• 제목/요약/키워드: cyclic act

검색결과 55건 처리시간 0.022초

담즙분비와 Cyclic nucleotides간의 상호관계에 관한 연구 (Study on the Relationship between Biliary Secretion and Cyclic Nucleotides)

  • 이향우;김원준;홍사석;조석준;홍사오;임중기
    • 대한약리학회지
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    • 제18권1호
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    • pp.43-54
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    • 1982
  • Bile formation is a complex process comprised of three separate physiologic mechanism operating at two anatomical sites. At present time, it was known that at least two processes are responsible for total canalicular secretion at the bile canaliculus. One of the processes is bile salt-dependent secretion (BSDS) hypothesis that the active transport of bile salts from plasma to bile provided a primary stimulus for bile formation: the osmotic effect of actively transported bile acid was responsible for the movement of water and ions into bile. The other process is bile salt-independent secretion (ESIS), which is unrelated to bile salt secretion at the canaliculus and which may involve the active transport of sodium. The third process for bile formation involves the biliary ductal epithelium. Secretin-stimulated bile characteristically contained bicarbonate in high concentration. Therefor, it was suggested that secretin stimulated water and bicarbonate secretion from the biliary ductules. One the other hand, it was found that a large amounts of cAMP was present in canine bile but no apparent relationship between bile salt secretion and cAMP content in dog bile. However, bile flow studies in human have demonstrated that secretin and glucagon increase bile cAMP secretion as does secretin in baboons. Secretin increases baboon bile duct mucosal cAMP levels in addition to bile CAMP levels suggesting that in that species secretin-stimulated bile flow may be cAMP mediated. It has been postulated that glucagon and theophylline which increase the bile salt-independent secretion in dogs might act through an increased in liver cAMP content. In a few studies, the possible role of cAMP on bile formation has teen tested by administration of an exogenous derivative of cAMP, dibutyryl cAMP. In the rat, DB cAMP did not modify bile flow, but injection of DB cAMP in the dog promoted an increase in the bile salt-independent secretion. Because of these contradictory results, this study was carried out to examine the relationship between cyclic nucleotides and bile flow due to various bile salts as well as secretin or theophylline. Experiments were performed in rabbits with anesthesia produced by the injection of seconal(30 mg/kg). Rabbits had the cystic duct ligated and the proximal end of the divided common duct cannulated with an appropriately sized polyethylene catheter. A similar catheter was placed into the inferior vena cava for administration of drugs. Bile was collected for determination of cyclic nucleotides and total cholate in 15 min. intervals for a few hours. The results are summerized as followings. 1) Administrations of taurocholic acid or chenodeoxycholic acid increased significantly the concentrations of cAMP and cGMP in bile of rabbits. 2) Concentration of cAMP in bile during the continuous infusion of ursodeoxycholic acid, was remarkedly increased in accordance with the increase of bile flow, while on the contrary concentration of cGMP in bile was decreased significantly. 3) Dehydrocholic acid and deoxycholic acid significantly increased bile flow, total cholate output and cyclic nucleotides in bile. 4) Only cAMP concentration in bile was significantly increased from control value by secretin, while theophylline increased cAMP as well as cGMP in rabbit bile. 5) In addition, the administration of secretin to taurocholic acid-stimulated bile flow increased cAMP while theophylline produced the increases of cAMP and cGMP in bile. 6) The administration of insulin to taurocholic acid-stimulated bile flow decreased cAMP concentration, while on the contrary cGMP was remarkedly increased in rabbit bile.

