• Biomolecules & Therapeutics
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• v.24 no.2
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• pp.191-198
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• 2016

The vitamin D receptor (VDR) is a member of the nuclear receptor (NR) superfamily. The VDR binds to active vitamin $D_3$ metabolites, which stimulates downstream transduction signaling involved in various physiological activities such as calcium homeostasis, bone mineralization, and cell differentiation. Quercetin is a widely distributed flavonoid in nature that is known to enhance transactivation of VDR target genes. However, the detailed molecular mechanism underlying VDR activation by quercetin is not well understood. We first demonstrated the interaction between quercetin and the VDR at the molecular level by using fluorescence quenching and saturation transfer difference (STD) NMR experiments. The dissociation constant ($K_d$) of quercetin and the VDR was $21.15{\pm}4.31{\mu}M$, and the mapping of quercetin subsites for VDR binding was performed using STD-NMR. The binding mode of quercetin was investigated by a docking study combined with molecular dynamics (MD) simulation. Quercetin might serve as a scaffold for the development of VDR modulators with selective biological activities.

• Journal of Korean Society for Atmospheric Environment
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• v.22 no.2
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• pp.179-189
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• 2006

Ambient gas phase mercury concentrations including elemental mercury ($Hg^0$) were measured at the Potsdam, Stockton, and Sterling sites in NY from 2000 to 2003. Also, concentrations of ambient reactive gaseous mercury (RGM; $Hg^{2+}$) were measured at the Potsdam site during one year. The contribution of RGM($4.2{\pm}6.4pg/m^3$) was about $0.2{\sim}3%$ of the total gas phase mercury concentration measured (TGM: $1.84{\pm}1.24,\;1.83{\pm}0.32,\;3.02{\pm}2.14ng/m^3$ in Potsdam. Stockton, and Sterling, respectively) at the receptor sites. Potential Source Contribution Function (PSCF), a hybrid receptor modeling incorporating backward trajectories was performed to identify source areas of TGM. Using PSCF, southern New York, North Carolina, and eastern Massachusetts were identified as important source areas in the United States, while the copper smelters and waste incinerators located in eastern Quebec and Ontario were determined to be significant sources in Canada. The Atlantic Ocean was suggested to be a possible mercury source. PSCF incorporating back-dispersion and deposition was applied for RGM , as well as PSCF based on 2-days back-trajectories. Two different approaches yielded considerably different results, primarily due to the consideration of dispersion rather than deposition. Using back-trajectory based PSCF, eastern Ohio, southern New York, and southern Pennsylvania where large coal -fired power plants area located were identified as the large sources in US. Metallurgical industry located in eastern Quebec was resolved as well. From the result of back-dispersion and deposition based PSCF, Pennsylvania, mining facilities around Lake Superior, Toronto, Boston, MA, Quebec, and coal power plants in NY were identified to be the significant source areas for Potsdam site.

• The Korean Journal of Pharmacology
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• v.22 no.1 s.38
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• pp.24-33
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• 1986

