• Title/Summary/Keyword: inhibitory

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Pharmacetical Characteristics of Solvent Fractions Isolated from Glycyrrhiza uralensis

  • Kim, Jun-Ho;Oh, Hae-Sook
    • Biomedical Science Letters
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    • v.16 no.3
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    • pp.161-167
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    • 2010
  • In this study, the biological activities of Glycyrrhiza uralensis were investigated, including antioxidative, fibrinolytic, thrombin inhibitory, and a-glucosidase inhibitory activity. The hot water extract of Glycyrrhiza uralensis was fractionated into hexane, $CHCl_3$, ethyl acetate, butanol, and water fractions, and each of these fractions were assayed individually. The water fraction showed the highest extraction yield of 19.45% (w/w). Using the DPPH method, the free radical scavenging activity was to be the strongest in the $CHCl_3$ fraction at 89.3%. Using the fibrin plate method, only the butanol fraction showed a substantial plasmin activity of 0.62 units/ml. In thrombin inhibitory activity tests, a 100-fold dilution of the ethyl acetate fraction showed the strongest activity of 46.9%. In the a-glucosidase inhibitory activity assay, a 100-fold dilution of the $CHCl_3$ fraction showed the strongest activity of 80.6%. In conclusion, the combined results of this study demonstrate that the extracts of Glycyrrhiza uralensis can be used as a material for the development of biofunctional foods for diabetics.

Protective Effect of Natural Medicinal Plants against Oxidative Damage Induced by Reactive Oxygen Species (천연약용식물의 활성산조종에 의한 산화적 손상의 보호 효과)

  • 이시은;주은미;김정희
    • Environmental Analysis Health and Toxicology
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    • v.15 no.4
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    • pp.147-155
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    • 2000
  • In order to evaluate anti -oxidant activities and protective effect against oxidatve damage, DPPH radical scavenging activity and lipid peroxidation inhibitory activity were measured among methanol extracts prepared from natural medicinal plants. Fourteen natural medicinal plants which were reported to have anti -oxidative or anti-inflammatory effects were selected based on our previous report. In addition to the total methanol extracts, n-hexane, dichloromethane, ethylacetate, n-butanol and water fractions were prepared from each total extract. DPPH radical scavenging assay was performed against 14 total extracts and all samples showed dose-dependent activities in various extent. Among those, 6 samples, methanol extracts of Euryale ferox, paeonia suffruticosa, Areca catechu var. dulcissima, Cinnamomun cassia, Alpinia katsumadai and Betula platyphlla var. japonica showed IC$\sub$50/ value lower than 6.0 $\mu\textrm{g}$/ml. The highest DPPH radical scavenging activity was found in ethylacetate fraction of paeonia suffruticosa with IC$\sub$50/ value of 1.1 $\mu\textrm{g}$/ml. Analysis of lipid peroxidation inhibitory activity on hydrogen peroxide-induced oxidative damage in Chinese hamster lung fibroblast (V79-4) cells revealed that the highest inhibitory effect was observed in methanol extract of Betula platyhpylla var. japonica. Lipid peroxidation inhibitory activity was observed as a dose-dependent manner in all samples used in this study. Among fraction samples, ethylacetate fraction of Alpinia katsumadai had the strongest inhibitory activity with IC$\sub$50/ value of 0.9 $\mu\textrm{g}$/ml.

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Effects of Nitric Oxide on Inhibitory Receptors of Rod Bipolar Cells of Rat Retina

  • Park, No-Gi;Bai, Sun-Ho;Jung, Chang-sub;Chun, Mynng-Hoon
    • The Korean Journal of Physiology and Pharmacology
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    • v.9 no.6
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    • pp.347-352
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    • 2005
  • The effects of nitric oxide (NO) on inhibitory neurotransmitter receptors and some types of inhibitory receptors in dissociated rod bipolar cell (RBC) were investigated. In the whole cell voltage-clamping mode, the gamma-aminobutyric acid (GABA) activated current showed both sustained and transient components. GABA activated transient current was fully blocked by bicuculine, a $GABA_A$ receptor antagonist. The cis-4-aminocrotonic acid (CACA), a $GABA_C$ receptor agonist, evoked the sustained current that was not blocked by bicuculline (BIC). Glycine activated the transient current. These results indicate that the RBCs possess $GABA_A$, $GABA_C$, and glycine inhibitory receptors. Sodium nitroprusside (SNP), a NO analogue, reduced the currents activated by $GABA_A$ receptor only, however, did not reduce the currents activated by either $GABA_C$ or glycine receptors. This study signifies further that only NO depresses the fast inhibitory response activated by $GABA_A$ receptor in RBC. We, therefore, postulate that NO might depress the light-on/off transient inhibitory responses in RBCs in the rat retina.

