• Title/Summary/Keyword: Inhibitory Activity

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Synthesis and Biological Activity of Indazole-Derived HMG-CoA Reductase Inhibitors

  • Kim, Jin-Il;Jahng, Yurng-Dong
    • Archives of Pharmacal Research
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    • v.18 no.3
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    • pp.206-212
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    • 1995
  • New hypolipaemic agents, in which substituted indazole nucleus is connected to tetrahydro-4-hydroxy-2H-pyran-2-one by a two-carbon bridge, were designed and synthesized to show significant inhibitory activity against microsomal HMG-CoA reductase in rat liver.

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The Growth Inhibitory Effects of Epigallocatechin Gallate Against Human Skin Melanoma Cells and Human Oral Epitheloid Carcinoma Cells (Epigallocatechin gallate의 인체 피부흑색종세포와 인체 구강유상피암종세포에 대한 성장억제효과)

  • 한두석;박승택;백승화
    • Environmental Mutagens and Carcinogens
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    • v.18 no.2
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    • pp.98-103
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    • 1998
  • Epigallocatechin gallate (EGCG) was reported to exert weak cytotoxicity against normal healthy cells such as C3H10T1/2 cells, but profound inhibitory effects on the initiation or promotion stage of chemical carcinogenesis in mammary gland, blood and mouse skin. This study was carried out to develop antitumor agents with weak side effects and strong antitumor activity. Human skin melanoma cells (HBT 69) and human oral epitheloid carcinoma cells (OCL 17) were cultured in RPMI-1640 media containing 10% fetal bovine serum, antibiotic, and fungizone. After incubation for 24 hrs, the cells were treated with various amounts of (EGCG) for 48 hrs. The growth inhibitory effects of EGCG in human oral epitheloid carcinoma cells were evaluated by the 3- (4,5-djmethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT), neutral red (NR), and sulforhodamine B protein (SRB) assays of colorimetric methods. The light microscopic study was also carried out to observe morphological changes of the treated cells. These results obtained were as follows; 1. Significantly inhibitory effects of EGCG against cultured human oral epithelioid carcinoma cells. 2. Significantly inhibitory effects against cultured human skin melanoma cells treated with 50 $\mu$M EGCG, but decreased inhibitory effects in 100 $\mu$M EGCG. 3. Degenerative changes against cultured human oral epitheloid carcinoma cells. 4. Degenerative changes against human skin melanoma cells treated with 50 UM EGCG, but recovered degenerative changes in 100 $\mu$M EGCG.

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Angiotensin Ⅰ Converting Enzyme(ACE) Inhibitory Activities of Laver(Porphyra tenera) Protein Hydrolysates (김 단백질 가수분해물의 Angiotensin Ⅰ 전환효소 저해 활성)

  • Kim Young-Myoung;Do Jeong-Ryong;In Jae-Pyung;Park Jong-Hyuk
    • The Korean Journal of Food And Nutrition
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    • v.18 no.1
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    • pp.11-18
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    • 2005
  • Angiotensin Ⅰ converting enzyme(ACE) inhibitory activities of laver(Porphyra tenera) protein hydrolysates were investigated by enzymes used for hydrolysis, molecular fractions and drying methods. For the enzymatic hydrolysis, crude laver protein, separated by filtration of water extract of dried laver extracted with 20 times(w/v) water for 3 hours at boiling temperature, were hydrolyzed with three commercial protease, Pepsin, alcalase and maxazyme NNP at optimal conditions. The yield of hydrolysis and ACE inhibitory activities of which were high in order of pepsin, alcalase and maxazyme NNP. ACE inhibitory activities of laver hydrolysates by molecular levels were high in order of 3 kDa > 10 kDa > 3∼10 kDa, and the IC/sub 50/ ACE inhibitory activities by molecular lebels were 4 mg/mL(3 kDa), 5 mg/mL(total hydrolysate), and 20 mg/mL(10 kDa), respectively. The storage stability of dried laver hydrolysates at 20℃ were strongly affected by drying methods, hot air dried of which were much stabler than freeze-dried one.

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.

