• Journal of Microbiology and Biotechnology
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• 제16권5호
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• pp.757-763
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• 2006

Angiotensin I-converting enzyme (ACE) inhibitors have generally been very useful to remedy or prevent hypertension. This study describes the extraction and characterization of an ACE inhibitor from the fruiting body of Pholiota adiposa ASI 24012, which can be used as an antihypertensive drug. The maximal ACE inhibitory activity $(IC_{50};0.25mg)$ was obtained when the fruiting body of Pholiota adiposa ASI 24012 was extracted with distilled water at $30^{\circ}C$ for 12 h. After the purification of ACE inhibitor with ultrafiltration, Sephadex G-25 column chromatography, and reverse-phase HPLC, an active fraction with an $IC_{50}$ of 0.044 mg was obtained. The purified ACE inhibitory peptide was a novel pentapeptide, showing very little similarity to other ACE inhibitory peptide sequences. The molecular mass of the purified ACE inhibitor was estimated to be 414 daltons with a sequence of Gly-Glu-Gly-Gly-Pro, and showed a clear antihypertensive effect on spontaneously hypertensive rats (SHR) at a dosage of 1 mg/kg.

• Journal of Microbiology and Biotechnology
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• 제5권5호
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• pp.280-284
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• 1995

Aspergi11us niger F-580, a potent producer of aminopeptidase M inhibitor, was isolated from the brown spots of plant leaves with a pathological trait. The inhibitory activity was found only in the fungal mat formed by surface culture of Aspergi11us niger F-580, but not in the culture supernatant or cell pellet. The inhibitor was purified from the hot water extract of this fungal mat by using chromatographies on Diaion HP-20, DEAE-cellulose, Sephadex G-l0 and YMC-ODS-AQ columns. The purified inhibitor was analyzed by UV, mass, and NMR spectroscopies, and identified as OF494911, which had been isolated as an aminopeptidase B inhibitor from Penicillium rugulosum OF4949

• Journal of Microbiology and Biotechnology
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• 제5권1호
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• pp.36-40
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• 1995

Valistatin, a new inhibitor of aminopeptidase M(AP-M) was discovered in the culture broth of Streptomyces sp. SL20209 isolated from a soil sample. The inhibitor was purified by extraction with n-butanol and the various column chromatographies, and then isolated as whitish powder. The $^1 H-and ^1 H, ^1 H-COSY$ NMR studies, amino acid analysis, and fragmentation patterns by FAB-MS suggested the presence of one 3-amino-2-hydroxy-4-phenylbutanoic acid and two valine residues in the inhibitor. Thus, the structure of valistatin was determined as 3-amino-2-hydroxy-4-phenylbutanoyl-valyl-valine. Valistatin has the molecular formular $C_20H_31N_3 O_5$ (MW 394), and its $IC_50$ value against hog kidney AP-M was determined to be 3.12 $mu g/ml$.

• 한국추진공학회지
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• 제19권1호
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• pp.42-49
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• 2015

3차원 Large Eddy Simulation(LES)와 Proper Orthogonal Decomposition(POD) 기법을 이용하여 고체로켓의 인히비터에서 발생하는 연소실내 압력 진동 특성을 분석하였다. 인히비터 후방에서 발생한 와류는 Flow-acoustic coupling에 의해 주기적으로 반복하여 생성, 소멸이 이루어지는 것을 확인하였고, 이 와류가 내삽 노즐 입구 도출부에 충돌하면서 유동이 불균질하게 분해되고, 후방 돔으로 유입된 유동에 의한 압력 진동은 연소실 압력 진동 가진의 원인이 된다. 또한 인히비터에서 발생하는 와흘림(vortex shedding) 주기는 연소실내 와류 발생 주기와 일치하며, 실험에서 측정된 압력 진동 주파수와 비교 분석하였다.

• Corrosion Science and Technology
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• 제16권3호
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• pp.91-99
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• 2017

The objective of this work was to develop efficient synergistic inhibitor combinations comprising sodium nitrite ($NaNO_2$) and an inhibitor-blend code named (SN-50), keeping in view of their application in industrial cooling water systems. The electrochemical characteristics of the carbon steel working electrode in simulated cooling water (SCW), without and with the addition of different combinations of the inhibitors, were investigated using electrochemical impedance spectroscopy (EIS), open circuit potential (OCP). The electrode surface changes were followed by visual characterization methods. It was demonstrated in this study that all the combinations of the inhibitors exhibited synergistic benefit and higher inhibition efficiencies than did either of the individual inhibitors. The addition of SN-50 inhibitor to the SCW shifted the OCP to more anodic values and increased the polarization resistance ($R_p$) values of carbon steel at all applied concentrations. The higher the applied sodium nitrite concentration (in the protection concentration range), the higher the obtained $R_p$ values and the inhibition efficiency improved by increasing the inhibitor concentration.

