• Journal of Microbiology and Biotechnology
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• v.14 no.1
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• pp.202-204
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• 2004

Polysaccharides and saponins were isolated from the root of Panax ginseng C.A. Meyer (Family Araliaceae), treated at various temperatures, and their inhibitory effects on rotavirus were investigated. As the temperature of processing increased, the molecular weight of the polysaccharides decreased, but the yields of water extracted increased. These polysaccharides inhibited rotavirus infection in MA104 cells, but there were no significant differences in rotavirus infection-inhibitory potency. However, ginseng saponins did not exhibit rotavirus infection-inhibitory activity.

• Journal of the Korean Society of Food Science and Nutrition
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• v.28 no.4
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• pp.816-821
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• 1999

Cholesterol esterase(pCEH, pancreas cholesterol ester hydrolase, E.C.3.1.1.13) which is secreted from pancreas has been known as an important lipase for cholesterol uptake. cholesteryl acyl esters from a diet must be hydrolyzed to free cholesterol and fatty acid by cholesterol esterase before the absorption in small intestine. For the development of inhibitory substances from natural source, we screened many extracts of oriental herbs for the inhibition of cholesterol esterase in vitro. The ethanol extract of Ephedra herba showed strong inhibitory activity. Solvent fractionation and silica gel column chromatography with the extract lead to the purification of the inhibitory principle in Ephedra herba. Crystallized inhibitor was identified as ( ) ephedrine by using UV, FT IR, 1H NMR, 13C NMR and GC/Mass. These results suggest that ( ) ephedrine can be used as a potential lead compound for the development of inhibitor for cholesterol uptake by cholesterol esterase inhibition.

• Archives of Pharmacal Research
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• v.27 no.7
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• pp.738-741
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• 2004

Three lignans isolated from the roots of A. koreanum (Araliaceae), namely eleutheroside E(1), tortoside A(2), and hemiariensin(4), were evaluated for their ability to inhibit NFAT transcription factor. Of these compounds, compound 4, possessing a diarylbutane skeleton, exhibited potent inhibitory activity against NFAT transcription factor (($IC_{50}$ ： 36.3${\pm}2.5{\mu}\textrm{M}$). However, the activities of 1 (($IC_{50}$：＞500 11M) and 2 (($IC_{50}$： 136.1 ${\pm}9.4\mu\textrm{M}$), which possess bisaryldioxabicy-clooctane skeletons, were lower. As the lignan derivatives of the same skeletons, hinokinin (5) and (-)-yatein (6) with diarylbutane skeletons and(＋)-syringaresinol (3) with a bisaryldioxabicy-clooctane skeleton were also studied for their inhibitory effects on NFAT transcription factor.

• Archives of Pharmacal Research
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• v.26 no.3
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• pp.197-201
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• 2003

Novel $\beta$-hydroxy propenamides as analogues of the active metabolite of leflunomide (A 771726) were synthesized and evaluated for their inhibitory activity on dihydroorotate dehydrogenase (DHODH) in an investigation into their immunosuppressive activity. Compounds 2a, 3a, and 3h were approximately 4-40 times more potent than leflunomide in their activity while they were-less active than A 771726.

• 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.

• Journal of Life Science
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• v.20 no.10
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• pp.1511-1518
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• 2010

The antimicrobial activity of 70% ethanol extracts from Rosa multiflora Thunberg fruit against Helicobacter pylori was examined. The inhibitory activity of Rosa multiflora Thunberg fruit extracts against H. pylori was determined to clear a zone of 14 mm with 70% ethanol extracts. Purification of inhibitory compounds was carried on Sephadex LH-20 and $C_{18}$ cartridge column chromatography using a gradient procedure, with increasing ethanol ($0{\rightarrow}100%$) in $H_2O$. The chemical structure of the purified inhibitory compounds on H. pylori was identified to be protocatechuic acid, chlorogenic acid and quercetin by FAB-MS, NMR and IR spectrum.

