• Title/Summary/Keyword: enzyme inhibitory

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Phytol, SSADH Inhibitory Diterpenoid of Lactuca sativa

  • Bang, Myun-Ho;Choi, Soo-Young;Jang, Tae-O;Kim, Sang-Kook;Kwon, Oh-Shin;Kang, Tae-Cheon;Won, Moo-Ho;Park, Jin-Seu;Baek, Nam-In
    • Archives of Pharmacal Research
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    • v.25 no.5
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    • pp.643-646
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    • 2002
  • The succinic semialdehyde dehydrogenase (SSADH) inhibitory component was isolated from the EtOAc fraction of Lactuca sativa through repeated column chromatography; then, it was identified as phytol, a diterpenoid, based on the interpretation of several spectral data. Incubation of SSADH with the phytol results in a time-dependent loss of enzymatic activity, suggesting that enzyme modification is irreversible. The inactivation followed pseudo-first-order kinetics with the second-rate order constant of $6.15{\times}10^{-2}mM^{-1}min^{-1}.$ Complete protection from inactivation was afforded by the coenzyme $NAD^{+}$, whereas substrate succinic semialdehyde failed to prevent the inactivation of the enzyme; therefore, it seems likely that phytol covalently binds at or near the active site of the enzyme. It is postulated that the phytol is able to elevate the neurotransmitter GABA levels in central nervous system through its inhibitory action on one of the GABA degradative enzymes, SSADH.

Assessment of the Inhibitory Activity of Peptide Extracts from Hanwoo Musculus Longissimus on Angiotensin I-Converting Enzyme

  • Seol, Kuk-Hwan;Song, Ji-Hye;Prayad, Thirawong;Kim, Hyoun-Wook;Jang, Ae-Ra;Ham, Jun-Sang;Oh, Mi-Hwa;Kim, Dong-Hun;Lee, Moo-Ha
    • Food Science of Animal Resources
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    • v.31 no.5
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    • pp.663-667
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    • 2011
  • This study was performed to measure the angiotensin I-converting enzyme (ACE) inhibitory activity of peptide extracts derived from the enzymatic proteolysis of Hanwoo Musculus longissimus (M. longissimus) during cold storage. Thermolysin (80 ppm, w/w) and protease type XIII (100 ppm, w/w) were injected separately or in combination for the enzymatic proteolysis of sarcoplasmic and myofibrillar proteins prior to storage at $5^{\circ}C$ (T1) or at $-1^{\circ}C$ (T2) in a chilling room for 9 days. Beef injected with thermolysin (E2) and thermolysin+protease type XIII (E3) showed a significantly higher degree of hydrolysis at both storage temperatures (p<0.05). During the storage period, T1E2 at day 6 and T1E3 at day 9 showed the strongest ACE inhibitory activity with sarcoplasmic and myofibrillar protein proteolysates. Macromolecules greater than 10,000 Da were removed by ultra filtration, and the filtrates were separated into fractions using gel filtration. Five and three major fractions were collected from S-T1E2-6 and M-T1E3-9 extracts, respectively, and the $4^{th}$ fraction of the S-T1E2-6 extracts showed the highest ACE inhibitory rate of $61.96{\pm}7.41%$.

Alpha-glucosidase Inhibitory Activities of Some Wild Vegetable Extracts

  • Kim, Jong-Sang;Kwon, Chong-Suk;Son, Kun-Ho;Kim, Jung-In
    • Preventive Nutrition and Food Science
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    • v.5 no.3
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    • pp.174-176
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    • 2000
  • Seventeen wild vegetables consumed commonly in Korea were tested for inhibitory activities against alpha-glucosidase, followed by Bupleurum longeradiatum and Angelica decursiva. The hexane-soluble fractions of Hosta longipes, Ainsliaea acerifolia, Pedicularis resupinata, Bupleurum longeradiatum, and Angelica decursiva all at the concentration of 5 mg/ml, inhibited enzyme activity by greater than 50%, and the ethylacetate-soluble fractions of Hosta longipes, and Codonopsis lanceolata, and Bupleurum longeradiatum had relatively strong inhibitory activity against the enzyme. These results suggest that some edible plants merit further evaluation for clinical usefulness as anti-diabetic drugs.

