NOVEL COMPOUND, CIS-FUMAGILLIN, INHIBITING ANGIOGENESIS AND ANGIOGENESIS-INHIBITING COMPOSITION CONTAINING THE SAME

摘要

PURPOSE: A novel compound, cis-fumagillin, inhibiting angiogenesis and an angiogenesis-inhibiting composition containing the compound are provided for the prevention and treatment of cancer, rheumatic arthritis, chronic inflammation, diabetic retinopathy or angioma. CONSTITUTION: The cis-fumagillin of formula (I) is isolated and purified by the following steps of: incubating Penicillium janczewskii F2641 at 24 to 26deg.C for 3 to 5 days; extracting the fermented medium with organic solvents; concentrating the extract under reduced pressure and drying it to obtain the crude extract; passing the crude extract through the column packed with silica gel by using methanol/chloroform mixture to isolate the active fraction; passing the active fraction through the column using methanol/distilled water mixture as an eluent to obtain the active fraction; esterifying the active fraction then treating it the thin layer chromatography to obtain the active fraction; and treating the active fraction with the liquid chromatography using cyanide methane/distilled water mixture as an eluent. The angiogenesis-inhibiting composition contains cis-fumagillin of formula (I) or pharmaceutically acceptable salts thereof as an active ingredient.