• Title/Summary/Keyword: PDE

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Synthesis of Methoxy Polyoxyethlene Dodecanoates (Methoxy Polyoxyethylene Dodecanoate의 합성)

  • Kang, Yun-Seog;Noh, Sueng-Ho;Choi, Seung-Ok;Nam, Ki-Dae
    • Applied Chemistry for Engineering
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    • v.9 no.5
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    • pp.749-753
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    • 1998
  • Methoxy polyoxyethylene dodecanoates, kinds of nonionic surfactants, could be obtained from addition of ethylene oxide (5, 7, 9, and 12mol) with fatty acid methyl ester utilizing solid catalyst, metal oxide. Because ethylene oxide (EO) couldn't react directly in acid or alkali catalyst with dodecanoic acid methyl ester (DME) that had no active hydrogen, the reaction to add EO was carried out using active solid catalyst. By using IR, HPLC and $^1H$ NMR analysis, structural confirmation of methyl polyoxy ethylene dodecanate showed high yield ranging from 93 to 97%. EO unit mol number of reacted products was 5.2, 7.1, 9.2 and 12.1 mol respectively. Also, EO adduct distrobution of ethoxylated methyl laurate (MPD) had normal distribution curve like polyoxyethylene alkyl ether (AE).

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Numerical Study of Detonation Wave Structure and Dynamics in a Circular Tube (원형관 내 데토네이션 파 구조 및 동적 특성 수치 연구)

  • Cho, Deok-Rae;Kim, Jong-Kwan;Jang, Keun-Jin;Choi, Jeong-Yeol
    • Proceedings of the Korean Society of Propulsion Engineers Conference
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    • 2012.05a
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    • pp.278-281
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    • 2012
  • Numerical studies were performed to investigate the three-dimensional front structure and dynamics features of detonation wave propagating in a circular tube such as Pulse Detonation Engine (PDE). By carrying out a series of parametric study using one step irreversible Arrhenius kinetics model, mechanisms of the three-dimensional front structure were investigated for two-, three-, four and six-cell mode detonations. A comparison with two-dimensional results, the effects of slapping transverse waves in radial direction were confirmed. In the all muti-cell modes, the detonation front structures and smoked-records on the wall are formed by the propagation of transverse waves along the wall in clockwise and counter-clockwise while the slapping move in radial direction. And the strength of reflected waves on the curved wall is changed by the multi-dimensional confinement effect.

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Status Analysis of Adulterated Herbal Medicine (국내외 위변조 한약 현황 분석)

  • Lee, Soojin
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.34 no.5
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    • pp.215-221
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    • 2020
  • Adulterated herbal medicine is intentionally added with undeclared improper or inferior ingredients which should not be in herbal medicine. The contamination with potentially hazardous substances such as heavy metal, pesticides, fungus, and microorganism sometimes can be regarded as one of adulteration in a broad sense. The problem of adulteration is that adulterated herbal medicine shows poor quality and/or can cause adverse events. Therefore, it is important to control adulteration issues for quality assurance and qualitative improvement of herbal medicines. This study aims to summarize and make a reference how to control adulterated herbal medicine. In this process, this study is to investigate studies about adulterated herbal medicine via searching Korean and foreign electronic databases such as PubMed, NDSL and OASIS. Finally eighteen papers were included to this study and analyzed according to the type of study, the category and efficacy of adulterants, the type of analysis methodologies and possible adverse events of adulterants. Phosphodiesterase type 5 (PDE-5) inhibitors for male sexual enhancement and anorexic, laxative, diuretic agents for weight loss and treating obesity has been used frequently as adulterants. The range of adverse event caused by adulterated herbal medicine were very wide from mild symptoms such as diarrhea, constipation, dizziness and blurred vision to very severe symptoms such as heart failure, hypoglycemia and renal impairment. This study showed the recent trend on the research of adulterated herbal medicine and this will be the ground to develop more detailed systems to control adulterated herbal medicine.

