• Title/Summary/Keyword: 14{\alpha},\

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Selective Reduction of $\alpha,\beta$-Unsaturated Ketones with Borohydride Exchange Resin-$CuSO_4$ in Methanol

  • Yoon, Nung-Min;Sim, Tae-Bo
    • Bulletin of the Korean Chemical Society
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    • v.14 no.6
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    • pp.749-752
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    • 1993
  • Borohydride exchange resin $(BER)-CuSO_4$ system readily reduces {\alpha},{\beta}$-unsaturated ketones to the corresponding saturated alcohols quantitatively. This reduction tolerates many functional groups such as carbon-carbon multiple bonds, chlorides, epoxides, esters, amides and nitriles.

Cytotoxic Ergosterols from Paecilomyces sp. J300

  • Kwon, Hak-Cheol;Zee, Sang-Deuk;Cho, Sae-Yun;Choi, Sang-Un;Lee, Kang-Ro
    • Archives of Pharmacal Research
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    • v.25 no.6
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    • pp.851-855
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    • 2002
  • Seven ergosterol derivatives (1-7) were isolated from silkworm larvae infected with Paecilomyces sp. J300. On the basis of spectroscopic means, their structures have been elucidated as 3$\beta$,5$\alpha$-dihydroxy-ergosta-7,22-diene (1), 5$\alpha$,6$\alpha$-epoxy-(22E,24R)-ergosta-8(14), 22-diene-3$\beta$,7$\alpha$-diol (2), 5$\alpha$,6$\alpha$-epoxy-(22E,24R)-ergosta-8, 22-diene-3$\beta$,7$\alpha$-diol (3), ergosta-4, 6, 8(14), 22-tetraene-3-one (4), ergosterol (5), ergosterol endoperoxide (6), 3$\beta$,5$\alpha$-dihydroxy-6$\beta$-methoxyergosta-7,22-diene (7). Compounds 3~7 showed moderate cytotoxicity against five tumor cells.

Effect of Renal Denervation on Diuretic Action of UK 14,304, $\alpha$$_2$-Adrenergic Agonist, in Dog ($\alpha$$_2$-아드레날린 효능제인 UK 14,304의 이뇨작용에 대한 신장신경 제거의 영향)

  • KO, Suk-Tai;NA, Han-Kwang
    • Biomolecules & Therapeutics
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    • v.5 no.4
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    • pp.351-356
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    • 1997
  • This study was performed in order to investigate the effect of renal denervation on diuretic action of UK 14, 304, $\alpha$$_2$-Adrenergic Agonist, administered into the vein and the carotid artery in dog. The diuretic action of UK 14, 304 administered into the vein or the carotid artery was reversed to the antidiuretic action by renal denervation, this time, the decrease of N $a^{+}$excretion amounts in urine ( $E_{Na}$ ) and the increase of N $a^{+}$ reabsorption rates in renal tubule ( $R_{Na}$ ) were exhibited. This results suggest that central diuretic action of UK 14, 304 is mediated by renal nerves and the antidiuretic action of UK 14, 304 in denervation kidney is caused by the increase of N $a^{+}$reabsorption rates ( $R_{Na}$ ) in renal tubules in dog.n dog.

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Prediction and Analysis of Ligands against Estrogen Related Receptor Alpha

  • Chitrala, Kumaraswamy Naidu;Yeguvapalli, Suneetha
    • Asian Pacific Journal of Cancer Prevention
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    • v.14 no.4
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    • pp.2371-2375
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    • 2013
  • Breast cancer is one of the most common malignancies in women around the world. Among the various hormonal types of breast cancer, those that are estrogen receptor (ER) positive account for the majority. Among the estrogen related receptors, estrogen related receptor ${\alpha}$ is known to have a potential role in breast cancer and is one of the therapeutic target. Hence, prediction of novel ligands interact with estrogen related receptor alpha is therapeutically important. The present study, aims at prediction and analysis of ligands from the KEGG COMPOUND database (containing 10,739 entries) able to interact against estrogen receptor alpha using a similarity search and molecular docking approach.

