• Proceedings of the Korean Society of Applied Pharmacology
• /
• 1994.04a
• /
• pp.286-286
• /
• 1994

Thrombin (0.25 U/ml : TB), 소-피부 collagen (200 $\mu\textrm{g}$/ml : CG), adenosine 5'-diphesphate (4,0 $\times$ $10^{-5}$M : ADP), 및 epinephrine (4,0 $\times$ 10 $^{-5}$M : EPI)의 가토-혈소판 응집과 단백인산화작용에 미치는 PDE-I (3-isobutyl-1-methylxanthine : IBMX, 및 KR 30075), amitriptyline (AP), chlorpromazine (CP), 및 sodium nitrogrosside (SNP)의 염향을 비교-검토하였다. 그 결과, KR은 2,2 $\times$ $10^{-7}$M 이하의 $IC_{50}$/에서 EPI > ADP > CG > TB 순으로 각각을 억제하였으며, SNP 보다도 강하였고; KR-30075보다 약하나 IBMX, AP, 및 CP도 각 응집재의 작용을 억제하였으며 특히 EPI에 대하여 $10^{-8}$M 이하의 $IC_{50}$/에서 유의한 억제력을 보였다. 각 응집제들은 41 kD 인산화는 유의하게 증가시키며 47 kD와 20 kD 단백인산화는 감소시켰는데; 모든 항응집성 약물이 41 kD 인산화-증가는 유의하게 억제하였다, 아울러, AP와 CP는 47 kD 단백인산화-감소에 영향을 미치지 않았으나 20 kD 단백인산화-감소는 억제하였다. PDE-I (IBMX와 KR)와 SNP는 47 kD와 20 kD 단백인산화-감소를 다소 약화시켰으며, 43 kD와 22 kD 단백인산화를 KR > IBMX > SNP순으로 유의하게 증가시켰고, KR의 22 kD 단백인산화작용은 현저하였다.

• Proceedings of the Korean Society of Propulsion Engineers Conference
• /
• 2008.11a
• /
• pp.326-329
• /
• 2008

DARPA's hypersonic propulsion program VULCAN is aimed for development of Mach 4+ capable engine by combining current production turbofan engine such as F119 with CVC (Constant Volume Combustion) engine. Final goal is a TBCC(Turbo-based Combined Cycle) engine by combining with dual mode ramjet/scramjet engine. CVC is a common designation of new concept of high efficiency engines, such as Pulse Detonation Engine (PDE) or Continuous Detonation Engine (CDE), which use the detonation as a combustion mechanism. Present paper introduces the internationally collaborative research activities carried out in Aerospace Combustion and Propulsion Laboratory of the department of Aerospace Engineering of the Pusan national University.

• Tuberculosis and Respiratory Diseases
• /
• v.73 no.4
• /
• pp.231-233
• /
• 2012

Tadalafil is a phosphodiesterase-5 inhibitor (PDE5I), which is widely used to treat erectile dysfunction. Although PDE5Is have excellent safety profiles, and most of the side effects are mild, rare serious adverse events have been reported in association with PDE5Is. Thrombosis is one of those events, and a few previous reports have suggested the association of PDE5Is with thrombosis. We report the case of a 61-year-old male who developed pulmonary embolism combined with pulmonary infarction directly after taking tadalafil. Both the patient and the physician suspected tadalafil as the culprit drug, as the patient was in an otherwise healthy condition. However, after extensive evaluation, we noticed that factor VIII levels were elevated. Prior reports suggesting the association between thrombosis and PDEIs either lack complete information on coagulation factors, or show inconsistencies in their results. Physicians should operate caution prior to accepting the diagnosis of adverse drug reaction.

• The Journal of Internal Korean Medicine
• /
• v.37 no.4
• /
• pp.591-600
• /
• 2016