To ascertain the existence of various adrenoceptors involved in active transport of sodium in the frog skin and to delineate their physiological roles, the influence of various adrenergic agonists and antagonists on the potential difference (PD), short-circuit current (SCC) and total skin conductance (TSC) of the isolated frog skin of Rana nigromaculata were investigated. PD and SCC were determined with Ussing's technique. Drugs were administered to the serosal side of the skin. Experimental results were summarized as follows: 1. The responses to norepinephrine (NE, $6{\times}10^{-8}-6{\times}10^{-5})M$), phenylephrine (PE, $5{\times}10^{-6}-5{\times}10^{-4}M$) and epinephrine (Epi, $5.5{\times}10^{-7}-5.5{\times}10^{-5}M$) were characterized by marked elevation of PD & SCC in dose-related fashion, but the maximal effect attained by Epi was less than those of NE and PE. 2. These increments of PD & SCC were significantly inhibited by prazosin $(2{\times}10^{-6}M)$, a speciflc ${\alpha}_1$-adrenoceptor blocker. The stimulatory effect on PD & SCC were completely abolished by phenoxybenzamine (PBZ, $3.3{\times}10^{-5}M$), an irreversible ${\alpha}$-adrenoceptor blocking agent. Furthermore, with a larger doses of Epi produced marked decline of PD & SCC after the PBZ pretreatment. 3. Isoproterenol (ISP), a ${\beta}$-adrenoceptor agonist, in concentrations ranging from $5{\times}10^{-7}$ to $5{\times}10^{-6}M$ produced dose-related decrease in PD & SCC, which could be abolished by pretreatment with propranolol $(4{\times}10^{-6}M)$, a specific ${\beta}$-adrenoceptor blocker. It was further noted that the effects of Epi on PD & SCC were markedly potentiated by Propranolol pretreatment. 4. Clonidine as well as guanabenz produced increases in PD & SCC and these effects were inhibited more specifically by prazosin pretreatment than by yohimbine. These results indicated that there exist in the frog skin two distinctive types of adrenoceptors, ${\alpha}$ and ${\beta}$, which roughly corresponds to those in mammals, and that the ${\alpha}$ type of adrenoceptors mediate the stimulation of PD & SCC, whereas ${\beta}$-adrenoceptors mediate the inhibition. However, based on evidence at hand, no conclusion could be drawn on the subtype of ${\alpha}$-adrenoceptors which is involved in the stimulation of sodium transport in the frog skin.

• The Korean Journal of Physiology and Pharmacology
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• v.1 no.1
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• pp.1-12
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• 1997

As it has been reported that the depolarization induced acetylcholine (ACh) release is modulated by activation of presynaptic $A_1$ adenosine heteroreceptor and various evidence suggest that indicate the $A_2$ adenosine receptor is present in the striatum, this study was undertaken to delineate the role of adenosine receptors on the striatal ACh release. Slices from the rat striatum were equilibrated with $[^3H]$choline and then the release amount of the labelled product, $[^3H]$ACh, which was evoked by electrical stimulation (rectangular pulses, 3 Hz, 2 ms, 24 mA, $5\;Vcm^{-1}$, 2 min), was measured, and the influence of various agents on the evoked tritium outflow was investigated. And also, quantitative receptor autoradiography and drug-receptor binding assay were performed in order to confirm the presence and characteristics of $A_1$ and $A_2$ adenosine receptors in the rat striatum. Adenosine $(10{sim}100\;{mu}M)$ and $N^6$-cyclopentyladenosine (CPA, $1{sim}100\;{mu}M)$ decreased the $[^3H]$ACh release in a dose-dependent manner without changing the basal rate of release in the rat striatum. The reducing effects of ACh release by adenosine and CPA were abolished by 8-cyclopentyl-1,3-dipropy-Ixanthine (DPCPX, 2 ${mu}M$), a selective $A_1$, adenosine receptor antagonist, treatment. The effect of adenosine was potentiated markedly by 3,7-dimethyl-1-propargylxanthine (DMPX, 10 ${mu}M$), a specific $A_2$ adenosine receptor antagonist. 2-P-(2-carboxyethyl)phenethylamimo-5'-N- ethylcarboxamidoadenosine hydrochloride (CGS-21680C), in concentrations ranging from 0.01 to 10 ${mu}M$, a recently introduced potent $A_2$ adenosine receptor agonist, increased the $[^3H]$ACh release in a dose related fashion without changing the basal rate of release. These effects were completely abolished by DMPX $(10\;{mu}M)$. In autoradiograrhy experiments, $[^3H]$2-chloro-$N^6$-cyclopentyladenosine ($[^3H]$ CCPA) bindings were highly localized in the hippocampus and the cerebral cortex. Additionally, lower levels of binding were found in the striatum. However, $[^3H]$CGS-21680C bindings were highly localized in the striatal region with the greatest density of binding found in the caudate nucleus and putamen. Lower levels of binding were also found in the nucleus accumbens and olfactory tubercle. In drug-receptor binding assay, binding of $[^3H]$ CCPA to $A_1$ adenosine receptors of rat striatal membranes was inhibited by CPA ($K_i$ = 1.6 nM) and N-ethylcarboxamidoadenosine (NECA, $K_i$ = 12.9 nM), but not by CGS-21680C ($K_i$ = 2609.2 nM) and DMPX ($K_i$ = 19,386 nM). In contrast, $[^3H]$CGS-21680C binding to $A_2$ denosine receptors was inhibited by CGS-21680C ($K_i$ = 47.6 nM) and NECA ($K_i$ = 44.9 nM), but not by CPA ($K_i$ = 2099.2 nM) and DPCPX ($K_i$ = 19,207 nM). The results presented here suggest that both types of $A_1$ and $A_2$ adenosine heteroreceptors exist and play an important role in ACh release in the rat striatal cholinergic neurons.

