• Title/Summary/Keyword: and receptors

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Anisomycin, an Inhibitor of Protein Synthesis, Overcomes TRAIL Resistance in Human Hepatocarcinoma Cells via Caspases Activation and Bid Downregulation (Caspase 활성 및 Bid의 발현 저하를 통한 단백질 생성 억제제인 anisomycin의 인체간암세포에서 TRAIL 매개 apoptosis 유발의 활성화)

  • Jin, Cheng-Yun;Park, Cheol;Hong, Su Hyun;Choi, Yung Hyun
    • Journal of Life Science
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    • v.24 no.7
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    • pp.769-776
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    • 2014
  • Anisomycin, also known as flagecidin, is an antibiotic produced by Streptomyces griseolus that inhibits protein synthesis by binding to the ribosomal 28S subunit. The tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) is a protein that induces apoptotic cell death. TRAIL primarily causes apoptosis in tumor cells by binding to death receptors. Many human cancer cell lines are refractory to TRAIL-induced cell death. In this study, we investigated whether anisomycin could enhance TRAIL-mediated apoptosis in TRAIL-resistant human hepatocarcinoma Hep3B cells. Treatment with anisomycin and TRAIL alone did not reduce cell viability in Hep3B cells. However, in the presence of TRAIL, the anisomycin concentration dependently reduced the cell viability. Our results indicate that anisomycin sensitizes Hep3B cells to TRAIL-mediated apoptosis and that this occurs, at least partly, via caspase activation. Interestingly, Bid knockdown by small interfering RNA significantly reduced the induction of apoptosis in combination with anisomycin and TRAIL, indicating that anisomycin effectively acts to lower the threshold at which TRAIL-mediated truncated Bid triggers the mitochondrial-mediated apoptosis program in Hep3B cells. Therefore, the use of TRAIL in combination with anisomycin might provide an effective therapeutic strategy for the safe treatment of some TRAIL-resistant cancer cells.

Prolactin Response to Cimetidine in the Schizophrenics - In Unmedicated Male Positive and Negative Patients - (정신분열증 환자에서 Cimetidine에 의한 Prolactin 분비 반응 - 양성 및 음성 아형 남자 환자에서 -)

  • Jin, Hyuk Hee;Kwon, Young Joon;Jeong, Hee Yeon;Han, Sun Ho
    • Korean Journal of Biological Psychiatry
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    • v.3 no.1
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    • pp.121-126
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    • 1996
  • Objects : There is considerable interest in the role of serotonin(5-HT) in the pathophysiology of schizophrenia. Cimetidine, $H_2$ antagonist, produces transient increase in serum prolactin(PRL) levels by indirect serotonergic mechanism in man following intravenous administration. Therefore the authors investigated the effects of cimetidine on serum PRL levels of male unmedicated schizophrenics. Method : Baseline serum prolactin level and psychopathology were measured at 9:00 AM. in the two groups(12 positive schizophrenics, 7 negative schizophrenics) and $T_{30}$ levels were measured 30 minutes after intravenous injection of cimetidine (ie, 9:30 AM) Results: 1) Baseline prolactin levels were not different in the three groups. 2) Prolactin levels of 30 minutes after intravenous injection of cimetidine($T_{30}$) compared with baseline prolactin levels were increased all in the three groups. 3) Degrees of interval change from baseline to $T_{30}$ were significantly different between normal control and negative schizophrenics(p<0.05). Conclusion : The prolactin response to cimetidine was significantly blunted in negative male schizophrenics than normal control. These data are consistent with the hypothesis of an abnormality of serotonergic activity, including down-regulation $5-HT_2$ receptors, in male negative schizophrenics.

