A novel inhibitor of topoisomerase I designated as isoaurostatin (1) was is
olated from the culture filtrate of Thermomonospora alba strain No. 1520. T
he structure of 1 was determined to be 6,4'-dihydroxyisoaurone on the basis
of spectroscopic (NMR and MS) methods. Compound 1 inhibited the relaxation
activity of calf thymus topoisomerase I in a noncompetitive manner and did
not inhibit the relaxation and decatenation of human placenta topoisomeras
e II. Compound 1 is an inhibitor belonging to cleavable complex-nonforming
type without DNA intercalation.