• Archives of Pharmacal Research
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• v.28 no.10
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• pp.1170-1176
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• 2005

2-Methyl-2-(2-methylpropenyl)-2,3-dihydronaphthoquinone[2,3-b]furan-4,9-dione (N FD-37) is a synthetic furonaphthoquinone compound. In this study, we determined that NFD-37 could inhibit the lipopolysaccharide (LPS)-induced production of inflammatory mediators in macrophages RAW 264.7. This compound inhibited LPS-induced nitric oxide (NO) or prostaglandin (PG) $E_{2}$ production in dose-dependent manners, with $IC_{50}$ values of 7.2 ${\mu}M$ and 5.3 ${\mu}m$, respectively. As the positive controls, pyrrolidine dithiocarbamate (30 ${\mu}M$) exhibited a $57{\%}$ inhibition of NO production, and NS-398 ($1{\mu}M$) manifested a $48{\%}$ inhibition of $PGE_2$ production. The inhibitory effects of NFD-37 on NO and $PGE_2$ production were determined to occur in conjunction with the suppression of inducible NO synthase or cyclooxygenase-2 expression. NFD-37 also inhibited the production of LPS-inducible tumor necrosis factor-${\alpha}$, interleukin (IL)-$1{\beta}$ and IL-6, at $IC_{50}$ values of 4.8-8.9 ${\mu}M$. We also determined the anti-inflammatory efficacy of NFD-37 using carrageenin-induced paw edema in experimental mice.

• Bulletin of the Korean Chemical Society
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• v.34 no.11
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• pp.3429-3443
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• 2013

Chemokine receptor (CCR2) is a G protein-coupled receptor that contains seven transmembrane helices. Recent pharmaceutical research has focused on the antagonism of CCR2 and candidate drugs are currently undergoing clinical studies for the treatment of diseases like arthritis, multiple sclerosis, and type 2 diabetes. In this study, we analyzed the time dependent behavior of CCR2 docked with a potent 4-azetidinyl-1-aryl-cyclohexane (4AAC) derivative using molecular dynamics simulations (MDS) for 20 nanoseconds (ns). Homology modeling of CCR2 was performed and the 4AAC derivative was docked into this binding site. The docked model of selected conformations was then utilized to study the dynamic behavior of the 4AAC enzyme complexes inside lipid membrane. MDS of CCR2-16b of 4AAC complexes allowed us to refine the system since binding of an inhibitor to a receptor is a dynamic process and identify stable structures and better binding modes. Structure activity relationships (SAR) for 4AAC derivatives were investigated and reasons for the activities were determined. Probable binding pose for some CCR2 antagonists were determined from the perspectives of binding site. Initial modeling showed that Tyr49, Trp98, Ser101, Glu291, and additional residues are crucial for 4AAC binding, but MDS analysis showed that Ser101 may not be vital. 4AAC moved away from Ser101 and the hydrogen bonding between 4AAC and Ser101 vanished. The results of this study provide useful information regarding the structure-based drug design of CCR2 antagonists and additionally suggest key residues for further study by mutagenesis.

• Molecules and Cells
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• v.44 no.9
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• pp.688-695
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• 2021

The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) pandemic has become a global health concern. Various SARS-CoV-2 vaccines have been developed and are being used for vaccination worldwide. However, no therapeutic agents against coronavirus disease 2019 (COVID-19) have been developed so far; therefore, new therapeutic agents are urgently needed. In the present study, we evaluated several hepatitis C virus direct-acting antivirals as potential candidates for drug repurposing against COVID-19. Theses include asunaprevir (a protease inhibitor), daclatasvir (an NS5A inhibitor), and sofosbuvir (an RNA polymerase inhibitor). We found that asunaprevir, but not sofosbuvir and daclatasvir, markedly inhibited SARS-CoV-2-induced cytopathic effects in Vero E6 cells. Both RNA and protein levels of SARS-CoV-2 were significantly decreased by treatment with asunaprevir. Moreover, asunaprevir profoundly decreased virion release from SARS-CoV-2-infected cells. A pseudoparticle entry assay revealed that asunaprevir blocked SARS-CoV-2 infection at the binding step of the viral life cycle. Furthermore, asunaprevir inhibited SARS-CoV-2 propagation in human lung Calu-3 cells. Collectively, we found that asunaprevir displays broad-spectrum antiviral activity and therefore might be worth developing as a new drug repurposing candidate for COVID-19.

• The Journal of Korean Institute of Electromagnetic Engineering and Science
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• v.21 no.1
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• pp.28-35
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• 2010

In this paper, we designed and fabricated a ultra-wideband(UWB) bandpass filter with a good performance of a stopband, and a notched band in passband. The transformed equivalent circuit of the highpass filter was realized by distributed element. A wide-passband with 3-dB fractional bandwidth of more than 100 % was achieved by using optimum response of the HPF. For improving lower and upper stopband characteristic, a cross coupling between feed lines was employed, which was analyzed by desegmentation technique. In order to reject interference of Wireless LAN and Hyper LAN(5.15~5.825 GHz), the narrow notched(rejection) band was realized by a spurline. The fabricated BPF indicated the passband from 3.1 to 10.55 GHz and the flat group delay of less than 0.94 ns over the entire passband except the rejection band. The filter shown sharp attenuation both inside and outside the band and notched band from 5.2 to 6.12 GHz.

