• Title/Summary/Keyword: Inhibition model

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Use of Capparis decidua Extract as a Green Inhibitor for Pure Aluminum Corrosion in Acidic Media

  • Al-Bataineh, Nezar;Al-Qudah, Mahmoud A.;Abu-Orabi, Sultan;Bataineh, Tareq;Hamaideh, Rasha S.;Al-Momani, Idrees F.;Hijazi, Ahmed K.
    • Corrosion Science and Technology
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    • v.21 no.1
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    • pp.9-20
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    • 2022
  • The aim of this paper is to study corrosion inhibition of Aluminum with Capparis decidua extract. The study was performed in a 1.0 M solution of hydrochloric acid (HCl) and was monitored both by measuring mass loss and by using electrochemical and polarization methods. A scanning electron microscopy (SEM) technique was also applied for surface morphology analysis. The results revealed high inhibition efficiency of Capparis decidua extract. Our data also determined that efficiency is governed by temperature and concentration of extract. Optimum (88.2%) inhibitor efficiency was found with maximum extract concentration at 45 o C. The results also showed a slight diminution of aluminum dissolution when the temperature is low. Based on the Langmuir adsorption model, Capparis decidua adsorption on the aluminum surface shows a high regression coefficient value. From the results, the activation enthalpy (∆H#) and activation entropy (∆S#) were estimated and discussed. In conclusion, the study clearly shows that Capparis decidua extract acted against aluminum corrosion in acidic media by forming a protective film on top of the aluminum surface.

Study on the Effect of Yipahnsan(立安散) on Angiogenic Inhibition Mechanism (입안산(立安散)이 Angiogenesis 억제기전(抑制棋戰)에 미치는 영향(影響))

  • Lee, Gi-Ryong;Choi, Seung-Hoon;Ahn, Kyoo-Seok
    • THE JOURNAL OF KOREAN ORIENTAL ONCOLOGY
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    • v.4 no.1
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    • pp.177-197
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    • 1998
  • This experimental study was carried out to evaluate the effect of Yipahnsan on angiogenic inhibition mechanism. This study investigates the effects of Yipahnsan on angiogenic inhibition mechanism evaluate cell adhesive inhibition effect, DNA fragmantaion analysis, nuclear condensation assay, FACScan analysis, angiogenic lumen formation assay, immunocytochemistry analysis, RT-PCR for mRNA expression, western blot analysis, confocal analysis for $Ca^{2+}influx$. The results were summarized as follows : 1. The cell adhesive inhibition ability was strongly increased from $5{\mu}g/ml$ on ECV304 cell line and ECVPAR cell line. 2. YY water extract caused $G_0/G_1$ arrest peak to existed on the ECV304 cell line. 3. YY water extract caused inhibition of proliferation and inducement of apoptosis on the collagen coated plate in ECV304 cell line. 4. YY water extract inhibited the lumen formation on the matrigel coated plate in ECV304 cell line. 5. YY water extract inhibited the expressions of LFA-1 and ELAM-1 on ECV304 cell line and ECVPAR cell line. 6. YY water extract inhibited the expressions of MMP-9 and uPA on ECV304 cell line and ECVPAR cell line. 7. YY water extract inhibited the expression of integrin ${\alpha}_v{\beta}_3$ on ECV304 cell line and ECVPAR cell line. 8. YY water extract decreased the change of $Ca^{2+}$ in intracellular on ECV304 cell line and ECVPAR cell line. According to the results, Yipahnsan showed to be a key antagonist of integrin ${\alpha}_v{\beta}_3$, and to be induction of apoptosis by p53 through flow cytometry. This report also demonstrated that expressions of MMP-9 and uPA were blocked under the angiogenesis model. Thus, we suggested that Yipahnsan blocks angiogenesis by inducing apoptosis in ECV304 and ECVPAR cell lines, and another oriental herbal medicine that treats qi-stagnation and blood-stasis type also has angiogenic inhibition effects.