• Journal of Environmental Science International
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• v.12 no.2
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• pp.217-225
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• 2003

Samples of size-fractionated PM10 (airborne particulate matter with aerodynamic diameter less than $10\mu\textrm{m}$) were collected at an urban site in Jeju city from May to September 2002. The mass concentration and chemical composition of the samples were measured. The data sets were then applied to the CMB receptor model to estimate the source contribution of PM10 in Jeju area. The average PM10 mass concentration was 28.80$\mu\textrm{g}/m^3$ ($24.6~33.49\mu\textrm{g}/m^3$), and the FP (fine particle with aerodynamic diameter less than $2.l\mu\textrm{m}$ fraction in PM10 was approximately 8% higher than the CP (coarse particle with aerodynamic diameter greater than $2.l\mu\textrm{m}$ and less than $10\mu\textrm{m}$ fraction in PM10. The CP composition was obviously different from the FP composition, that is, the most abundant water soluble species was nitrate ion in the FP, but sulfate ion in the CP. Also sulfur was the most dominant element in the FP, however, sodium was that in the CP. From CMB receptor model results, it was found that road dust was the largest contributor to the CP mass concentration (45% of the CP) and ammonium nitrate, domestic boiler, and marine aerosol were major sources to the CP mass. However, the secondary aerosol was the most significant contributor to the FP mass concentration (45% of the FP). In this study, it was suggested that the contributions of soil dust and gasoline vehicle became very low due to collinearity with road dust and diesel vehicle, respectively.

• Journal of Community Nutrition
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• v.4 no.1
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• pp.3-11
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• 2002

The purpose of this study is to evaluate the iron nutritional status by investigating dietary intake and analyzing the hematological iron status indices including serum transferrin receptor (sTfR) in 8 to 28 month old infants md young children taking supplementary foods. The nutrient intake of 60 healthy infants and young children from 8 to 24 months of age was investigated by means of a 24-hour recall method, and the subjects were divided into 2 groups (8- 12 months and 13-28 months) according to age. Venous blood samples from these groups were collected and measured for the following : hemoglobin(Hb), hematocrit(Hct) , mean corpuscular volume (MCV), mean corpuscular hemoglobin, mean corpuscular hemoglobin concentration (MCHC), serum ferritin, serum iron, total iron binding capacity (TIBC), and sTfR. Anemia is defined as hemoglobin < 11g /dl , serum ferritin level < 10ng1m1 for iron deficiency , serum transferring receptor(sTfR) > 4.5mg / 1 for iron deficient erythropoiesis. Total daily calorie intake was 934.6 ${\pm}$ 284.5kcal (98.32% of RDA) on average. Average daily iron intake in infants aged 8 to 12 months was 8.92 ${\pm}$ 3.32mg. The mean daily iron intake in infants aged 13 to 28 months was 7.15 ${\pm}$ 3.35mg (90% of Recommended Dietary Allowance, RDA). Mean values for Hb, Hct sew ferritin and sTfR were 12.10 ${\pm}$ 0.77g141,36.02 ${\pm}$ 2.31%,20.91 ${\pm}$ 11.58ng/m1 and 3.78 ${\pm}$ 1.47mg /1, respectively. In the young children from 13 to 28 months of age, the prevalence of anemia was 5.6%. The prevalence of iron deficiency was 9.5% in those from 8 to 12 months of age, and 27.8% in those from 13 to 28 months of age. The prevalence of iron deficient erythropoiesis was 16.7% in infants aged 8 to 12 months and 44.4% in those aged 13 to 28 months. The prevalence of both serum ferritin level < 10ng/m1 sTfR > 4.5mg/1 was 22% in the young children aged 13 to 28 months. The measureand ment of sTfR may be a promising new tool in diagnosis of iron deficiency in early childhood when the iron deficiency is prevalent. It seems appropriate to emphasize nutritional education and evaluation to promote the iron nutritional status of infants and young children.