Genome-wide association analysis of nine reproduction and morphological traits in three goat breeds from Southern China

  • Xiaoyan, Sun;Jing, Jiang;Gaofu, Wang;Peng, Zhou;Jie, Li;Cancan, Chen;Liangjia, Liu;Nianfu, Li;Yuanyou, Xia;Hangxing, Ren
    • Animal Bioscience
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    • v.36 no.2
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    • pp.191-199
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    • 2023
  • Objective: This study aimed to investigate the significant single nucleotide polymorphisms (SNPs) and genes associated with nine reproduction and morphological traits in three breed populations of Chinese goats. Methods: The genome-wide association of nine reproduction and morphological traits (litter size, nipple number, wattle, skin color, coat color, black dorsal line, beard, beard length, and hind leg hair) were analyzed in three Chinese native goat breeds (n = 336) using an Illumina Goat SNP50 Beadchip. Results: A total of 17 genome-wide or chromosome-wide significant SNPs associated with one reproduction trait (litter size) and six morphological traits (wattle, coat color, black dorsal line, beard, beard length, and hind leg hair) were identified in three Chinese native goat breeds, and the candidate genes were annotated. The significant SNPs and corresponding putative candidate genes for each trait are as follows: two SNPs located on chromosomes 6 (CSN3) and 24 (TCF4) for litter size trait; two SNPs located on chromosome 9 (KATNA1) and 1 (UBASH3A) for wattle trait; three SNPs located on chromosome 26 (SORCS3), 24 (DYM), and 20 (PDE4D) for coat color trait; two SNPs located on chromosome 18 (TCF25) and 15 (CLMP) for black dorsal line trait; four SNPs located on chromosome 8, 2 (PAX3), 5 (PIK3C2G), and 28 (PLA2G12B and OIT3) for beard trait; one SNP located on chromosome 18 (KCNG4) for beard length trait; three SNPs located on chromosome 17 (GLRB and GRIA2), 28 (PGBD5), and 4 for hind leg hair trait. In contrast, there were no SNPs identified for nipple number and skin color. Conclusion: The significant SNPs or genes identified in this study provided novel insights into the genetic mechanism underlying important reproduction and morphological traits of three local goat breeds in Southern China as well as further potential applications for breeding goats.

The Effect of the Combination of Ginseng, Tribulus Terrestris, and L-arginine on the Sexual Performance of Men with Erectile Dysfunction: a randomized, double-blind, parallel, and placebo-controlled clinical trial

  • Reza Tahvilian;Mohammad Amin Golesorkhi;Farajollah Parhoudeh;Fatemeh Heydarpour;Hossein Hosseini;Hojjat Baghshahi;Hossein Akbari;Mohammad Reza Memarzadeh;Mehdi Mehran;Hosna Bagheri
    • Journal of Pharmacopuncture
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    • v.27 no.2
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    • pp.82-90
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    • 2024
  • Objectives: Nitric oxide is the most important mediator of penile erection after the onset of sexual excitement. It activates cyclic guanosine monophosphate (cGMP), increasing penile blood flow. Most pharmaceutical medications prevent enzyme phosphodiesterase type 5 (PDE-5) from breaking down cGMP, thus keeping its level high. However, due to the adverse effects of pharmacological therapies, herbal drugs that improve sexual function have gained attention recently. This study aimed to investigate the combined effects of ginseng, Tribulus terrestris, and L-arginine amino acid on the sexual performance of individuals with erectile dysfunction (ED) using the 5-item version of the International Index of Erectile Function (IIEF-5) questionnaire. Methods: Over three months, 98 men with erectile dysfunction were randomly assigned to receive either 500 mg of herbal supplements or placebo pills. Each herbal tablet contained 100 mg of protodioscin, 35 mg of ginsenosides, and 250 mg of L-arginine. Results: The results showed that the changes in the average scores of ILEF-5 within each group before and after the intervention indicated that all parameters related to the improvement of sexual function in patients with erectile dysfunction improved in the herbal treatment group (p < 0.001). The herbal group significantly improved IIEF-5 scores in nondiabetics (p < 0.05). However, there was no significant difference in the changes of IIEF-5 scores between the two intervention and control groups in diabetic patients. Conclusion: In conclusion, ginseng, Tribulus terrestris, and L-arginine have properties that increase energy and strengthen sexual function, making them suitable for patients with sexual disorders.

