Sang-Bum Lee

Estrogenic/antiestrogenic activities of a Epimedium koreanum extract and its major components: in vitro and in vivo studies.

The estrogenic and antiestrogenic activities of Epimedii Herba, which is a traditional medicinal herb used in Korea and China were investigated in this study. The in vitro estrogen receptor (ER) mediated estrogenic/antiestrogenic activities of an Epimedii Herba extract (Epi ext) and its major components were determined using an estrogen responsive element driven reporter gene assay in MCF-7/ERE and HEK293T cells. The Epi ext exhibited ERα- and ERβ-mediated estrogenic activity with an EC(50) of 5.0 and 17.8 μM in HEK293T cells, respectively. Prenylflavonoid glycosides such as icariin (ICA), epimedin A, B, and C did not show any in vitro estrogenic or antiestrogenic activities. Icaritin (ICT) and quercetin exhibited in vitro ER mediated estrogenic activity with a more potent interaction with ERβ. In vivo estrogenic activities of the Epi ext, ICA and ICT were compared using an uterotrophic assay. Although the potency of in vitro estrogenic activity was in the order of ICT>Epi ext>ICA, ICA had the strongest estrogenic activity and next ICT in ovariectomized rats. These results collectively suggest that phytoestrogens possess both estrogenic and antiestrogenic activity, and that the differential expression of these two compounds with opposing activities is dependent on the physiological environment in terms of estrogen level, which may be the case in humans.

Identification of 2,3,6-trisubstituted quinoxaline derivatives as a Wnt2/β-catenin pathway inhibitor in non-small-cell lung cancer cell lines.

We screened 1434 small heterocyclic molecules and identified thirteen 2,3,6-trisubstituted quinoxaline derivatives that were able to inhibit the Wnt/β-catenin signal pathway and cell proliferation. In the screen, some of the hit compounds such as the ethylene group-coupled quinoxaline derivatives were shown to hold promise for use as potential small-molecule inhibitors of the Wnt/β-catenin signal pathway in non-small-cell lung cancer cell lines.

A novel 3-arylethynyl-substituted pyrido[2,3,-b]pyrazine derivatives and pharmacophore model as Wnt2/β-catenin pathway inhibitors in non-small-cell lung cancer cell lines.

We developed Wnt/β-catenin inhibitors by identifying 13 number of 3-arylethynyl-substituted pyrido[2,3,-b]pyrazine derivatives that were able to inhibit the Wnt/β-catenin signal pathway and cancer cell proliferation. In the optimization process, a series of 2,3,6-trisubstituted pyrido[2,3,-b]pyrazine core skeletons showed were shown to higher activity than 2,3,6-trisubstituted quinoxalines and thus hold promise for use as potential small-molecule inhibitors of the Wnt/β-catenin signal pathway in non-small-cell lung cancer cell (NSCLC) lines. And we have studied the pharmacophore mapping for compound 954, which presented the highest activity with a fit value of 2.81. The pharmacophore mapping for the compounds including 954, pyrido[2,3,-b]pyrazine core had hydrogen-bond acceptor site and hydrophobic center roles.

Effects of CYP2C19 and MDR1 genotype on the eradication rate of Helicobacter pylori infection by triple therapy with pantoprazole, amoxycillin and clarithromycin

Backgrounds:  CYP2C19 polymorphism plays an important role in the metabolism of proton pump inhibitors. The multidrug resistance (MDR)1 genotype is associated with the successful eradication of Helicobacter pylori. The aim of the present study was to investigate the effects of CYP2C19 and MDR1 genotypes on the eradication rate of H. pylori using a pantoprazole‐based triple therapy.

Peripubertal administration of icariin and icaritin advances pubertal development in female rats.

Epimedii Herba is a traditional medicinal herb used in Korea and China and exerts estrogenic activity. In this study, we investigated the effect of peripubertal administration of Epimedii Herba on pubertal development in female rats using a modified protocol of the rodent 20-day pubertal female assay. Female Sprague-Dawley rats (21 days old after weaning, 10 rats per group) were divided into five groups: saline (Con), ethinyl estradiol (E2), Epimedii Herba ext (Ext), icariin (ICI), and icaritin (ICT), which were administered by oral gavage (E2 by subcutaneous injection) from postnatal day (PND) 21 through PND40. The time to vaginal opening (VO) was shorter for the Epimedii groups, particularly for the ICT group (p<0.05). Treatment with ICI and ICT significantly increased the duration of the estrus cycle (ICI, 2.78 days; ICT, 4.0 days; control, 1.78 days). Ovary weight was reduced by E2 treatment and increased by the Ext, ICI, and ICT treatments while the weight of the uterus and pituitary glands increased significantly only in the E2 and ICT groups. Although Epimedii Herba displayed relatively weak estrogenic activity, its repeated administration could affect pubertal development in female rats.

