• Advances in Traditional Medicine
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• 제7권4호
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• pp.379-384
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• 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.

• 약학회지
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• 제60권3호
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• pp.107-111
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• 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.

• 한국식품영양과학회지
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• 제28권4호
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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.

• 약학회지
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• 제47권6호
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• pp.456-460
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• 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
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• 제14권4호
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• pp.220-225
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• 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
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• 제27권7호
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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.

• 한국식품영양과학회지
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• 제45권3호
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• pp.333-341
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• 2016

본 연구는 물과 ethanol을 추출용매로 사용한 번행초(Tetragonia tetragonioides) 추출물이 미용 식품 소재로 사용 가능한 기능성을 증명하고자 하였다. Phenolic compounds는 물 추출물에서 3.29 mg/g, 50% ethanol 추출물에서 4.14 mg/g의 결과를 각각 나타내었다. 전자공여능 측정 결과 $200{\mu}g/mL$ phenolic compounds의 농도에서 물 추출물은 98.45%, 50% ethanol 추출물은 91.20%의 활성을 나타내었다. ABTS radical 활성 측정 결과 $100{\mu}g/mL$ phenolic compounds의 농도에서 물 추출물은 97.28%, 50% ethanol 추출물은 97.03%의 활성을 나타내었다. Antioxidant protection factor(PF) 측정 결과 $200{\mu}g/mL$ phenolic compounds의 농도에서 물과 ethanol 추출물 모두 1.77 PF의 같은 결과를 나타내었다. Thiobarbituric acid reactive substance(TBARS) 측정 결과 $100{\mu}g/mL$ phenolic compounds의 농도에서 물과 ethanol 추출물은 94.77%와 95.64%의 높은 활성을 나타내었다. 미백과 관련 있는 tyrosinase 저해 활성을 측정한 결과 $200{\mu}g/mL$ phenolic compounds의 농도에서 ethanol 추출물은 34.96%의 억제력을 나타내었다. 주름 개선 효과를 측정하는 elastase 저해 활성과 collagenase 저해 활성을 측정한 결과 $200{\mu}g/mL$ phenolic compounds의 농도에서 ethanol 추출물만 78.90%와 61.3%의 높은 저해 활성을 나타내었다. 수렴 효과를 나타내는 astringent effect에서 $200{\mu}g/mL$ phenolic compounds 농도의 ethanol 추출물은 7.82%의 효과를 나타내었다. Hyaluronidase 저해 효과 측정 결과 물 추출물 $200{\mu}g/mL$ phenolic compounds의 농도에서 81.04%의 염증 억제 효과를 나타내었다. 이러한 결과들로 미루어 보았을 때 번행초 추출물은 항산화 작용과 미용 식품으로서의 기능성을 기대할 수 있다.

• Applied Biological Chemistry
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• 제41권1호
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• pp.110-117
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• 1998

Ghana산 cacao bean으로부터 acetone으로 추출하고 Sephadex LH-20, MCI-gel CHP-20, Bondapak $C_{18}$ 및 Fuji gel ODS $G_3$, chromatography 등을 이용하여 7종의 polyphenol 화합물(compound 1 - compound 7)을 분리 정제하였고, 이들 화합물의 화학구조를 $^1H-NMR$, $^{13}C-NMR$, IR 및 MS를 사용하여 검색하였고 아울러 angiotensin converting enzyme(ACE) 저해효과를 조사 검토하였다. 분리정제한 7종의 polyphenol 화합물의 구조를 분석한 결과, 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], compound 6 : (procyanidin B-2,3,3'-O-digallate) 및 compound 7: [cinnamtannin A-2, (-)-epicatechin-$(4{\beta}{\rightarrow}8)$-(-)-epicatechin-$(4{\beta}{\rightarrow}8)$-(-)-epicatechin-$(4{\beta}{\rightarrow}8)$-(-)-epicatechin]임을 동정하였다. ACE의 저해효과는 procyanidin B-2,3,3'-O-digallate (compound 6)가 $100\;{\um}M$에서 94.6%로 매우 우수하였으며, (+)-catechin (compound 1), (-)-epicate -chin (compound 2), procyanidin B류 (compound 3, 4, 5) 및 cinnamtannin A-2 (compound 7)도 각각 67.9%, 61.9%, 88.6%, 82.5%, 72.2% 및 82.3%의 비교적 우수한 저해효과가 있었다. 아울러 결합방식에서는 $4{\beta}{\rightarrow}6$보다 $4{\beta}{\rightarrow}8$의 결합방식이, 그리고 procyanidin 류에서는 gallate를 갖는 물질이 이를 함유하지 많은 물질보다 더욱 높은 ACE의 저해효과를 나타내었으며, 또한 hydroxyl 기가 많을수록 효소 저해효과도 증가하는 것으로 나타났다. 이와 같은 결과는 chocolate의 주원료인 cacao bean의 polyphenol 성분 또한 녹차 등에서 볼 수 있는 생리활성효과에 손색없는 것으로 판단되고, 이러한 기능성에 기초하여 chocolate, 음료 등의 식품이나 의약품의 기능성 소재로서의 산업적 응용 가능성이 높은 것으로 사료된다.

• Journal of Microbiology and Biotechnology
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• 제27권6호
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• pp.1065-1070
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• 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.

• 동의생리병리학회지
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• 제23권2호
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• pp.381-388
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• 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.