• Journal of Microbiology and Biotechnology
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• v.9 no.1
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• pp.106-112
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• 1999

The therapeutic potential of phosphodiesterase 4(PDE4) inhibitors in inflammatory diseases including some autoimmune diseases has been explored recently with some hopeful results. These PDE4 inhibitors are thought to show their anti-inflammatory effect by down-regulating tumor necrosis factor-a (TNF-$\alpha$) production in lymphocytes and macrophages. A high concentration of TNF-$\alpha$has been found in rheumatoid arthritis (RA) synovium and reducing TNF-$\alpha$using biological agents was proven to be an effective RA treatment. To test the possibility of using PDE4 inhibitors for RA treatment, the effects of a newly synthesized PDE4 inhibitor, DWP205505, on TNF-$\alpha$ and IL-10 production was tested in cells isolated from normal peripheral blood and rheumatoid arthritis synovial fluid. Cytokine production was assayed at the protein level by sandwich enzyme-linked immunosorbent assay (ELISA) and at the mRNA expression level by semi-quantitative RT-PCR. Another PDE4 inhibitor, RP73401, was used for comparison. DWP205505 and RP73401 had no harmful effect on cell viability up to 10 $\mu$M concentration during the 24 h culture period. DWP205505 as well as RP73401 significantly reduced TNF-$\alpha$ secretion from lipopolysaccharide (LPS)-stimulated peripheral blood mononuclear cells (pBMC) and synovial fluid mononuclear cells (SFMC). The effect of DWP205505 or RP73401 treatment on the mRNA expression of TNF-$\alpha$ was also studied in LPS-stimulated PBMC and SFMC. TNF-$\alpha$ mRNA expression was increased by LPS stimulation and both of the PDE4 inhibitors suppressed TNF-$\alpha$ mRNA expression. For interleukin-l0 (IL-l0), a little different results were obtained from PBMC and SFMC; IL-l0 secretion was unaffected by LPS stimulation and only minimally affected by both of the PDE4 inhibitors in PBMC. In unstimulated SFMC, DWP205505 and RP73401 slightly enhanced IL-10 secretion, while they reduced IL-l0 secretion from LPS-stimulated SFMC where IL-l0 secretion was a lot higher than unstimulated SFMC. These results suggest that the newly synthesized PDE4 inhibitor DWP205505 may have anti-rheumatoid arthritis activity.

• Proceedings of the Korea Information Processing Society Conference
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• 2009.04a
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• pp.146-147
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• 2009

본 논문에서는 단일 프레임 내에서 인접한 매크로 블록 간의 움직임의 유사도를 이용한 개선된 PDE 알고리즘을 제안한다. 제안한 방법은 기존의 방법보다 불필요한 후보 블록을 효율적으로 제거하기 위하여 인접한 매크로블록간의 유사도를 고려하여 인접 4개의 매크로블록 가운데 서브 블록간 최대 복잡도를 가지는 서브블록의 CDF(cumulative distribution function)와 개선된 매칭스캔 방법을 이용하여 효율적으로 계산량을 줄였다. 제안한 알고리즘은 화질의 저하 없이 기존의 PDE 알고리즘에 비해 55% 이상의 계산량을 줄였으며, MPEG-2 및 MPEG-4 AVC를 이용하는 비디오 압축 응용분야에 유용하게 사용될 수 있을 것이다.

• Proceedings of the Plant Resources Society of Korea Conference
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• 2018.04a
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• pp.81-81
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• 2018

The present study was investigated on in vitro anti-obesity effect of 4-hydroxybenzyl alcohol from Cudrania tricuspidata. We isolated various compounds from Cudrania tricuspidata. Among these compounds, anti-obesity effects of 4-hydroxybenzyl alcohol was examined by lipase activity assay, cyclic adenosine monophosphate (cAMP)-specific phosphodiesterase type IV (PDE4) activity assay, and citrate synthase activity assay. 4-hydroxybenzyl alcohol and Cudrania tricuspidata extracts inhibited the enzymatic activities of lipase, PDE4, and citrate synthase. Lipase is known to mediate the hydrolysis of triacylglycerol in adipose tissue and cholesterol esters in other tissue or cells. Also, PDE4 hydrolyses cAMP, a crucial secondary messenger for in metabolic pathways including glucose and lipid metabolism, lipolysis, and thermogenic function. 4-hydroxybenzyl alcohol and Cudrania tricuspidata extracts induced the inhibitory effect against each enzymatic activity on several specific substrates as observed by detection at 405 or 412 nm. These findings might be attributable to the inhibition of adipogenesis, and partial prevention of obesity. In conclusion, these results show that 4-hydroxybenzyl alcohol and Cudrania tricuspidata may be a critical candidate as a natural anti-obesity source.

• Korean Journal of Mathematics
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• v.27 no.4
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• pp.879-898
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• 2019

In this paper we prove some interesting inclusions concerning the numerical range of some operators and the numerical range of theirs ranges with a convex function. Further, we prove some inequalities for the numerical radius. These inclusions and inequalities are based on some classical convexity inequalities for non-negative real numbers and some operator inequalities.