Effect of $\alpha$-Tocopherol and Cysteamine on Maturation Male Pronuclear Formation and Development of Porcine Oocytes In Vitro ($\alpha$-Tocopherol과 Cysteamine 첨가가 돼지 미성숙난포란의 체외성숙, 체외수정 및 배발달에 미치는 영향)

  • 이경호;문승주;김재홍
    • Journal of Embryo Transfer
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    • v.14 no.1
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    • pp.9-15
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    • 1999
  • This study was conducted to investigate the effect of $\alpha$-tocopherol and cysteamine with Whitten's medium in supporting the development on in vitro maturation(IVM), in vitro fertilization (IVF) and in culture(IVC) on porcine oocytes. When the immature oocytes were cultured of $\alpha$-tocopherol for 40h, the nuclear maturation rates were 39, 4, 52.5 and 54.1%, respectivley. The nuclear maturation rates of treat groups were signficantly (P<0.05) higher than those of non-treat groups. After matureation, the oocytes were inseminated in vitro in medium 199 with ejaculated spermatoza for examination of sperm penetration, polyspermy, male pronuclear(MPN) formation, and cleavage rate. Sperm penetration rates of treat higher than the control groups(P<0.05), and MPN formation rates were significantly(P<0.05) higher on treated groups (24.3~53.1%) than control groups(14.2~21.4%). After insemination, the cleavage rates at 120hr were groups higher than control groups(P<0.05).

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WEAK* QUASI-SMOOTH α-STRUCTURE OF SMOOTH TOPOLOGICAL SPACES

  • Min, Won Keun;Park, Chun-Kee
    • Korean Journal of Mathematics
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    • v.14 no.2
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    • pp.233-240
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    • 2006
  • In this paper we introduce the concepts of several types of $weak^*$ quasi-smooth ${\alpha}$-compactness in terms of the concepts of weak smooth ${\alpha}$-closure and weak smooth ${\alpha}$-interior of a fuzzy set in smooth topological spaces and investigate some of their properties.

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Reproductive Monitoring and Estrus Induction Using Ultrasonography and Hormone Assay in Dairy Cows III. Estrus Induction Using $PGF_2{\alpha}$ (초음파검사 및 호르몬검사에 의한 젖소 번식검진과 발정유도 III. $PGF_2{\alpha}$ 제제에 의한 발정유도)

  • 오기석;박상국;김방실;고진성;신종봉;백종환;홍기강;문광식;임원호
    • Journal of Veterinary Clinics
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    • v.20 no.3
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    • pp.384-388
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    • 2003
  • To establish the method of estrus induction using the injection of PGF$_2$$\alpha$ㆍ the 60 dairy cows treated by PGF$_2$$\alpha$ㆍ at 6, 8, 10, 12, 14, and 16 day of estrous cycle, recpectively. The plasma progesterone concentrations at day of injection of PGF$_2$$\alpha$ㆍ were $1.5\pm$1.3 (mean$\pm$SD) ng/ml at 6 days of estrous cycle, 3.7$\pm$1.4 ng/ml at 8 days, 6.5$\pm$1.8 ng/ml at 10 days, 7.9$\pm$2.0 ng/ml at 12 days, 6.5$\pm$2.5 ng/ml at 14 days, and 2.5$\pm$1.2 ng/m] at 16 days, respectively. The percentages of induction of estrus after PGF$_2$$\alpha$ㆍ treatment were 52.8% at 3th day after treatment, 21.7% at 4th day, 8.3% within 2th day, and ] 7.2% after 5th day, respectively. The percentages of cows conceived at first service after induction of estrus were 73.3% on 16 days of estrous cycle at treatment, 66.7% on 10 and 14 days, 63.3% on 8 and 12 days, and 53.3% on 6 day, respectively. The percentages of cows conceived on first service were 70.5% at 3th day after induction, 66.7% at 4th day and 65% at 5th day, respectively. These results suggest that the PGF$_2$$\alpha$ㆍ treatment at regressing stage of corpus luteum showed high induction of estrus and pregnancy rate, and there were high induction of estrus and pregnancy rate at 3th and 4th day after PGF$_2$$\alpha$ㆍ treatment.

