상세 정보

underline
Metadata Downloads : dc(xml) or Excel
Cited 0 time in scopus ci

Title 

Thelephoric acid and kynapcin-9 in mushroom Polyozellus multiflex inhibit prolyl endopeptidase in vitro

Authors 

Ju Yeon KwakIn Koo RheeKyung Bok LeeJi Sook HwangIck Dong YooKyung Sik Song

Publisher 

The Korean Society for Applied Microbiology

Issue Date 

1999

Citation 

Journal of Microbiology and Biotechnology, vol. 9, no. 6, pp. 798-803

Keywords 

Prolyl endopeptidaseinhibitorPolyozellus multiflexthelephoric acid12-acetyl-2,3,7,8-tetrahydroxy[12H]-12-hydroxymethylbenzobis[1.2b,3.4b] benzofuran- 11-one (Kynapcin-9)

Abstract 

Prolyl endopeptidase [PEP; EC 3.4.21.26], a serine protease which is known to cleave peptide bonds on the carboxy side of a proline residue, plays an important role in the degradation of proline-containing neuropeptides that have been suggested to participate in learning and memory processes. An abnormal increase in the level of PEP, which can lead to generation of Aβ, is also suggested to be involved in Alzheimer's type senile dementia. In the course of screening PEP inhibitors from Basidiomycetes, the mushroom Polyozellus multiplex exhibited a high inhibitory activity against PEP. Two active compounds were isolated from the ethyl acetate soluble fraction by consecutive purification, using silica gel, Sephadex LH-20, and Lobar RP-18 chromatography. The chemical structures of these compounds were identified as thelephoric acid and 12-acetyl-2,3,7,8-tetrahydroxy-[12H]12- hydroxymethylbenzobis[1.2b,3.4b'] benzofuran-11-one (kynapcin-9) by spectral data including UV, IR, MS, HR-MS, 'H-, 13C-, and 2D-NMR. The IC50 values of the thelephoric acid and kynapcin-9 were 0.157 ppm (446 nM) and 0.087 ppm (212 nM) and their inhibitor constants (K1) were 0.73 ppm (2.09 μM) and 0.060 ppm (146 nM), respectively. Furthermore, they were non-competitive with a substrate in Dixon plots.

ISSN 

1017-7825

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2017-04-19


There are no files associated with this item.
qrcode

FusionCharts.
DSpace Software Coptright(c) 2010 MIT and Hewleft-Packard  /  KRIBB-REPOSITORY ( Email:jakim@kribb.re.kr)