• Biomolecules & Therapeutics
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• v.17 no.4
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• pp.418-421
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• 2009

Structural alterations of wogonin were conducted to observe the role of each functional group at the A-ring of wogonin on the inhibitory activities against COX-2 catalyzed $PGE_2$ production from LPS-induced RAW 264.7 cells. Serial deletion of the functional groups at the A-ring of wogonin exhibited low to comparable bioactivity. The present study validated that all the functional groups at the A-ring of wogonin are important factors to exhibit the optimum inhibitory activities.

• Preventive Nutrition and Food Science
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• v.5 no.3
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• pp.174-176
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• 2000

Seventeen wild vegetables consumed commonly in Korea were tested for inhibitory activities against alpha-glucosidase, followed by Bupleurum longeradiatum and Angelica decursiva. The hexane-soluble fractions of Hosta longipes, Ainsliaea acerifolia, Pedicularis resupinata, Bupleurum longeradiatum, and Angelica decursiva all at the concentration of 5 mg/ml, inhibited enzyme activity by greater than 50%, and the ethylacetate-soluble fractions of Hosta longipes, and Codonopsis lanceolata, and Bupleurum longeradiatum had relatively strong inhibitory activity against the enzyme. These results suggest that some edible plants merit further evaluation for clinical usefulness as anti-diabetic drugs.

• Biomedical Science Letters
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• v.14 no.1
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• pp.63-68
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• 2008

The aqueous extract from the fruit body of Lentinus edodes was evaluated for inhibitory activities against $\alpha$-glucosidase isolated from Spargue-Dawley male rats. A aqueous extract of Lentinus edodes exhibited 13.8% inhibitory activity on using 2 mM p-nitrophenyl $\alpha$-D-glucopyranoside as a substrate ($IC_{50}$ 75.3 mg/ml). The aqueous extract of Lentinus edodes inhibition type on $\alpha$-glucosidase was determined to be competitive inhibition. When it was oral administered to increase of blood glucose levels after STZ-induced in a dose dependent dietary. These results suggest that aqueous extract of Lentinus edodes effect a metabolism of intestine, and thereby reducing the increase of blood glucose after STZ-induced.

• Natural Product Sciences
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• v.16 no.4
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• pp.223-227
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• 2010

The DNA Topoisomerase I (DNA Topo I) inhibitory effect of ten isolated compounds (1.10) from the leaf and stem of Vitis amurensis were examined. Among them, amurensin G (5) and r-2-viniferin (7) showed high potent inhibitory activity against DNA Topo I. DNA Topo I, an important target for anticancer drugs, can cause DNA breaks and play a key role during cell proliferation, transcription and repair. Thus, the results suggest that the selected compounds (5 and 7) from Vitis amurensis have a possibility as DNA Topo I-targeting anticancer agents.

• Natural Product Sciences
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• v.23 no.2
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• pp.97-102
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• 2017

Fourteen compounds were isolated from the stem of Angelica polymorpha. On the basis of spectral data, these compounds were identified as isoimperatorin (1), phellopterin (2), bergapten (3), xanthyletin (4), cnidilin (5), geijerine (6), (-)-3'-acetyl hamaudol (7), 7-demethylsuberosine (8), dehydrogeijerin (9), (-)-hamaudol (10), (+)-visamminol (11), divaricatol (12), scopoletin (13), and decursidate (14), respectively. Among them, compounds 4-6, 8, 9, 13, and 14 were isolated for the first time from A. polymorpha. Dehydrogeijerin (6) and geijerin (9) were isolated for the first time from genus Angelica. All isolates tested for inhibitory activity against acetylcholinesterae. Compounds 1 to 13 showed acetylcholinesterase inhibitory activity with $IC_{50}$ values ranging from 1.4 to $37.5{\mu}M$.