• Bulletin of the Korean Chemical Society
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• v.25 no.12
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• pp.1769-1774
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• 2004

Jun/Fos, a crucial factor in transmitting the tumor-promoting signal from the extracellular environment to the nuclear transcription machinery, has a dimerization interface possessing several coiled structural properties. Jun and Fos can interact with the DNA regulatory region, AP-1 (Activator Protein-1), which is composed of 5'-TGAC/GTCA-3'.$^1$ Curcumin is a well-known anticancer and anti-inflammatory compound.$^{2,3}$ It also acts as an inhibitor of the Jun-Fos function. c-Fos and c-Jun with a bZIP region are overexpressed in BL21 E. coli and purified with an $Ni^{2+}$ affinity column. The inhibitors of Fos-Jun-AP-1 complex formation were searched through the EMSA (electrophoresis mobility shift assay) experiment, and new curcuminoids were synthesized and investigated as to their inhibitory effect on the same system. Two curcuminoids showed a stronger inhibitory effect than curcumin. This inhibitory activity was quantified with EMSA. 1,7-bis(4-methyl)-1,6-heptadiene-3,5-dione (BJC003) and 1,7-bis(4-hydroxy-5-methoxy-3-nitrophenyl)-1,6-heptadiene-3,5-dione (BJC005) showed remarkably high inhibitory activities. $IC_{50}$ of 1,7-bis(4-methyl)-1,6-heptadiene-3,5-dione (BJC003) and 1,7-bis(4-hydroxy-5-methoxy-3-nitrophenyl)-1,6-heptadiene-3,5-dione (BJC005) are 8.98 ${\mu}M$ and 5.40 ${\mu}M$, respectively. However, 1,7-bis(4-methyl-3-nitrophenyl)-1,6-heptadiene-3,5-dione (BJC004) did not show inhibitory activity.

• Korean journal of applied entomology
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• v.23 no.3 s.60
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• pp.137-141
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• 1984

Crude sap, which was extracted from six Amaranthaceae plants, inhibited local lesion formation on Nicotiana glutinosa by tobacco mosaic virus(TMV) infection. Especially the remark. able inhibitory effect to TMV infection was shown on leaves of N. glutinosa precoated with the sap from Amaranthus mangostanus. The inhibitory activity of the sap from A. mangostanus was stable to storage in vitro for I day and to dilution 1/4 of the sap with distilled water. However, its activity was lost when the sap was heated at $70^{\circ}C\;to\;100^{\circ}C$ for 10 minutes. When the leaves of N. glutinosa precoated with the sap were sprayed with water, the inhibitory effect to TMV infection was maintained for 2 days. The A. mangostanus sap readjusted pH 3, pH 5, or pH 9 with 1 N HCl or 1 N NaOH did not decline the inhibitory action but the sap absorbed with $5\%\;to\;15\%$ charcoal completely lost their action. The protein components purified from A. mangostanus sap revealed three major bands by $5\%\;to\;15\%$ polyacrylamide gel electrophoresis and the top component of which showed the inhibitory action to TMV infection.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.34 no.2
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• pp.109-115
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• 2008

The comparative molecular field analyses(CoMFA) models between the substituents with changing groups($R_1{\sim}R_4$) of $3{\beta}$-hydroxy-12-oleanen-28-oic acid derivatives as substrate molecule and their inhibitory activities($pI_{50}$) against protein tyrosine phosphatase(PTP)-1B were derived and discussed quantitatively. The optimized CoMFA F1 model have best predictability and fitness($r^2_{cv.}=0.654$ and $r^2_{ncv.}=0.995$). The order of contribution ratio (%) with CoMFA fields on the inhibitory activities was a steric field(53.0%), electrostatic field(36.2%) and hydrophobic field(10.8%). From the analytical results of CoMFA contour maps, the inhibitory activities were dependent on the R4 group in substrate molecules. Particularly, the new active compounds(P1 & P2) with the inhibitory activity against melanin synthesis were expected.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.41 no.2
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• pp.151-157
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• 2015

In this study, we prepared Eriobotrya japonica leaf extracts by several extraction processes and then evaluated their biological activities for their potential application as a new raw material of functional cosmetic. Their whitening effects were measured by tyrosinase inhibitory activities, and anti-inflammatory effects were determined by inhibitory activities of nitric oxide (NO) production. Among the several extracts obtained from E. japonica leaf, supercritical fluid extract showed tyrosinase inhibitory activities at the concentration of 10%. Inhibitory activity on NO production effect related to anti-inflammatory efficacy was in the order: supercritical fluid extract > ethanol extract > hot water extract. According to the results of MTT assay, cell cytotoxicity was not observed at all concentrations except for a 5% concentration of the 70% ethanol extract. For whitening effects, 30% ethanol and 70% ethanol extract showed mushroom tyrosinase inhibitory activity at the concentration of 5%. These results indicated that E. japonica leaf extracts could have the functional effects when they are added as ingredients in cosmetics.