• Preventive Nutrition and Food Science
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• v.6 no.2
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• pp.117-121
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• 2001

Changes in antioxidative activity and Angiotensin converting enzyme(ACE) inhibitory activity in juice prepared from Dolsan leaf mustard kimchi (DLMK) ar various fermentation temperatures were investigated. Antioxidative activity of juice from optimally ripened DLMK at 20 and 3$0^{\circ}C$ showed 80 and 83%, respectively. Juice from 10-day fermented DLMK at 3$0^{\circ}C$ showed 62% inhibitory activity against the ACE. In the juice fermented DLMK at 2$0^{\circ}C$~3$0^{\circ}C$, physiological activity was higher than that of the 4~1$0^{\circ}C$. In particular, optimally ripened DLMK at 3$0^{\circ}C$ showed the highest physiological activity. The physiological activity in DLMK juice at the fermentation period increased significantly with an increase in the growth of microbes. Consequently, a maximum physiological activity was shown at the maximum cell number. These results suggest that the microorganisms in DLMK juice would play an important role in the physiological activity.

• The Journal of Internal Korean Medicine
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• v.27 no.4
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• pp.888-894
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• 2006

Objectives : For the purpose of developing new anti-HIV agents from natural sources, the extracts of Ricinus communis were tested for their inhibitory effects on essential enzymes reverse transcriptase (RT), protease and alpha-glucosidase. Inhibition activity of major compounds of Ricinus communis were predicted from quantitative structure activity relationships (QSAR) in silico. Methods and Results : In the anti-HIV-1 RT using enzyme-linked oligonucleotide sorbent assay (ELOSA) method, water and methanol extracts (100ug/ml) of Ricinus communis showed strong activity of 94.2% and 82.7%, respectively. In the HIV-1 protease and alpha-glucosidase inhibition assay, neither water nor methanol extracts of Ricinus communis inhibited the activity of the enzyme to cleave any substrates as oligopeptides and oligosaccharides. Conclusions : We found that for these samples it is possible that the inhibition of the RT in vitro is due to the secondary metabolites of Ricinus communis such as ricinine and quercetin. It would beof great interest to identify the compounds which are responsible for this inhibition, since all therapeutically useful agents up to date are RT inhibitors.

• Food Science and Biotechnology
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• v.14 no.6
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• pp.772-777
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• 2005

The goal of this study was to screen and characterize the physiological functions of Korean traditional wines (TW) and liquors (TL). Forty-two TW and TL were collected and evaluated for quality and cardiovascular activities. Ethanol content ranged from $9.0%{\sim}41%$, and pH ranged from $3.0{\sim}7.8$, and they also contained 0.01% to 0.67% of total acid. Samples contained a maximum of 2.0% of crude protein and $0.1%{\sim}14.0%$ of reducing sugar. Commercial CM-wine showed the highest antihypertensive angiotensin I-converting enzyme (ACE) inhibitory activity, 85.9%. The greatest fibrinolytic activity and platelet aggregation inhibitory activity were also found in commercial CM-wine (31.8U) and commercial SS2-wine (38.6 %), respectively. Commercial SHBI-liquor showed the highest HMG-CoA reductase inhibitory activity, 78%. The ACE inhibitor from commercial CM-wine was a peptide compound and also showed an antihypertensive effect in spontaneous hypertensive rats at a dosage of 1.5 mg/kg.

• Preventive Nutrition and Food Science
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• v.10 no.2
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• pp.134-139
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• 2005