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Reevaluation of the Effect of Phenobarbital on the Response to Pain in Rat (백서에서 동통에 미치는 Phenobarbital 효과의 재평가)

  • So, Byoung-Gyoum;Kim, Kee-Won;Ko, Myoung-Kyu;Yang, Won-Mo;Cho, Kyu-Park
    • The Korean Journal of Pharmacology
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    • v.22 no.2
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    • pp.88-95
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    • 1986
  • Clinically, subhypnotic doses of barbiturates have been known to elicit hyperalgesia. In this experiment, effect of acute or chronic phenobarital treatment on the response to pain in rat was reevaluated by hot-plate method. To elucidate its mechanism, changes of ${\beta}-endorphin$ contents and [3H]-morphine binding of the rat midbrain as well as functional opiate receptor in vas deferens were also measured. Intraperitoneal injection of sub anesthetic dose phenobarbital induced initial hyperalgesia followed by successive analgesia, while chronic phenobarbital-treatment decreased reactivity to pain. Naloxone (10mg/kg, i.p.) markedly shortened hot plate latency period, and significantly inhibited the analgesic action of phenobarbital. Single dose of phenobarbital did not affect ${\beta}-endorphin$ contents and [3H]-morphine binding in rat mid brain, but in the chronic phenobarbital-treated groups, ${\beta}-endorphin$ contents was increased, while Bmax of opiate receptor binding was decreased. Moreover, very significant correlations among responses to pain, changes of ${\beta}-endorphin$ contents and opiate receptor binding were observed. However, Kd values of opiate receptor bindings were not changed in all preparations. In the chronic phenobarbital-treated vas deferens preparations, ID50 of morphine was increased witb concomittant decrease of maximum effect. But $pA_2 $, value for naloxone was not changed. From these results, it is suggested that phenobarbital can produce analgesia due to changes of ${\beta}-endorphin$ contents as well as functional opiate receptors by receptor regulation.

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Expression Study of The Mouse Collectin-Placenta 1 Gene (마우스 Collectin-Placenta 1 유전자의 발현 연구)

  • Kim, Geun Ho;Kim, Youn Uck
    • Journal of the Korea Academia-Industrial cooperation Society
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    • v.20 no.8
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    • pp.477-484
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    • 2019
  • Several types of scavenger receptors, including the Collectin-Placenta 1 (CL-P1) receptorthat is present in mammals, are molecules that are expressed on the surfaces of endothelial cells, macrophages and smooth muscle cells. These molecules are cell surface glycoproteins that can be conjugated to oxidized low density lipoprotein (oxLDL). Among these molecules, the effect of quercetin on CL-P1 activation has been confirmed. Quercetin is known as an antioxidant that stops oxidation because it acts to remove free radicals that are responsible for the oxidation reaction. In this study, fragments from the transcription start site of the mouse CL-P1 gene promoter to the -500th base were cloned using DNA polymerase. These fragments were then introduced into macrophage like RAW264.7 cells and fibroblast-like NIH3T3 cells to study the effect of quercetin on the CL-P1 gene expression. As a result, we found that bases ranging from -250 to -350 in the anterior part where gene expression starts are important for producing CL-P1 protein. Among them, the DNA mutation experiments we performed confirmed that the E2F binding sites are critical for producing the CL-P1 protein? In addition, when quercetin was added to the RAW264.7 culture medium, which was a culture of adherent cells, observedthe phenomenon of the cells falling off from the surface of the culture container.

Inhibitory Effect of Purified Bee Venom(Apis mellifera L.) on Adipogenesis in Korea (국내 양봉농가에서 채취한 정제봉독(Apis mellifera L.)의 지방세포 분화 억제 효과)

  • Han, Sang Mi;Kim, Hyo Young;Woo, Soon Ok;Kim, Se Gun;Choi, Hong Min;Moon, Hyo Jung
    • Journal of Apiculture
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    • v.35 no.1
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    • pp.49-54
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    • 2020
  • Bee (Apis mellifera L.) venom is used for the treatment of various human diseases due to its known anti-inflammatory and antibacterial properties. This study investigated the effect of purified bee venom (PBV) on adipogenesis in 3T3-L1 preadipocytes. There was no cytotoxicity while cells were treated with PBV by various concentrations. In the PBV treated cells increases in fat storage were inhibited and also confirmed by oil red o staining. To understand the underlying mechanism at the molecular level were examined on the expression of the genes involved in adipogenesis by using real-time PCR. In this cell model, the mRNA level of adipogenic genes such as peroxisome-proliferator-activated receptors gamma (PPARγ) and CAAAT/enhancer binding protein alpha(C/EBPα) were decreased by PAE treatment, comparing with those of control group. Theses results suggest that PBV inhibits adipocyte differentiation in 3T3-L1 cells and can be used as an efficient natural substance to manage anti-obesity.