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Studies on the Epitope of Neuronal Growth Inhibitory Factor (GIF) with Using of the Specific Antibody

  • Pang, Li-Yan;Ru, Bing-Gen
    • BMB Reports
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    • v.38 no.6
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    • pp.646-649
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    • 2005
  • Human neuronal growth inhibitory factor (GIF), a metalloprotein classified as metallothionein-3, is specifically expressed in mammal central nervous system (CNS). In these Studies the specific antibody to human GIF was prepared and used to search the epitope of human GIF by enzyme-linked immunosorbent assay (ELISA) and sequence comparison. The result of ELISA showed the epitope of human GIF may locate on a octapeptide (EAAEAEAE) in the $\alpha$-domain of human GIF, and the result of nerve cell culture indicated that the biological activity of GIF may be affected by the specific antibody.

Effects of Some Heavy Metals(Al, Cd, Hg, and Pb) on ATP Content in Plant Leaves (식물엽의 ATP함량에 미치는 중금속(Al, Cd, Hg 및 Pb)의 영향)

  • 성민웅
    • Journal of Plant Biology
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    • v.22 no.4
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    • pp.107-113
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    • 1979
  • The present study was carried out to estimate the comparative effects of hydroponic heavy metals (Al, Cd, Hg, and Pb) on ATP content in plant leaves grown with Hoagland solution under green house condition. The two plants, kidneybean(Phaseolus vulgaris L.) and buckwheat(Fagopyrum esculentum M nch), showed similar inhibitory effect of heavy metals on ATP content in order of Hg, Cd, Pb, and Al. But the overall inhibitory effect was greater in kidneybean than in buckwheat. The affinity of heavy metals, in vitro, toward the enzyme (luciferin-luciferase) is in order of Hg, Al, Cd, and Pb, similar to that toward ATP. The results showed that the inhibitory effect of heavy metals on ATP hydrolysis is mainly due to the coordination of heavy metals with enzyme than ATP.

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3D-QSAR of Angiotensin-Converting Enzyme Inhibitors: Functional Group Interaction Energy Descriptors for Quantitative Structure-Activity Relationships Study of ACE Inhibitors

  • Kim, Sang-Uk;Chi, Myung-Whan;Yoon, Chang-No;Sung, Ha-Chin
    • BMB Reports
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    • v.31 no.5
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    • pp.459-467
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    • 1998
  • A new set of functional group interaction energy descriptors relevant to the ACE (Angiotensin-Converting Enzyme) inhibitory peptide, QSAR (Quantitative Structure Activity Relationships), is presented. The functional group interaction energies approximate the charged interactions and distances between functional groups in molecules. The effective energies of the computationally derived geometries are useful parameters for deriving 3D-QSAR models, especially in the absence of experimentally known active site conformation. ACE is a regulatory zinc protease in the renin-angiotensin system. Therapeutic inhibition of this enzyme has proven to be a very effective treatment for the management of hypertension. The non bond interaction energy values among functional groups of six-feature of ACE inhibitory peptides were used as descriptor terms and analyzed for multivariate correlation with ACE inhibition activity. The functional group interaction energy descriptors used in the regression analysis were obtained by a series of inhibitor structures derived from molecular mechanics and semi-empirical calculations. The descriptors calculated using electrostatic and steric fields from the precisely defined functional group were sufficient to explain the biological activity of inhibitor. Application of the descriptors to the inhibition of ACE indicates that the derived QSAR has good predicting ability and provides insight into the mechanism of enzyme inhibition. The method, functional group interaction energy analysis, is expected to be applicable to predict enzyme inhibitory activity of the rationally designed inhibitors.

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Changes in the Quality Characteristics of Cheonggukjang prepared with Hazelnut (헤이즐넛 첨가에 따른 청국장의 품질 특성 변화)

  • Kim, Jong-Duk;Yi, Young-Hyoun;Lee, Nan-Hee;Kim, Dae-Hyun;Choi, Ung-Kyu
    • The Korean Journal of Food And Nutrition
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    • v.31 no.6
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    • pp.926-932
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    • 2018
  • This research was conducted to investigate the changes in quality characteristics of cheonggukjang fermented with the addition of hazelnut (10, 20, 30 and 40%) including; water content, pH, hydrophilic and lipophilic substances, color, viscosity and angiotensin converting enzyme inhibition activity. There was no significant change in pH with the addition of hazelnut. The water content significantly decreased with the addition of hazelnut. Hazelnut was also found to brighten the color of cheonggukjang. L-value and b-value increased with the addition of cheonggjuang. There was an insignificant change in the a-value. There was a slight decrease in the content of hydrophilic with addition of hazelnuts. Where there was more than 20% addition of hazelnut to soybean, the viscous substance content in cheonggukjang decreased significantly. Angiotensin converting enzyme inhibitory activity increased proportionally to the amount of hazelnut added. It was identified that the addition of 40% of hazelnut made its angiotensin converting enzyme inhibitory activity 10% point higher than that of control. These results suggests that the addition of hazelnut makes it possible to produce cheongkukjang of excellent angiotensin converting enzyme inhibitory activity.

