• Archives of Pharmacal Research
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• 제28권2호
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• pp.172-176
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• 2005

Phytochemical investigation of the whole plant of Amberboa ramosa led to the isolation of six sesquiterpene lactones which could be identified as $8{\alpha}$-hydroxy-$11{\beta}$-methyl-$1{\alpha}H,\;5{\alpha}H,\;6{\beta}H,\;7{\alpha}H,\;11{\alpha}H-guai-10(14)$, 4(15)-dien-6, 12-olide(2), $3{\beta},\;8{\alpha}-dihydroxy-11{\alpha}-methyl-1{\alpha}H,\;5{\alpha}H,\;6{\beta}H,\;7{\alpha}H,\;11{\beta}H-guai-10(14)$, 4(15)-dien-6, 12-olide (2), $3{\beta},\;4{\alpha},\;8{\alpha}-trihydroxy-4{\beta}(hydroxymethyl)-1{\alpha}H,\;5{\alpha}H,\;6{\beta}H,\;7{\alpha}H-guai-10(14)$, 11(13)-dien-6, 12-olide (3), $3{\beta},\;4{\alpha},\;8{\alpha}-trihydroxy-4{\beta}-(chloromethyl)-1{\alpha}H,\;5{\alpha}H,\;6{\beta}H,\;7{\alpha}H-guai-10(14)$, 11(13)-dien-6, 12-olide(4), $3{\beta},\;4{\alpha},\;dihydroxy-4{\beta}-(hydroxymethyl)-1{\alpha}H,\;5{\alpha}H,\;6{\beta}H,\;7{\alpha}H-guai-10(14)$, 11(13)-dien-6, 12-olide(5), $3{\beta},\;4{\alpha}-dihydroxy-4{\beta}-(chloromethyl)-8{\alpha}-(4-hydroxymethacrylate)-1{\alpha}H,\;5{\alpha}H,\;6{\beta}H,\;7{\alpha}H-guai-10(14)$, 11(13)-dien-6, 12-olide (6) by spectroscopic methods. All of them showed inhibitory potential against butyrylcholinesterase.

• 약학회지
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• 제39권4호
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• pp.433-437
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• 1995

Optically pure(-)-and (+)-$\alpha$-hydroxy-$\alpha$-(p-chlorobiphenyl)acetic acids were prepared. The racemate was synthesized through three steps. By condensation of p-cnorobiphenyl with diethyl ketomalonate in the presence of SnCl$_{4}$, diethyl $\alpha$-hydroxy-$\alpha$-(p-chlorobiphenyl)malonate (1) was formed and subsequently ($\pm$)-$\alpha$-hydroxy-$\alpha$-(p-chlorobiphenyl)acetic acid (3) was obtained through hydrolysis and decarboxylation. For the separation of the racemate the classical resolution method, derivatization of a racemate by reaction with an optically pure compound was employed. In this case the optically pure compound were [R]-(+)-$\alpha$-methylbenzylamine and [S]-(-)-$\alpha$-methylbenzylamine. Diastereomeric salts between acids and bases could be easily separated by crystallization in absolute ethanol.

• Nutrition Research and Practice
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• 제1권4호
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• pp.247-253
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• 2007

Alpha-tocopherol transfer protein (${\alpha}$-TTP) is a liver cytosolic transport protein that faciliates ${\alpha}$-tocopherol (${\alpha}$-T) transfer into liver secreted plasma lipoproteins. Genetic defects in ${\alpha}$-TTP, like dietary vitamin E deficiency, are associated with infertility, muscular weakness and neurological disorders. Both human and ${\alpha}$-TTP deficient (${\alpha}-TTP^{-/-}$) mice exhibit severe plasma and tissue vitamin E deficiency that can be attenuated by sufficient dietary ${\alpha}$-T supplementations. In this review, we summarize the literature concerning studies utilizing the ${\alpha}-TTP^{-/-}$ mice. Levels of vitamin E in the ${\alpha}-TTP^{-/-}$ mice do not appear to be directly related to the amounts of dietary ${\alpha}$-T or to the levels of ${\alpha}$-TTP protein in tissues. The ${\alpha}-TTP^{-/-}$ mice appear to present a good model for investigating the specific role of ${\alpha}$-T in tissue vitamin E metabolism. Furthermore, ${\alpha}-TTP^{-/-}$ mice appear to be useful to elucidate functions of ${\alpha}$-TTP beyond its well recognized functions of transferring ${\alpha}$-T from liver to plasma lipoprotein fractions.

