• 제목/요약/키워드: YS 49

검색결과 18건 처리시간 0.027초

EFFECT OF A NEW POSITIVE INOTROPIC AGENT, YS-49, A NOVEL TETRAHYDROISOQUINOLINE COMPOUND

  • Lee, Y. S.;Park, H. S. Yoon-;K. C. Chang
    • 한국응용약물학회:학술대회논문집
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    • 한국응용약물학회 1995년도 춘계학술대회
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    • pp.88-88
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    • 1995
  • Tetrahydroisoquinoline (THI) compounds have various pharmacological actions in the cardiovascular system. Recently, we have synthesized 1-${\alpha}$-naphthylmethyl-6,7-dihydroxy-1,2,3,4-tetrahydroisoquinoline, YS 49. In the present study, we evaluated the effect of YS-49 on positive inotropic and chronotropic action using isolated rat heart and on blood pressure and heart rate using anesthesized rabbit. Vasodilating action was also assessed in isolated rat thoracic aorta. YS 49, concentration-dependently relaxed rat aorta precontracted with phenylephrine (PE, 0.3 ${\mu}$M) and high potassium (high K$\^$+/, 65.4 mM). The 50% inhibitory concentration (IC$\sub$50/) of YS 49 in PE-induced and high K$\^$+/-induded contraction was 5.36 ${\mu}$M and 2.52 ${\mu}$M, respectively. In isolated rat atria, YS 49 increased both heart rate and force, and in anesthesized rabbit it decreased blood pressure but increased heart rate. In addition, to know the mechanism of action of the compound, propranolol, nonselective ${\beta}$-antagonist, and phentolamine, ${\alpha}$-blocker, were used. Furthermore, a comparison with the effect of higenamine, trimetoquinol on the vasodilating action in rat thoracic aorta was also made. The action of YS 49 was inhibited by the presence of propranolo, not pentolamine. These results indicate that cardiotonic and vasodilatory action of YS 49 is attributable, at least in part, for ${\beta}$-receptor stimulation.

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YS 49, a Synthetic Isoquinoline Alkaloid, Protects Sheep Pulmonary Artery Endothelial Cells from tert-butylhydroperoxide-mediated Cytotoxicity

  • Chong, Won-Seog;Kang, Sun-Young;Kang, Young-Jin;Park, Min-Kyu;Lee, Young-Soo;Kim, Hye-Jung;Seo, Han-Geuk;Lee, Jae-Heun;ChoiYun, Hye-Sook;Chang, Ki-Churl
    • The Korean Journal of Physiology and Pharmacology
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    • 제9권5호
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    • pp.283-289
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    • 2005
  • Endothelium, particularly pulmonary endothelium, is predisposed to injury by reactive oxygen species (ROS) and their derivatives. Heme oxygenase (HO) has been demonstrated to provide cytoprotective effects in models of oxidant-induced cellular and tissue injuries. In the present study, we investigated the effects of YS 49 against oxidant [tert-butylhydroperoxide (TBH)]-induced injury using cultured sheep pulmonary artery endothelial cells (SPAECs). The viability of SPAECs was determined by quantifying reduction of a fluorogenic indicator Alamar blue. We found that TBH decreased cell viability in a timeand concentration-dependent manner. YS 49 concentration- and time-dependently increased HO-1 induction on SPAECs. As expected, YS 49 significantly decreased the TBH-induced cellular injury. In the presence of zinc protophorphyrin, HO-1 inhibitor, effect of YS 49 was significantly inhibited, indicating that HO-1 plays a protective role for YS 49. Furthermore, YS 49 showed free radical scavenging activity as evidenced by 1,1-diphenyl-2-picrylhydrazyl (DPPH) and inhibition of lipid peroxidation. However, YS 49 did not inhibit apoptosis induced by lipopolysaccharide (LPS) in SPAECs. Taken together, HO-1 induction along with strong antioxidant action of YS 49 may be responsible for inhibition of TBH-induced injury in SPAECs.