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콜라겐-유도의 혈소판에서 사이클릭 뉴클레오티드의 조절을 통한 Artemether의 항혈전 효과 (Inhibitory effects of artemether on thrombus formation via regulation of cyclic nucleotides in collagen-induced platelets)

  • 박창은;이동하
    • Journal of Applied Biological Chemistry
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    • 제65권4호
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    • pp.239-245
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    • 2022
  • 지혈이 일어나는 과정에서 혈소판의 정상적인 활성화가 중요하지만, 혈소판의 과도하거나 비정상적인 활성화는 뇌졸중, 죽상동맥 경화증 및 혈전증과 같은 심혈관 질환을 유발할 수 있다. 따라서, 혈소판 활성화를 조절하거나 억제할 수 있는 새로운 물질의 발견은 심혈관 질환의 예방 및 치료에 도움이 될 수 있다. Artemether는 Artemisia annua의 유효성분으로 알려진 artemisinin의 유도체로서 말라리아 치료에 효과적이라고 보고된 바 있고, 항산화 및 대사 효소 억제를 통해 기능하는 것으로 알려져 있다. 그런데, 혈소판 활성화 및 응집에 있어서의 artemether의 역할과 collagen으로 유도한 사람 혈소판에서 artemether의 작용기전은 현재까지 알려진 바가 없다. 본 연구는 artemether가 collagen에 의해 유도된 혈소판 활성화와 혈전 형성에 어떤 영향을 미치는 지 연구하였다. 그 결과, cAMP level이 artemether에 의해 유의하게 증가되었고, cAMP-의존성 kinase의 기질인 VASP 및 IP3R이 인산화되었다. Artemether에 의한 IP3R 인산화는 세포질 내로의 Ca2+ 동원을 억제하였고, 인산화된 VASP는 혈소판 막에 위치한 αIIb/β3 불활성화를 일으켜 fibrinogen 결합을 억제하였다. 결과적으로, artemether는 thrombin으로 유도한 fibrin clot의 형성을 억제하였다. 따라서, 우리는 artemether가 과도한 혈소판 활성화 및 혈전 형성으로 인한 심혈관 질환의 효과적인 예방 및 치료제로 작용할 수 있음을 제안한다.

Seismic performance of high-strength steel framed-tube structures with bolted web-connected replaceable shear links

  • Lian, Ming;Cheng, Qianqian;Guan, Binlin;Zhang, Hao;Su, Mingzhou
    • Steel and Composite Structures
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    • 제37권3호
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    • pp.323-339
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    • 2020
  • In steel framed-tube structures (SFTSs), the plastic hinges at beam-ends cannot be adequately improved because of the large cross sections of spandrel beams, which results in the lower ductility and energy dissipation capacities of traditional SFTSs. To address this drawback, high-strength steel fabricated SFTSs with bolted web-connected replaceable shear links (HSFTS-SLs) have been proposed. In this system, shear links use conventional steel and are placed in the middle of the deep spandrel beams to act as energy dissipative components. In this study, 2/3-scaled HSFTS-SL specimens were fabricated, and cyclic loading tests were carried out to study the seismic performance of both specimens. The finite element models (FEMs) of the two specimens were established and the numerical results were compared with the test results. The results showed that the specimens had good ductility and energy dissipation capacities due to the reliable deformation capacities. The specimens presented the expected failure modes. Using a shorter shear link can provide a higher load-carrying capacity and initial elastic lateral stiffness but induces lower ductility and energy dissipation capacity in HSFTS-SLs. The performance of the specimens was comparable to that of the original sub-structure specimens after replacing shear links. Additionally, the expected post-earthquake recoverability and resilience of the structures could be achieved by replacing shear links. The acceptable residual interstory drift that allows for easy replacement of the bolted web-connected shear link was 0.23%. The bolted web-connected shear links had reliable hysteretic responses and deformation capacities. The connection rotation had a notable contribution to total link rotation. The results of the numerical analysis run for the proposed FEMs were consistent with the test results. It showed that the proposed FEMs could be used to investigate the seismic performance of the HSFTS-SL.

Differential role of endothelium in hawthorn fruit extract-induced relaxation of rat cerebral, coronary, carotid, and aorta