Effects of Sinetrol-XPur on Leptin-Deficient Obese Mice and Activation of cAMP-Dependent UCP-2 (Leptin 유전자 결핍 동물모델을 이용한 시네트롤(Sinetrol-XPur)의 항비만 효과와 cAMP를 통한 UCP-2 활성화 기전 연구)

  • Yoo, Jae Myeong;Lee, Minhee;Kwon, Han Ol;Choi, Sei Gyu;Bae, Mun Hyoung;Kim, Ok-Kyung
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.45 no.4
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    • pp.484-491
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    • 2016
  • The present study investigated the effect of Sinetrol-XPur (polyphenolic Citrus spp. and Paullinia cupana Kunth dry extract) and defined the action mode for cyclic adenosine monophosphate (cAMP)-dependent uncoupling protein (UCP)-2 activation. Leptin-deficient obese mice were treated with two different doses, 100 mg/kg body weight (BW) and 300 mg/kg BW of each AIN93G supplement, for 7 weeks. Treatment of obese mice with both low and high doses of Sinetrol-XPur significantly reduced body weight gain compared to control obese mice. White adipose tissue weight of mice was reduced by 30.96% in high dose-supplemented groups. Serum total cholesterol and triglyceride were reduced by a high dose of Sinetrol-XPur by 20.02% and 30.96%, respectively. Serum level of high density lipoprotein (HDL) was significantly increased by treatment with both doses, as the ratio of HDL to low density lipoprotein increased by 138.78% and 171.49%, respectively. Regarding expression of biochemical factors related to lipid metabolism, fatty acid synthase significantly decreased and UCP-2 increased upon treatment with a high dose of Sinetrol-XPur, but there was no significant difference in lipoprotein lipase and hormone-sensitive lipase. To define cellular mechanism, intracellular cAMP levels in 3T3-L1 adipocytes significantly increased in a dose-dependent manner over the range of $50{\sim}250{\mu}m/mL$. The phosphodiesterase (PDE) inhibitor 3-isobutyl-1-methylxanthine clearly blocked cAMP, suggesting that Sinetrol-XPur promotes lipolysis of adipocytes through inhibition of cAMP-dependent PDE, resulting in induction of cAMP response element binding protein and UCP-2. These results suggest that Sinetrol-XPur supplementation is a viable option for reducing body weight and fat by improving serum lipid profiles and genetic expression of lipid metabolic factors, especially activation of cAMP-dependent UCP-2.

Development of Rapid Analytical Method of Forbidden Medicines in Dietary Supplements Using LC-ESI-Tandem MS (LC-ESI-tandem MS를 이용한 기능성표방식품 중 부정유해물질 신속검사체계 개발)

  • Kim, Hee-Yun;Jang, Young-Mi;Joo, Hyun-Jin;Jung, Young-Hyun;Lee, Myoung-Sook;Park, Jong-Seok;Lee, Kwang-Ho;Lee, Hwa-Mi
    • Korean Journal of Food Science and Technology
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    • v.39 no.4
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    • pp.372-379
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    • 2007
  • A high-performance liquid chromatography-electrospray ionization (HPLC-ESI) tandem MS was developed for the rapid and simultaneous determination of forbidden medicines in dietary supplements. Thirteen medicinal components such as PDE-5 inhibitors and their analogues, and the newly identified dimethylsildenafil and xanthoanthrafil, were included in this study. After tentative standardization of molecular ions in both polarities using thirteen references on the mass spectrometer, with ESI-continuous infusion via the syringe pump method, the relative intensity of the ions present in the resulting spectra was quantitatively compared. From the results, the ion mode was selected depending on each reference's characteristics. A HPLC method coupled with the ESI mode was developed considering the matrix effect and interference depending on the type of sample. The validation test of the developed method was followed by carrying out precision, accuracy, recovery, sensitivity and linearity, etc. The method showed sufficiently high sensitivity, reproducibility, and specificity, and produced 4 times faster results when compared with the existing HPLC/UV method for the determination of forbidden compounds in dietary supplements.

