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N-4-Substituted-benzyl-N'-tert-butylbenzyl Thioureas as Vanilloid Receptor Ligands: Investigation on the Role of Methanesulfonamido group in Antagonistic Activity

  • Park, Hyeung-Geun;Choi, Je-Yeon;Choi, Sea-Hoon;Park, Mi-Kyung;Lee, Ji-Hye;Suh, Young-Ger;Cho, Ha-Won;Oh, Uh-Taek;Lee, Ji-Youn;Kang, Sang-Uk;Lee, Jee-Woo;Kim, Hee-Doo;Park, Young-Ho;Jeong, Yeon-Su;Choi, Jin-Kyu;Jew, Sang-Sup
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.173.2-173.2
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    • 2003
  • Vanilloid receptor I (VR1) is a nonselective cation ion channel placed in the plasma membrane of peripheral sensory neurons that is potential target for analgesia A series of N-4-substituted-benzyl-N'-tert-butylbenzyl thioureas were prepared for the study of their agonistic/antagonistic activities to the vanilloid receptor in rat DRG. Their structure-activity relationship in reveals that not only the two oxygens and amide hydrogen of sulfonamido group but also the optimal size of methyl in methanesulfonamido group play an integral role for the antagonistic activity on vanilloid receptor.

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Regurgitation and Gastroesophageal Reflux Disease in Six to Nine Months Old Indonesian Infants

  • Hegar, Badriul;Satari, Debora Hindra I.;Sjarif, Damayanti R.;Vandenplas, Yvan
    • Pediatric Gastroenterology, Hepatology & Nutrition
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    • v.16 no.4
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    • pp.240-247
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    • 2013
  • Purpose: Regurgitation is known to peak at the age of 3-4 months, with a sharp decrease around the age of 6 months. Little is known about the natural evolution of infants who still regurgitate after the age of 6 months. Methods: Hundred thirty-one infants older than 6 months regurgitating more than once a day were followed for a period of 3 months. Results: According to our data, gastroesophageal reflux disease (GERD) is seldom at this age. Most of the infants regurgitated 3 or more times/day and spit up an estimated volume of more than 15 mL. Eighty-five parents were educated regarding frequency of feeding. There were only 6 infants that still had frequent regurgitation (>3 times/day) despite an appropriate feeding schedule. The Infant GER Questionnaire score reached a score of 0 in 50% of the infants after one month of follow-up and in 81.9% at the third month of follow-up. There was an increase of the "weight for age z-score" trends in infants that still regurgitated at the end of follow-up and a declining z-score in infants that no longer regurgitated. An explanation may be that infants that regurgitate drink larger volumes than infants who do not regurgitate. Conservative treatment (reassurance, dietary treatment, behavioral advice) resulted in a significant better outcome than natural evolution. Conclusion: Regurgitation that persisted after the age of 6 months, strongly decreased during a 3-month follow-up with conservative treatment. GERD is rare in this age group; therefore, anti-reflux medication is only seldom needed.

Peroxyl Radical Scavenging Capacity of the Flavonolignan Silybin, Ginkgo Biloba Extract EGb 761, American Green Tea and a Series of Germacranolides

  • Winston, Gary W.;Kim, Young Chul;Dugas, Alton J.;Castaneda-Acosta, Jose;Fischer, Nikolaus H.
    • Toxicological Research
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    • v.17
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    • pp.271-280
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    • 2001
  • We report on the applicability oj a method recently developed in our laboratory for measuring the antioxidant potential of isolated chemicals and extracts derived from natural products. Peroxyl radicals generated by thermal homolysis of 2,2'-azobis-amidinopropane (ABAP) oxidize $\alpha$-keto-${\gamma}$-methiolbutyric acid (KMBA) to ethylene, which is monitored by gas chromatography. Inhibition of ethylene formation in the presence of antioxidants that compete with KMBA for peroxyl radicals is the basis of the Total Oxyradical Scavenging Capacity Assay (TOSCA; Winston et al., 1998). Antioxidative activities of water-soluble extracts of American green tea, the anti-hepatotoxic flavonolignan from milk thistle (Silybum marianum) silybin, Ginkgo biloba extract EGb 761, and a series of naturally occuring sesquiterpene lactones (all ger-macranolides found in in fungi, liverworts, and plants) were studied. The specific TOSC value per $\mu$M silybin was 5.2, which is essentially comparable to that of Trolo $x^{ⓡ}$, a water-soluble vitamine E analog. Tea and Ginkgo extracts exhibited potent peroxyl radical scavenging capacity with values, respectively of =1700 and 1000 $\mu$mols Trolo $x^{ⓡ}$ equivalent per gram dry matter. The known anti-inflammatory activity of some germacranolides prompted study of their antioxidant capacity. None of the lactones exhibited antioxidant capacity toward peroxyl radicals comparable to Trolo $x^{ⓡ}$; costunilide, the most lipophilic, had a TOSC value = to glutathione. The potential role of peroxyl radicals in lipidperoxidation, other cellular damage, and var-ious disease states suggest a possible preventive role for silybin, green tea and Ginkgo biloba in oxidative stress caused by these free radical species.ecies.

