• YAKHAK HOEJI
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• v.41 no.2
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• pp.153-160
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• 1997

One hundred and seventy crude drugs were screened for prolyl endopeptidase (PEP) inhibitors. Among them, 80% methanolic extract of 18 medicinal plants such as Polygonum cuspi data, Sanguisorba officinalis, Eugenia caryophyllata, Rubus coreanus, Cinnamomum cassia (Cassiae Cortex and Cinammomi Ramulus), Rheum palmatum, Ulmus pumila, Sorbus commixta, Areca catechu, Uncaria sinensis, Terminalia chebula, Caesalpinia sappan, Nelumbo nucifera, Machilus thunbergii, Paeonia moutan, Elscholtzia patrini and Cynomorium coccineum inhibited more than 70% of PEP activity at a concentration of 40 ppm. The active principles of P. moutan, M. thunbergii, T chebula, A. catechu, S. commixta, R. palmatum, R. coreanus, E. caryophyllata and P. cuspidata were transferred into organic solvents, which showed more than 75% inhibition at 5 ppm.

• Applied Biological Chemistry
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• v.42 no.4
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• pp.351-355
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• 1999

In order to find anti-dementia drugs from natural products, prolyl endopeptidase inhibitors were purified from Puerariae Flos by consecutive solvent partition, followed by silica gel, Sephadex LH-20, and HPLC. Four isoflavonoid inhibitors were isolated and identified as tectorigenin, genistein, 5,7-dihydroxy-4',6-dimethoxyisoflavone, and 5-hydroxy-6,7,4'-trimethoxyisoflavone by means of instrumental analyses including $^{1}H-$, $^{13}C-$, $^{2}D-NMR$ and MS and $IC_{50}$ values against PEP were 5.30 ppm$(17.7\;{\mu}M)$, 10.39 ppm$(38.5\;{\mu}M)$, 13.92 ppm$(44.3\;{\mu}M)$, and 20.61 ppm$(62.8\;{\mu}M)$, respectively. Some previous mistakes in $^{13}C-NMR$ assignment were revised by careful investigation of HMBC and HMQC data.

• Journal of Applied Biological Chemistry
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• v.55 no.3
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• pp.195-198
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• 2012

Four chromone derivatives (1-4) were isolated from the clove buds (Syzygium aromaticum). Of these, two chromone C-glucosides (1 and 2) showed significant PEP inhibition with $IC_{50}$ values of $1.48{\pm}0.02$ and $1.74{\pm}0.03{\mu}M$ and $K_i$ values of $0.27{\pm}0.02$ and $0.50{\pm}0.05{\mu}M$, respectively. They also exhibited strong antioxidant capacities against the 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid diammonium salt radical system with $EC_{50}$ values of $4.13{\pm}0.04$ and $4.79{\pm}0.03{\mu}M$, respectively.

• Journal of Microbiology and Biotechnology
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• v.9 no.6
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• pp.798-803
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• 1999

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 $A{\beta}$, 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-acety1-2,3,7,8-tetrahydroxy-[12H]-12-hydroxymethylbenzobis[I.2b,3.4b'] benzofuran-11-one (kynapcin-9) by spectral data including UV, IR, MS, HR-MS, $^1H-,{\;}^{13}C-$, and 2D-NMR. The $IC_{50}$ values of the thelephoric acid and kynapcin-9 were 0.157 ppm (446nM) and 0.087 ppm (212nM) and their inhibitor constants ($K_i$) were 0.73ppm ($2.09{\;}\mu\textrm{m}$) and 0.060 ppm (146 nM), respectively. Furthermore, they were non-competitive with a substrate in Dixon plots.

• Applied Biological Chemistry
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• v.42 no.4
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• pp.336-343
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• 1999

Fifty six mycelial cultured Basidiomycetes were screened for their inhibitory effects against prolyl endopeptidase(PEP), acetylcholine esterase(AChE) and thrombus coagulation. Out of them, methanolic extract of mycelium and/or ethylacetate(EtOAc) soluble fraction from culture broth of Peniophora quercina, Amanita aspera, Phellinus chrysoloma, Grifola frondosa, Wolfiporia extensa, Clavicorona pyxidata and Phanerochaete sordida inhibited more than 90% of PEP activity at 40 ppm. The extracts of Lenzites betulina, Phellinus chrysoloma, Wolfiporia extensa, Phanerochaete sorrlida, Hypocrea nigricans, Coriolus azureus, Flammulina velutipes, Phlebiopsis gigantea and Bondarzewia montana exhibited about 40% of inhibitory activity against AChE at 40 ppm. In thrombin times assay, the extracts of Amanita aspera, Oxyporus latemarginata, Peniophora quercina, Fomes fomenfarius, Trametes versicolor, and Phlebiopsis gigantea delayed coagulation of thrombus about two to three times over control at ca 550 ppm. In activated partial thromboplastin times assay, none of the tested Basidiomycetes showed significant effect.