The Carboxyl Terminal Amino Acid Residues Glutamine276-Threonine277 Are Important for Actin Affinity of the Unacetylated Smooth ${\alpha}$-Tropomyosin

  • Cho, Young-Joon
    • BMB Reports
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    • v.33 no.6
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    • pp.531-536
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    • 2000
  • Tropomyosin (TM) is an important actin binding protein involved in regulation of muscle contraction. Unacetylated striated tropomyosin failed to bind to actin whereas unacetylated smooth tropomyosin bound well to actin. It has been demonstrated that high actin affinity of unacetylated ${\alpha}-tropomyosin$ was ascribed to the carboxyl terminal amino acid residues. In order to define the role of the carboxyl terminal residues of tropomyosin molecule on actin binding, two mutant tropomyosins were constructed. TM11 is identical to the striated tropomyosin except that the carboxyl terminal last three amino acids was replaced with $^{282}NNM^{284}$ whereas in TM14 $^{276}HA^{277}$ was substituted with smooth specific $^{276}QT^{277}$. TM11 and TM14 were overproduced in Escherichia coli and analyzed for actin affinity. The apparent binding constants (Kapp) of unacetylated tropomyosins were $2.2{\times}10^6M^{-1}$ for sm9, $1.03{\times}10^6M^{-1}$ for TM14, $0.19{\times}10^6M^{-1}$ for TM11, $>0.1{\times}10^6M^{-1}$ for striated, respectively. This result indicated that higher actin affinity of the unacetylated smooth tropomyosin was primarily attributed to the presence of QT residues in the smooth sequence. In case of the Ala-Ser (AS) dipeptide extension of the amino terminus of tropomyosin, Kapp were $21.1{\times}10^6M^{-1}$ for AS-sm9, $8.0{\times}10^6M^{-1}$ for AS-11, $4.7{\times}10^6M^{-1}$ for AS-14, $3.8{\times}10^6M^{-1}$ for AS-striated. AS-TM11 showed considerably higher actin affinity than AS-TM14, implying that interaction of Ala-Ser of the amino terminus with the carboxyl terminal residues. Since Kapp of AS-TM11 was significantly lower than that of AS-sm9, the presence of QT might be required for restoration of high actin affinity of the smooth ${\alpha}-tropomyosin$. These results suggested that the carboxyl terminal amino acid residues Glutamine275-Threonine276 are important for actin affinity of the recombinant smooth ${\alpha}-tropomyosin$, particularly of unacetylated smooth ${\alpha}-tropomyosin$.

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Chemical Reactivity between Ni(II)-Macrocycle Complex Ions ($NiL_m{^{2+}}$) and $CN^-$ (Ni(II)-거대고리 리간드 착이온 ($NiL_m{^{2+}}$) 과 $CN^-$ 이온간의 반응성)

