• Title/Summary/Keyword: $5{\alpha}H,\

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Butyrylcholinesterase Inhibitory Guaianolides from Amberboa ramosa

  • Khan Sher Bahadar;Haq Azhar-ul;Perveen Shagufta;Afza Nighat;Malik Abdul;Nawaz Sarfraz Ahmad;Shah Muhammad Raza;Choudhary Muhammad lqbal
    • Archives of Pharmacal Research
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    • v.28 no.2
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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.

The constituents of taraxacum hallaisanensis roots

  • Yang, Deuk-Suk;Whang, Wan-Kyunn;Kim, Il-Hyuk
    • Archives of Pharmacal Research
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    • v.19 no.6
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    • pp.507-513
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    • 1996
  • Three sesquiterpene lactone compounds, two novel(1.betha.,3.betha.-dihydroxy-6.betha.,11.betha.,4.alpha.,5.alpha.,7.alpha.H -eudesm-12, 6-olide-1-O-.betha.-D-glucopyranoside, 1.betha.,3.betha.-dihydroxy-6.betha.,11.betha.,4.alpha.,5.alpha.,7.alpha.H-eudes m-12,6-olide-1-O-.betha.-D-glucopyranoside) and 1.betha.,3.betha.-dihydroxy-6.betha.,11.betha.,4.alpha.,5.alpha., 7.alpha.H-eudesm-12,6-olide were isolated from the aqueous fraction of MeOH extract of the roots from Taraxacum hallaisanensis (Compositae) employing Amberlite XAD-2, ODS-gel, silica gel and Sephadex LH-20 column chromatographics. Another known compound, (-)-epicatechin, was isolated from the aqueous fraction of the MeOH extract. The total MeOH extract also contained phytosterol and a mixture of .betha.-amyrin acetate, .alpha.-amyrin acetate and lupeol acetate. Structures of isolated compounds were elucidated by spectroscopic parameters of IR, Mass, /sup 13/C-NMR, /sup 1/H-NMR, /sup 1/H-/sup 1/H COSY, /sup 13/C-/sup 1/H COSY and HMBC.

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The Kinetics and Mechanism of Nucleophilic Addition of n-Propylmercaptan to $\alpha$-Cyano-$\beta$-piperonylacrylic Acid ($\alpha$-Cyano-$\beta$-piperonylacrylic Acid에 대한 n-Propylmercaptan의 친핵성 첨가반응에 관한 연구)

  • Kim, Tae-Rin;Huh, Tae-Seong
    • Journal of the Korean Chemical Society
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    • v.17 no.5
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    • pp.363-370
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    • 1973
  • The rate constants of the nucleophilic addition of n-propyl-mercaptan to $\alpha$-cyano-$\beta$-piperonylacrylic acid were determined at various pH and a rate equation which can be applied over wide pH range is obtained. The rate equation reveals that below pH 4.5 the reaction is initiated by the attack of n-propylmercaptan to $\alpha$-cyano-$\beta$-piperonylacrylic acid. At pH 4.5~6.5, however, n-propylmercaptan is added to $\alpha$-cyano-$\beta$-piperonylacrylate ion; at pH 7.04~9.5 the competitive reaction between n-propylmercaptan and n-propylmercaptide ion is anticipated to occur. Above pH 10 the addendum is n-propylmercaptide ion and the acceptor is $\alpha$-cyano-$\beta$-piperonylacrylate ion.

