2001
DOI: 10.1021/np010194b
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A Prolyl Endopeptidase-Inhibiting Benzofuran Dimer from Polyozellus multiflex

Abstract: 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.

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Cited by 48 publications
(17 citation statements)
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“…IC 50 values of compounds 1 and 2 were comparable to those of the reported strong natural inhibitors such as staurosporine [13], isotamarixen (IC 50 = 0.25 mM [14]), propeptin (IC 50 = 1.1 mM [15]), and kinapsin-24 (IC 50 = 1.14 mM [16]); thus, these compounds may have a potential use in the prevention and treatment of Alzheimer's disease in spite of their allergic effect [10].…”
supporting
confidence: 68%
“…IC 50 values of compounds 1 and 2 were comparable to those of the reported strong natural inhibitors such as staurosporine [13], isotamarixen (IC 50 = 0.25 mM [14]), propeptin (IC 50 = 1.1 mM [15]), and kinapsin-24 (IC 50 = 1.14 mM [16]); thus, these compounds may have a potential use in the prevention and treatment of Alzheimer's disease in spite of their allergic effect [10].…”
supporting
confidence: 68%
“…asc.wiley-vch.de tures are found in natural products, [19] in organic chiral electrodes [20] and in diphosphinel igands. [21] However, under the optimised indole-indole homocoupling conditions,t he reactionw as only applicable to the coupling of electronr ich 2-(4-methoxyphenyl)-substituted benzofuran and benzothiophene with low isolated yields ( Table 2, entries 10 and 11).…”
Section: Scopeoft He Reactionmentioning
confidence: 99%
“…Another new benzofuran dimer, kynapcin-24 (83), was later isolated from P multiplex. It inhibited PEP with an IC 50 value of 1.14 µM [183]. Separation of a methanol extract of fruiting bodies of P multiplex collected in Korea afforded linoleic acid and oleic acid together with thelephoric acid [184].…”
Section: Polyozellus Multiplex (Underw) Murrillmentioning
confidence: 99%
“…Polyozellic acid (79) (antiangiogenesis [181], β-secretase (BACE1) inhibitory activities [175] and neuroprotective effects [175]), compound 80 (antiangiogenesis activity [181]). Kynapcin-13 (81) and -28 (82) (PEP inhibitory activity [182]), Kynapcin-24 (83) (PEP inhibitory activity [183]).…”
Section: Thelephora Ganbajun M Zangmentioning
confidence: 99%