Seven brown algal species (Ecklonia cava, Ishige okamurae, Sargassum fulvellum, Sargassum horneri, Sargassum coreanum, Sargassum thunbergii and Scytosiphon lomentaria) were hydrolyzed using five proteases (Protamex, Kojizyme, Neutrase, Flavourzyme and Alcalase) and screened for angiotensin 1-converting enzyme (ACE) inhibitory activities. Most algal species examined showed good ACE inhibitory activities after the enzymatic hydrolysis. However, E. cava was the most potent ACE inhibitor of the seven species. Flavourzyme digest of E. cava exhibited an $IC_{50}$ of around $0.3\;{\mu}g/mL$ for ACE; captopril has an $IC_{50}$ of $\~0.05\;{\mu}g/mL$. The Flavourzyme digest was separated to three fractions by an ultrafiltration membrane (5, 10, 30 kDa MWCO) system according to the molecular weights. The active components were mainly concentrated in >30 kD fraction which are composed of the highest protein content $(27\%)$ and phenolic content (261 mg/100 mL) compared to the other two smaller molecular weight fractions. Therefore, the active compounds appear to be relatively high molecular weight complex molecules associated with protein (glycoprotein) and polyphenols. Therefore, E. cave is a potential source of antihypertensive compound.

• Food Science and Biotechnology
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• v.27 no.6
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• pp.1781-1789
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• 2018

In this study, whey proteins were fermented with 34 lactic acid bacteria for 48 h at $37^{\circ}C$ and their ability to inhibit angiotensin 1-converting enzyme (ACE) activity were compared. All the lactic acid bacteria displayed varying proteolytic abilities in whey. Their fermentates also displayed varying abilities to inhibit ACE in vitro. Seven fermentates showed strong ACE inhibitory abilities between $84.70{\pm}0.67$ and $52.40{\pm}2.1%$ with $IC_{50}$ values between $19.78{\pm}1.73$ and $2.13{\pm}0.7mg/ml$. Pediococcus acidilactici SDL1414 showed the strongest ACE inhibitory activity of $84.7{\pm}0.67%$ ($IC_{50}=19.78{\pm}1.73{\mu}g/ml$). Mass spectrometry revealed that more than half (57.7%) of the low molecular weight peptides (< 7 kDa) in the P. acidilactici SDL1414 fermented samples were ACE inhibitory peptides. Our results show that P. acidilactici SDL1414 could be used as a starter culture in the dairy industry to develop antihypertensive functional foods for hypertension management.

• Journal of Applied Biological Chemistry
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• v.62 no.1
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• pp.81-86
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• 2019

A yellow resin (gamboge) from Garcinia hanburyi has been widely used as folk medicine due to its antibacterial and antitumor activities. We isolated four ${\alpha}$-glucosidase inhibitory compounds from the methanol extract of gamboge. The compounds (1-4) were identified as gambogoic acid (1), moreollic acid (2), gambogic acid (3), and 10-methoxygambogenic acid (4), respectively through spectroscopic data including 2D-NMR and HREIMS. All compounds were examined in the enzyme inhibition assay against ${\alpha}$-glucosidase to identify their inhibitory potencies and kinetic behavior. All compounds (1-4) showed enzyme inhibition against ${\alpha}$-glucosidase, but the activity was significantly affected by the methoxy group on C-10 of ring A and pentenyl pyran moiety of ring D. For example, compound 1 ($IC_{50}=41.4{\mu}M$) bearing pyran ring eight times effective that 4 ($IC_{50}=350.6{\mu}M$) having geranyl group itself. Most active compound was found out to be gambogoic acid (1) which was analyzed most abundant metabolite in gamboge by LC-ESI-MS/MS. In kinetic study, compounds 1 and 2 were proved as noncompetitive inhibitors.

• YAKHAK HOEJI
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• v.28 no.6
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• pp.313-319
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• 1984

Phenylurea, phenylthiourea, benzylcarbamate and toluenesulfonate of L-alanyl-L-proline(comp. $3{\sim}6$) were synthesized and their effects against angiotensin-converting enzyme (ACE) were tested. Comp. 3 showed only mild inhibitory activities against ACE while comp. $4{\sim}6$ were inert indicating that those functional groups were not suitable for interactions with ACE. Ortho-hydroxy- or ortho-carboxy-benzamide of proline (comp. 7) and phenylalanine (comp. 8 and 9) were also tested. Of the benzamides, ortho-hydroxy function was unsuitable to exert inhibitory activities against ACE. Ortho-carboxy group of 9 seemed to have mild interactions with active site of ACE possibly because of the shorter distance between the amide and ortho-carboxyl group of the compound than the corresponding two active sites of the enzyme.