• Asian-Australasian Journal of Animal Sciences
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• v.28 no.8
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• pp.1187-1193
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• 2015

This study determined the effects of dietary restriction on growth and the expression of lipid metabolism and growth hormone signaling genes in the longissimus dorsi muscle (LM) of Korean cattle. Thirty-one Korean cattle steers (average age 10.5 months) were allocated to normal (N; n = 16) or dietary restriction (DR; n = 15) groups. The feeding trial consisted of two stages: for the 8-month growing period, the DR group was fed 80% of the food intake of the normal diet, and for the 6-month growth-finishing period, the DR group was fed a DR total mixed ration with 78.4% of the crude protein and 64% of the net energy for gain of the normal diet. The LM was biopsied 5 months (period 1 [P1] at 15.5 months of age) and 14 months (period 2 [P2] at 24.5 months of age) after the start of feeding. The mRNA levels were determined using real-time polymerase chain reaction. Body weight, daily feed intake, average daily gain, and feed efficiency were lower in the DR group compared with the normal group at both P1 and P2. At P1, the lipogenic fatty acid synthase (FASN) mRNA levels were lower (p<0.05) in the DR group compared with the normal group. The DR group tended (p = 0.06) to have higher of levels of growth hormone receptor (GHR) mRNA than the normal group. At P2, the DR group tended to have lower (p = 0.06) androgen receptor (AR) mRNA levels than the normal group. In conclusion, our results demonstrate that dietary restriction partially decreases the transcription of lipogenic FASN and growth hormone signaling AR genes, but increases transcription of the GHR gene. These changes in gene transcription might affect body fat accumulation and the growth of the animals.

• Journal of Ginseng Research
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• v.23 no.2 s.54
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• pp.105-114
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• 1999

To investigate the effects of korean ginseng on the expression of transferrin receptor (TfR) in the liver cell membrane, we had carried out the experiments of $[^{3}H]thymidine$ uptake, $^{125}I-transferrin$ binding, and TfR mRNA expression in the liver after partial hepatectomy of normal and 3'-methyl-4-dimethylaminoa-zobenzene (3'-Me-DAB) treated rat with or without treatment of korean gingseng. $[^3H]thymidine$ uptake was not changed in the liver of 3'-Me-DAB or ginseng treated rat compared to that of control rat, but increased in that of partial hepatectomy of normal or 3'-Me-DAB treated rat. And this increased $[^{3}H]thymidine$ uptake was lowered slightly by the treatment of ginseng. Transferrin binding sites in the liver plasma membrane of ginseng treated rat with or without partial hepatectomy were similar, but increased in that of 3'-Me-DAB treated rat with or without partial hepatectomy compared to those of each control rat and these increased binding sites were reduced by ginseng treatment. Transferrin binding affinity (l/kd) was not changed by ginseng treatment, but tended to decrease in the liver of 3'-Me-DAB treated rat or in those after partial hepatectomy of all groups and reverse by ginseng treatment in 3'-Me-DAB treated rat. The expression of TfR mRNA was increased in the liver of 3'-Me-DAB treated rat with partial hepatectomy (peak at 24 hours), but lowered by ginseng treatment in this rat. From these results, it is suggested that korean ginseng has no effect on the increased expression of TfR with decreased affinity in the cell membrane of regenerated liver after partial hepatectomy of rat, but could inhibt that of 3'-Me-DAB treated rat through the regulation of DNA synthesis or TfR mRNA in partial.

