• Advances in Traditional Medicine
• /
• v.7 no.4
• /
• pp.379-384
• /
• 2007

Two medicinal plant of Sundarbans mangrove forest has been tested for the evaluation of growth inhibitory and antibacterial activity. The methanol extract of Xylocarpus granatum stem bark showed potent wheat rootlet ($IC_{50}=0.01{\mu}g/ml$) and shoot ($IC_{50}=0.23{\mu}g/ml$) growth inhibitory activity in a concentration related manner. The growth inhibitory activity was markedly decreased in residual methanol extract. The methanol extract showed antibacterial activity (MIC > 3 mg/ml) against Bacillus subtilis, Staphylococcus aureous and Proteus vulgaris. The residual methanol extract did not show any antibacterial activity. The results suggest the bioactive principle(s) of Xylocarpus granatum may be relatively non polar compound(s). The methanol extract and residual methanol extract of Sarcolobus globosus stem showed poor wheat rootlet and shoot growth inhibitory activity and no antibacterial activity.

• YAKHAK HOEJI
• /
• v.60 no.3
• /
• pp.107-111
• /
• 2016

Inhibitory activities of 1,5-diarylimidazole analogs with methylthiophenyl group on prostaglandin $E_2$ ($PGE_2$) production from LPS-treated RAW 264.7 cells, were evaluated and compared with those of the corresponding analogs with 4-methanesulfonylphenyl group. Among the tested nineteen analogs with methylthiophenyl group, fourteen analogs showed strong inhibitory activities (>88%) when compared with the reference compound NS-398, and fifteen analogs have similar inhibitory activities with those of parent analogs with 4-methanesulfonylphenyl group. Those results suggest that most of 1,5-diarylimidazole analogs with methanesulfonylphenyl group can be also active even after they are metabolized by reduction.

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

• YAKHAK HOEJI
• /
• v.47 no.6
• /
• pp.456-460
• /
• 2003

In vitro $\beta$-lactamase inhibitory activity of 6-exomethylenepenam compounds ( 1, 2, 3, 4 and 5) was compared with clavulanic acid, sulbactam and tazobactam. The inhibitory activity of compound 3 was stronger than those of sulbactam and clavulanic acid against Type I and II enzymes and stronger than tazobactam against Type III, IV, TEM enzymes. The inhibitory activity of 5 was stronger than sulbactam and clavulanic acid against Type I and II enzymes and stronger than tazobactam against Type III, and IV enzymes. The in vitro antimicrobial activity of 3, 4 and 5 combined with ampicillin and cefoperazone was compared with the sulbactam against $\beta$-lactamase producing 27 strains. But, synergistic activity of 3 and 5 was inferior to tazobactam.

• Biomolecules & Therapeutics
• /
• v.14 no.4
• /
• pp.220-225
• /
• 2006

Derivatives of penicillanic acid sulfones are known to be irreversible inhibitors of $\beta$-lactamase. Eight 6-tricyclic methylene penicillanic acid sulfones were prepared, and their $\beta$-lactamase inhibitory activities were evaluated against $\beta$-lactamase types I, II, III and IV. Among the tricycles attached to 6-exomethylenepenam sulfones, thiazolobenzimidazole(12a-12b), fluorene(12c), and carbazole(12e), showed inhibitory activity on type I, II and III $\beta$-lactamase. But phenanthrene(12d), and anthracene(12f-12h) derivatives showed little $\beta$-lactamase inhibitory activity. The synergic effects of the selected compound(l2b) in 1:4 combination with piperacillin showed some protection to piperacillin for the resistant strains of E. coli DC2 and P. aeruginosa 1771.

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

• Journal of the Korean Society of Food Science and Nutrition
• /
• v.45 no.3
• /
• pp.333-341
• /
• 2016

This study examined the beauty food activities of water and ethanol extracts from Tetragonia tetragonioides. Content of phenolic compounds extracted with water and 50% ethanol extracts were 3.29 mg/g and 4.14 mg/g, respectively. 1,1-Diphenyl-2-picrylhydrazyl free radical scavenging activities of water and ethanol extracts were 98.45% and 91.20%, respectively, at $200{\mu}g/mL$ of phenolics. 2,2'-Azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) radical decolorization activity was 97.28% for water extracts and 97.83% for ethanol extracts at $100{\mu}g/mL$ of phenolics. Antioxidant protection factor (PF) was 1.77 PF for water and ethanol extracts at $200{\mu}g/mL$ of phenolics. Thiobarbituric acid reactive substances of water and ethanol extracts were 94.77% and 95.64%, respectively, at $100{\mu}g/mL$ of phenolics. Tyrosinase inhibitory activity, which is related to skin-whitening, was confirmed to be 34.96% for ethanol extracts at $200{\mu}g/mL$ of phenolics. Elastase inhibitory activity and anti-wrinkle effect of 50% ethanol extracts were 78.9% at $200{\mu}g/mL$ of phenolics. Collagenase inhibitory activity of ethanol extracts was 61.29% at $200{\mu}g/mL$ of phenolics. Astringent effect was not detected in water extracts but was 7.82% for 50% ethanol extracts at $200{\mu}g/mL$ of phenolics. Hyaluronidase inhibitory activity as a measure of anti-inflammation was confirmed to be 81.04% for water extracts at $200{\mu}g/mL$ of phenolics. Based on these results, Tetragonia tetragonioides extracts can be used as a functional material and functional beauty food with antioxidant effects.