Inhibition of Inducible Nitric Oxide Synthase Expression by YS 49, a Synthetic Isoquinoline Alkaloid, in ROS 17/2.8 Cells Activated with $TNF-{\alpha},\;IFN-{\gamma}$ and LPS

  • Kang, Young-Jin;Kang, Sun-Young;Lee, Young-Soo;Park, Min-Kyu;Kim, Hye-Jung;Seo, Han-Geuk;Lee, Jae-Heun;YunChoi, Hye-Sook;Chang, Ki-Churl
    • The Korean Journal of Physiology and Pharmacology
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    • 제8권5호
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    • pp.273-280
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    • 2004
  • Nitric oxide (NO) has been suggested to act as a mediator of cytokine-induced effects of turn over of bone. Activation of the inducible nitric oxide synthase (iNOS) by inflammation has been related with apoptotic cell death in osteoblast. YS 49, a synthetic isoquinoline alkaloid, inhibits NO production in macrophages activated with cytokines. In the present study, we investigated the molecular mechanism of YS 49 to inhibit iNOS expression in ROS 17/2.8 cells, which were activated with combined treatment of inflammatory cytokines $(TNF-{\alpha},\;IFN-{\gamma})$ and lipopolysaccharide (LPS). Results indicated that YS 49 concentration-dependently reduced iNOS mRNA and protein expression, as evidenced by Northern and Western blot analysis, respectively. The underlying mechanism by which YS 49 suppressed iNOS expression was not to affect iNOS mRNA stability but to inhibit activation and translocation of $NF-_kB$ by preventing the degradation of its inhibitory protein $I_kB_{\alpha}$. As expected, YS 49 prevented NO-induced apoptotic cell death by sodium nitroprusside. Taken together, it is concluded that YS 49 inhibits iNOS expression by interfering with degradation of phosphorylated inhibitory $_kB_{\alpha}\;(p-I_kB_{\alpha})$. These actions may be beneficial for the treatment of inflammation of the joint, such as rheumatoid arthritis.

Comparison of Inodilator Effect of Higenamine, YS49, YS51, Tetrahydroisoquinoline Analogs, and Dobutamine in the Rat

  • Chong, Won-Seog;Lee, Young-Soo;Kang, Young-Jin;Lee, Duck-Hyung;Ryu, Jae-Chun;Yun-Choi, Hye-Sook;Chang, Ki-Churl
    • The Korean Journal of Physiology and Pharmacology
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    • 제2권3호
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    • pp.323-330
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    • 1998
  • Tetrahydroisoquinoline (THI) alkaloids can be considered as cyclized derivatives of simple phenylethylamines. Many of them, especially with 6,7-disubstitution, demonstrate a relatively high affinity for catecholamines. Present study examines the pharmacological action of limited series of THI, using rats' isolated atria and aorta. In addition, a $[^3H]$ prazosin displacement binding study with THI compounds was performed, using rat brain homogenates to investigate whether these probes have ?${\alpha}$-adrenoceptor affinity. We also compared the vascular relaxation potency of these probes with dobutamine. YS 49, YS 51, higenamine and dobutamine, concentration-dependently, relaxed endothelium-denuded rat thoracic aorta precontracted with phenylephrine (PE, 0.1 ${\mu}M$) in which $pEC_{50}$ were $5.56{\pm}0.32$ and $5.55{\pm}0.21$, $5.99{\pm}1.16$ and $5.57{\pm}0.34$, respectively. These probes except higenamine also relaxed KCl (65.4 mM)-contracted aorta. In isolated rat atria, all THIs and dobutamine increased heart rate and contractile force. In the presence of propranolol, the concentration response curves of YS 49 and YS 51 shifted to the right and resulted in $pA_2$ values of $8.07{\pm}0.84$ and $7.93{\pm}0.11$, respectively. The slope of each compound was not deviated from unity, indicating that these chemicals are highly competitive at the cardiac ?${\beta}-adrenoceptors$. YS 49, YS 51, and higenamine showed ?${\alpha)-adrenoceptor$ affinity in rat brain, in which the dissociation constant $(K_i)$ was 2.75, 2.81, and 1.02 ${\mu}M$, respectively. It is concluded, therefore, that THI alkaloids have weak affinity to ${\alpha)_1-adrenoceptor$ in rat aorta and brain, respectively, while these probes show relatively high affinity for cardiac ${\beta}-adrenoceptors$. Thus, these chemicals may be useful in the treatment of congestive heart failure.