• Molecules and Cells
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• v.24 no.1
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• pp.119-124
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• 2007

TLR4 together with CD14 and MD-2 forms a pattern recognition receptor that plays an initiating role in the innate immune response to Gram-negative bacteria. Here, we employed the surface plasmon resonance technique to investigate the kinetics of binding of LPS to recombinant CD14, MD-2 and TLR4 proteins produced in insect cells. The dissociation constants ($K_D$) of LPS for immobilized CD14 and MD-2 were $8.7{\mu}m$, and $2.3{\mu}m$, respectively. The association rate constant ($K_{on}$) of LPS for MD-2 was $5.61{\times}10^3M^{-1}S^{-1}$, and the dissociation rate constant ($K_{off}$) was $1.28{\times}10^2S^{-1}$, revealing slow association and fast dissociation with an affinity constant $K_D$ of $2.33{\times}10^6M$ at $25^{\circ}C$. These affinities are consistent with the current view that CD14 conveys LPS to the TLR4/MD-2 complex.

• The Korean Journal of Physiology
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• v.24 no.1
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• pp.67-76
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• 1990

The contractile mechanisms of serotonin were investigated in the renal artery of a rabbit. The helical strips of isolated renal artery were immersed in the normal or $Ca^{2+}$-free tris-buffered Tyrode's solution, which was equilibrated with 100% $O_{2}$ at $35^{\circ}C$. The contraction by serotonin or norepinephrine (NE) began at $1{\times}10^{-7}\;M$ and reached the maximal contraction at $1{\times}10^{-5}\;M$. The maximal contraction by serotonin corresponded to $58.1{\pm}4.2%$ of maximal contraction by NE. Cyproheptadine, a serotonin receptor blocker, shifted the concentration-response curve to the right without any reduction in the maximum response but shifted that of NE to the right with reduction in maximum response. And phentolamine, an ${\alpha}-receptor$ blocker, shifted the concentration-response curve of serotonin or NE without any reduction in maximum responses. The $pA_{2}$ values for cyproheptadine against serotonin and NE were $10.35{\pm}0.04$ and $8.45{\pm}0.13$, respectively. The $pA_{2}$ values for phentolamine against serotonin and NE were $6.87{\pm}0.04$ and $8.14{\pm}0.08$, respectively. after the pretreatment with 6-hydroxydopamine, the contraction induced by 100 mM $K^{+}$, tyramine and serotonin reduced to $83.0{\pm}2.0$, $26.8{\pm}6.2$ and $82.0{\pm}3.5%$ of control, respectively. The contraction by serotonin in the $Ca^{2+}$-free Tyrode's solution was increased and sustained with the addition of $Ca^{2+}$ extracellulary. The serotonin-sensitive intracellular $Ca^{2+}$ pool was depleted completely by the pretreatment with NE, but the NE-sensitive intracellular $Ca^{2+}$ pool was depleted partially by the pretreatment with serotonin. From the above results, it is suggested that the contraction induced by serotonin in the renal artery of a rabbit may be due to mechanisms in which serotonin acts directly on specific serotonin receptors and also acts indirectly on ${\alpha}-adrenoceptors$ by displacing NE from neuronal stores.