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Synthesis of Glycosides by Transglycosylation of α-Amylase from Starch (전분으로부터 α-amylase에 의한 배당체의 합성)

  • Park, Jong Yi;Lee, Tae Ho
    • Korean Journal of Microbiology
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    • v.34 no.3
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    • pp.137-143
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    • 1998
  • Glycosides were synthesized using transglycosylation reaction of amylase in water system. The glycosides synthesized in water phase by a-amylase with starch as a glycosyl donor and benzylalcohol as an acceptor were identified as benzylalcohol-${\alpha}$-glucoside (BG) and benzylalcohol-${\alpha}$-maltoside (BM) of which one molecule of benzylalcohol was bound to 1-OH of glucose. The final products were BG in reaction system of pH 5.0, and BM in that of pH 8.0. The transglycosylation reaction by ${\alpha}$-amylase were carried out in water system containing 50 mg starch, 50 mg benzylalcohol, and 10 units enzyme at $30-35^{\circ}C$ for 3 days. The synthesized BG was hydrolyzed to glucose and benzylalcohol by ${\alpha}$-glucosidase, while ${\alpha}$-amylase hydrolyzed BM to glucose and benzylalcohol-${\alpha}$-glucoside in pH 5.0. Maltotriose resemble structurally to BM was rapidly hydrolyzed to glucose and maltose by ${\alpha}$-amylase at pH 5.0, being slightly hydrolyzed at pH 8.0, but not transglycosylated in present of benzylalcohol.

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Kinetics and Mechanism of the Hydrolysis of ${\alpha}$-Cyano-${\beta}$-piperonylacrylic Acid (${\alpha}$-Cyano-${\beta}$-Piperonylacrylic Acid의 가수분해 메카니즘과 그의 반응속도론적 연구)

  • Tae Rin Kim;Kwang Il Lee
    • Journal of the Korean Chemical Society
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    • v.17 no.4
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    • pp.269-274
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    • 1973
  • The rate constants of the hydrolysis of ${\alpha}$-Cyano-${\beta}$-piperonylacrylic acid were determined by Ultraviolet spectrophotometry at various pH and a rate equation which can be applied over wide pH range was obtained. The reaction mechanism of hydrolysis of ${\alpha}$-Cyano-${\beta}$-piperonylic acid and especially the catalytic contribution of hydroxide ion which not studied carefully before in acidic media, can be fully explained by the rate equation obtained. The rate equation reveals that; below pH 4.0, the reaction is initiated by the addition of water molecule to ${\alpha}$-Cyano-${\beta}$-piperonyl acrylic acid. At pH $5.0{\sim}7.5$, ${\alpha}$-Cyano-${\beta}$-piperonylacrylic acid compete with ${\alpha}$-Cyano-${\beta}$-piperonyl acrylate ion in adding of water. At pH 8.0, water is the only nucleophile for ${\alpha}$-Cyano-${\beta}$-piperonylacrylate ion, however, above pH 12.0, hydroxide ion is an addendum and the accepter is ${\alpha}$-Cyano-${\beta}$-piperonylacrylate ion.

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Stabilization of Bacillus lichemiformis $\alpha$-Amulase by Modification with IO$_4$-Oxidized Soluble Starch (과요오드산 산화당에 의한 효소의 안정성)

  • 금종화
    • The Korean Journal of Food And Nutrition
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    • v.14 no.3
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    • pp.263-268
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    • 2001
  • NaIO$_4$-산화 전분당을 Bacillus licheniformis의 $\alpha$-아밀라아제의 반응시켜서 시프염기 형성으로 당단백질로 변형시켜서 안정성을 확인하였다. 10$0^{\circ}C$에서의 열안정성은 10분 뒤에, pH 9.7에서 변형한 효소 비변형 효소의 순으로 높았다. 그러나 변형 및 안정성에 $\alpha$-cyclodextrin($\alpha$-CD)을 사용한 결과 큰 차이는 나지 않았다. pH 8.0에서 $\alpha$-CD 존재하에 변형한 효소는 pH 8~11dml 알칼리쪽에서 가장 높은 안정성을 나타냈으나, pH 5~7사이에는 다른 효소보다 낮았다. pH 9.7에서 변형하지 않은 효소는 pH 5부터 pH 13까지 서서히 증가하였고 pH 9.7에서 $\alpha$-CD존재 하의 효소는 pH 5부터 7까지 증가하다가 그 후 pH13까지 서서히 감소하였다. $\alpha$-CD존재하의 비변형 효소는 pH 7과 10에서 피크를나타낸 다음 pH12이후에는 급격히 낮아졌다. 변형한 효소는 HPLC 의 유출시간이 빨라wu서 변형하지 않은 효소보다 분자량이 큰 것으로 나타났다. 분자량 크기는 비변형 효소