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황해 및 북서태평양 확장해역 정밀조석모의 (Precise Tidal Simulation on the Yellow Sea and Extended to North Western Pacific Sea)

  • 서승원;김현정
    • 한국해안·해양공학회논문집
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    • 제23권3호
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    • pp.205-214
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    • 2011
  • 정밀조석모의를 위한 유한요소 격자가 황해 영역에서 절점밀집도 14 K, 52 K 및 211 K 등으로 세련화되어 구축되었으며, 북서태평양을 포함하는 광역에 대해 57K의 절점을 갖는 격자체계가 구축되었다. 수치실험은 32개의 병렬프로세서에서 pADCIRC v 49.21 모형을 이용하여 수행하였다. 조석모의는 YS-G52K, YS-G211K 격자에서 KorBathy30s와 ETOPO1 수심자료를 적용하고, FES2004로부터 추출된 4 분조를 개방경계에 적용하여 모의한 결과 관측치와는 진폭에서 RMS오차 0.138 m, 위상은 RMS오차 14.80 deg로 이전 황해 연구에 비해 개선된 결과가 나타났다. 북서태평양으로 확장된 영역인 NWP-G57K 격자의 개방경계에서 8 분조를 정의하여 모의한 결과 황해 조석모의 결과와 유사한 매우 만족스러운 결과가 도출되었다.

The In Vitro and In Vivo Efficacy of Hen IgY Against Vibrio parahaemolyticus and Vibrio vulnificus

  • Kassim, Neema;Mtenga, Adelard B.;Shim, Won-Bo;Chung, Duck-Hwa
    • Journal of Microbiology and Biotechnology
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    • 제22권10호
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    • pp.1423-1431
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    • 2012
  • The inhibitory effect of IgY against Vibrio parahaemolyticus and Vibrio vulnificus responsible for seafood-borne diseases was investigated in this study. Water-soluble fractions (WSF) of protein containing IgYs were isolated from the egg yolk of hens initially immunized with formalin-inactivated V. parahaemolyticus or V. vulnificus. Protein, total and specific IgY contents of the WSF were determined. The inhibitory and protective effects of IgYs on the growth of V. parahaemolyticus and V. vulnificus were assayed in liquid medium and in mice. IgYs showed high affinity to their corresponding antigens with high titer from day 28 onwards. Protein contents and total IgY concentrations remained stable throughout the immunization period, whereas specific IgY concentrations increased steadily and reached a plateau at day 49. Specific IgY powder (150 mg/ml) significantly inhibited further multiplication of both V. parahaemolyticus and V. vulnificus in liquid medium as compared with the control IgY. The bacteria count in mice feces was lower in mice pretreated with specific IgYs than in those pretreated with PBS or control IgY. Higher survival of mice was observed in the experimental groups pretreated with either anti-V. parahaemolyticus (75% survival) or anti-V. vulnificus (87% survival) IgYs, compared with those in the control groups pretreated with PBS or nonspecific IgY. All mice in the control groups died within three days after bacteria inoculation; hence, the protective effect of specific IgYs against infection caused by V. parahaemolyticus and V. vulnificus was demonstrated.

Optimal Medium Composition Suitable for Enhancement of Biofertilizer's Shelf Life

  • Lee, Yong-Seong;Park, Yun-Suk;Kim, Kil-Yong
    • 한국토양비료학회지
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    • 제49권5호
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    • pp.456-460
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    • 2016
  • Biofertilizers are increasingly available in the market as one of the alternatives to chemical fertilizers. The supply of a high number of viable microorganisms is important for farmers. Lysobacter capsici YS1215 producing chitinases and gelatinases, isolated from soil in Korea, was evaluated for the establishment of an optimal medium condition of its shelf life under an in vitro condition. In this study, the population density of a biofertilizer (L. capsici YS1215) in media containing crab shell and gelatin powder (M1, M2, M3 and M4) was observed to be higher than that of populations grown in TSB (Tryptic soy broth) media (M5, M6 and M7) during experimental period. In addition, the population density at 11 months was over $10^6\;CFU\;mL^{-1}$ in M1, M3 and M4, but under $10^6\;CFU\;mL^{-1}$ in M2, M5, M6 and M7. The best optimal medium for the shelf life was M1 ($2.6{\times}10^6\;CFU\;mL^{-1}$) containing both chitinous and gelatinous materials at 11 months. Therefore, this study provided results of the appropriate medium composition for the enhancement of the shelf life of L. capsici YS1215.