항 바이러스성 Carbocyclic nucleoside류의 합성

  • 김희두;최명희
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1994.04a
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    • pp.229-229
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    • 1994
  • 선택성이 높고 뛰어난 약효를 지닌 항 바이러스제의 개발은 신약개발의 중요한 영역중에 하나이다. 현재 AIDS 치료제로 사용되고 AZT를 비롯하여 항virus 효과를 나타내는 약물의 대부분은 구조적으로 nucleoside계에 속하는 화합물로서 수 많은 약리학적 연구 및 합성 화학적 연구가 이루어져 왔다. 특히 합성 화학적 측면에서 이들 화합물의 합성은 크게 두가지로 나누어지는데 그것은 sugar 부위의 변형을 통한 방법과 염기 부위의 변형을 통한 방법에 의해 새로운 항 바이러스제를 개발하는 것이다. 최근의 연구 동향에 있어서 주목할 만한 변화의 하나는 sugar 부위의 구조적 변형을 시도하는데 있어서 종래의 5원환 형태에서 환이 개열된 형태의 acyclic nucleoside에 대한 연구가 이루어져 좋은 효과를 거두고 인다는 사실이다. Acyclovir, Ganciclovir등 의 개발이 그것이다. 본 연구에서는 종래의 acyclic nucleoside가 ribose sugar의 2'번 및 3'번 탄소를 제거한 acyclic ether 형태로 되어있는 것과는 다르게 ether 부위의 산소를 탄소 치환한 carbo-acyclic nucleoside를 합성하고자 하였다. Acyclic nucleoside를 합성하고자 하였다. Acyclic nucleoside의 side chain의 conformation이 항 바이러스 작용을 나타내는데 필수 불가결한 점을 감안할때, carbo-acyclic nucleoside계 화합물은 보다 다양하게 변형될 수 있는 장점을 가지고 있다. 이러한 관점에서 side chain의 2'번 및 3'번 탄소는 side chain의 conformation을 좌우하는 결정적 요인으로 작용할 것으로 판단된다. 따라서 본 연구에서는 이들 탄소를 중심으로한 분자수식을 시도하기로 하고 bioisosterism을 이용하여 3'위치의 수소를 fluoride로 치환한 화합물을 설계하여 합성을 시도하였다.silyl group-5'-무치환 화합물을 tosyl, azido화 한다음 desilylation하여 얻었다. 목적하는(1) 화합물의 diasteromer 인 2',3'-dihydroxy-5'-무치환 유도체(3)는 (4)화합물 합성시 얻은 hemiactal을 key intermediate로 하여 TsNHNH$_2$, NaB(CN)H$_3$ 및 NaOAc로 처리하므로서 얻을수 있었다. 이들 화합물들의 각종 DNA 및 RNA virus에 대한 항 바이러스작용을 검토한 결과 현저한 항 바이러스 작용을 나타내지 않았다.분화유도 활성을 나타내어 항종양제로의 개발에 많은 흥미가 기대된다.기대된다.oxylic acid (compound 10)를 합성하였다.10^{-7}$ M)에 의한 단백인산화에 대하여는 더 미약한 억제-효과를 나타내었다. 이상의 결과는 PDE-1과 항우울약들의 항혈소판작용은 PKC-기질인 41-43 kD와 20 kD의 인산화를 억제함에 기인되는 것으로 사료된다.다. 것으로 사료된다.다.바와 같이 MCl에서 작은 Dv 값을 갖는데, 이것은 CdCl$_{4}$$^{2-}$ 착이온을 형성하거나 ZnCl$_{4}$$^{2-}$ , ZnCl$_{3}$$^{-}$같은 이온과 MgCl$^{+}$, MgCl$_{2}$같은 이온종을 형성하기 때문인것 같다. 한편 어떠한 용리액에서던지 NH$_{4}$$^{+}$의 경우 Dv값이 제일 작았다. 바. 본 연구의 목적중의 하나인 인체유해 중금속이온인 Hg(II), Cd(II)등이 NaCl같은 염화물이 함유된 시료용액에 공해이온으로 존재할 경우 흡착에 의한 제거가 가능하다. 한편 이같은 중금속이온의 흡착실험은 특히 해수중의 금속이온의 회수연구에도