Objective: This study aimed to examine the relaxation effects and underlying mechanisms of Cynomorii herba (CH) extract in isolated rabbit corpus cavernous tissues.Methods: We experimented with CH extract (0.01-3.0 mg/mL). Nω-nitro-L-arginine (L-NNA) was experimented before the CH extract to contracted strips induced by phenylephrine (PE, 1 μM)and compared with nonexperimented. In addition, we experimented with calcium chloride (Ca²⁺, 1 mM) after pretreatment of the CH extract in Ca²⁺-free Krebs-Ringer solution to contracted strips induced by PE. The cell viability and nitric oxide (NO) concentration of human umbilical vein endothelial cells (HUVECs) were measured by an methylthiazol-2-yl-2, 5-diphenyl tetrazoliumbromide (MTT) assay and Griess reagent system. The ratio of smooth muscles to collagen fibers, in addition to eNOS- and PDE-5-positive reactions, was examined by histochemical and immunohistochemical staining.Results: The CH extract significantly induced the relaxation of the cavernous strips, and the pretreatment with L-NNA inhibited CH extract-induced relaxation. The L-NNA pretreatment reduced the increased contraction induced by the addition of Ca²⁺in Ca²⁺-free solution. Furthermore, the NO concentration of the HUVECs increased. When the CH extract was applied to the corpus cavernosum of the penis (CCP) of Sprague Dawley rats, the ratio of smooth muscles to collagen fibers by PE and the formation of eNOS around the helicine artery increased. However, the CH extract treatment decreased PDE-5 positive reactions.Conclusions: These results show that the relaxation effects induced by the CH extract are associated with the suppression of the influx of extracellular Ca²⁺ via the production of NO and eNOS and inhibition of PDE-5.

• Korean Journal of Pharmacognosy
• /
• v.45 no.3
• /
• pp.268-274
• /
• 2014

The aim of this study is to explore the potent phosphodiesterase 4 and 7 inhibitor from various herbal medicines for atopy treatment. In this study, 51 kinds of each herbal medicine, which were extracted with ethanol, was carried out the screening of PDE 4 and 7 inhibition using enzyme inhibitory assay. Of these, 8 species of herbal medicines, Rubus coreanus, Duchesnea chrysantha, Alisma orientale, Rehmannia glutinosa, Angelica dahurica, Thuja orientalis, Astragalus membranaceus and Perilla frutescens were screened as potential inhibitor against PDE 4 and 7. Among 8 species, Duchesnea chrysantha showed poteinial anti-atopic effect on DNCB-induced atopic model. Duchesnea chrysantha extract decreased serum IgE and histamine release significantly.

• Information and Communications Magazine
• /
• v.20 no.4
• /
• pp.38-48
• /
• 2003

• Journal of Pharmaceutical Investigation
• /
• v.40 no.2
• /
• pp.117-123
• /
• 2010

Ibudilast, 3-isobutyryl-2-isopropyrazolo[1,5-a]pyridine, is a nonselective inhibitor of cyclic nucleotide phosphodiesterase (PDE). It preferentially inhibits PDE 3A, PDE4, PDE10 and PDE11 as well as a number of the other PDE families, albeit to a lesser extent. Ibudilast is used clinically to treat bronchial asthma and cerebrovascular disorders. Thes e clinical uses are based on the ability of ibudilast to inhibit platelet aggregation, improve cerebral blood flow and attenuate allergic reactions. The purpose of the present study was to evaluate the bioequivalence of two ibudilast capsules, Ketas capsule (Handok Pharmaceuticals Co., Ltd.) and Pinatos capsule (Sam Chun Dang Pharm. Co., Ltd.), according to the guidelines of the Korea Food and Drug Administration (KFDA). The in vitro release of ibudilast from the two ibudilast formulations was tested using KP Apparatus method with various dissolution media. Twenty six healthy male subjects, 23.31${\pm}$1.09 years in age and 70.45${\pm}$8.51 kg in body weight, were divided into two groups and a randomized $2{\times}2$ cross-over study was employed. After a single capsule containing 10 mg as ibudilast was orally administered, blood samples were taken at predetermined time intervals and the concentrations of ibudilast in serum were determined using HPLC/UV detector. The dissolution profiles of two formulations were similar in all tested dissolution media. The pharmacokinetic parameters such as $AUC_t$, $C_{max}$ and $T_{max}$ were calculated, and computer programs (Equiv Test and K-BE Test 2002) were utilized for the statistical analysis of the parameters using logarithmically transformed $AUC_t$, $C_{max}$ and untransformed $T_{max}$. The results showed that the differences between two formulations based on the reference drug, Ketas, were 6.99%, -2.48% and 9.93% for $AUC_t$, $C_{max}$ and $T_{max}$, respectively. There were no sequence effects between two formulations in these parameters. The 90% confidence intervals using logarithmically transformed data were within the acceptance range of log 0.8 to log 1.25 (e.g., log 0.8791~log 1.1861 and log 0.8347~log 1.1199 for $AUC_t$ and $C_{max}$, respectively). Thus, the criteria of the KFDA bioequivalence guideline were satisfied, indicating Pinatos capsule was bioequivalent to Ketas capsule.