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A study of Train Running Simulation for Electronic Performance Analysis of Propulsion (추진 장치의 전기적 성능 시험을 위한 열차 운행 모의 성능 분석 연구)

  • Kim, Young-Chan;Seo, Young-Ger;Lee, Byung-Song;Hong, Soon-Chan;Ko, Jung-Sun
    • The Transactions of the Korean Institute of Power Electronics
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    • v.12 no.6
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    • pp.483-490
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    • 2007
  • The aim of the paper is to analysis on train propulsion system and to study for energy saving. For this study, we make the program that simulate actual operation of the train route. The train running simulation is performed from starting station to 4th station by using the route datas of Deajeon Metro Subway. The study for control method of electrical motor and energy recovery to save energy is selected. The train propulsion system is constituted as a M-G Set, which is realized via Space Vector Modulation(SVM) - Direct Torque Control(DTC), the energy consumption during train operation and energy recovery during breaking is simulated by Simplorer program, from this result, the energy consumption and recovery of train with SVM-DTC is studied.

Alaternin and Emodin with Hydroxyl Radical inhibitory and/or Scavenging Activities and Hepatoprotective Activity on Tacrine-Induced Cytotoxicity in HepG2 Cells

  • Jung, Hyun-Ah;Chung, Hae-Young;Takaka, Yokezawa;Kim, Youn-Chul;Hyun, Sook-Kyung;Choi, Jae-Sue
    • Archives of Pharmacal Research
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    • v.27 no.9
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    • pp.947-953
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    • 2004
  • The antioxidative and hepatoprotective potentials of two anthraquinones, alaternin (2-hydroxy-emodin) and emodin, to scavenge and/or inhibit hydroxyl radicals generated by the Fenton reaction and to protect tacrine-induced cytotoxicity in human liver derived HepG2 cells were evaluated, respectively. The inhibitory activity on hydroxyl radical generated in a cell-free chemical system (FeSO$_4$/$H_2O$$_2$) was investigated by a fluorescence spectrophotometer using a highly fluorescent probe, 2$^1$,7$^1$-dichlorofluorescein. The hydroxyl radical scavenging activity was determined by electron spin resonance spectroscopy using 5,5-dimethy-1-pyrroline-N-oxide as hydroxyl radicals trapping agents. Tacrine-induced HepG2 cell toxicity was determined by a 3-[4,5-dimethylthiazole-2yl]-2,5-diphenyltertrazolium bromide assay. Although the scavenging activity of alaternin on hydroxyl radical was similar to that of emodin in dose-dependent pat-terns, the inhibitory activity exhibited by the former on hydroxyl radical generation was stron-ger than that of the latter, with $IC_{50}$/ values of 3.05$\pm$0.26 $\mu$M and 13.29$\pm$3.20 $\mu$M, respectively. In addition, the two anthraquinones, alaternin and emodin showed their hepatoprotective activ-ities on tacrine-induced cytotoxicity, and the EC$_{50}$ values were 4.02 11M and 2.37 $\mu$M, respec-tively. Silymarin, an antihepatotoxic agent used as a positive control exhibited the EC$_{50}$ value of 2.00 $\mu$M. These results demonstrated that both alaternin and emodin had the simultaneous antioxidant and hepatoprotective activities.ies.