Corni Fructus Inhibits Wrinkle Formation by Reduced Advanced glycation end product (AGEs) (산수유의 최종당화산물 억제로 인한 주름 개선효과)

  • Lee, AhReum;Kim, SooHyun;Kim, SuJi;Kim, KyeongJo;Kwon, Ojun;Choi, JoonYoung;Roh, Seong-Soo
    • The Korea Journal of Herbology
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    • v.32 no.5
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    • pp.1-6
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    • 2017
  • Objectives : Corni Fructus (CF) is traditional herbal medicine used on polyuria, low back pain, and tinnitus. This study aimed to evaluate inhibits skin wrinkle formation effect of CF. Methods : To evaluate the produce inhibition effect of CF, SD-rats were distributed into four groups; normal rats (Nor), AGEs (advenced glycation end product)-induced rats (Con), AGEs-induced rats treated with 100mg/kg CF (CF). To induce AGEs, streptozotocin (50mg/kg) was administered intraperitoneally and after 3 days oral administrated 100mM methyl glyoxal for 3 weeks. Results : The oral administration of CF suppressed the reactive oxygen specis (ROS) in serum. The AGEs in skin tissues was significantly reduced through treatment of CF. Furthermore, the expressions of AGEs related proteins such as polyclonal anti-$N^e$-(carboxymethyl)lysine (CML), anti-$N^e$-(carboxyethyl)lysine (CEL), AGE receptors (RAGE) were decreased in CF treated group compared with the control group in skin tissues. Inflammation-related proteins such as Nuclear factor kappa-light-chain-enhancer of activated B cells (NF-kB), monocyte chemoattractant protein-1 (MCP-1), interleukin-6 (IL-6) reduced in CF treatment group than control group. AGE-induced rats exhibited that the significant decreased collagen however, CF treatment (100mg/kg of body weight) up regulated collagen by improved the expression levels of skin fibril-related genes such as Matrix metalloproteinase (MMP-1). Conclusion : Taken together, our study suggests that CF regulates ROS to prevent accumulation of AGEs and inhibits skin wrinkles. Our finding indicate that CF may be an effective agent for inhibits AGEs formation, and improved skin wrinkle.

Tight junctional inhibition of entry of Toxoplasma gondii into MDCK cells (MDCK세포의 tight junction 형성이 Toxoplusmu gondii의 숙주세포 침투에 미치는 효과)

  • 남호우;윤지혜
    • Parasites, Hosts and Diseases
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    • v.28 no.4
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    • pp.197-206
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    • 1990
  • Various conditions of cultures were performed to investigate the role of tight junctions formed between adjacent MDCK cells on the entry of Toxoplasma. When MDCK cells were cocultured with excess number of Toxoplasma at the seeding density of 1×105, 3×105, and 5×105 cells/ml for 4 days, the number of intracellular parasites decreased rapidly as the host cells reached saturation density, i.e., the formation of tight junctions. When the concentration of calcium in the media (1.8 mM in general) was shifted to $5{\mu}M$ that resulted in the elimination of tight junction, the penetration of Toxoplasma increased about 2-fold(p<0.05) in the saturated culture, while that of non-saturated culture decreased by half. Trypsin-EDTA which was treated to conquer the tight junctions of saturated culture favored the entry of Toxoplasma about 2.5-fold(P<0.05) compared to the non-treated, while that of non- saturated culture decreased to about one fifth. It was suggested that the tight junctions of epithelial cells play a role as a barrier for the entry of Toxoplasma and Toxoplasma penetrate into hoot cells through membrane structure-specific, i.e., certain kind of receptors present on the basolateral rather than apical surface of MDCK cells.