  • Chan, Hoi Yun;Chen, Zhen-Yu;Yao, Xiaoqiang;Lau, Chi-Wai;Zhang, ZeSeng;Ho, Walter Kwok Keung;Huang, Yu
    • Advances in Traditional Medicine
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    • 제2권2호
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    • pp.87-93
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    • 2002
  • The present study was aimed to examine the role of endothelium in the relaxant effect of hawthorn fruit extract of Crataegus pinnatifida in four different types of rat arteries, posterior cerebral communicating artery, right descending coronary artery, common carotid artery, and aorta. In $9,11-dideoxy-11{\alpha}$, $9{\alpha}-epoxy-methanoprostaglandin$ $F_{2{\alpha}}$ (U46619)-preconstricted arterial rings except for aorta, the extract produced endothelium-independent relaxations with similar potency. This relaxation was unaffected by pretreatment with $100\;{\mu}M\;N^G-nitro-L-arginine$ methylester (L-NAME, the nitric oxide synthase inhibitor), $3\;{\mu}M$ 1H-[l,2,4]oxadiazolo$[4,2-{\alpha}]$quinoxalin-1-one (ODQ, the guanylate cyclase inhibitor), or $10\;{\mu}M$ indomethacin (the cyclooxygenase inhibitor). Putative $K^+$ channel blockers (charybdotoxin plus apamin or glibenclamide) did not affect the extract-induced relaxation in cerebral or coronary artery rings. In contrast, in rat aortic rings the extract produced significantly smaller relaxant response in endothelium-denuded rings than that in endothelium-intact rings. Pretreatment with L-NAME or ODQ abolished the extractinduced endothelium-dependent aortic relaxation, whilst indomethacin $(3\;{\mu}M)$ had no effect. The present results indicate that hawthorn fruit extract possesses a vasorelaxing effect in cerebral, coronary and carotid arteries and this effect is independent of the presence of a functional endothelium. However, the extract-induced endothelium-dependent relaxation in rat aorta was mediated through endothelial nitric oxide and cyclic GMP-dependent mechanisms, suggesting that active components in the extract may act on endothelium to stimulate release of nitric oxide in large conduit arteries of the rats.

흰쥐 대동맥 수축에 대한 xylamine의 억제효과 (Inhibitory effects of xylamine on the arterial contraction in rats)

  • 김상진;강형섭;김진상
    • 대한수의학회지
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    • 제44권3호
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    • pp.389-397
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    • 2004
  • The therapeutic efficacy of xylamine in the field of psychological medicine has been recognized for years and the drug is used to treat depression and some other conditions, but little is known about its mechanism of action on vascular system. Therefore, the present study was designed to investigate the influence of xylamine on the contractile responses of isolated rat thoracic arteries to phenylephrine(PE) and potassium chloride(KCl). Xylamine produced a concentration-dependent relaxation in PE-precontracted endothelium intact(+E) rat aortic rings, but not in a KCl-precontracted aortic rings. Also, xylamine inhibited the PE-induced contraction in concentration-dependent manner, but not in the high KCl-induced contraction in +E rings. This concentration-dependent inhibition was suppressed by the removal of the endothelium (-E). The inhibitory effects of xylamine($0.3{\mu}M$) on the PE-induced contractions were suppressed by N(G)-nitro-L-arginine(L-NNA), N(omega)-nitro-L-arginine methyl ester(L-NAME), aminoguanidine, dexamethasone, methylene blue, 1H-[1,2,4]oxadiazolo [4,3-a]quinoxalin-1-one(ODQ), indomethacin, ryanodine, tetrabutylammonium(TBA), lidocaine, procaine and 0 mM extracellular $Na^+$, but not by 2-nitro-4-carboxyphenyl-n,n-diphenylcarbamate(NCDC), lithium, nifedipine, verapamil, 0 mM extracellular $Ca^{2+}$, glibenclamide and clotrimazole. These findings suggest that xylamine could act as a vasorelaxant and direct inhibitor of arterial contraction. This vasorelaxation involves an endothelial nitric oxide (NO)/cGMP (guanosine 3',5'-cyclic monophosphate) pathway or cyclooxygenase system, and an interference with $Ca^{2+}$ release, TBA-sensitive $Ca^{2+}$-activated $K^+$ channels and $Na^+$$ channels.

