ICM0301s, New Angiogenesis Inhibitors from Aspergillus sp. F-1491: I. Taxonomy, Fermentation, Isolation and Biological Activities

Abstract

In the course of screening program for inhibitors of angiogenesis, novel substances designated as ICM0301A-H (1-8) were isolated from the culture broth of Aspergillus sp. F-1491. ICM0301s inhibited the growth of human umbilical vein endothelial cells (HUVECs) induced by basic fibroblast growth factor (bFGF) with IC₅₀ values of 2.2-9.3μg/ml. ICM0301A (1) showed significant anti-angiogenic activity at lower than 10μg/ml in the angiogenesis model using rat aorta cultured in fibrin gel. ICM0301s showed very low cytotoxicity against various tumor cells. Furthermore, ICM0301A did not show any toxic symptom in mice by intraperitoneal injection at 100mg/kg.