FR258900, a novel glycogen phosphorylase inhibitor isolated from Fungus No. 138354. I. Taxonomy, fermentation, isolation and biological activities.
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.
Furukawa
Shigetada
S
Fermentation Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., 5-2-3 Tokodai, Tsukuba, Ibaraki 300-2698, Japan. shigetada.furukawa@jp.astellas.com
Tsurumi
Yasuhisa
Y
Murakami
Kana
K
Nakanishi
Tomoko
T
Ohsumi
Keisuke
K
Hashimoto
Michizane
M
Nishikawa
Motoaki
M
Takase
Shigehiro
S
Nakayama
Osamu
O
Hino
Motohiro
M
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*
D002934:Cinnamates; D004791:Enzyme Inhibitors; C506313:FR258900; D005977:Glutarates; D006003:Glycogen; D024981:Glycogen Phosphorylase