Interaction of the Lysophospholipase PNPLA7 with Lipid Droplets through the Catalytic Region

  • Chang, Pingan;Sun, Tengteng;Heier, Christoph;Gao, Hao;Xu, Hongmei;Huang, Feifei
    • Molecules and Cells
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    • 제43권3호
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    • pp.286-297
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    • 2020
  • Mammalian patatin-like phospholipase domain containing proteins (PNPLAs) play critical roles in triglyceride hydrolysis, phospholipids metabolism, and lipid droplet (LD) homeostasis. PNPLA7 is a lysophosphatidylcholine hydrolase anchored on the endoplasmic reticulum which associates with LDs through its catalytic region (PNPLA7-C) in response to increased cyclic nucleotide levels. However, the interaction of PNPLA7 with LDs through its catalytic region is unknown. Herein, we demonstrate that PNPLA7-C localizes to the mature LDs ex vivo and also colocalizes with pre-existing LDs. Localization of PNPLA7-C with LDs induces LDs clustering via non-enzymatic intermolecular associations, while PNPLA7 alone does not induce LD clustering. Residues 742-1016 contains four putative transmembrane domains which act as a LD targeting motif and are required for the localization of PNPLA7-C to LDs. Furthermore, the N-terminal flanking region of the LD targeting motif, residues 681-741, contributes to the LD targeting, whereas the C-terminal flanking region (1169-1326) has an anti-LD targeting effect. Interestingly, the LD targeting motif does not exhibit lysophosphatidylcholine hydrolase activity even though it associates with LDs phospholipid membranes. These findings characterize the specific functional domains of PNPLA7 mediating subcellular positioning and interactions with LDs, as wells as providing critical insights into the structure of this evolutionarily conserved phospholipid-metabolizing enzyme family.

Future drought assessment in the Nakdong basin in Korea under climate change impacts

  • 김광섭;노반콴
    • 한국수자원학회:학술대회논문집
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    • 한국수자원학회 2012년도 학술발표회
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    • pp.458-458
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    • 2012
  • Climate extreme variability is a major cause of disaster such as flood and drought types occurred in Korea and its effects is also more severe damage in last decades which can be danger mature events in the future. The main aim of this study was to assess the effectives of climate change on drought for an agriculture as Nakdong basin in Korea using climate change data in the future from data of General Circulation Models (GCM) of ECHO-G, with the developing countries like Korea, the developed climate scenario of medium-high greenhouse gas emission was proposed of the SRES A2. The Standardized Precipitation Index (SPI) was applied for drought evaluation. The drought index (SPI) applied for sites in catchment and it is evaluated accordingly by current and future precipitation data, specific as determined for data from nine precipitation stations with data covering the period 1980-2009 for current and three periods 2010-2039, 2040-2069 and 2070-2099 for future; time scales of 3month were used for evaluating. The results determined drought duration, magnitude and spatial extent. The drought in catchment act intensively occurred in March, April, May and November and months of drought extreme often appeared annual in May and November; drought frequent is a non-uniform cyclic pattern in an irregular repetitive manner, but results showed drought intensity increasing in future periods. The results indicated also spatial point of view, the SPI analysis showed two of drought extents; local drought acting on one or more one of sites and entire drought as cover all of site in catchment. In addition, the meteorology drought simulation maps of spatial drought representation were carried out with GIS software to generate for some drought extreme years in study area. The method applied in this study are expected to be appropriately applicable to the evaluation of the effects of extreme hydrologic events, the results also provide useful for the drought warning and sustainable water resources management strategies and policy in agriculture basins.

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Determination of tyrosinase inhibitory activity and betanin content changes in beetroot (Beta vulgaris) extracts fermented by EM

