title: FR258900, a novel glycogen phosphorylase inhibitor isolated from Fungus No. 138354. I. Taxonomy, fermentation, isolation and biological activities.
abstract: FR258900 is a novel glycogen synthesis activator produced by Fungus No. 138354. This compound was isolated from the culture broth by solvent extraction and reverse-phase column chromatography. FR258900 stimulated glycogen synthesis and glycogen synthase activity in primary rat hepatocytes. FR258900 exhibited a potent inhibitory effect on the activity of liver glycogen phosphorylase, suggesting that this compound may activate hepatic glycogen synthesis via glycogen phosphorylase inhibition. Thus, this glycogen phosphorylase inhibitor may be useful in the treatment of postprandial hyperglycemia in type 2 diabetes.
authors.affiliation: Fermentation Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., 5-2-3 Tokodai, Tsukuba, Ibaraki 300-2698, Japan. shigetada.furukawa@jp.astellas.com
authors.forename: Shigetada
authors.initials: S
authors.lastname: Furukawa
authors.forename: Yasuhisa
authors.initials: Y
authors.lastname: Tsurumi
authors.forename: Kana
authors.initials: K
authors.lastname: Murakami
authors.forename: Tomoko
authors.initials: T
authors.lastname: Nakanishi
authors.forename: Keisuke
authors.initials: K
authors.lastname: Ohsumi
authors.forename: Michizane
authors.initials: M
authors.lastname: Hashimoto
authors.forename: Motoaki
authors.initials: M
authors.lastname: Nishikawa
authors.forename: Shigehiro
authors.initials: S
authors.lastname: Takase
authors.forename: Osamu
authors.initials: O
authors.lastname: Nakayama
authors.forename: Motohiro
authors.initials: M
authors.lastname: Hino
mesh_terms: D002851:Chromatography, High Pressure Liquid; D002934:Cinnamates / Q000302:isolation & purification* / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000302:isolation & purification* / Q000494:pharmacology; D005285:Fermentation; D005658:Fungi / Q000737:chemistry / Q000145:classification* / Q000378:metabolism; D005977:Glutarates / Q000302:isolation & purification* / Q000494:pharmacology; D006003:Glycogen / Q000378:metabolism; D024981:Glycogen Phosphorylase / Q000037:antagonists & inhibitors*
chemical_list: D002934:Cinnamates; D004791:Enzyme Inhibitors; C506313:FR258900; D005977:Glutarates; D006003:Glycogen; D024981:Glycogen Phosphorylase