Antioxidant and Cholinesterase Inhibitory Activities of Aqueous Extract from Rainbow Trout Oncorhynchus mykiss

  • Baek, Jae-Min;Yoon, Na-Young;Kim, Yeon-Kye;Lee, Doo-Seog;Yoon, Ho-Dong;Park, Jeung-Sook
    • Fisheries and Aquatic Sciences
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    • v.14 no.2
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    • pp.89-92
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    • 2011
  • We investigated the antioxidant and cholinesterase inhibitory activities of the aqueous extract of rainbow trout Oncorhynchus mykiss. The antioxidant activity of O. mykiss aqueous extract was determined by in vitro peroxynitrite scavenging activity and reducing power assays. The aqueous extract of O. mykiss showed potent peroxynitrite radical scavenging activity ($IC_{50}=0.12{\pm}0.001\;mg/mL$) and reducing power (absorbance=$0.47{\pm}0.001$) at the concentration of 1 mg/mL. The in vitro cholinesterase inhibitory activity of O. mykiss aqueous extract was examined using spectrophotometric analyses of acetyl- and butyrylcholinesterase. The aqueous extract of O. mykiss showed acetylcholinesterase inhibitory activity ($IC_{50}=1.61{\pm}0.13\;mg/mL$), but did not exhibit inhibitory activity against butyrylcholinesterase. These results suggest that O. mykiss possesses antioxidant and acetylcholinesterase inhibitory activities and provide scientific evidence for the health benefits of O. mykiss aqueous extract.

T-Cell Dysfunction and Inhibitory Receptors in Hepatitis C Virus Infection

  • Lee, Jino;Suh, William I.;Shin, Eui-Cheol
    • IMMUNE NETWORK
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    • v.10 no.4
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    • pp.120-125
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    • 2010
  • Dysfunction of the virus-specific T cells is a cardinal feature in chronic persistent viral infections such as one caused by hepatitis C virus (HCV). In chronic HCV infection, virus-specific dysfunctional CD8 T cells often overexpress various inhibitory receptors. Programmed cell death 1 (PD-1) was the first among these inhibitory receptors that were identified to be overexpressed in functionally impaired T cells. The roles of other inhibitory receptors such as cytotoxic T lymphocyte-associated antigen-4 (CTLA-4) and T cell immunoglobulin and mucin domain-containing molecule 3 (Tim-3) have also been demonstrated in T-cell dysfunctions that occur in chronic HCV patients. Blocking these inhibitory receptors in vitro restores the functions of HCV-specific CD8 T cells and allows enhanced proliferation, cytolytic activity and cytokine production. Therefore, the blockade of the inhibitory receptors is considered as a novel strategy for the treatment of chronic HCV infection.

Effects of Source Recall Conditions on the Relationships among Source Monitoring, Inhibitory Control, and Working Memory (출처 회상 조건이 출처 감찰과 억제적 통제, 작업 기억 간의 관계에 미치는 영향)

  • Lee, Seungjin
    • Korean Journal of Child Studies
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    • v.38 no.2
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    • pp.107-117
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    • 2017
  • Objective: Whereas some studies have suggested that source monitoring is significantly associated with working memory and inhibitory control, both of which are components of executive functioning, other studies have argued otherwise. The author of this study determined that such contradictory findings are a result of heterogeneity in the assessment methods for source monitoring. Therefore, this study aimed at exploring whether the relationships among source monitoring, working memory, and inhibitory control may be altered depending on the differences of source recall conditions. Methods: Eighty children aged 5-8 years saw interesting activities via two different sources. Their source memories on the activity were assessed subsequently. The children were assigned to either the "continuous" source recall group or "non-continuous" source recall group. Both groups participated in working memory and inhibitory control tasks. Results: The results showed that working memory was significantly related to source monitoring regardless of the condition of source recall (continuous vs non-continuous). On the other hand, inhibitory control was significantly associated with source monitoring only in the non-continuous source recall group. Conclusion: Based on these results, the author discussed the need to consider the conditions of source recall during investigative interviews with children in order to induce accurate source monitoring, as part of our effort to interpret the inconsistency of results in the literature and to draw potential applications.

Structural Requirements of Minoxidil Analogs for Enhancing Lysyl Hydroxylase Inhibitory Activity (Lysyl Hydroxylase의 저해활성을 증가시키기 위한 Minoxidil 유도체들의 구조적인 요건)

  • Myung, Pyung-Keun;Sung, Nack-Do;Lee, Jae-Heung
    • KSBB Journal
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    • v.27 no.2
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    • pp.121-126
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    • 2012
  • In order to explore structural features of minoxidil analogs with a view of enhancing lysyl hydroxylase (LH) inhibitory activity, molecular holographic QSAR (HQSAR) and CoMSIA (comparative molecular similarity indices analysis) were performed. The results from the atomic contributions with optimized the HQSAR 6-2 model indicated that, in case of pyrimidine-1-N-oxide substituent, C2 atom of pyrimidine ring and C'3-C'4 bond of 4-piperidinol group showed the highest impact on the inhibitory activity towards LH enzyme. It was also evident from the information of the optimized CoMSIA F5 model that the inhibitory activity mainly depended on the hydrophobic field contribution (36%) and the hydrogen bond (H-bond) field contribution (49.2%) of substrate molecule. Particularly, it is predicted that the functional groups which disfavor H-bond acceptors in large space around the piperidinol group and also the functional groups which favor the H-bond acceptors at C'4 (& C'5) atom in $R_5$ group play a role for increased inhibitory activity. With this in mind, it is likely that a novel candidate having more improved inhibitory activity on hair growth could be designed in the future.