  • Yoo, Jong Hee;Kim, Hyun Ki;Yoon, Tae Wou;Mekapogu, Manjulatha;Ahn, Myung Suk;Kwon, Oh Keun;Bang, Keuk Soo;Kim, Yong Ju
    • 한국자원식물학회:학술대회논문집
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    • 한국자원식물학회 2019년도 춘계학술대회
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    • pp.110-110
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    • 2019
  • Beet (Beta vulgaris) is a crop similar to sugar beet, chard and leaf beets, and its origin is the Mediterranean coast of southern Europe and Central Asia. Among the components contained in beet, betalain, the main component of the root, has been reported to prevent lipid peroxidation induced by active oxygen and free radicals due to its high radical scavenging ability. Among these, the betalain, betanin (Betanidin 5-O-${\beta}$-glucoside) contains both phenolic and cyclic amine groups, all of which are highly electron-donating and act as antioxidants and has tyrosinase inhibitory activity. Betanin accounts for about 75-95% of the total pigment found in the beet. EM stands for effective microorganisms and is a collection of beneficial microorganisms. EM includes yeast, lactic acid bacteria, mycelia, photosynthetic bacteria, actinomycetes, etc. Human patch test according to CTFA guidelines was observed to be a safe source of no stimulation when 5% (v/v) of the EM fermentation liquid was applied to the human body. In addition, beneficial microorganisms are synergistic in the process of co-existence and cultivation and it has the effect of increasing antioxidant capacity and inhibiting corruption. This study confirms the difference in tyrosinase inhibitory activity and betanin content of beetroot extracts and EM fermented beetroot extracts. Hence, these results confirm that EM fermented beetroot extracts are highly beneficial for the human body.

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토목섬유-정규압밀점토의 접촉면 동적 전단거동 평가 (Dynamic Shear Behaviors on the Normally Consolidation Clay-Geosynthetic Interface)

  • 배효곤;장동인;곽창원;박인준
    • 한국지반환경공학회 논문집
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    • 제19권12호
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    • pp.33-39
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    • 2018
  • 본 연구에서는 토목섬유-점토의 접촉면 압밀 전단거동 평가를 위하여 상재하중 및 해수와 담수를 이용해 토목섬유-점토의 경계면에 대한 중요 특성인자를 규명하였다. 또한 폐기물 매립으로 바다에 매립공간을 확보하고 폐기물 처리 및 향후 토지이용 등 새롭게 필요 공간으로 변모가 가능하다. 토목섬유-점토의 접촉면에 거동특성을 분석한 결과 표준 압밀시험기를 이용하여 분석한 경우 해수보다 담수에서 압밀응력이 크게 증가하는 경향을 보였고, 동적 접촉면 전단 시험기를 이용하여 분석한 경우 해수와 담수 두 개의 조건에서 모두 동일하게 하부모듈에 가까운 와이어게이지일수록 변위값이 증가하고, 담수보다 해수의 조건에서 전단파괴가 급격히 일어나는 경향을 볼 수 있다. 따라서 토목섬유-점토의 접촉면에 작용하는 해수와 담수, 차수시설 설치여부(토목섬유)는 차수 시설 동적설계인자에 반드시 필요한 중요 변수로써 고려하여야 한다.

Portable Amperometric Glucose Detection based on NiS/CuS Nanorods Integrated with a Smartphone Device

  • Heyu Zhao;Kaige Qu;Haoyong Yin;Ling Wang;Yifan Zheng;Shumin Zhao;Shengji Wu
    • Journal of Electrochemical Science and Technology
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    • 제14권3호
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    • pp.252-261
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    • 2023
  • Glucose detection is particularly important for clinical diagnosis and personal prevention and control. Herein, the smartphone-based amperometric glucose sensors were constructed using the NiS/CuS nanorods (NRs) as sensing electrodes. The NiS/CuS NRs were prepared through a facile hydrothermal process accompanied by the subsequent vulcanization treatment. The morphological and structural properties of NiS/CuS NRs were characterized with SEM, EDS, XRD, and XPS. Electrochemical measurements including cyclic voltammetry, chronoamperometry, and electrochemical impedance spectroscopy display that NiS/CuS NRs can act as highly efficient electrocatalyst for glucose detection. The NiS/CuS NRs electrodes present a wide detection range of 1-8000 µM for glucose sensing with the sensitivity of 956.38 µA·mM-1·cm-2. The detection limit was 0.35 µM (S/N=3). When employed in smartphone-based glucose sensing device, they also display a high sensitivity of 738.09 µA·mM-1·cm-2 and low detection limit of 1.67 µM. Moreover, the smartphone-based glucose sensing device also presents favorable feasibility in determination of glucose in serum samples with the recoveries ranging between 99.5 and 105.8%. The results may provide a promising viewpoint to design other new portable glucose sensors.