• Bulletin of the Korean Chemical Society
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• v.32 no.4
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• pp.1241-1248
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• 2011

Three dimensional quantitative structure-activity relationships (3D-QSARs) between new thiosemicarbazone analogues (1-31) as a substrate molecule and their inhibitory activity against tyrosinase as a receptor were performed and discussed quantitatively using CoMFA (comparative molecular field analysis) and CoMSIA (comparative molecular similarity indices analysis) methods. According to the optimized CoMSIA 2 model obtained from the above procedure, inhibitory activities were mainly dependent upon H-bond acceptor favored field (36.5%) of substrate molecules. The optimized CoMSIA 2 model, with the sensitivity of the perturbation and the prediction, produced by a progressive scrambling analysis was not dependent on chance correlation. From molecular docking studies, it is supposed that the inhibitory activation of the substrate molecules against tyrosinase (PDB code: 1WX2) would not take place via uncompetitive inhibition forming a chelate between copper atoms in the active site of tyrosinase and thiosemicarbazone moieties of the substrate molecules, but via competitive inhibition based on H-bonding.

• BMB Reports
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• v.30 no.1
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• pp.13-17
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• 1997

The inhibitory effect of herbicides such as sulfonylurea derivatives, imidazolinones and pyrimidylsalicylate has been examined on the purified valine sensitive acetolactate synthase (ALS) from Serratia marcescens. The concentration of sulfometuron methyl which inhibits 50% of the ALS activity was 2.5 mM. The required concentrations of triasulfuron, primisulfuron methyl and imazaquin for the 50% inhibition of the ALS activity were 1 mM. The resistance of Serratia ALS to sulfometuron methyl, imazapyr and imazaquin is similar to that of E. coli ALS 1. However, pyrimidylsalicylate showed a potent inhibitory effect on the Serratia ALS almost 13 times more potent than on E. coli ALS II, which is known as herbicide-sensitive isozyme. The inhibitory mode was competitive against pyruvate. 150 value was determined to be $17{\mu}M$ in an assay mixture containing 20 mM pyruvate, and the $K_1$, value was calculated to be $0.4{\mu}m$ from the modified double reciprocal plot of 1/V versus $1/S^2$.

• Biomolecules & Therapeutics
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• v.12 no.2
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• pp.129-132
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• 2004

During the screening program to discover antiatopic agents from herbal formulas, we investigated the inhibitory effect of Hwangryunhaedoktang (HT) on passive cutaneous anaphylaxis and oxazolone-induced mouse ear dermatitis. HT significantly inhibited PCA reaction in mice at doses of 50 and 200 mg/kg with inhibitory activity of 31 and 53%, respectively. HT at concentration of 0.05 and 0.1% inhibited ear swelling by 23 and 46% at 16 days in oxazolone-induced mouse ear dermatitis. Both HT with anti without human intestinal microflora showed potent inhibitory activity on the ${\beta}$-hexosaminidase release induced by IgE. Based on these findings, HT may be a usable agent for skin disorder contact dermatitis.

• Korean Journal of Pharmacognosy
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• v.34 no.2 s.133
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• pp.150-155
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• 2003

The nuclear factor of activated T cells (NFAT) protein induce transcription of cytokine genes required for T-cell activation, including the IL-2 gene. Activation of NFAT normally plays a significant role in inducing immune response. However, excessive activation provokes immunopathological reactions including autoimmunity, transplant rejection and inflammation. Thus, several natural products were screened on the inhibitory activity against the NFAT transcription factor. Among them, Euonymus sieboldiana showed strong inhibitory activity against the NFAT transcription factor without affecting cell viability.

• Korean Journal of Pharmacognosy
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• v.34 no.1 s.132
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• pp.28-32
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• 2003

In order to search for the anti-HIV agents from natural products, eighty MeOH extracts of medicinal plants were applied to a syncytia formation inhibition assay which is based on the interaction between the HIV-1 envelope glycoprotein gp120/gp41 and the cellular membrane protein CD4 of T lymphocytes. Among them, Ailanthus altissima showed a potent virus-cell fusion inhibitory activity. Repeated column chromatoghaphy of the methylene chloride fraction of A. altissima afforded compounds 1$({\beta}-sitosterol-3-O-{\beta}-D-glucoside)$, 2(tetramethoxycoumarin), and 3(ocotillone). Virus-cell fusion inhibitory activity of compound 3(ocotillone) was $70.76{\pm}4.09%$ at the concentration of $100\;{\mu}g/ml$.