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Cardiovascular Responses over the Time Course during Muscle Group III Stimulation in Prehypertensive Individuals (고혈압 전단계자들에 대한 골격근 Group III 자극 시 시간에 따른 심혈관 반응)

  • Park, Won-Il;Park, Si-Young;Choi, Hyun-Min;Lee, Joon-Hee;Jeon, Jong-Mok;Kim, Jong-Kyung;Shim, Jae-Kun;Nho, Ho-Sung
    • Journal of Life Science
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    • v.19 no.11
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    • pp.1568-1574
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    • 2009
  • The purpose of this study was to investigate whether group III muscle afferents play an important role eliciting abnormal blood pressure response mediated during passive muscle stretch in prehypertensive individuals. Eleven middle-aged prehypertensive men (average BP 133/80 mmHg) and nine middle-aged normotensive men (average BP 119/74 mmHg) participated in this study. After 1 min rest baseline data collection, the subject's foot was flexed (dorsiflexion) by an automated cybex for one minute. Systolic blood pressure (SBP), diastolic blood pressure (DBP), mean arterial blood pressure (MAP), heart rate, stroke volume, cardiac output, and total peripheral resistance were continuously measured on a beat-by-beat basis from a finger via a Finapres device for 1 minute. To evaluate the role of mechanoreflex, a component of exercise pressor reflex, SBP, DBP, and MAP responses over the course of time were examined. The results showed that the pressor response mediated by the muscle mechanoreflex was faster in prehypertensive individuals compared to the normotensive individuals. The substantial pressor response was observed within mean 20 sec of the onset of passive stretch in prehypertension, while mean 45 sec in normotension (p<0.05). It is concluded that excessive pressor response produced during exercise in prehypertension may be due to the dysfunction of the mechano-receptors.

Studies on Secretion of Catecholamines Evoked by Panaxadiol in the Isolated Rabbit Adrenal Gland (파낙스디올의 가토적출부신의 카테콜아민분비 작용에 관한 연구)

  • Lim Dong Yoon;Park Kyu Baik;Kim Kyu Hyung;Choi Cheol Hee;Cha Jong Hee
    • Proceedings of the Ginseng society Conference
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    • 1988.08a
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    • pp.55-62
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    • 1988
  • The effect of panaxadiol (PD). an active component of Korean ginseng saponins on the secretion of catecholamines (CA) from the rabbit adrenal gland and its mode of action were investigated. PD ($400\;{\mu}g$) increased significantly the secretion of CA from the isolated perfused rabbit adrenal gland. PD-induced secretion of CA was reduced markedly by treatment with atropine. CA secretion induced by Ach or PD was potentiated by physostigmine treatment. Chlorisondamine inhibited CA secretion of PD or Ach. Perfusion of PD ($400\;{\mu}g$) for 30 minutes enhanced the secretory activity of CA by Ach. Ouabain weakened the secretory rsponse caused by PD but enhanced the response by Ach. Adenosine treatment resulted in marked increase in CA secretion by PD or Ach. Perfusion with calcium free Krebs solution containing 5 mM EDTA for 30 minutes completely blocked the secretory effect induced by Ach and also weakened that evoked by PD. It is suggested that PD causes the secretion of CA from the rabbit adrenal gland by a calcium dependent exocytotic process. The secretory effect of PD is due to the stimulation of cholinergic muscarinic and nicotinic-receptors present in the adrenal gland partly by direct action on the chromaffin cell.

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Numerical Study on the Ozone Formation Sensitivity of Precursors Using Adjoint Model around the South-eastern Area of the Korean Peninsula (수반모형을 이용한 한반도 남동지역의 오존 전구물질의 오존 생성 민감도에 관한 수치연구)

  • Park, Soon-Young;Lee, Soon-Hwan;Lee, Hwa Woon;Kim, Dong-Hyeok
    • Journal of the Korean earth science society
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    • v.34 no.7
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    • pp.669-680
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    • 2013
  • Ozone sensitivity analysis with respect to $NO_x$ is conducted around the south-eastern area of the Korean Peninsula. WRF-CMAQ modeling system is used to simulate a local circulation and high ozone episode day. To analyze the sensitivity, the adjoint model for CMAQ is adopted in this study. The purpose of current study is to investigate the location that affects a day time ozone concentration of these receptors on the high ozone episode day. Adjoint sensitivity analysis for Daegu shows two areas of influence. One is the range from the neighboring location to Pohang and it affects mainly on the same day as receptor time. The other is the remote south-eastern area from Daegu. This remote influence area suggests that $NO_x$ emitted on the previous day can change the ozone concentration at receptor time. The influence area for Busan, on the other hand, is originated only from the emission on the previous day because the sea-breeze occurred on the episode day makes low influence of surrounding emission. The cross sectional analysis reveals that $NO_x$ advection is important not only near the surface of land but also around the height of boundary layer.