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Oral Sildenafil in Persistent Pulmonary Hypertension of the Newborn (신생아의 지속성 폐동맥 고혈압증에서 Sildenafil 치료 경험)

  • Son, Su-Bin;Kim, Kyung-Ah;Yun, So-Young;Ko, Sun-Young;Lee, Yeon-Kyung;Shin, Son-Moon
    • Neonatal Medicine
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    • v.18 no.1
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    • pp.124-129
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    • 2011
  • Purpose: To evaluate the effect of oral sildenafil therapy in neonates with persistent pulmonary hypertension of the newborn (PPHN) Methods: We conducted a retrospective review of 32 neonates ${\geq}$35 weeks' gestation and fraction of inspired oxygen ($FiO_2$) 1.0 with PPHN. The first dose (0.5 mg/kg) of oral sildenafil was started and 1 mg/kg was given every 6 hour thereafter. Mean airway pressure (MAP), $FiO_2$, oxygenation index (OI), mean arterial blood pressure (MBP) were documented before and 6, 12, 24, and 48 hours after sildenafil. For adverse effects, gastrointestinal symptoms, brain ultrasound, funduscopy and auditory brainstem response results were evaluated. Results: The underlying diseases of PPHN (n=32) were meconium aspiration syndrome (n=9), respiratory distress syndrome (n=8), pneumonia (n=3), and idiopathic (n=12). Thirty-one neonates survived; 3 neonates were transferred for inhaled nitric oxide (iNO) and all of them survived. In 28 infants, $FiO_2$ and OI improved significantly by 6 hours and MAP improved significantly by 48 hours after initiation of sildenafil. There were no clinically significant adverse effects of sildenafil. Conclusion: Sildenafil may be an effective and safe agent for near-term and term neonates with PPHN, providing significant improvement in oxygenation, and thus may be especially useful in the treatment of PPHN in hospitals without iNO.

The Prediction of the Expected Current Selection Coefficient of Single Nucleotide Polymorphism Associated with Holstein Milk Yield, Fat and Protein Contents

  • Lee, Young-Sup;Shin, Donghyun;Lee, Wonseok;Taye, Mengistie;Cho, Kwanghyun;Park, Kyoung-Do;Kim, Heebal
    • Asian-Australasian Journal of Animal Sciences
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    • v.29 no.1
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    • pp.36-42
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    • 2016
  • Milk-related traits (milk yield, fat and protein) have been crucial to selection of Holstein. It is essential to find the current selection trends of Holstein. Despite this, uncovering the current trends of selection have been ignored in previous studies. We suggest a new formula to detect the current selection trends based on single nucleotide polymorphisms (SNP). This suggestion is based on the best linear unbiased prediction (BLUP) and the Fisher's fundamental theorem of natural selection both of which are trait-dependent. Fisher's theorem links the additive genetic variance to the selection coefficient. For Holstein milk production traits, we estimated the additive genetic variance using SNP effect from BLUP and selection coefficients based on genetic variance to search highly selective SNPs. Through these processes, we identified significantly selective SNPs. The number of genes containing highly selective SNPs with p-value <0.01 (nearly top 1% SNPs) in all traits and p-value <0.001 (nearly top 0.1%) in any traits was 14. They are phosphodiesterase 4B (PDE4B), serine/threonine kinase 40 (STK40), collagen, type XI, alpha 1 (COL11A1), ephrin-A1 (EFNA1), netrin 4 (NTN4), neuron specific gene family member 1 (NSG1), estrogen receptor 1 (ESR1), neurexin 3 (NRXN3), spectrin, beta, non-erythrocytic 1 (SPTBN1), ADP-ribosylation factor interacting protein 1 (ARFIP1), mutL homolog 1 (MLH1), transmembrane channel-like 7 (TMC7), carboxypeptidase X, member 2 (CPXM2) and ADAM metallopeptidase domain 12 (ADAM12). These genes may be important for future artificial selection trends. Also, we found that the SNP effect predicted from BLUP was the key factor to determine the expected current selection coefficient of SNP. Under Hardy-Weinberg equilibrium of SNP markers in current generation, the selection coefficient is equivalent to $2^*SNP$ effect.