Characterization of β-Secretase Inhibitory Peptide Purified from Blackfin flounder (Glyptocephalus stelleri) Protein Hydrolysate

  • Lee, Jung Kwon;Kim, Sung Rae;Byun, Hee-Guk
    • Journal of Marine Bioscience and Biotechnology
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    • v.10 no.1
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    • pp.1-8
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    • 2018
  • The objective of this study was to purify and characterize the ${\beta}-secretase$ inhibitor from enzymatic hydrolysates of blackfin flounder muscle, for development of a novel anti-dementia agent that may be used in the drug or functional food industries. ${\beta}-secretase$ inhibitory peptide was purified from various enzymatic hydrolysates of blackfin flounder muscle. Among six enzymatic hydrolysates, the Alcalase hydrolysate revealed highest ${\beta}-secretase$ inhibitory activity. Consecutive purification of the blackfin flounder muscle hydrolysate using Sephadex G-25 column chromatography and octadecylsilane C18 reversed phase HPLC techniques were used to isolate a potent ${\beta}-secretase$ inhibitory peptide composed of 5 amino acids, Leu-Thr-Gln-Asp-Trp (MW: 526.7 Da). The $IC_{50}$ value of purified ${\beta}-secretase$ inhibitory peptide was $126.93{\mu}M$. Results of this study suggest that peptides derived from blackfin flounder muscle may be beneficial as anti-dementia compounds in functional foods or as pharmaceuticals.

Inhibitory Activity on Monoamine Oxidase of Chrysanthemum indicum L. (감국의 Monoamine Oxidase 저해활성)

  • Chang, Eun-Ju;Choi, Dong-Kug;Park, Tae-Kyu;Hwang, Keum-Hee
    • Korean Journal of Pharmacognosy
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    • v.38 no.1
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    • pp.27-30
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    • 2007
  • We examined the inhibitory activities against monoamine oxidase (MAO) of Chrysanthemum indicum L. in vitro and in vivo methods. Methanolic extract of C. indicum showed significant inhibitory activities on MAO-A that were prepared from rat brain in vitro. The inhibitory activities were measured by serotonin as a substrate. The $IC_{50}$ value of methanolic extract of C. indicum was 0.24 mg/ml for the inhibition of MAO-A. The ethylacetate fraction of methanolic extract of C. indicum exhibited the best activity toward MAO-A with $IC_{50}$ value of 0.05 mg/ml in vitro. It was observed that those activities in vivo tests have different tendency each other. Ethanolic extract of C. indicum was have no effect on rat MAO by the oral administration (p<0.05). However, MAO inhibitory activities of ethanolic extract of C. indicum by the oral administration have similar tendency to those of iproniazid. Consequently, we suggest that C. indicum may have the effects on the inhibitory activities against MAO both in vitro and in vivo. These results indicates that the C. indicum extract has properties indicative of potential neuroprotective ability.

Production of Angiotensin-I Converting Enzyme Inhibitory Hydrolysates from Egg Albumen

  • Kim, H.S.;Ham, J.S.;Jeong, S.G.;Yoo, Y.M.;Chae, H.S.;Ahn, C.N.;Lee, J.M.
    • Asian-Australasian Journal of Animal Sciences
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    • v.16 no.9
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    • pp.1369-1373
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    • 2003
  • ACE (Angiotensin-I converting enzyme) inhibitory peptides derived from foods are thought to suppress high blood pressure by inhibiting ACE. We tried to make efficient production of the ACE inhibitory hydrolysate from egg albumen. A hydrolysate digested by neutrase presented the highest ACE inhibitory activity ($IC_50\;value=256.35{\mu}g/ml$) and the proper proteolysis was occurred by 1.0% enzyme addition and 4 h incubation at $47^{\circ}C$. Antihypertensive effect of neutrase hydrolysate was investigated in spontaneously hypertensive rats (SHR, n=5). Systolic blood pressure (SBP) was decrease by 6.88% (-14.14 mmHg, p<0.05) at 3 h after oral administration of 300 mg/kg body weight, and by 13.33% (-27.72 mmHg, p<0.05) by emulsified hydrolysate. These results showed that it is very effective to utilize egg albumen as a protein source for the production of ACE inhibitory peptides. However, further studies are required to investigate the methods to increase recovery yield and the isolation of active peptide is necessary for determining its sequence responsible for ACE inhibitory activity.