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Study on the Effect of Hwallakhyoreungdan(活絡效靈丹) on Angiogenic Inhibition Mechanism (활락효령단(活絡效靈丹)이 Angiogenesis 억제기전(抑制機轉)에 미치는 영향(影響))

  • Na, Ki-Whan;Choi, Seung-Hoon;Ahn, Kyoo-Seok
    • THE JOURNAL OF KOREAN ORIENTAL ONCOLOGY
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    • v.4 no.1
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    • pp.17-36
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    • 1998
  • This experimental study was carried out to evaluate the effects of Hwallakhyoreungdan on angiogenic inhibition mechanism. In order to investigate the effects of Hwallakhyoreungdan on angiogenic inhibition mechanism, MTT assay, cell adhesive inhibition effect, DNA fragmantaion analysis, Nuclear condensation assay, FACScan analysis, Angiogenic lumen formation assay, Immunocytochemistry analysis, RT-PCR for mRNA expression, Western blot analysis and Confocal analysis for $Ca^{2+}$ change were performed. The results were summarized as follows: 1. The cell adhesive inhibition ability was strong from $5{\mu}g/ml$. 2. The $G_0/G_1$ arrest peak was existed on ECV304 cell-line. 3. The cells on Collagen plate were inhibition of proliferation and inducement of apoptosis by HR water extract. 4. Angiogenic lumen formation was inhibited by HR water extract. 5. LFA-1 and ELAM-1's expression were inhibited by HR water extract. They are commenly participation on inflammation and tumor regeneration. 6. The expression of MMP-9 and uPA were inhibited by HR water extract. 7. The expression of integrin ${\alpha}_v{\beta}_3$ was inhibited by HR water extract. 8. The expression of intracellular molecule were successively inhibited by HR water extract therefore the proliferation of ECV304 cell line was stopped and apoptosis was induced. 9. The change of $Ca^{2+}$ was decreased by HR water extract it cause confusion of signal transduction pathway therefore it was take part in apoptosis. According to the results, Hwallakhyoreungdan showed to be a key antaonist of integrin ${\alpha}_v{\beta}_3$, and to be induction of apoptosis by p53 through flow cytometry. This report also demonstrated that expressions of MMP-9 and uPA was blocked under the angiogenesis model. Thus, we suggests that Hwallakhyoreungdan blocks angiogenesis by inducing apoptosis of ECV304 and ECVPAR cell lines and another oriental herbal medicine that treats blood-stasis type also has angiogenic inhibition effects.

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An Application of Toxicity Test to Water Management and Water Treatment (수질관리와 수처리에의 독성시험의 응용)

  • Kim, Berm-Soo
    • Journal of Korean Society of Water and Wastewater
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    • v.19 no.5
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    • pp.639-646
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    • 2005
  • In this research, we tried to develop the application method to water management and treatment using toxicity test method. When we measure the toxicity of environmental samples, we have to decide whether we take some countermeasures to reduce the toxicity or not. The first issue is how to set these action levels in each bioassays. A new idea was attempted to authorize indirect approach of each bioassays through the response characteristics against mixture of chemicals in water quality standard. The significant response in the cell-growth-inhibition bioassay was detected for standards-mixture(STDs). For acute toxicity assay, STDs-based implicit correlation between risks to humans and bioassay data showed a rational approach to set action levels in practical management. A simple model was proposed to describe and predict the changes in the total toxicity based on the concentrations of toxic-controlling chemicals during the ozonation of landfill leachates. On the basis of this simple model, toxicity reduction was predicted for pre-aggregation treatment before ozonation and ozone concentration during the ozonation. The method proposed in this study would be useful in optimizing water treatment processes and their running conditions in terms of the toxicity reduction efficacy.