기공전구체를 이용한 고체전해질 연료전지의 동시소성 연구 (Co-firing of Solid Oxide Fuel Cell Using Pore Former)

  • 문지웅;이홍림;김구대;김재동;이해원
    • 한국세라믹학회지
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    • 제35권3호
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    • pp.273-279
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    • 1998
  • Unite cell of soid oxide fuel cell (SOFC) that consists of a dense yttria-stabilized zirconia(YSZ) electrolyte a porous nickel-YSZ cermet anode and a porous strontium- doped lanthanum manganate(LSM) cathod was fabricated from using pore former through co-firing technique. Initial sintering shrinkage rates of each layer were identified for fabricating SOFC. Heterogenous sintering was very effective in tailoring shrinkage rate for three layers. The powder tailoring necessary for shrinkage rate matching are as follows ; electrolyte of 60% TZ8YS/ 40% TZ8Y mixture anode of 51wt% NiO/49 wt% (70wt% TZ8YS/30 wt% UT ZrO2) mixture and cathode of 80% LSM/20% UT ZrO2 mixture . The overall sintering shrinkage rate differences of three layers using these compositions were maintained in a few percent.

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이질아메바(Entamoeba histolytica)의 미세구조 및 효소활성에 관한 전자현미경적 연구 (Electron-microscopic studies on fine structure and enzyme activity in the axenic and conventional strains of Entamoeba histolytica)

  • 용태순;정평림;이근태
    • Parasites, Hosts and Diseases
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    • 제23권2호
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    • pp.269-284
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    • 1985
  • The metabolism of Entamoeba histolytica would be affected by various environmental factors, and alteration of the environment was known to afEect the fine structure of 5. histolytica. The present study was designed electronmicroscopically to investigate the ultrastructure and enzyme activities in the aEonic and conventional strains of 5. histolytica. The trophozoites of axenically cultivated HK-9 strain and conventional YS-27 and YS-49 strains of 5. histolytica were collected and liKed with 4% paraformaldehyde/0.1M cacodylate buffier(pH 74), After washing them by centrifugation, 1% warm agar was added in the sediment. Solidified agar with the trophozoites was cut into $lmm^3$ cubes, and incubated in the various substrates to observe enzyme activities. Then, the specimen was post-fixed with 3% glutaraldehyde/0.1M cacodylate buffer (PH 7.4) and 1% osmium tetroBide/0.1M cacodylate buffier (pH 7.4) , dehydrated in ascending ethanol series and embedded in epoxy resin. These were sectioned on an ultramicrotome and observed with a transmission electronmicroscope. The procedures for the observation of the fine structure were same as the above, except for the incubation in the substrate. The sections were stained with uranyl acetate and lead citrate. For the observation of the surface of the amoebae, scanning-electronmicroscopy was carried out. The results obtained in the present study are summarized as follows: 1. The fuzzy coat around double-layered plasma membrane of 5. histolytica was more irregularly and densely distributed in the conventional strains (YS-27, YS-49 strains) than in the axonic strain (HK-9 strain). 2. The endosomes, button bodies and chromatin material were surrounded by a double-layered nuclear membrane having scattered nuclear fores. The paranuclear body, mono- or double-layered vacuoles, vacuolar membrane whorls, rosette-like cylindrical bodies, aggregation of cylindrical bodies and helical bodies were found in the cytoplasm of the amoebae. Helical bodies and glycogen granules were generally abundant, while a few smooth endoplasmic reticula were observed in the cytoplasm. 3. Alkaline phosphatase activity was mainly demonstrated in the plasma membrane, limiting membranes of vacuoles and smooth endoplasmic reticula. ATPase activity was observed in the nucleus, limiting membranes of vacuoles and vacuolar membrane whorls. 4. Acid phosphatase activity was commonly demonstrated in the limiting membranes an contents of vacuoles, Iysosome-like organelles, plasma membrane and the button bodies in the nucleus. The activity was more weakly demonstrated in the HK-9 strain than in the other conventional strains of 5. histolytica. No peroBidase activity was observed in the amoeba strains employed in the present study. 5. With a scanning electron-microscope, no distinct structural differences were observed between the amoeba strains. All the trophozoite forms of the amoebae showed crater-like depressions and rugged features on the outer surface.

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