• The Korean Journal of Community Living Science
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• v.16 no.4
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• pp.95-102
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• 2005

The present study was performed to investigate the 1,1-diphenyl-2-picryl hydrazyl (DPPH) radical scavenging and Proly1 endopeptidase (PEP) inhibitory activities of plant extracts. The whole extract of Fragaria yezoensis inhibited the DPPH radical by $90.4\%$ and the stem of Gingko biloba, Gardenia jasminoides for. grandiflora and Rhododendron yedoensa var. poukhanene, the loaves of Rhododendron mucronulatum var. ciliatum, Gardenia jasminoides for. grandiflora and Corylus sieboldiana var. mandshurice, the fruit of Cornus officinalis, and the root of Gingko biloba showed high DPPH radical scavenging activities. In the case of PEP inhibitory activities, high inhibition was observed in the whole Plant of Fragaria ananassa, Fragaria yezoensis and Hypericum erectum, the stem of Actinidia arguta and Rhododendron yedoensa var. poukhanese, the leaves of Rhododendron yedoensa var. poukhanense and Rosa davurica, the fruit of Cornus officinalis. and the root of Acer okamotoanum. There was significant correlation (P=0.000) between DPPH radical scavenging and prolyl endopeptidase inhibitory activities, thus some of plant extracts such as whole Fragaria yezoensis, fruit of Cornus officinalis had high activities in both DPPH-scavenging and prolyl endopeptidase inhibition. Therefore, it is required to examine the mechanical interaction between DPPH-scavenging and prolyl endopeptidase inhibitory activities and further studying plant extracts with both these activities is desired to develop agents for preventing and treating of Alzheimer's disease.

• The Korean Journal of Mycology
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• v.26 no.4 s.87
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• pp.519-524
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• 1998

Four minor compounds were isolated from fruiting bodies of Polyozellus multiflex by consecutive chromatographic separation. Their structures were identified as ergost-4,6,8,22-tetraen-3-one, 4-methoxy-6-methyl-2H-pyran-2-one, p-anisic acid, and p-hydroxybenzoic acid by spectral analysis. They could not inhibit prolyl endopeptidase nor acetylcholine esterase at the concentration up to 100 ppm.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1995.04a
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• pp.47-49
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• 1995

• Korean Journal of Fisheries and Aquatic Sciences
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• v.49 no.2
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• pp.131-136
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• 2016

Marine organisms are sources of many bioactive compounds, such as essential fatty acids, essential amino acids, vitamins, and minerals, making them useful candidates for the production of safe bioactive substances. They also synthesize glutamic acid, which can be used to produce γ-aminobutyric acid (GABA), the major inhibitory neurotransmitter in the central nervous system (CNS), via fermentation with Lactobacillus brevis BJ-20. This study investigated the degree to which fermented sea tangle (FST) inhibits enzymes such as acetylcholine esterase (AChE) and prolyl endopeptidase (PEP) and affects memory of normal mice using the T-maze test. FST inhibited more than 90% of AChE at 1 mg/mL and 50% of PEP at 8 mg/mL. Oral FST (100 mg/kg) significantly improved performance of normal mice on the T-maze. Therefore, sea tangle fermented with L. brevis BJ20 effectively contributes to memory improvement and might be a useful functional food ingredient.

• Korean Journal of Pharmacognosy
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• v.36 no.3 s.142
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• pp.235-239
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• 2005

Changes in chemical composition of the ethanolic extract of roasted Asparagi Tuber were investigated by HPLC. One dramatically increased peak $(t_R\;14.85 min)$ was isolated by silica gel column chromatograph and identified as 5-hydroxymethyl furfural (HMF) by comparing its $1^H-NMR$ data with that of a commercial standard. HMF content reached its maximum level at $190^{\circ}C$ for 60 minutes. Under these conditions, HMF contents in the roasted Asparagi Tuber was increased about thirteen times (9.26mg/g) over the not-roasted control (0.71 mg/g). No significant differences were found in macrophage-activating, prolyl endopeptidase-inhibiting, antioxidative (DPPH), anti-coagulating (activated partial thromboplastin times), and ACE-inhibiting activities between roasted and not-roasted Asparagi Tuber.