• Journal of the Korean Institute of Gas
• /
• v.7 no.4 s.21
• /
• pp.44-52
• /
• 2003

In this work dynamic heat transfer in a CPFS (cable penetration fire stop) system built in the firewall of nuclear power plants is three-dimensionally investigated to develop a test-simulator that can be used to verify effectiveness of the sealant. Dynamic heat transfer in the fire stop system is formulated in a parabolic PDE (partial differential equation) subjected to a set of initial and boundary conditions. First, the PDE model is divided into two parts; one corresponding to heat transfer in the axial direction and the other corresponding to heat transfer on the vertical planes. The first PDE is converted to a series of ODEs (ordinary differential equations) at finite discrete axial points for applying the numerical method of SOR (successive over-relaxation) to the problem. The ODEs are solved by using an ODE solver In such manner, the axial heat flux can be calculated at least at the finite discrete points. After that, all the planes are separated into finite elements, where the time and spatial functions are assumed to be of orthogonal collocation state at each element. The initial condition of each finite element can be obtained from the above solution. The heat fluxes on the vertical planes are calculated by the Galerkin FEM (finite element method). The CPFS system was modeled, simulated, and analyzed here. The simulation results were illustrated in three-dimensional graphics. Through simulation, it was shown clearly that the temperature distribution was influenced very much by the number, position, and temperature of the cable stream, and that dynamic heat transfer through the cable stream was one of the most dominant factors, and that the feature of heat conduction could be understood as an unsteady-state process.

• Applied Chemistry for Engineering
• /
• v.5 no.3
• /
• pp.466-477
• /
• 1994

PEG 600-diglycidyl ethers(PDE) were synthesized using $BF_3$ catalyst by the reaction of epichlorohydrin and PEG 600 which is known to have the hygroscopicity, softening property, and antistatic property. Water-soluble long chain polyamines(PDET) were synthesized by coreaction of PDE and triethylenetetramine which is high conductive aliphatic amine curing agent. To prevent the gelation of the PDET and increase the water-solution stability, water-soluble quaternary ammonium polyamines were synthesized by cationation of PDET with acetic acid. Antistatic agents PDET-2A, PDET-5A, PDET-6A, PDETA-2A and PDETA-4A were prepared by the mixing of PDET-2, PDET-5, PDET-6, PDETA-2 and PDETA-4 with water. Synthesized antistatic agents were treated on PET textiles with and without resin. Then surface electrical resistivity and half life characteristics value were tested. As the results there were no remarkable decreasing changes in antistatic abilities of the textiles treated with PDETA-2A and PDETA-4A after 50 times washing. So PDETA-2A and PDETA-4A were proved to be durable antistatic agents. Surface electrical resistivity of the textiles treated with PDETA-2A and PDETA-4A before washing were $1{\times}10^7{\Omega}$ and $2{\times}10^7{\Omega}$, respectively, and half life characteristics values were 0.8sec and 1.1sec, respectively. Therefore PDETA-2A and PDETA-4A were proved to be good antistatic agents.

• Reproductive and Developmental Biology
• /
• v.35 no.4
• /
• pp.435-439
• /
• 2011

Sildenafil citrate (SIL) a phosphodiesterase 5 inhibitor (PDE5I) has been used for long time as a first line oral drug for erectile dysfunction. Though it has beneficial effects on erectile organ it also has some adverse effects in other cells and/or tissues related to reproductive system when exposed to longer duration. The objective of the present study is to evaluate the long term effect of SIL on sperm parameters in Wistar albino rat. The animals are divided into two groups, for group I - rats were treated with saline (vehicle alone) and group - II oral administration of 5 mg/kg b.w. of SIL was administrated orally once in a day for 120 days. At the end of the trial period animals were sacrificed and epididymal sperm were subjected to various analysis. Results showed significant reduction in sperm count, motility, viability and morphologically intact sperm in long term PDE5I exposed animals when compared to control. Acrosomal status and fertility test also showed significant reduction in long term PDE5I exposed animals. The present study clearly indicated that long term SIL has shown to induce alteration in sperm quality and quantity, leading to decline in fertility rate. Indicate that SIL impinge on spermatogenesis as well as epididymal function. Understanding the molecular down-stream events involved in long-term exposure to PDE5 inhibitor can be valuable to supervise on related infertility issues and to suggest corrective measures.