• Archives of Pharmacal Research
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• 제20권6호
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• pp.525-528
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• 1997

Steroid $9{\alpha}$.-hydroxylase is a key enzyme system in steroid nucleus degradation in company with ${\Delta}$-dehydrogenase. To examine $9{\alpha}$-hydroxylase activity during microbial transformation of steroids, 9(11)-dehydro-$17{\alpha}$-methyl-testosterone was adopted as a stable substrate for preventing the rupture of steroid nucleus. Using Nocardia restrictus ATCC 14887 capable of introducing a $9{\alpha}$-hydroxyl group into steroids, $9{\alpha}$,$11{\alpha}$-oxido-$17{\beta}$-hydroxy-$17{\alpha}$-methyl-4-androstene-3-one and $9{\alpha}$-hydroxyl group into steroids,$9{\alpha}$,$11{\alpha}$-oxido-$17{\beta}$-hydroxy-$17{\alpha}$-methyl-1,4-androstadiene-3- one were obtained. These microbiologically transformed products could be used as reference compounds in the enzyme assay.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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• pp.67.1-67.1
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• 2003

Three new guaianolide type of sesquiterpene lactones, 8${\alpha}$-angeloyloxy-1${\alpha}$-hydroxy-3${\alpha}$,4${\alpha}$-epoxy-5${\alpha}$, 7${\alpha}$H-10(14), 11(13)-guaiadien-12,6${\alpha}$-olide (1), 8${\alpha}$-methylbutyryloxy-1${\alpha}$-hydroxy-3${\alpha}$, 4${\alpha}$-epoxy-5${\alpha}$, 7${\alpha}$H-10(14),11(13)-guaiadien-12,6${\alpha}$-olide (2), and 8${\alpha}$-isovaleryloxy-1${\alpha}$-hydroxy-3${\alpha}$, 4${\alpha}$-epoxy-5${\alpha}$, 7${\alpha}$H-10(14),11 (13)- guaiadien-12,6${\alpha}$-olide (3), together with six known sesquiterpenes, artemisolide (4), 3-methoxytanapartholide (5), deacetyllaurenobiolide (6), moxartenolide (7), arteminolide B (8), and arteminolide D (9) were isolated by bioassay-guided fractionation using the NF-kB mediated reporter gene assay system. (omitted)

• 대한수학회지
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• 제47권3호
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• pp.455-466
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• 2010

For an endomorphism $\alpha$ of a ring R, we introduce the weak $\alpha$-skew Armendariz rings which are a generalization of the $\alpha$-skew Armendariz rings and the weak Armendariz rings, and investigate their properties. Moreover, we prove that a ring R is weak $\alpha$-skew Armendariz if and only if for any n, the $n\;{\times}\;n$ upper triangular matrix ring $T_n(R)$ is weak $\bar{\alpha}$-skew Armendariz, where $\bar{\alpha}\;:\;T_n(R)\;{\rightarrow}\;T_n(R)$ is an extension of $\alpha$ If R is reversible and $\alpha$ satisfies the condition that ab = 0 implies $a{\alpha}(b)=0$ for any a, b $\in$ R, then the ring R[x]/($x^n$) is weak $\bar{\alpha}$-skew Armendariz, where ($x^n$) is an ideal generated by $x^n$, n is a positive integer and $\bar{\alpha}\;:\;R[x]/(x^n)\;{\rightarrow}\;R[x]/(x^n)$ is an extension of $\alpha$. If $\alpha$ also satisfies the condition that ${\alpha}^t\;=\;1$ for some positive integer t, the ring R[x] (resp, R[x; $\alpha$) is weak $\bar{\alpha}$-skew (resp, weak) Armendariz, where $\bar{\alpha}\;:\;R[x]\;{\rightarrow}\;R[x]$ is an extension of $\alpha$.

• BMB Reports
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• 제29권4호
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• pp.365-371
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• 1996

Partially reduced interferon-a ($IFN-{\alpha}$) was cross-linked with thymosin ${\alpha}1$ ($T{\alpha}1$) using sulfo-succinimidyl (4-iodoacetyl) amino benzoate (SIAB), a bifunctional cross-linking reagent. The partially reduced $IFN-{\alpha}$ optimal for the cross-linking reaction was obtained by incubating native $IFN-{\alpha}$ with 0.5 mM DTT at $30^{\circ}C$ for 60~100 min. $T{\alpha}1$ was activated by incubating with sulfo-SIAB at $37^{\circ}C$ for 30 min to produce $T{\alpha}1-IAB$. The $T{\alpha}1-IFN-{\alpha}$ cross-linking was achieved by the reaction of the partially reduced $IFN-{\alpha}$ with $T{\alpha}1-IAB$. This cross-linking was between the sulfhydryl group of Cys1 in $IFN-{\alpha}$ and the N-terminal amino group of $T{\alpha}1$ through acetyl amino benzoate as a spacer. The immunological activity of the cross-linked molecule showed the same extent as that of $T{\alpha}1$, and most of the antiviral activity was retained compared to that of the partially reduced $IFN-{\alpha}$.

