• Bulletin of the Korean Chemical Society
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• v.33 no.7
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• pp.2365-2368
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• 2012

The $11{\beta}$-hydroxysteroid dehydrogenase type 1 ($11{\beta}$-HSD1) enzyme is involved in modulation of glucocorticoid activity within target tissues. This enzyme may contribute to obesity and/or metabolic disease through its action in adipose or liver tissue. Inhibition of $11{\beta}$-HSD1 has major therapeutic potential for glucocorticoid-associated diseases, including obesity, diabetes (wound healing), and muscle atrophy. To develop such therapeutics, we performed a pharmacophore-based virtual screening (VS) for identification of novel $11{\beta}$-HSD1 inhibitors and found that the VS hit compounds show potent inhibition of $11{\beta}$-HSD1 enzyme activity. Further, we present a binding model for active compounds. The proposed pharmacophore may serve as a useful guideline for future design of new chemical entities as $11{\beta}$-HSD1-targeted antidiabetic agents.

• Journal of Plant Biology
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• v.27 no.2
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• pp.73-80
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• 1984

Palmitoyl CoA was found to inhibit corn embryo axis glucose-6-phosphate dehydrogenase and 6-phosphogluconate dehydrogenase, which were also inhibites by polyamines. However, reversal of inhibition of both enzymes by palmitoyl CoA was made by spermine. Activity of corn embryo axis protein kinase was found to increase steadily after germination. Activation and inhibition of protein kinase were made by MgCl$_2$and all polymines, respectively. Suc results suggest that fatty acid biosynthesis and lypolysis could be regulated to some extent by polyamines in corn embryo axis.

• Bulletin of the Korean Chemical Society
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• v.31 no.5
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• pp.1355-1360
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• 2010

In order to search new inhibitors against farnesyl protein transferase (FPTase), a series of 2,3-bis-benzylidenesuccinaldehyde derivatives (1-29) were synthesized and their inhibition activities ($pI_{50}$) against FPTase were measured. From based on the reported results that the inhibitory activities of dimers 2,3-bis-benzylidenesuccinaldehydes were higher than those of monomers cinnamaldehydes, 3D-QSARs on FPTase inhibitory activities of the dimers (1-29) were studied quantitatively using comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA) methods. The statistical qualities of the optimized CoMFA model II ($r^2{_{cv.}}$= 0.693 and $r^2{_{ncv.}}$= 0.974) was higher than those of the CoMSIA model II ($r^2{_{cv.}}$ = 0.484 and $r^2{_{ncv.}}$ = 0.928). The dependence of CoMFA models on chance correlations was evaluated with progressive scrambling analyses. And the inhibitory activity exhibited a strong correlation with steric factors of the substrate molecules. Therefore, from the results of graphical analyses on the contour maps and of predicted higher inhibitory active compounds, it is suggested that the structural distinctions and descriptors that contribute to inhibitory activities ($pI_{50}$) against FPTase will be able to applied new inhibitor design.

• Biomolecules & Therapeutics
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• v.28 no.4
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• pp.311-319
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• 2020

Middle East Respiratory Syndrome Coronavirus (MERS-CoV) is a newly emerging viral disease with fatal outcomes. However, no MERS-CoV-specific treatment is commercially available. Given the absence of previous structure-based drug discovery studies targeting MERS-CoV fusion proteins, this set of compounds is considered the first generation of MERS-CoV small molecule fusion inhibitors. After a virtual screening campaign of 1.56 million compounds followed by cell-cell fusion assay and MERS-CoV plaques inhibition assay, three new compounds were identified. Compound numbers 22, 73, and 74 showed IC₅₀ values of 12.6, 21.8, and 11.12 µM, respectively, and were most effective at the onset of spike-receptor interactions. The compounds exhibited safe profiles against Human embryonic kidney cells 293 at a concentration of 20 µM with no observed toxicity in Vero cells at 10 µM. The experimental results are accompanied with predicted favorable pharmacokinetic descriptors and drug-likeness parameters. In conclusion, this study provides the first generation of MERS-CoV fusion inhibitors with potencies in the low micromolar range.

• Archives of Pharmacal Research
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• v.27 no.1
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• pp.106-110
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• 2004

The antioxidant activities of Acanthopanax senticosus stems were evaluated in $CCl_4$-intoxicated rats. The n-butanol fraction from the water extract of the stems, when pretreated orally at 200 mg/kg/day for 7 consecutive days in rats, was demonstrated to exhibit significant increases in antioxidant enzyme activities such as hepatic cytosolic superoxide dismutase, catalase and glutathione peroxidase by 30.31, 19.82 and 155%, respectively. The n-butanol fraction whereas showed a significant inhibition of serum GPT activity (65.79% inhibition) elevated with hepatic damage induced by $CCl_4$-intoxication. Eleutheroside B, a lignan component, isolated from the n-butanol fraction was found to cause a moderate free radical scavenging effection DPPH, its scavenging potency as indicated in $IC_{50}$ value, being 58.5$\mu$ M. These results suggested that the stems of A. senticosus possess not only antioxidant but also hepatoprotective activities.