Etude sur le v tement dans le Proche-Orient (근동지역의 복식 연구(I) -성서에서의 복식의 상징성과 고대 근동지역의 복식 연구-)

  • 오춘자
    • Journal of the Korean Society of Costume
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    • v.19
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    • pp.175-194
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    • 1992
  • Le Proche-Orient est le pays de la Bible, Le peuple He breu ancien, appartenant la race des S mits s mi-nomades, est venu avec Abraham, de m sopotamie en Palestine, terre de Canaan. Nous avons consid r les v tements du peuple des anciens H breux en nous basant sur la Bible et en observant des peintures murales et des bas-reliefs des divers payes de l'ancienne poque, Pour comprendre l' volution des v tements des gens de la pr sente r gion palestinienne, nous avons tudi les v tements traditionnels de la race b douine qui m nent jusqu' maintenant une vie nomade dans le m nent jusqu' maintenant une vie nomade dans le d sert, parce que nous n'avons pas pu connaitre le processus d' volution des v tements apr s l'ancienne poque la suite d' v nements historiques compliques. En conclusion, nous pouvons nous r sumer comme suit: 1) Nous pensons que la kimlah, costume important du peuple h breu ancien est devenu abajeh, manteau des B douins, puisque ces v tements servent prot ger le corps lors des changments de temps, et la nuit on les utilise comme couverture et comme sac pour y mettre des objets, et comme tente lors su travail. en un mot, les fonctions de la Simlah et celles de l'abajeh sont les memes l' poque ancienne et maintenant. 2) Nous pensons que la forme et l'utilisation de la Kethoneth ayant une forme de tunique et de la thob des B douins sont presque semblable. La kethoneth et la thob sont la tuniqu importante que portent jusqu' maintenant tous les peuples du Proche-Orient. 3) Comme on le voit dans la Bible, les femmes du peuple h breu et celles des B douins utilisent le voile pour couvrir la e te, et se servent d'accessoires pour d corer leur corps. A l'avenir, les vVtements des Palestiniens, dans une recherche pous approfondie, feront l'objet de a 2 me partie de l' tude des costumes du Proche-Orient.

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Synthesis and Antiinflammatory Effects of a New Tricyclic Diterpene and Its Analogues as Potent COX-2 Inhibitors

  • Suh, Young-Ger;Kim, Young-Ho;Park, Hyoung-Sup;Lee, Hye-Kyung;Park, Young-Hoon;Kim, Ji-Young;Min, Kyung-Hoon;Shin, Dong-Yun;Jun, Ra-Ok
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 2000.04a
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    • pp.10-14
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    • 2000
  • The cycloooxygenase enzymes catalyze the oxidative conversion of arachidonic acid into prostag1andin H$_2$Which mediates both benificial and pathological effects. The COX-1 is constitutively expressed in most tissues and in blood platelets wherease the expression of COX-2 isoform is induced in response to inflmmatory stimuli such as cyctokynes. Thus the identification of a novel COX-2 selective inhibitor should offer excellent antiinflammatory activity with minimal side effects such as gastrointestinal toxicity. Recently, a group of structurally unique and biologically active pimarane diterpenoids has been isolated from indigenous Korean medicinal plants. These new diterpenoids turned out to be potential analgesic and antiinflammatory agent due to their potent inhibitory activities of prostaglandin synthesis. We have also found that the inhibition of PGE$_2$synthesis is attributed to the potent COX inhibition by pimarane diterpenoid in arachidonic acid cascade. In conjunction with development of new analgesic and nonsteroidal antiinflammatory agent, a series of works on these diterpenoids have been extensively carried out in our laboratories. These efforts involve the structure-activity relationship of pimaradienoic acid, molecular modelings and COX inibitory activities as well as actiinflammatory effects of its structural analogues. In addition, the total syntheses of the new natural pimarane diterpenoids, their stereoisomers and other structural variants were intensively investigated.

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On the Project of the Sport Biomechanics of IAAF World Championships Daegu 2011 (2011 대구세계육상선수권대회 운동역학 프로젝트 수행 방안)

  • Lee, Joong-Sook;Park, Jong-Jin;Bae, Young-Sang;Chae, Woen-Sik;Ryu, Jae-Kyun;Park, Seung-Bum
    • Korean Journal of Applied Biomechanics
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    • v.20 no.3
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    • pp.253-259
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    • 2010
  • The aim of IAAF's Biomechanics project, initially launched at the 1987 World Championships in Rome, is to support athletes and coaches in the optimization and improvement of their training and competition performance. The IAF and the IAAF supports biomechanical projects, as a service to their Member Federations, starting from the IAAF World Championships in Rome 1987. In 1997, at the IAAF World Championships of Athens. In 1995, at the IAAF World Championships in Goteborg and in co-operation with the Swedish Sport Institute of Karlstad and under the leadership of Anders Bergstrom a biomechanical research on "Throws" was conducted. In 2005, at the IAAF World Championships in Helsinki on 100m - Pole vault, High Jump, Triple Jump, Javelin, under the leadership of Prof. Paavo Komi. The IAAF published the final report in 2008 with a supplement of NSA. In 2007, at the IAAF World Championships of Osaka, in co-operation with Osaka University of Health and Sport Sciences and under the leadership of Prof. Michiyoshi Ae the IAAF received a final report on; short sprint, distance running, high jump, long jump, shot put and javelin. In 2009, at the IAAF World Championships of Berlin, in co-operation with the DLV and the leadership of Helmar Hommel (GER). The purpose of this study is to draw up a plan to perform an effective biomechanics project at 2011 IAAF World championship in Daegu.