  • Yu-Chul Park;Jong-Chul Byun
    • Journal of the Korean Chemical Society
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    • v.31 no.4
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    • pp.334-343
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    • 1987
  • The Chemical reactions between $NiL_m{^{2+}}\{$Ni(rac-1[14]7-diene)^{2+},\;Ni(meso-1[14]7-diene)^{2+},\;Ni(1[14]4-diene)^{2+},\;{\alpha}-Ni(rac-[14]-decane)^{2+},\;{\beta}-Ni(rac-[14]-decane)^{2+},\;and\;Ni(meso-[14]-decane)^{2+}$}\and\ CN^-$ ion were studied by the spectrophotometric method. The equilibrium constants (K_1$) for the 1:1 complex ion, $[NiL_m(CN)]^+\;with\;NiL_m{^{2+}}\;and\;CN^-$ ion were determined in the range of 3 to $25^{\circ}C$. The $K_1\;for\;Ni(rac-1[14]7-diene)^{2+},\;Ni(meso-1[14]7-diene)^{2+},\;Ni(1[14]4-diene)^{2+},\;{\alpha}-Ni(rac-[14]-decane)^{2+},\;{beta}-Ni(rac-[14]-decane)^{2+},\;and\;Ni(meso-[14]-decane)^{2+}\;at\;15^{\circ}C$ was 4.7, 5.3, 6.2, 7.5, 9.4, and 9.8, respectively. The values of $K_1$ decreased with increasing temperature. From the temperature effect on equilibrium constant ($K_1$), thermodynamic parameters $({\Delta}H^{\circ},\;{\Delta}S^{\circ},\;{\Delta}G^{\circ})$ for reaction were evaluated and the reaction of $NiL_m{^{2+}}\;and\;CN^-$ ion was exothermic. $NiL_m{^{2+}\;reacts\;with\;CN^-$ ion to give $Ni(CN)_4{^{2-}}$ ion and macrocyclic ligand $(L_m)$. The kinetics of formation of the $Ni(CN)_4{^{2-}}$ ion of varying the $[CN^-],\;[HCN],\;and\;[OH^-]$ have been investigated at 3∼$25^{\circ}C\;and\;0.5M\;NaClO_4$. Maintaining a constant $[CN^-],\;k_{obs}/[CN^-]^2$ increases linearly with increasing [HCN]. In the presence of large quantities of $[OH^-],\;k_{obs}/[CN^-]^2$ also increases linearly with $[OH^-]$. From the temperature effect on kinetic constant (k_{obs})$, parameter of activation $({\Delta}H^{\neq},\;{\Delta}S^{\neq})$ of reaction of $NiL_m{^{2+}}\;with\;CN^-$ ion were determined. For the $Ni(rac-1[14]7-diene)^{2+},\;Ni(meso-1[14]7-diene)^{2+},\;{\alpha}-Ni(rac-[14]-decane)^{2+},\;{\beta}-Ni(rac-[14]-decane)^{2+},\;and\;Ni(meso-[14]-decane)^{2+}\;series\;{\Delta}H^{\neq}$ gradually decrease as the d-d transition energy, $ν(cm^{-1})$ decrease. And the reaction of the five $NiL_m{^{2+}}\;with\;CN^-$ ion take place by way of equal paths.

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Effects of Exogenous Oxytocin on Steroid Hormones and Oxytocin Receptor Concentrations in Pregnant Rats (Oxytocin 투여가 임신 Rat의 Steroid Hormones 및 Oxytocin Receptors 농도에 미치는 영향)

  • 박용수;조현수;변명대
    • Korean Journal of Animal Reproduction
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    • v.26 no.2
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    • pp.183-192
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    • 2002
  • The present studies were carried out to examine the effects of exogenous oxytocin(OT) on plasma, uterine and placenta of estradiol-17$\beta$, progesterone, prostaglandin F$_2$$_{\alpha}$ (PGF$_2$$_{\alpha}$), Prostaglandin E$_2$(PGE$_2$) and OT receptor concentrations in pregnant rats. Pregnant rats received an injection of exogenous OT on days 14, 16, 18, 20, 22 of pregnancy and day 1 of postpartum. Concentrations of plasma estradiol-17 $\beta$ after OT injection started to increase after day 18 and peaked on day 22 of pregnancy but decreased on day 1 of postpartum. Plasma progesterone concentrations declined gradually from day 18 of pregnancy and decreased more rapidly until postpartum 1 day. Concentrations of estradiol-17$\beta$in uterine tissues after OT injection were sharply increased from day 20 to 22 of pregnancy and progestrone concentrations were peaked on day 16 and decreased rapidly from day 16 to 20 and maintained the same level until day 1 of postpartum. Uterine concentrations of PGF$_2$$_{\alpha}$ and PGE$_2$increased gradually until day 20 and peaked on day 22 of pregnancy but showed a marked decrease on day 1 of postpartum. Concentrations of PGF$_2$$_{\alpha}$ in placental tissues increased rapidly from day 14 of pregnancy and decreased sharply on day 1 of postpartum. Concentrations of PGE$_2$increased gradually after day 14 and peaked on day 20 of pregnancy. The concentration of OT receptor in uterus was significantly elevated from day 20 and rose to maximum on day 22 of pregnancy. These findings show that OT suppress the concentration of progestrone and stimulate productions of estradiol-17 $\beta$, PGF$_2$$_{\alpha}$, PGE$_2$ and oxytocin receptor concentrations in pregnant rats.