Docking Study of Flavonols and Human c-Jun N-terminal Kinase 1

  • Lee, Jee-Young;Jeong, Ki-Woong;Heo, Yong-Seok;Kim, Yang-Mee
    • Bulletin of the Korean Chemical Society
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    • v.31 no.8
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    • pp.2147-2150
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    • 2010
  • c-Jun N-terminal kinase 1 (JNK1) is involved in apoptosis, cell differentiation and proliferation. It has been reported that a flavonol, quercetin, induces cell apoptosis and JNK inhibition. In order to understand the interactions of quercetin and JNK1, we performed receptor-oriented pharmacophore based in silico screening and determined a binding model of human JNK1 and quercetin at the ATP binding site of JNK1. 5-OH of A-ring and carbonyl oxygen of C-ring of quercetin participated in hydrogen bonding interactions with backbone of E109 and M111. Additionally, 3'-OH of quercetin formed a hydrogen bond with backbone of I32. One hydrophobic interaction is related on the binding of quercetin to JNK1 with I32, N114, and V158. Based on this model, we conducted a docking study with other 8 flavonols to find possible flavonoids inhibitors of JNK1. We proposed that one flavonols, rhamnetin, can be a potent inhibitor of JNK and 5-OH of A-ring and 3'-OH of B-ring of flavonols are the essential features for JNK1 inhibition.

Basal Ganglia Motor Circuit and Physiology of Parkinsonism (기저핵 운동회로와 파킨슨 증상의 신경생리)

  • Sohn, Young Ho
    • Annals of Clinical Neurophysiology
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    • v.8 no.2
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    • pp.107-124
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    • 2006
  • The basal ganglia are a group of nuclei located in the deep portion of the brain. Along with the cerebellum, the basal ganglia have a major role in controlling human voluntary movements, and their dysfunction is apparently responsible for various involuntary movements. Although the exact mechanism of how the basal ganglia control movements has yet to be clarified, the model of focused selection (through the direct pathway) and tonic inhibition (via the indirect pathway) is proposed to be a principal functional model of the basal ganglia. Parkinson's disease (PD) is classically characterized by bradykinesia, rigidity and tremor-at-rest. All features seem to be associated with dopamine depletion resulting from the degeneration of the nigrostriatal pathway, which produces reduced activity of the direct pathway and a concurrent enhancement of excitatory output from STN. This change may result in increased tonic background inhibition and reduced focused selection via the direct pathway, causing difficulties in performing voluntary movements selectively. However, it has not been possible to define a single underlying pathophysiologic mechanism that explains all parkinsonian symptoms. Here the data that give separate understanding to each of the three classic features are discussed.

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Acebutolol, a Cardioselective Beta Blocker, Promotes Glucose Uptake in Diabetic Model Cells by Inhibiting JNK-JIP1 Interaction

  • Li, Yi;Jung, Nan-Young;Yoo, Jae Cheal;Kim, Yul;Yi, Gwan-Su
    • Biomolecules & Therapeutics
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    • v.26 no.5
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    • pp.458-463
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    • 2018
  • The phosphorylation of JNK is known to induce insulin resistance in insulin target tissues. The inhibition of JNK-JIP1 interaction, which interferes JNK phosphorylation, becomes a potential target for drug development of type 2 diabetes. To discover the inhibitors of JNK-JIP1 interaction, we screened out 30 candidates from 4320 compound library with In Cell Interaction Trap method. The candidates were further confirmed and narrowed down to five compounds using the FRET method in a model cell. Among those five compounds, Acebutolol showed notable inhibition of JNK phosphorylation and elevation of glucose uptake in diabetic models of adipocyte and liver cell. Structural computation showed that the binding affinity of Acebutolol on the JNK-JIP1 interaction site was comparable to the known inhibitor, BI-78D3. Our results suggest that Acebutolol, an FDA-approved beta blocker for hypertension therapy, could have a new repurposed effect on type 2 diabetes elevating glucose uptake process by inhibiting JNK-JIP1 interaction.