A Study on the Noise by working Process in Dental Laboratory (치과기공실(齒科技工室)의 작업공정별(作業工程別) 소음(騷音)에 관한 연구(硏究))

  • Nam, Sang-Yong
    • Journal of Technologic Dentistry
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    • v.15 no.1
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    • pp.27-41
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    • 1993
  • Degree of noise by personal dental laboratory working process and degree of noise by complex dental laboratory working process were measured separtely. The time of exposure to noise greater than 70dB was analyzed. Then, the whole degree of noise in dental laboratory was estimated on the basis of afore-mentioned information. Questionaire were employed to investigate the mental, emotional and physiological effects of noise in dental technicians, The purpose of this study was to provide basic information on keeping dental techneicans who are exposed to noise pollution in good working condition and good health. Results obtained are as follows ; 1. Polishing process in each working part showed high degree of noise greater than 70dB in terms of degree of noise by personal working. 2. Degree of noise by complex working process in each working part was greater than that of personal working process. 3. Time of exposure to noise complex working process the part of porcelain 150min, partial denture 120 min, crown and bridge 100 min, full denture 80 min. 4. Degree of noise by time in dental laboratory was 80dB in general for polishing process and below 75dB for waxing process. 5. Effects of noise on mental and emotional state of dental technicians showed that they felt irritated every day(14%), irritated once in a while(29%) and easily ger mad(19%). 6. Effects of noise on heart and stomach were hyper-gastric acid(38%), gastric ulcer(11%), gastritis(5%), deuodenal ulcer(3%) and weak heart function(32%). 7. Effects of noise in the hearing ability were weak(39%), moderate(33%) and normal(14%) Data presented in this study demonstrated that noise in the dental laboratory exerts profound effect on dental technicians mentally, physiologically and emotionally, in light of the above results, therefore, it appears advisable to devots substantial on the management of working condition and put further(continuing) efforts in the investigation for reducing noise problem.

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Genetically Engineered Biosynthesis of Macrolide Derivatives Including 4-Amino-4,6-Dideoxy-L-Glucose from Streptomyces venezuelae YJ003-OTBP3

  • Pageni, Binod Babu;Oh, Tae-Jin;Liou, Kwang-Kyoung;Yoon, Yeo-Joon;Sohng, Jae-Kyung
    • Journal of Microbiology and Biotechnology
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    • v.18 no.1
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    • pp.88-94
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    • 2008
  • Two sugar biosynthetic cassette plasm ids were used to direct the biosynthesis of a deoxyaminosugar. The pOTBP1 plasmid containing TDP-glucose synthase (desIII), TDP-glucose-4,6-dehydratase (desIV), and glycosyltransferase (desVII/desVIII) was constructed and transformed into S. venezuelae YJ003, a strain in which the entire gene cluster of desosamine biosynthesis is deleted. The expression plasmid pOTBP3 containing 4-aminotransferase (gerB) and 3,5-epimerase (orf9) was transformed again into S. venezuelae YJ003-OTBP1 to obtain S. venezuelae YJ003-OTBP3 for the production of 4-amino-4,6-dideoxy-L-glucose derivatives. The crude extracts obtained from S. venezuelae ATCC 15439, S. venezuelae YJ003, and S. venezuelae YJ003-OTBP3 were further analyzed by TLC, bioassay, HPLC, ESI/MS, LC/MS, and MS/MS. The results of our study clearly shows that S. venezuelae YJ003-OTBP3 constructs other new hybrid macrolide derivatives including 4-amino-4,6-dideoxy-L-glycosylated YC-17 (3, [M+ $Na^+$] m/z=464.5), methymycin (4, m/z=480.5), novamethymycin (6, m/z=496.5), and pikromycin (5, m/z=536.5) from a 12-membered ring aglycon (10-deoxymethynolide, 1) and a 14-membered ring aglycon (narbonolide, 2). These results suggest a successful engineering of a deoxysugar pathway to generate novel hybrid macrolide derivatives, including deoxyaminosugar.