• The Journal of Korean Institute of Communications and Information Sciences
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• v.29 no.7B
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• pp.685-696
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• 2004

Real-time multimedia applications that require large amount of bandwidth need resource reservation before starting service for providing the QoS(i.e., Quality of Service). To reserve resources in advance, each reservation request has to notify its expectation on the required amount of resources and service duration. Using this information, a resource manager can schedule advance reservations. However, most existing resource management systems are adopting straightforward call admission control process (i.e., only immediate reservation) by checking currently available resources without considering the service duration. Hence, the resource management system that supports advance reservation has to manage confliction caused by indefinite service duration of immediate reservation. Even though the separation of resource pool according to type of reservation can prevent the confliction, it causes low resource utilization. In this paper, we propose an effective resource management scheme that supports both immediate and advance reservations by sharing resources dynamically. Using network cost function, the proposed scheme determines and adaptively adjusts resource boundary according to the confliction rate by varying weight parameters. And also, we define user utility function to quantify user satisfaction based on how well the reserved resource is guaranteed during service time. Simulation results using NS-2 network simulator show that the proposed scheme can achieve better resource utilization with preferable QoS than other schemes like static resource partitioning.

• The Journal of Korean Institute of Communications and Information Sciences
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• v.31 no.4B
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• pp.291-302
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• 2006

With the increasing deployment of mobile devices and the advent of broadband wireless access systems such as WiBro, WiMAX, and HSDPA, an efficient IP mobility management protocol becomes one of the most important technical issues for the successful deployment of the broadband wireless data networking service. IETF has proposed the Mobile IPv6(MIPv6) as the basic mobilitymanagement protocol for IPv6 networks. To enhance the performance of the basic MIPv6, researchers have been actively working on HMIPv6 and FMIPv6 protocols. In this paper, we propose a new mobility management protocol, HIMIPv6 (Highly Integrated MIPv6), which tightly integrates the hierarchical mobility management mechanism of the HMIPv6 and the proactive handover support of the FMIPv6 to enhance the handover performance especially for the cellular networking environment with high frequent handover activities. We have performed extensive simulation study using ns-2 and the results show that the proposed HIMIPv6 outperforms MIPv6, FMIPv6 and HMIPv6 in terms of signaling overhead, service interruption and packet lost during handovers.

• The Korean Journal of Pain
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• v.9 no.2
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• pp.380-384
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• 1996

Background: To determine the effectiveness of continuous epidural infusion of droperidol, combined with epidural morphine, in reducing nausea or vomiting associated with epidural morphine and minimizing the side effects of droperidol, 48 patients undergoing elective thoracic surgery were randomly assigned to one of two study groups. Methods: Patients received continuous infusion of epidural morphine(6.0 mg/day) following a bolus loading dose of 3.0 mg(Group A), or epidural mixture of morphine(6.0 mg/day) plus droperidol(5.0 mg/day) following a bolus loading dose(morphine 3.0mg, droperidol 1.5 mg)(Group B). For the first 48 postoperative hours, the incidence of nausea or vomiting, the need for antiemetic therapy, level of sedation, and adverse effects associated with droperidol were evaluated. Results: The incidence of nausea or vomiting and the number of patients who required antiemetic therapy were significantly less in Group B than in Group A(P<0.05). There were no significant differences between groups with regard to the adverse effects associated with droperidol such as mental depression, respiratory depression and abnormal movements(P=NS). Conclusion: We conclude that simultaneous titration of morphine and droperidol via epidural continuous infusion following epidural bolus injection of the mixture reduces nausea or vomiting associated with epidural morphine while it prevents the side effects of droperidol.

• Journal of the Korean Institute of Electrical and Electronic Material Engineers
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• v.21 no.7
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• pp.585-593
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• 2008

In this work, we report several experimental data capable of evaluating the phase transformation characteristics of GeSbTe pseudobinary thin films comprehensively utilized as phase change materials. The phase transformation of the GeSbTe thin films was confirmed by XRD measurement from amorphous to hexagonal structure via fee structure except for $Ge_8Sb_2Te_{11}$. In addition, X-ray photoelectron spectra analysis revealed to weaken Ge-Te bond for $Ge_2Sb_2Te_5$ and to strengthen the bonds of all elements for $Ge_8Sb_2Te_{11}$ during the amorphous to crystalline transition. The values of optical energy gap $(E_{OP})$ were around 0.71 and 0.50 eV and the slopes of absorption in extended region (B) were ${\sim}5.1{\times}10^5$ and ${\sim}10{\times}10^5cm^{-1}{\cdot}V^{-1}$ for the amorphous and fcc-crystalline structures, respectively. Finally, the kinetics of amorphous-to-crystalline phase change on the GeSbTe films was characterized using a nano-pulse scanner with 658-nm laser diode (power; $1{\sim}17$ mW, pulse duration; $10{\sim}460$ ns).