• Journal of Microbiology and Biotechnology
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• v.9 no.4
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• pp.414-421
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• 1999

Helicobacter pylori were found to be resistant to azide but sensitive to vanadate, suggesting that defect in the P-type ATPase activity rather than F-type ATPase would be lethal to cell survival or growth. To elucidate the relationship between this enzyme inhibition and H. pylori death, we determined the effect of omeprazole (OMP) plus vanadate on enzyme activity and cell growth. The minimum inhibitory concentration (MIC; ca. 0.8$\mu$mol/disk) of vanadate for H. pylori growth was lowered over l0-fold with the aid of OMP, whereby its inhibitory potential toward the P-type ATPase activity was diametrically increased. Alternatively, we found that this enzyme activity was essential for active transport in H. pylori. From these observations, we strongly suggest that the immediate cause of the growth inhibition of H. pylori cells with OMP and/or vanadate might be defective in the cell's active transport due to the lack of P-type ATPase activity. From the spectral data with circular dichroism (CD) spectroscopy, we found that activated OMP (OAS) at concentration below MIC did not disrupt helical structures of membrane proteins. Separately, we determined the cytopathic effect of OAS by SDS-PAGE, indicating the change in the production of cytoplasmic protein but not cell membrane.

• Archives of Pharmacal Research
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• v.29 no.11
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• pp.1006-1017
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• 2006

A series of 3-(substituted-benylidene)-1, 3-dihydro- indolin-2-one, 3-(substituted-benylidene)-1, 3-dihydro- indolin-2-thione and 2, 2'-dithiobis 3-(substituted-benylidene)-1, 3-dihydro-indole derivatives was investigated as inhibitor of $p60^{c-Src}$tyrosine kinase by performing receptor docking studies and inhibitory activity toward tyrosine phosphorylation. Some compounds were shown to be docked at the site, where the selective inhibitor PP1 [1-tert-Butyl-3-p-tolyl-1H-pyrazolo[3,4-d]pyrimidine-4-yl-amine] was embedded at the enzyme active site. Evaluation of all compounds for the interactions with the parameters of lowest binding energy levels, capability of hydrogen bond formations and superimposibility on enzyme active site by docking studies, it can be assumed that 3-(substituted-benzylidene)-1, 3-dihydro-indolin-2-one and thione derivatives have better interaction with enzyme active site then 2, 2'-dithiobis 3-(substituted-benzylidene)-1, 3-dihydro indole derivatives. The test results for the inhibitory activity against tyrosine kinase by Elisa method revealed that 3-(substituted-benylidene)-1, 3-dihydro- indolin-2-thione derivatives have more activity then 3-(substituted-benylidene)-1, 3-dihydro- indolin-2-one derivatives.

• Natural Product Sciences
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• v.13 no.4
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• pp.289-294
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• 2007

Ethanolic extract (50% v/v) and alkaloid fraction of Tylophora indica leaves were examined for lysosomal enzyme inhibitory activity in adjuvant-induced arthritic rats. The alkaloid fraction showed statistically significant inhibition of arthritic lesions (p < 0.05) from day 18, (p < 0.025) from day 20 and (p < 0.001) from day 21 onwards in the adjuvant-induced arthritis, which was comparable to the response of standard drug Indomethacin. The ethanolic extract was less significant than the alkaloidal fraction in inhibition of arthritis. Alkaloid fraction showed significant (p < 0.001) inhibitory effect on the lysosomal enzyme activities in adjuvantinduced arthritic rats. It also significantly prevented decrease in collagen levels and synovial damage observed during arthritis and also inhibited increase in urinary excretion levels of collagen degradation products like hydroxyproline, hexosamine, hexuronic acid, etc. Both ethanolic extract as well as the alkaloid fraction, however, did not show any significant activity in normal nonarthritic rats. The ethanolic extract and the alkaloid fraction may thus be able to inhibit the progress of inflammation and inhibit the destructive activity of lysosomal enzymes on structural macromolecules like collagen etc. in the synovial capsule in joints during arthritic states. They may thus prevent synovial damage observed during arthritis.