• Journal of Physiology & Pathology in Korean Medicine
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• v.38 no.1
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• pp.27-31
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• 2024

Dried fruits of Amomum villosum Lour. have been used an korean medicine to treat digestive diseases for a long time. It has been reported that Amomum villosum extracts(AVE) have effects for diabetes and steatosis in experimental models. But we did not find the report about the cholesterol synthesis inhibition effects of AVE. The objective of this study is to clarify the inhibitory effect of AVE against oleic acid and glucose-induced hypercholesterolemia in HepG2 cells. The results show that AVE had a significant inhibitory effect against oleic acid and glucose-induced cholesterol accumulation. Those effects seem to be caused by inhibition of AVE on oleic acid and glucose-induced decrease of HMG CoA reductase, which is the rate-limiting enzyme for cholesterol biosynthesis in liver. It is believed that the results of this study can provide basic data for the drug and functional food development of hypercholesterolemia treatments.

• Journal of Environmental Science International
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• v.30 no.5
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• pp.369-378
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• 2021

In this study, we investigated the effects of indole on biofilm formation inhibition in Pantoea agglomerans (P. agglomerans). In the biofilm growth assay, indole inhibited biofilm formation across all the growth time. Depending on biofilm growth stage, indole exhibited biofilm inhibition and anti-bacterial effects on planktonic cells. Through the analysis of the proportion rate between biofilm and Colony Forming Units (CFU) and inhibition rate of indole, we confirmed that depending on the biofilm stage of P. agglomerans, indole treatment timing was more important than the treatment duration. By comparing gene expression rates through rt-qPCR P.agglomerans affected by indole was found to significantly change quorum sensing (pagI/R) and indole transportation (bssS) gene expressions. Throughout all, indole exhibited both antimicrobial and anti-biofilm effects on P. agglomerans. In addition, we confirmed the anti-biofilm effects of indole on mature biofilm. In conclusion, indole as a signal molecule, can exhibit anti-biofilm effects through bacterial quorum sensing inhibition and indole affects. Therefore, indole can regulate biofilm bacteria especially gram-negative opportunistic pathogens.

• Proceedings of the Korean Ceranic Society Conference
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• 2000.10a
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• pp.171.1-171
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• 2000

• Proceedings of the Korean Powder Metallurgy Institute Conference
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• 2006.09a
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• pp.334-335
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• 2006

WC/WC interface in VC mono-doped WC-10mass%Co submicro-grained hardmetals of $0.5\;{\mu}m$ was investigated together with WC/Co interface by using HRTEM and XMA. The thickness of V-rich layer and the analytical value of V at WC/WC interface were almost the same as those at WC/Co interfaces. These results, etc., suggested that the V-rich layers at both interfaces were not generated by an equilibrium segregation mechanism in the sintering stage, but generated by a preferential precipitation mechanism during the solidification of Co liquid phase in the cooling stage. Based on this suggestion, we succeeded in developing a nano-grained hardmetal with 100 nm $(0.1\;{\mu}m)$.

• Journal of the Korean Society of Food Science and Nutrition
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• v.26 no.2
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• pp.236-241
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• 1997

Inhibitory effects of several edible plant extracts against 3-hydroxy-3-methylglutaryl coenzyme A(HMG-CoA) reductase, a rate-limiting enzyme in the biosynthesis of cholesterol, were screened. Inhibition rates of $10{\sim}15%$ were observed with hot water extracts of Allium fistulosum, Allium sativum and Cucurbita maxima. Methanol extracts of Aster scaber, Allium sativum, Zingiber officinale, Oenanthe javanica and Angelica keiskei effectively reduced the enzyme activity with inhibition rates of $29{\sim}51%$. The methanol extract of Angelica keiskei was fractionated sequentially with chloroform, ethyl acetate and n-butanol. Of the fractions ethyl acetate fraction showed the highest inhibition against the enzyme. $Luteolin-7-O-{\beta}-D-glucoside$ and hyperoside isolated from the ethyl acetate fraction of Angelica keiskei inhibited the enzyme activity by 65.5% and 14.8%, respectively, at the concentration of $30{\mu}M$.