Hologram Quantitative Structure-Activity Relationships Study of N-Phenyl-N'-{4-(4-quinolyloxy)phenyl} Urea Derivatives as VEGFR-2 Tyrosine Kinase Inhibitors

  • Keretsu, Seketoulie;Balasubramanian, Pavithra K.;Bhujbal, Swapnil P.;Cho, Seung Joo
    • Journal of Integrative Natural Science
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    • v.10 no.3
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    • pp.141-147
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    • 2017
  • Vascular endothelial growth factor (VEGF) is an important signaling protein involved in angiogenesis, which is the formation of new blood vessels from pre-existing vessels. Consequently, blocking of the vascular endothelial growth factor receptor (VEGFR-2) by small molecule inhibitors leads to the inhibition of cancer induced angiogenesis. In this study, we performed a two dimensional quantitative structure activity relationship (2D-QSAR) study of 38 N-Phenyl-N'-{4-(4-quinolyloxy) phenyl} urea derivatives as VEGFR-2 inhibitors based on hologram quantitative structure-activity (HQSAR). The model developed showed reasonable $q^2=0.521$ and $r^2=0.932$ values indicating good predictive ability and reliability. The atomic contribution map analysis of most active compound (compound 7) indicates that hydrogen and oxygen atoms in the side chain of ring A and oxygen atom in side chain of ring C contributes positively to the activity of the compounds. The HQSAR model developed and the atomic contribution map can serve as a guideline in designing new compounds for VEGFR-2 inhibition.

The effective model of the human Acetyl-CoA Carboxylase inhibition by aromatic-structure inhibitors

  • Minh, Nguyen Truong Cong;Thanh, Bui Tho;Truong, Le Xuan;Suong, Nguyen Thi Bang;Thao, Le Thi Xuan
    • Journal of IKEEE
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    • v.21 no.3
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    • pp.309-319
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    • 2017
  • The research investigates the inhibition of fatty acid biosynthesis of the human Acetyl-CoA Carboxylase enzyme by the aromatic-structure inhibitors (also known as ligands) containing variables of substituents, contributing an important role in the treatment of fatty-acid metabolic syndrome expressed by the group of cardiovascular risk factors increasing the incidence of coronary heart disease and type-2 diabetes. The effective interoperability between ligand and enzyme is characterized by a 50% concentration of enzyme inhibitor ($IC_{50}$) which was determined by experiment, and the factor of geometry structure of the ligands which are modeled by quantum mechanical methods using HyperChem 8.0.10 and Gaussian 09W softwares, combining with the calculation of quantum chemical and chemico-physical structural parameters using HyperChem 8.0.10 and Padel Descriptor 2.21 softwares. The result data are processed with the combination of classical statistical methods and modern bioinformatics methods using the statistical softwares of Department of Pharmaceutical Technology - Jadavpur University - India and R v3.3.1 software in order to accomplish a model of the quantitative structure - activity relationship between aromatic-structure ligands inhibiting fatty acid biosynthesis of the human Acetyl-CoA Carboxylase.

Inhibition of Chronic Skin Inflammation by Topical Anti-inflammatory Flavonoid Preparation, Ato $Formula^{\circledR}$

  • Lim, Hyun;Son, Kun-Ho;Chang, Hyeun-Wook;Kang, Sam-Sik;Kim, Hyun-Pyo
    • Archives of Pharmacal Research
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    • v.29 no.6
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    • pp.503-507
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    • 2006
  • Flavonoids are known as natural anti-inflammatory agents. In this investigation, an anti-inflammatory potential of new topical preparation (SK Ato $Formula^{\circledR}$) containing flavonoid mixtures from Scutellaria baicalensis Georgi roots and Ginkgo biloba L. leaves with an extract of Gentiana scabra Bunge roots was evaluated in an animal model of chronic skin inflammation. Multiple 12-O-tetradecanoylphorbol-13-acetate treatments for 7 consecutive days on ICR mouse ear provoked a chronic type of skin inflammation: dermal edema, epidermal hyperplasia and infiltration of inflammatory cells. When topically applied in this model, this row formulation $(5-20\;{\mu}L/ear/treatment)$ reduced these responses. Furthermore, it inhibited prostaglandin $E_2$ generation (17.1-33.3%) and suppressed the expression of proinflammatory genes, cyclooxygenase-2 and $interleulin-1{\beta}$ in the skin lesion. Although the potency of inhibition was lower than that of prednisolone, all these results suggest that Ato $Formula^{\circledR}$ may be beneficial for treating chronic skin inflammatory disorders such as atopic dermatitis.