FR258900, a novel glycogen phosphorylase inhibitor isolated from Fungus No 138354 Taxonomy, fermentation, isolation and biological activities

被引:24
作者
Furukawa, S [1 ]
Tsurumi, Y
Murakami, K
Nakanishi, T
Ohsumi, K
Hashimoto, M
Nishikawa, M
Takase, S
Nakayama, O
Hino, M
机构
[1] Fujisawa Pharmaceut Co Ltd, Fermentat Res Labs, Tsukuba, Ibaraki 3002698, Japan
[2] Fujisawa Pharmaceut Co Ltd, PMD Res Ctr, Osaka 5410046, Japan
[3] Fujisawa Pharmaceut Co Ltd, Exploratory Res Labs, Tsukuba, Ibaraki 3002698, Japan
[4] Fujisawa Pharmaceut Co Ltd, Res Planning Res Div, Osaka 5320031, Japan
关键词
fungal metabolite; glycogen phosphorylase inhibitor; diabetes;
D O I
10.1038/ja.2005.66
中图分类号
Q81 [生物工程学(生物技术)]; Q93 [微生物学];
学科分类号
071005 [微生物学]; 0836 [生物工程]; 090102 [作物遗传育种]; 100705 [微生物与生化药学];
摘要
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.
引用
收藏
页码:497 / 502
页数:6
相关论文
共 17 条
[1]
Hepatic glycogen synthesis is highly sensitive to phosphorylase activity -: Evidence from metabolic control analysis [J].
Aiston, S ;
Hampson, L ;
Gómez-Foix, AM ;
Guinovart, JJ ;
Agius, L .
JOURNAL OF BIOLOGICAL CHEMISTRY, 2001, 276 (26) :23858-23866
[2]
Specific features of glycogen metabolism in the liver [J].
Bollen, M ;
Keppens, S ;
Stalmans, W .
BIOCHEMICAL JOURNAL, 1998, 336 :19-31
[3]
COATS WS, 1991, J BIOL CHEM, V266, P16113
[4]
Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription [J].
Coghlan, MP ;
Culbert, AA ;
Cross, DAE ;
Corcoran, SL ;
Yates, JW ;
Pearce, NJ ;
Rausch, OL ;
Murphy, GJ ;
Carter, PS ;
Cox, LR ;
Mills, D ;
Brown, MJ ;
Haigh, D ;
Ward, RW ;
Smith, DG ;
Murray, KJ ;
Reith, AD ;
Holder, JC .
CHEMISTRY & BIOLOGY, 2000, 7 (10) :793-803
[5]
GSK3 inhibitors: Development and therapeutic potential [J].
Cohen, P ;
Goedert, M .
NATURE REVIEWS DRUG DISCOVERY, 2004, 3 (06) :479-487
[6]
ROLE OF LIVER IN PATHOPHYSIOLOGY OF NIDDM [J].
CONSOLI, A .
DIABETES CARE, 1992, 15 (03) :430-441
[7]
PATHOGENESIS OF NIDDM - A BALANCED OVERVIEW [J].
DEFRONZO, RA ;
BONADONNA, RC ;
FERRANNINI, E .
DIABETES CARE, 1992, 15 (03) :318-368
[8]
Increased insulin sensitivity and obesity resistance in mice lacking the protein tyrosine phosphatase-1B gene [J].
Elchebly, M ;
Payette, P ;
Michaliszyn, E ;
Cromlish, W ;
Collins, S ;
Loy, AL ;
Normandin, D ;
Cheng, A ;
Himms-Hagen, J ;
Chan, CC ;
Ramachandran, C ;
Gresser, MJ ;
Tremblay, ML ;
Kennedy, BP .
SCIENCE, 1999, 283 (5407) :1544-1548
[9]
Kinetic and functional characterization of 1,4-dideoxy-1,4-imino-D-arabinitol: A potent inhibitor of glycogen phosphorylase with anti-hyperglyceamic effect in ob/ob mice [J].
Fosgerau, K ;
Westergaard, N ;
Quistorff, B ;
Grunnet, N ;
Kristiansen, M ;
Lundgren, K .
ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS, 2000, 380 (02) :274-284
[10]
FR258900, a novel glycogen phosphorylase inhibitor isolated from Fungus No. 138354 - II. Anti-hyperglycemic effects in diabetic animal models [J].
Furukawa, S ;
Murakami, K ;
Nishikawa, M ;
Nakayama, O ;
Hino, M .
JOURNAL OF ANTIBIOTICS, 2005, 58 (08) :503-506