• 생약학회지
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• 제36권1호통권140호
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• pp.9-16
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• 2005

Twenty eight compounds were isolated from the whole plant of Euphorbia jolkinii and evaluated for inhibitory effect on $5{\alpha}-reductase$ activity. Among the tested compounds, 1-desgalloyl eugeniin, hippomanin A, euphorbin D, exocoecarianin, rugosin E, and pentagalloyl glucose showed potent inhibitory effect on the enzyme activity. The inhibitory potency of rugosin E and euphorbin D, which are dimeric ellagitannins on $5{\alpha}-reductase$ activity, was 7-to 8-fold stronger than that of ${\gamma}-linolenic$ acid.

• 한국수산과학회지
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• 제43권5호
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• pp.421-427
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• 2010

To isolate natural antihypertensive substances from edible seaweeds, we screened for and separated active compounds contained in natural Underia pinnatifida, cultural Underia pinnatifida, Laminaria japonica, Sporophylls and Agarum cribrosum. They were extracted using room temperature water, boiling water, acetone, and methanol in turn or using room temperature water, ether, acetone, methanol and boiling water in order. The in vitro antihypertensive activity was quantified as inhibitory efficacy against angiotensin-I converting enzyme (ACE), which is a factor inducing hypertension. For all of the seaweeds tested, the fractions soluble in room temperature water and in boiling water showed the strongest ACE inhibitory effect among the extracted fractions. Conversely, the methanol-extracted fractions for all of the seaweeds tested showed no antihypertensive activity. While the ether and acetone fractions had slight antihypertensive effects. The compounds in the aqueous extracts that had antihypertensive activity were presumed to be polysaccharides, such as fucoidan and alginate.

• Journal of Dairy Science and Biotechnology
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• 제41권2호
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• pp.45-56
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• 2023

This review serves two purposes: first, to promote the use of improved optimization techniques in response surface methodology (RSM); and second, to enhance the optimum conditions for the fermentation of probiotics. According to research in dairy science, Lactiplantibacillus plantarum K79 is a candidate probiotic that has beneficial health effects, such as lowering blood pressure. The optimum conditions for L. plantarumK79 to produce peptides with angiotensin-converting enzyme (ACE) inhibitory activity were proposed, through modeling each of ACE inhibitory activity and pH as a function of the four factors that are skim milk concentration (%), incubation temperature (℃), incubation time (hours), and starter added amount (%). To estimate optimum conditions, the researchers employed a desirability-based multi-response optimization approach, utilizing third-order models with a nonsignificant lack of fit. The estimated optimum fermentation conditions for L. plantarum K79 were as follows: a skim milk concentration of 10.76%, an incubation temperature of 36.9℃, an incubation time of 23.76 hours, and a starter added amount of 0.098%. Under these conditions, the predicted ACE inhibitory activity was 91.047%, and the predicted pH was 4.6. These predicted values achieved the objectives of the multi-response optimization in this study.

• Archives of Pharmacal Research
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• 제22권3호
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• pp.232-236
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• 1999

In this study, we present evidence that cotreatment of aloesin and arbutin inhibits tyrosinase activity in a synergistic manner by acting through a different action mechanism. Aloesin or arbutin similarly inhibited enzyme activity of human- and mushroom-tyrosinases with an IC50 value of 0.1 or 0.04 mM, respectively. Lineweaver-Burk plots of the enzyme kinetics data showed that aloesin inhibited tyrosinase activity noncompetitively with a Ki value of 5.3 mM, whereas arbutin did it competitively (Maeda, 1996). We then examined whether cotreatment of these agents inhibits the tyrosinase activity in a synergistic manner. The results showed that 0.01 mM aloesin in the presence of 0.03 mM arbutin inhibited activity of mushroom by 80% of the control value and the reverse was also true. The inhibitory effects were calculated to be synergistic according to the B rgi method. Taken together, we suggest that aloesin along with arbutin inhibits in synergy melanin production by combined mechanisms of noncompetitive and competitive inhibitions of tyrosinase activity.