A Study on the Growth Inhibition of Human Colon Cancer Cells by Eucommial Lea Extract (두충의 인체 암세포 증식억제 효과 연구)

  • 황우익
    • The Korean Journal of Food And Nutrition
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    • v.5 no.1
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    • pp.13-22
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    • 1992
  • This study was divised to observe the inhibitory effect of growth rate of human colon cancer cells by Eucommial leaf extract, in vitro. Three species of human colon cancer cells, HRT-18, HCT-48 and HT-29, were used for the experiment. Each extract of Eucommial leaf was prepared by extraction with water, 95% alcohol, acetone, chloroform and petroleum ether, and then the inhibitory effect of each extract on the growth rate of cells was compared with control group and each other. The experimental results obtained are summarized as follows; 1. Inhibitory effects on growth rate of human colon cancer fells were strongest in the petroleum ether extract and next in the chloroform extract. 2. Inhibitory effects on the growth rate of the cancer cells by extracts of water, 95% alcohol and acetone were weaker than that of petroleum ether and chloroform. 3. Inhibitory effect of each extract on the cancer cell growth was shown most strong activity in HT-29, and was in order of HRT 18 and HCT-48. In view of the results, it could be suggested that inhibitory effects of non-polar solvent's extracts against the cancer cell growth were more stronger than that of polar solvents and the effects were indicated difference according to the species of the cells.

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Purification of Angiotensin I-Converting Enzyme Inhibitory Peptide from Squid Todarodes pacificus Skin (오징어(Todarodes pacificus) 껍질로부터 Angiotensin I 전환효소 저해 펩티드의 분리 정제)

  • Lee, Jung-Kwon;Jeon, Joong-Kyun;Byun, Hee-Guk
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.44 no.2
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    • pp.118-125
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    • 2011
  • In this study, an angiotensin I-converting enzyme (ACE) inhibitor from squid skin was purified and characterized. Squid (Todarodes pacificus) skin protein isolates were hydrolyzed using six commercial proteases: alcalase, ${\alpha}$-chymotrypsin, neutrase, papain, pepsin, and trypsin. The peptic hydrolysate had the highest ACE inhibitory activity. The ACE inhibitory peptide was purified using Sephadex G-25 column chromatography and reverse phase high-performance liquid chromatography (HPLC) with a $C_{18}$ column. The purified ACE inhibitory peptide was identified and sequenced, and found to consist of seven amino acid residues: Ser-Ala-Gly-Ser-Leu-Val-Pro (657Da). The $IC_{50}$ value of the purified ACE inhibitory peptide was 766.2 ${\mu}M$, and Lineweaver-Burk plots suggested that the purified peptide acts as a noncompetitive ACE inhibitor. These results suggest that the ACE inhibitory peptide purified from the peptic hydrolysate of squid skin may be of benefit in developing antihypertensive drugs and functional foods.

Inhibitory Effects of Chinese Medicinal Plants on the Platelet-Activating Factor (PAF) Receptor Binding (중국 약용식물의 혈소판 활성화인자 수용체 결합 억제활성)

  • Kang, Young-Hwa
    • Korean Journal of Medicinal Crop Science
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    • v.13 no.4
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    • pp.178-181
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    • 2005
  • Methanolic extracts of fifteen Chinese medicinal plants were screened for platelet-activating factor (PAF) receptor binding inhibitory activity using rabbit platelet. Campsis grandiflora, Dalbergia odorifera, Vaccaria segetalis and Zanthoxylum nitidum showed significant inhibitory effects on the platelet-activating factor (PAF) receptor binding. Campsis grandiflora, Dalbergia odorifera, Vaccaria segetalis and Zanthoxylum nitidum inhibited 52%, 56%, 70%, and 66% respectively at the concentration of 0.2 mg/ml.

Inhibitory Effects of the Extract of Rhus verniciflua Stokes on the Reverse Transcriptase of AIDS

  • Kim, Myong-Jo;Choi, Won-Cheol;Barshinikov, A. M.;Kobayashi, A.
    • Korean Journal of Medicinal Crop Science
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    • v.10 no.4
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    • pp.284-287
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    • 2002
  • Four olefinic catechols, commonly referred to as urushiol were isolated from the sap of Korean Rhus verniciflua Stokes and had the stronger inhibitory effects on the reverse transcriptase of AIDS. The hexane extract with a inhibitory effects on reverse transcriptase was purified by silica and ODS gel column chromatography. The active compounds were identified by MS and $^1H-NMR$ as 3-[8' (Z), 11' (Z), 14' -pentadecatrienyl]catechol, 3-[8' (Z), 11' (Z)-pentadecadienyl]catechol, 3-[8' (Z)-penta- decenyl]catechol, and 3-pentadecylcatechol. All of these compounds showed strong inhibitory effects on reverse transcriptase of AIDS, in which 3-pentadecylcatechol exhibited the highest activity $(IC_{50}\;:\;10.87\;{\mu}g/ml)$.