• Applied Biological Chemistry
• /
• v.41 no.1
• /
• pp.110-117
• /
• 1998

Seven kinds of polyphenol compounds having ACE activities were isolated and purified by Sephadex LH-20, MCI-gel CHP-20, ${\um}-Bondapak\;C_{18}$ and Fuji-gel ODS $G_3$ sucessively from cacao bean(Ghana). The chemical structures of each compound were determined and identified using analyzers such as $^1H-NMR$, $^{13}C-NMR$, IR, MS, polarimeter and Elemental Analysis. Inhibition effects of isolated polyphenols on angiotensin converting enzyme (concerned with hypertension) were also observed. The results obtained were as follows,; The compounds isolated and identified were confirmed and determined as compound 1 [(+)-catechin], compound 2 [(-)-epicatechin], compound 3 [procyanidin B-1 : (-)-epicatechin-$(4{\beta}{\rightarrow}8)$-(+)catechin], compound 4 [procyanidin B-2 : (-)-epicatechin-$(4{\beta}{\rightarrow}8)$-(-)-epicatechin], compound 5 [procyanidin B-7 : (-)-epicatechin-$(4{\beta}{\rightarrow}6)$-(+)-catechin], campound 6 (procyanidin B-2,3,3'-O -digallate), compound 7 [cinnamtannin A-2 : (-)-epicatechin-$(4{\beta}{\rightarrow}8)$-(-)-epicatechin-$(4{\beta}{\rightarrow}8)$-(-)-epicatechin-$(4{\beta}{\rightarrow}8)$-(-)-epicatechin]. In the inhibition effect on ACE, procyanidin B-2,3,3'-O-digallate (compound 6) showed a higher value of 94.6% for ACE in $100\;{\um}M$ than other compounds such as (+)-catechin (compound 1), (-)-epicatechin (compound 2), procyanidin B-1 (compound 3), procyanidin B-2 (compound 4), procyanidin B-7 (compound 5) and cinnamtannin A-2 (compound 7) showing 67.9%, 61.9%, 88.6%, 82.5%, 72.2% and 82.3% for ACE, respectively. Inhibition of $4{\beta}{\rightarrow}8$ in coupling bond on the ACE enzyme was more effective than that of $4{\beta}{\rightarrow}6$. Procyanidin containing gallate inhibited more effectively than those containing not any. It was also observed that a lot of hydroxy group in the compounds increased the inhibitory effect.

• Journal of Microbiology and Biotechnology
• /
• v.27 no.6
• /
• pp.1065-1070
• /
• 2017

This study aimed to examine the anti-candidal efficacy of a novel ketone derivative isolated from Diaporthe sp. ED2, an endophytic fungus residing in medicinal herb Orthosiphon stamieus Benth. The ethyl acetate extract of the fungal culture was separated by open column and reverse phase high-performance liquid chromatography (HPLC). The eluent at retention time 5.64 min in the HPLC system was the only compound that exhibited anti-candidal activity on Kirby-Bauer assay. The structure of the compound was also elucidated by nuclear magnetic resonance and spectroscopy techniques. The purified anti-candidal compound was obtained as a colorless solid and characterized as 3-hydroxy-5-methoxyhex-5-ene-2,4-dione. On broth microdilution assay, the compound also exhibited fungicidal activity on a clinical strain of Candida albicans at a minimal inhibitory concentration of $3.1{\mu}g/ml$. The killing kinetic analysis also revealed that the compound was fungicidal against C. albicans in a concentration- and time-dependent manner. The compound was heat-stable up to $70^{\circ}C$, but its anti-candidal activity was affected at pH 2.

• Journal of Physiology & Pathology in Korean Medicine
• /
• v.23 no.2
• /
• pp.381-388
• /
• 2009

The present study was conducted to investigate the anti-allergic activity of Galgeunhaegi-Tang(GHT). We investigated the anti-allergic effects of GHT in RBL-2H3 basophilic leukemia cells by compound48/80, a mast cell degranulator and compound 48/80 induced anaphylactic shock in mice. GHT significantly inhibited ${\beta}$-hexosaminidase and histamine release from compound 48/80 stimulated RBL-2H3 cells. In addition, GHT effectively inhibited anaphylactic shock in mice by 40% at a dose 100 mg/mouse versus PBS treated control after the l.p injection(8 mg/kg) of compound 48/80. The in vitro anti-inflammatory activities of GHT in LPS-stimulated RAW 264.7 cells were investigated. GHT inhibited NO production in LPS-stimulated RAW 264.7 cells and effectively dowregulated the expression of iNOS mRNA and iNOS protein expression in LPS-stimulated RAW 264.7 cells. These result provide evidences that GHT may be beneficial in the treatment of allergic inflammtory disease.