• Molecules and Cells
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• 제26권3호
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• pp.285-290
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• 2008

Estrogen-induced proliferation in estrogen receptor (ER)-positive breast cancer cells is primarily mediated through two distinct intracellular receptors, $ER{\alpha}$ and $ER{\beta}$. Although tumor necrosis factor alpha ($TNF{\alpha}$) and $E2/ER{\alpha}$ are known to exert opposing effects on cell proliferation in MCF-7 cells, the mechanism by which $TNF{\alpha}$ antagonizes $E2/ER{\alpha}$-mediated cell proliferation is not well understood. The present study suggests that reduced cell survival in response to $TNF{\alpha}$ treatment in MCF-7 cells may be associated with the down-regulation of $ER{\alpha}$ protein. The decrease in $ER{\alpha}$ protein level was accompanied by an inhibition of $ER{\alpha}$ gene transcription. Cell viability was decreased synergistically by the combined treatment with $ER{\alpha}$-siRNA and $TNF{\alpha}$. Furthermore, pretreatment of cells with the PI3-kinase (PI3K)/ Akt inhibitor, LY294002, markedly enhanced $TNF{\alpha}$-induced down-regulation of the $ER{\alpha}$ protein, suggesting that the PI3K/Akt pathway might be involved in control of the $ER{\alpha}$ level. Moreover, down-regulation of $ER{\alpha}$ by $TNF{\alpha}$ was not inhibited in cells that were pretreated with the proteasome inhibitors, MG132 and MG152, which suggests that proteasome-dependent proteolysis does not significantly influence $TNF{\alpha}$-induced down-regulation of $ER{\alpha}$ protein. In contrast, the effect of the PI3K/Akt inhibitor on $ER{\alpha}$ was blocked in cells that were treated with LY294002 in the presence of the proteasome inhibitors. Collectively, our findings show that the $TNF{\alpha}$ may partly regulate the growth of MCF-7 breast cancer cells through the down-regulation of $ER{\alpha}$ expression, which is primarily mediated by a PI3K/Akt signaling.

• 충청수학회지
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• 제23권1호
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• pp.59-63
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• 2010

In this paper, we introduce the concept of weakly-ultra-${\alpha}{\psi}$-separation of two sets in a topological space using ${\alpha}{\psi}$-open sets. The ${\alpha}{\psi}$-closure and the ${\alpha}{\psi}$-kernel are defined in terms of this weakly ultra-${\alpha}{\psi}$-separation. We also investigate some of the properties of the ${\alpha}{\psi}$-kernel and the ${\alpha}{\psi}$-closure.

• 한국수산과학회지
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• 제30권2호
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• pp.203-210
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• 1997

동자개 난모세포의 성숙과 배란에 있어 스테로이드와 HCG(human chorionic gonadotropin)의 효과에 대한 실험이 in vitro에서 이루어졌으며, 난모세포들은 $17\alpha,\;20\alpha-dihydroxy4-pregnen-3-one\;(17\alpha\;20\alpha\;OHP),\;17\alpha-hydroxyprogesterone\;(17\alpha\;OHP),\;progesterone\;(P_4),\;estradiol-17{\alpha}E_2)$ 과 HCG가 첨가된 Leibovitz L15 배지에서 성숙되어졌다. 60시간 배양후에 난모세포의 성숙능력은 난핵포붕괴(germinal vesicle breakdown, GVBD) 비율에 의해 평가되었다. GVBD 비율은 $17\alpha\;20\alpha\;OHP,\;17\alpha\;OHP,\;P_4$ 그리고 HCG의 첨가에 의해 유의하게 (P<0.05) 증가하였으며, 그 중 $17\alpha\;20\alpha\;OHP$ HCG에서 가장 높은 GVBD 비율을 보였다. 난모세포들 $17\alpha\;20\alpha\;OHP,\;17\alpha\;OHP,\;P_4$가 $10\~1,000ng/ml$포함된 배지에서 16시간 배양한 결과, $17\alpha\;20\alpha\;OHP\;10\~100ng/m1(65\%)$의 GVBD 비율은 $17\alpha\;20\alpha\;OHP(40\%)$와 $P_4(35\%)$에서 보다 나은 효과를 보였다. GVBD유도에 대한 효과는 $17\alpha\;20\alpha\;OHP$에서 $10\~100\;ng/ml$배지, HCG를 첨가하여 60시간 배양한 배란유도 실험에서 $17\alpha\;20\alpha\;OHP\;10\~100ng/ml$에서, HCG는 $50\~500IU/ml$의 배지에서 배란율이 유의하게 증가하였다. 그러나 $17\alpha\;20\alpha\;OHP\;1,000ng/m1$와 HCG 5IU/ml의 배지에서는 대조구의 배란율과 차이를 보이지 않았다. 이러한 결과로 $E_2$를 제외한 스테로이드와 HCG는 동자개의 난모세포 성숙과 배란을 in vitro에서 유도할 수 있으며, $17\alpha\;20\alpha\;OHP$와 HCG는 다른 스테로이드에 비해 높은 율의 난모세포 성숙과 배란을 유도하였다.