Effect of Angiotensin-I Converting Enzyme Inhibitory from Hydrolysate of Soybean Protein Isolate (분리대두단백질 가수분해물의 Angiotensin-I Converting Enzyme 저해효과)

  • Back, Su-Yeon;Do, Jeong-Ryong;Do, Gun-Pyo;Kim, Hyun-Ku
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.39 no.1
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    • pp.8-13
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    • 2010
  • The angiotensin converting enzyme (ACE) inhibition effect of soybean protein isolate hydrolysate was studied using protease. Soybean protein isolate was hydrolysed by seven enzymes (Alcalase 2.4 L, Flavourzyme 500 MG, GC 106, Multifect Neutral, Neutrase 0.8 L, Papain 30,000 and Protamex), enzyme concentrations (0, 0.5, 1.0 and 1.5%), at various hydrolysis times (0, 1, 2, 3, 4, 5 and 6 hr) and suspension concentrations (1, 5, 7, 10 and 15%). Absorbance at 280 nm, brix and ACE inhibitory activity of soybean protein isolate hydrolysates were investigated. Absorbance at 280 nm and brix of Alcalase 2.4 L treatment were higher than other enzyme treatments. The optimum condition of hydrolysis was Alcalase 2.4 L, 1% enzyme concentration, 5% suspension concentration for 4 hr. $IC_{50}$ value of ACE inhibitory activity of soybean protein isolate hydrolysate was $79.94 {\mu}g/mL$. These results suggest that soybean isolate protein hydrolysate from Alcalase 2.4 L may be of benefit for developing antihypertensive therapeutics.

Production of Antihypertensive Angiotensin I-Converting Enzyme Inhibitor from Malassezia pachydermatis G-14

  • Jeong, Seung-Chan;Kim, Jae-Ho;Kim, Na-Mi;Lee, Jong-Soo
    • Mycobiology
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    • v.33 no.3
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    • pp.142-146
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    • 2005
  • To produce a novel antihypertensive angiotensin I-converting enzyme (ACE) inhibitor from yeast, a yeast isolate, designated G-14 showing the highest ACE inhibitory activity was obtained and identified as Malassezia pachydermatis based on morphological, biochemical and cultural characteristics. The maximal extracellular ACE inhibitor production was obtained from M. pachydermatis G-14 when the strain was cultured in YEPD medium containing 0.5% yeast extract, 3.0% peptone and 2.0% glucose at $30^{\circ}C$ for 24 h and the final ACE inhibitory activity was 48.9% under the above condition.

Screening of New Antibiotics Inhibiting Bacterial Methionyl-tRNA Synthetase (세균의 Methionyl-tRNA Synthetase를 저해하는 새로운 항생물질의 스크리닝)

  • 곽진환;조영준;송난규
    • YAKHAK HOEJI
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    • v.45 no.3
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    • pp.245-250
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    • 2001
  • Aminoacyl tRNA synthetases of bacteria are known as potential targets for new anti-microbial agents. To isolate new inhibitors of bacterial methionyl-tRNA synthetases from natural sources, a new target-oriented screening system using whole cells which are over-expressing a target enzyme was developed. Approximately 8,000 culture broths of microorganisms from soils were tested by this screening system. Among them, ten culture broths was found to contain inhibitory activity against methionyl -tRNA synthetases of Escherichia coli. For the validation of the screening system, this new method was compared with in vitro enzymatic method. Seven out of 10 culture broths showed inhibitory activity against methionyl-tRNA synthetases of E. coli. This result showed that the new screening system was comparable to the enzyme assay. Thus we believe that our screening system as a new method can be applied for the screening of new antibiotics inhibiting bacterial methionyl-tRNA synthetases from natural products.

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