• Clinical and Experimental Reproductive Medicine
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• v.32 no.4
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• pp.315-324
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• 2005

Objectives: To compare the efficacy of GnRH antagonist multiple dose protocol (MDP) with that of GnRH agonist long protocol (LP) in controlled ovarian hyperstimulation for in vitro fertilization in patients with high basal FSH (follicle stimulating hormone) level or old age, a retrospective analysis was done. Methods: Two hundred ninety four infertile women (328 cycles) who were older than 41 years of age or had elevated basal FSH level (> 8.5 mIU/mL) were enrolled in this study. The patients had undergone IVF-ET after controlled ovarian hyperstimulation using GnRH antagonist multiple dose protocol (n=108, 118 cycles) or GnRH agonist long protocol (n=186, 210 cycles). The main outcome measurements were cycle cancellation rate, consumption of gonadotropins, the number of follicles recruited and total oocytes retrieved. The number of fertilized oocytes and transferred embryos, the clinical pregnancy rates, and the implantation rates were also reviewed. And enrolled patients were divided into three groups according to their age and basal FSH levels; Group A - those who were older than 41 years of age, Group B - those with elevated basal FSH level (> 8.5 mIU/mL) and Group C - those who were older than 41 years of age and with elevated basal FSH level (> 8.5 mIU/mL). Poor responders were classified as patients who had less than 4 retrieved oocytes, or those with $E_2$ level <500 pg/mL on the day of hCG injection or those who required more than 45 ampules of exogenous gonadotropin for stimulation. Results: The cancellation rate was lower in the GnRH antagonist group than in GnRH agonist group, but not statistically significant (6.8% vs. 9.5%, p=NS). The amount of used gonadotropins was significantly lower in GnRH antagonist group than in agonist group ($34.8{\pm}11.3$ ampules vs. $44.1{\pm}13.4$ ampules, p<0.001). The number of follicles > 14 mm in diameter was significantly higher in agonist group than in antagonist group ($6.7{\pm}4.6$ vs. $5.0{\pm}3.4$, p<0.01). But, there were no significant differences in clinical pregnancy rate (24.5% in antagonist group vs. 27.4% in agonist group, p=NS) and implantation rate (11.4% in antagonist group vs. 12.0% in agonist group, p=NS) between two groups. Mean number of retrieved oocytes was significantly higher in GnRH agonist LP group than in GnRH antagonist MDP group ($5.4{\pm}3.5$ vs. $6.6{\pm}5.0$, p<0.0001). But, the number of mature and fertilized oocytes, and the number of good quality (grade I and II) and transferred embryos were not different between two groups. In each group A, B, and C, the rate of poor response did not differ according to stimulation protocols. Conclusions: In conclusion, for infertile women expected poor ovarian response such as who are old age or has elevated basal FSH level, a protocol including a controlled ovarian hyperstimulation using GnRH antagonist appears at least as effective as that using a GnRH agonist, and may offer the advantage of reducing gonadotropin consumption and treatment period. However, much work remains to be done in optimizing the GnRH antagonist protocols and individualizing these to different cycle characteristics.

• Journal of the Korean Institute of Telematics and Electronics A
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• v.31A no.2
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• pp.88-93
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• 1994

We fabricated a large-scale photovoltaic device for detecting-3-5$\mu$m IR, by forming of n$^{+}$-p junction in the $Hg_{1-x}Cd_{x}$Te (MCT) layer which was grown by LPE on CdTe substrate. The composition x of the MCT epitaxial layer was 0.295 and the hole concentration was 1.3${\times}10^{13}/cm^{4}$. The n$^{+}$-p junction was formed by B+ implantation at 100 keV with a does 3${\times}10^{11}/cm^{2}. The n$^{+}$ region has a circular shape with 2.68mm diameter. The vacuum-evaporated ZnS with resistivity of 2${\times}10^{4}{\Omega}$cm is used as an insulating layer over the epitaxial layer. ZnS plays the role of the anti-reflection coating transmitting more than 90% of 3~5$\mu$m IR. For ohmic contacts, gole was used for p-MCT and indium was used for n$^{+}$-MCT. The fabrication took 5 photolithographic masks and all the processing temperatures of the MCT wafer were below 90$^{\circ}C$. The R,A of the fabricated devices was 7500${\Omega}cm^{2}$. The carrier lifetime of the devices was estimated 2.5ns. The junction was linearly-graded and the concentration slope was measured to be 1.7${\times}10^{17}/{\mu}m$. the normalized detectivity in 3~5$\mu$m IR was 1${\times}10^{11}cmHz^{12}$/W, which is sufficient for real application.