• 한국환경보건학회지
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• 제29권3호
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• pp.65-71
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• 2003

The injection concentration of corrosion inhibitor increases under the pH 7, temperature of 2$0^{\circ}C$, and alkalinity of 35 mg/l (as CaCO$_3$), the corrosion rate gradually decreased. When the corrosion inhibitor of 10 mg/l is injected, the corrosion rate for carbon steel pipe, galvanized steel pipe, and copper pipe reduces for 37, 66 and 61 % respectively that it is more efficient on galvanized steel pipe and copper pipe. As a result of examination of corrosion rate at pH 6, 7, and 8 when injecting 10 mg/l of corrosion inhibitor under the conditions of 2$0^{\circ}C$ in water temperature and 35 mg/l (as CaCO$_3$) in alkalinity, the efficiency of the corrosion inhibitor increases as the pH increases. For carbon steel pipe, it does not show much a difference with the change of the pH condition, but galvanized steel pipe and copper pipe clearly show the corrosion rate depending on the change of the pH condition. The efficiency of corrosion inhibitor is low as the concentration of residual chlorine is high, but it does not show a great influence at 0.4 mg/l or less. For each pipe type, in the case of carbon steel pipe, the range of increase of corrosion speed following the residual chloride is higher than the other pipe types. In the meantime, the effect following the residual chlorine in copper pipe is low.

• Natural Product Sciences
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• 제24권2호
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• pp.88-92
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• 2018

The present study was undertaken to investigate the isolated compounds from the stem bark of Garcinia atroviridis as potential cholinesterase inhibitors and the ligand-enzyme interactions of selected bioactive compounds in silico. The in vitro cholinesterase results showed that quercetin (3) was the most active AChE inhibitor ($12.65{\pm}1.57{\mu}g/ml$) while garcinexanthone G (6) was the most active BChE inhibitor ($18.86{\pm}2.41{\mu}g/ml$). It is noteworthy to note that compound 6 was a selective inhibitor with the selectivity index of 11.82. Molecular insight from docking interaction further substantiate that orientation of compound 6 in the catalytic site which enhanced its binding affinity as compared to other xanthones. The nature of protein-ligand interactions of compound 6 is mainly hydrogen bonding, and the hydroxyl group of compound 6 at C-10 is vital in BChE inhibition activity. Therefore, compound 6 is a notable lead for further drug design and development of BChE selective inhibitor.

• Asian Pacific Journal of Cancer Prevention
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• 제17권3호
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• pp.1103-1110
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• 2016

In the present study, we investigated the effects of motesanib (AMG 706), a multikinase inhibitor alone and in combination with DuP-697, an irreversible selective inhibitor of COX-2, on cell proliferation, angiogenesis, and apoptosis induction in a human colorectal cancer cell line (HT29). Real time cell analysis (RTCA, Xcelligence system) was used to determine the effects on colorectal cancer cell proliferation. Apoptosis was assessed with annexin V staining and angiogenesis was determined with chorioallantoic membrane model. We found that motesanib alone exerted antiproliferative, antiangiogenic and apoptotic effects on HT29 colorectal cancer cells. Combination with DUP-697 increased the antiproliferative, antiangiogenic and apoptotic effects. Results of this study indicate that motesanib may be a good choice in treatment of colorectal tumors. In addition, the increased effects of combination of motesanib with DuP-697 raise the possibility of using lower doses of these drugs and therefore avoid/minimize the dose-dependent side effects generally observed.

• Asian Pacific Journal of Cancer Prevention
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• 제15권18호
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• pp.7913-7917
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• 2014

Apoptotic cell death plays a predominant role in histone deacetylase (HDAC) inhibitor-induced cytotoxicity. Nuclear morphological changes and activation of apoptotic executors are involved in CTS203-induced cell death. However, emerging issues of HDAC inhibitor-resistance have been observed in patients. Herein, MCF-7 cells were continuously exposed to CTS203 until the derived cells could proliferate normally in its presence. The newly obtained CTS203-resistant cells were nominated as MCF-7/203R. Compared to MCF-7 original cells, the MCF-7/203R cells were less sensitive to CTS203-induced apoptosis, with a minimal 6-fold higher $IC_{50}$ value. In contrast, the expression of Beclin-1 was dramatically up-regulated, positively correlated to the acquisition of CTS203-resistance. Our results revealed the participation of autophagy in acquired HDAC inhibitor-resistance and further identified Beclin-1 as a promising target for anti-drug resistance.

• 한국미생물·생명공학회지
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• 제24권1호
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• pp.101-104
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• 1996

During the screening of inhibitor of DNA topoisomerase I from microbial secondary metabolites, Streptomyces melanosporofaciens 7489 which was capable of producing high level of inhibitor was selected from soil. The active compound (7489-1) was purified from the culture broth by solvent extraction, silica gel column chromatography and HPLC. The inhibitor was identified as dibutyl phthalate by spectroscopic methods of UV, $^{1}H$-NMR, $^{13}C$-NMR, DEPT and EI-MS. 7489-1 showed a strong inhibitory activity against topoisomerase I with 10 ${\mu}$M of $IC_{50}$ value.