A prolyl endopeptidase-inhibiting benzofuran dimer from Polyozellus multiflex.
A new benzofuran dimer, 5,6,5',6'-tetrahydroxy[3,3']bibenzofuranyl-2,2'-dicarboxylic acid dimethyl ester (kynapcin-24), was isolated from Polyozellus multiflex and shown to noncompetitively inhibit prolyl endopeptidase (PEP), with an IC(50) value of 1.14 microM. Kynapcin-24 was less inhibitory to other serine proteases such as chymotrypsin, trypsin, and elastase.
Song
Kyung-Sik
KS
Department of Agricultural Chemistry, Kyungpook National University, 1370 Sankyuk-Dong, Taegu 702-701, Korea. kssong@bh.knu.ac.kr
Raskin
Ilya
I
D000363:Agaricales / Q000737:chemistry*; D001426:Bacterial Proteins; D001572:Benzofurans / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D002855:Chromatography, Thin Layer; D002918:Chymotrypsin / Q000037:antagonists & inhibitors; D004797:Enzyme-Linked Immunosorbent Assay; D020128:Inhibitory Concentration 50; D007723:Korea; D008968:Molecular Conformation; D015394:Molecular Structure; D019906:Nuclear Magnetic Resonance, Biomolecular; D010196:Pancreatic Elastase / Q000037:antagonists & inhibitors; D000085822:Prolyl Oligopeptidases; D012697:Serine Endopeptidases / Q000378:metabolism*; D015842:Serine Proteinase Inhibitors / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D013379:Substrate Specificity; D014361:Trypsin Inhibitors / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology
D001426:Bacterial Proteins; D001572:Benzofurans; D015842:Serine Proteinase Inhibitors; D014361:Trypsin Inhibitors; C449848:kynapcin-24; C005531:flavobacterin protein, Flavobacterium aquatile; D012697:Serine Endopeptidases; D002918:Chymotrypsin; D000085822:Prolyl Oligopeptidases; D010196:Pancreatic Elastase