DNA Topoisomerases, Type I / Q000378:metabolism; D004250:DNA Topoisomerases, Type II / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D004317:Doxorubicin / Q000378:metabolism / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000302:isolation & purification / Q000378:metabolism / Q000494:pharmacology*; D005047:Etoposide / Q000378:metabolism / Q000494:pharmacology; D006367:HeLa Cells; D006801:Humans; D051379:Mice; D008969:Molecular Sequence Data; D041681:NIH 3T3 Cells; D009828:Oleanolic Acid / Q000031:analogs & derivatives* / Q000737:chemistry / Q000302:isolation & purification / Q000378:metabolism / Q000494:pharmacology*; D012503:Saponins / Q000737:chemistry / Q000302:isolation & purification / Q000378:metabolism / Q000494:pharmacology*; D013302:Streptomyces / Q000737:chemistry*; D059004:Topoisomerase I Inhibitors; D059005:Topoisomerase II Inhibitors; D014709:Vero Cells
D004791:Enzyme Inhibitors; D012503:Saponins; D059004:Topoisomerase I Inhibitors; D059005:Topoisomerase II Inhibitors; C056684:soyasaponin I; D005047:Etoposide; D009828:Oleanolic Acid; D004317:Doxorubicin; D004247:DNA; D004264:DNA Topoisomerases, Type I; D004250:DNA Topoisomerases, Type II; D002166:Camptothecin