Co-expression of human cytochrome b5 increases expression of cytochrome P450 3A4 in Escherichia coli by stabilizing mRNA.

CYP3A4 is the most abundant cytochrome P450 in the human liver. The expression level of CYP3A4 when coexpressed with cytochrome b(5) (cyt b(5)) in Escherichia coli was 20-60% higher than that when it was expressed alone over an extended period (48-72 h). This time-dependent elevation in coexpression with cyt b(5) was a result of an increase in CYP3A4 mRNA half-life; no significant change in CYP3A4 degradation was seen in the bacterial protease fraction. These results suggest that the higher CYP3A4 levels observed upon coexpression with cyt b(5) primarily resulted from CYP3A4 mRNA stabilization by cyt b(5).

Measurement of MCG in Unshielded Environment Using a Second-Order SQUID Gradiometer

In this paper, we fabricated a low-TC second-order superconducting quantum interference device gradiometer (SQUID) to measure magnetocardiography (MCG) in unshielded environment. The second-order gradiometer consists of the pickup coil and the SQUID. The pickup coil is formed with two single-turn coils and one double-turn coil. The three coils are connected in order of single-, double-, and single-turn coil. The coupling polarity of two single coils is opposite to the double-turn coil. The SQUID is based on double relaxation oscillation SQUID (DROS), which consists of a hysteretic signal SQUID, a reference junction, and shunted a relaxation circuit with a resistor and an inductor. The DROS has ten times larger flux-to-voltage transfer coefficient (~ 1 mV/Phi0) than that of the conventional SQUID. Therefore, DROS could be operated with a simple flux-locked loop circuit. The pickup coil and the SQUID were fabricated on the independent wafers and connected superconductively using an Nb wire. The overall size of the second-order gradiometer is 94 times 12 mm2 with a baseline of 35 mm. The average field noise was about 8 fT /radicHz at 100 Hz with the second-order gradiometer in shielded or unshielded environment. The noise level is low enough to measure MCG signals in the unshielded environment. Finally, we measure the MCG in shielded and unshielded environments by using the second-order gradiometer and compared the signal characteristics measured in both environments.

3D boiler tube leak detection technique using acoustic emission signals for power plant structure health monitoring

This paper propose a 3D source location technique for locating leak in boiler tube of power plant using Acoustic Emission technique. In order to verify the effectiveness of the suggested technique, this paper presents a case study to locate the source of leak in the boiler tube of a 500MW class thermal power plant. Test were carry out using soot blower signal from 62 points with a pressure of 10 bar when plant is under a normal working condition. The conventional approaches for detection leak in power plant involved the measurements of RMS signal and peak value. In this study boiler tube leak from the inside of boiler is investigated using 3D source location technique as well as determination of the actual leak based on various analysis method such as amplitude, duration, RMS, and so on. Our results show that we can detect and prevent unexpected plant accident early, and contributes to maximize the effectiveness of power generation.

Early Shell Crack Detection Technique Using Acoustic Emission Energy Parameter Blast Furnaces

Blast furnaces are crucial equipment for steel production. A typical furnace risks unexpected accidents caused by contraction and expansion of the walls under an environment of high temperature and pressure. In this study, an acoustic emission (AE) monitoring system was tested for evaluating the large-scale structural health of a blast furnace. Based on the growth of shell cracks with the emission of high energy levels, severe damage can be detected by monitoring increases in the AE energy parameter. Using this monitoring system, steel mill operators can establish a maintenance period, in which actual shell cracks can be verified by cross-checking the UT. From this study, we expect that AE systems permit early fault detection for structural health monitoring by establishing evaluation criteria based on the severity of shell cracking.

Study of Quantitative Assessment Standard for Type 1 and Type 2 Gas Cylinders Using Acoustic Emission Testing

Abstract Acoustic emission testing (AET) of cylinders is advantageous in that it can be directly conducted on cylinders installed in a car, without needing to dissemble them on a real-time basis. Therefore, users prefer AET over other nondestructive testing methods. Owing to these advantages of AET, it has been approved by the Department of Transportation of the U.S. as a safety evaluation method for pressure containers or as an alternative to the hydroproof testing method. This paper presents a study of the quantitative evaluation criteria for a container having ultrasonic testing defects and also for Type 1 and Type 2 gas cylinders, which are defective seamless pressure containers provided by NK, a manufacturer of pressure containers. For the Type 1 cylinder, the process from crack growth to leak was observed in a repetitive fatigue test using a 113 L container according to ASTM E 1419-02. Further, for the Type 2 cylinder, integrity was evaluated using a 119 L sound container and a container damaged by hydraulic pressure, by the slow-fill method according to ASTM E 2191-02. Based on the AET results of the Type 1 and Type 2 cylinders, quantitative evaluation criteria were established for a defective and non-defective container.