• Biomolecules & Therapeutics
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• v.10 no.2
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• pp.117-123
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• 2002

CJ-10882, (E)-[(3-Cyclopentyloxy-4-methoxyphenyl)methylene]hydrazine-carboxamide, is a newly developed type IV phosphodiesterase isozyme (PDE IV) inhibitor. To investigate the subacute toxic effects of CJ-10882, it was administered to both male and female dogs at 0, 25, 50, 100 or 200 mg/kg/day orally for up to 2 weeks. During the test period, clinical signs, mortality, body weight, food consumption, ophthalmoscopy, urinalysis, hematology, serum biochemistry, gross finding, organ weight, and histopathology were evacuated. Several clinical signs were observed in treated dogs at above 25 mg/kg, including salivation and vomiting. A reduction in the body weight was observed in both sexes at above 50 mg/kg. There were no treatment-related effects on mortality, ophthalmoscopy, urinalysis, hematology, sect biochemistry, necropsy findings, and histopathology in any treatment group. The results of this study demonstrate that CJ-10882, a selective Inhibitor of the type IV class of PDE, may cause effects on gastrointestinal tract and salivary glands. Therefore, these organs should be closely examined in studies with other PDE IV inhibitors.

• YAKHAK HOEJI
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• v.49 no.1
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• pp.109-113
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• 2005

In the present study treatment of IBMX, a phosphodiesterase (PDE) inhibitor, alone induced osteoclast formation in co-cultures of mouse bone marrow cells and calvarial osteoblasts. However, treatment of IBMX in combination with prostaglandin $E_2\;(PGE_2)$ inhibited osteoclast formation in a dose-dependent manner. Among various isozyme-specific PDE inhibitors, a PDE4 specific inhibitor, rolipram, showed similar effects as IBMX on osteoclast formation. To address the involvement of cyclic adenosine monophosphate (cAMP) in osteoclast formation, cAMP concentration in calvarial osteoblasts was investigated. When calvarial osteoblasts were co-cultured with IBMX alone or in combination with $PGE_2$, the patterns of cAMP concentration in calvarial osteoblasts were differ each other suggesting that cAMP in calvarial osteoblasts subtly regulates osteoclast formation.

• Proceedings of the Korean Institute of Information and Commucation Sciences Conference
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• 2009.05a
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• pp.225-228
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• 2009

본 논문에서는 인접블록간의 움직임 유사도를 이용하여 불필요한 후보블록을 보다 빠르게 제거하는 PDE기반의 고속 블록매칭 알고리즘을 제안한다. 제안한 방법은 기존의 방법보다 불필요한 계수를 효율적으로 제거하기 위하여 인접 블록간의 영상의 유사성에 기초하여 네 개의 인접 매크로블록 가운데 최대 복잡도를 가지는 서브블록의 누적 분포 함수(cumulative distribution function-CDF)와 서브블록별 복잡도가 집중되지 않도록 하기위하여 normalized스캔 방법에 사용하여 효율적으로 계산량을 감소하였다. 제안한 알고리즘은 화질의 저하 없이 기존의 PDE 알고리즘에 비해 55% 이상의 계산량을 줄였으며, MPEG-2 및 MPEG-4 AVC를 이용하는 비디오 압축 응용분야에 유용하게 사용될 수 있을 것이다.

• Proceedings of the Korea Society of Information Technology Applications Conference
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• 2005.11a
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• pp.289-291
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• 2005

In this paper, we introduce the backward solution of nonlinear wave equation for denoising. The PDE method is approved about 4 PSNR value compare with any convolution method. In neuro images, denoising process using proposed PDE is good about 0.2% increased Voxel Region.

• Analytical Science and Technology
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• v.28 no.4
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• pp.278-287
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• 2015

Phosphodiesterase type 5 inhibitors (PDE-5 inhibitors) are used in the treatment of erectile dysfunction. In recent years, a number of reports have been conducted on dietary supplements contaminated with PDE-5 analogues. In this study, 58 analogues of PDE-5 inhibitors were sorted into five groups: tadalafil, sildenafil, hongdenafil, vardenafil, and other analogues. These analogues were then evaluated using a liquid chromatography-quadrupole-time of flight mass spectrometry (LC-QTOF-MS) electrospray ionization mass method. Each compound has a unique fragmentation ion, which can be easily analyzed qualitatively. The fragmentation pathways of the analogues were elucidated based on the QTOF-MS and MS/MS data. Common ions were confirmed for each group by analyzing the structural characteristics and fragmentation pathways. Specifically, common ions were observed at m/z 169.08 and 135.04 (tadalafil analogues), m/z 311.15 and 283.12 (sildenafil analogues and hongdenafil analogues), and m/z 312.16 and 151.09 (vardenafil analogues). The advantage of this method is that the structure of unknown components can be determined by interpreting the product ions. Hence, the developed method can be used for the identification of unknown compounds. Fragmentation pathways may also aid in the detection and identification of PDE-5 inhibitor analogues.

• Mass Spectrometry Letters
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• v.6 no.2
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• pp.38-42
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• 2015

Roflumilast analogs are a group of drugs which act as selective photodiesterase (PDE-4) inhibitor for the treatment severe chronic pulmonary disease associated with chronic brochnonities. Structural identification of degradation products using high resolution mass spectrometry and theoretical investigation by density functional theory have been successfully carried out on roflumilast to identify four degradation products namely, 3,5-dichloropyridin-4-amine, N-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)-3-hydroxy benzamide, N-(3,5-dichloropyridin-4-yl)-3-(cyclopropylmethoxy)-4-(difluoromethoxy) benzamide and 3-(cyclopropylmethoxy)-N-(3,5-dichloro-1-oxidopyridin-4-yl)-4-(difluoro methoxy) benzamide, generated in alkali, acidic and oxidative conditions.