• 생약학회지
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• 제45권4호
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• pp.366-375
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• 2014

Aldose reductase (AR) has been indicated the critical enzyme of the polyol pathway in the development of the diabetic complications. In this study, 119 Vietnamese herbal medicines have been investigated for inhibitory activities on AR. Among them, 7 herbal medicines, Synedrella nodiflora (stems and leaves), Combretum sundaicum (stems and leaves), Argyreia acuta (stems and leaves), Platea latifolia (whole plants), Linociera sangda (whole plants), Rhaphiolepis indica (whole plants), Harrisonia perforata (stems and leaves) and 2 fractions from Harrisonia perforata (stems and leaves) with EtOAc and BuOH, exhibited a significant inhibitory activity against AR. Particularly, S. nodiflora, A. acuta and H. perforata (stems and leaves) showed 1.0-1.8 times more potent inhibitory activity than the positive control, 3,3-tetramethyleneglutaric acid (TMG).

• 한국한의학연구원논문집
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• 제10권1호
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• pp.119-126
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• 2004

For the purpose of developing new anti-HIV agents from natural sources, the extracts of Solanum nigrum L. were tested for their inhibitory effects on HIV-1 replication and its essential enzymes as the reverse transcriptase (RT), protease and ${\alpha}$-glucosidase. In the assay of HIV-1-infected human T-cell line, water extracts inhibited the HIV- 1 -induced cytopathic effects with IC (inhibitory concentration) of 100 ug/ml. Moreover water extracts (100ug/ml) of aerial parts showed strong activity of 32.6% on anti-HIV-1 PR using the activity of the enzyme to cleave an oligopeptide. In the HIV-1 reverse transcriptase inhibition assay, aqueous extract a inhibited 17.4%, but no glucosidase inhibitory activities. We found out this result, for these samples it is possible that the inhibition of the viral replication in vitro is due to the inhibition at least one of PR and RT. It would be of great interest to identify the compounds which are responsible for this inhibition, since all therapeutically useful agent up to date are PR, RT and ${\alpha}$-glucosidase inhibitors.

• 생약학회지
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• 제42권2호
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• pp.187-194
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• 2011

Aldose reductase (AR), the key enzyme in the polyol pathway, plays an important role in the development of the diabetic complications. None of Aldose reductase Inhibitor (ARI) has achieved worldwide use because of limited efficacy or undesirable side effects. Therefore, evaluating natural sources for ARI potential may lead to the development of safer and more effective agents against diabetic complications. Fifty two Chinese herbal medicines have been investigated for inhibitory activities on AR. Among them, twelve herbal medicines, Artemisia anomala (aerial part), Centella asiatica (aerial part), Scutellaria baicalensis (root), Senecio chrysanthermoides (whole plant), Gleditsia japonica (twig), Zizyphus jujube (twig, leaf), Citrus aurantium (fruit), Hydnocarpus anthelmintica (fruit), Potaninia mongolica (aerial part), Tribulus terrestris (fruit), Artemisia apiacea (aerial part) and Eclipta prostrate (aerial part) exhibited a significant inhibitory activity against AR. Particularly, Artemisia anomala, Centella asiatica and Scutellaria baicalensis showed four times more potent inhibitory activity than the positive control, 3,3-tetramethyleneglutaric acid (TMG).

• Archives of Pharmacal Research
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• 제20권2호
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• pp.158-170
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• 1997

New HMG-CoA reductase inhibitors, in which 3-substituted 4, 5-polymethylenepyrazoles are employed as a hydrophobic anchor connected to tetrahydro-4-hydroxy-2H-pyran-2-one by a two-carbon bridge, were designed and synthesized to exhibit significant inhibitory activity comparable to mevinolin. The most potent enzyme inhibitor $(11cc, IC_{50}=0.01{\mu}M)$ is 4-fold more potent than lovastatin.

• Journal of Applied Biological Chemistry
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• 제64권2호
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• pp.195-195
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• 2021

• Preventive Nutrition and Food Science
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• 제10권2호
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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.