Protein glycation inhibitors from the fruiting body of Phellinus linteus.
To characterize active principles for prevention and treatment of diabetic complications, the isolation of protein glycation inhibitors from the fruiting body of Phellinus linteus was conducted in vitro using the model systems of hemoglobin-delta-gluconolactone (early stage), bovine serum albumin-methylglyoxal (middle stage), and N(alpha)-acetyl-glycyl-lysine methyl ester-D-ribose (last stage) assays. Nine compounds were isolated from the active ethylacetate fraction of the fruiting body and identified as protocatechuic acid (1), protocatechualdehyde (2), caffeic acid (3), ellagic acid (4), hispidin (5), davallialactone (6), hypholomine B (7), interfungins A (8), and inoscavin A (9) by spectroscopic analyses. At the early stage of protein glycation, compounds 6, 8, and 9 exhibited inhibitory activity on hemoglobin A(1C) formation. For the middle stage, compounds 2, 6, and 9 showed a significant inhibitory effect on methylglyoxal-medicated protein modification and their IC(50) values were 144.28, 213.15, and 158.66 muM, respectively. At the last stage of glycation, compound 8 was found to be a potent inhibitor of the cross-linking of proteins, which was more effective than that of aminoguanidine, a well-known inhibitor for advanced glycation end products. Consequently, compound 8 showed the most potent inhibitory effects at each stage of protein glycation. This mechanism may help to provide a protective effect against hyperglycemia-mediated protein damage.
Lee
Yeon Sil
YS
Department of Food Science and Nutrition, Hallym University, Chuncheon 200-702, Republic of Korea.
Kang
Young-Hee
YH
Jung
Ju-Young
JY
Lee
Sanghyun
S
Ohuchi
Kazuo
K
Shin
Kuk Hyun
KH
Kang
Il-Jun
IJ
Park
Jung Han Yoon
JH
Shin
Hyun-Kyung
HK
Lim
Soon Sung
SS
D001487:Basidiomycota / Q000737:chemistry*; D048690:Fruiting Bodies, Fungal / Q000737:chemistry*; D006442:Glycated Hemoglobin / Q000737:chemistry; D017127:Glycation End Products, Advanced / Q000037:antagonists & inhibitors*; D006031:Glycosylation / Q000187:drug effects; D006454:Hemoglobins / Q000378:metabolism; D009682:Magnetic Resonance Spectroscopy; D011506:Proteins / Q000737:chemistry; D011765:Pyruvaldehyde / Q000737:chemistry; D012710:Serum Albumin, Bovine / Q000737:chemistry
D006442:Glycated Hemoglobin; D017127:Glycation End Products, Advanced; D006454:Hemoglobins; D011506:Proteins; D011765:Pyruvaldehyde; D012710:Serum Albumin, Bovine