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Priority-Based Random Access control for M2M Service in 3GPP LTE-A System (3GPP LTE-A 시스템에서 M2M 서비스를 위한 우선순위 기반 임의접속제어)

  • Kim, Nam-Sun
    • The Journal of Korea Institute of Information, Electronics, and Communication Technology
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    • v.12 no.4
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    • pp.406-412
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    • 2019
  • In this paper, we propose two algorithms for classifying services with similar delay characteristics into three classes and allocating radio resources according to priority in LTE-A system where H2H and M2M services coexist. The first is to allocate resources from the higher priority class to the lower priority class, and each class gives priority to H2H over M2M, and the other is to give priority to H2H regardless of delay characteristics except for the class with the highest priority. The RA success probability was analyzed according to the access rate(${\alpha}$) of M2M devices in each class. In comparison with the conventional systems, it was improved from 0.5 to 0.52 for ${\alpha}_{2M}=0.05$ in two classes. In the three classes, the success probability was slightly increased from 0.5 to 0.57 for ${\alpha}_{2M}={\alpha}_{3M}=1$ and from 0.5 to 0.58 for ${\alpha}_{2M}=0.5$ and ${\alpha}_{3M}=0.1$. Although 6 services are considered in the proposed scheme, the RA success probability is almost similar to the previous scheme because the average arrival rate of H2H of each class is set to the same.

An Efficient Synthesis of$\alpha,\beta-enoyl-\eta^5-(C_5H_5)Fe(CO)(PPh_3)$ Complexes

  • Kwon, Hyok-Boong;Ojima, Iwao
    • Bulletin of the Korean Chemical Society
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    • v.15 no.10
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    • pp.849-852
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    • 1994
  • The ${\alpha},{\beta}$-enoyl chiral iron complexes, ${\alpha},{\beta}-enoyl-{\eta}^5-(C_5H_5)Fe(CO)(PPh_3)$ (1) were prepared from ${\alpha},{\beta}-enoyl-{\eta}^5-(C_5H_5)Fe(CO)_2$(2) and triphenylphosphine through a photochemical ligand substitution followed by carbonylation.

New inhibitors of the NF-kB activation and NO production from Artemisia sylvatica

  • Jin, Huizi;Lee, Jeong-Hyung;Lee, Dong-Ho;Kim, Young-Ho;Lee, Jung-Joon
    • Proceedings of the PSK Conference
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    • 2003.10b
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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)

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The Geometrical Isomerization on Acidification in Hexamolybdoheteropoly Oxometalate. The Crystal Structure of $(NH_{4})_{4.5}[H_{3.5}\alpha-PtMo_{6}O_{24}].\;1.5H_{2}O,\;(NH_{4})_{4}[H_{4}\beta-PtMo_{6}O_{24}].\;1.5H_{2}O,\;and\;K_{3.5}[H_{4.5}\alpha-PtMo_{6}O_{24}].\;3H_{2}O$

  • Lee, Uk;Yukiyoshi Sasaki
    • Bulletin of the Korean Chemical Society
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    • v.15 no.1
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    • pp.37-45
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    • 1994
  • $(NH_4)_{4.5}[H_{3.5}{\alpha}-PtMo_6O_{24}]{\cdot}1.5\;H_2O(A),\;(NH_4)_4[H_4{\beta}-PtMo_6O_{24}]{\cdot}1.5\;H_2O(B),\;and\;K_{3.5}[H_{4.5}{\alpha}-PtMo_6O_{24}]{\cdot}3\;H_2O(C)$ have been synthesized and their molecular structures have been also determined by single-crystal X-ray diffraction technique. The space groups, unit cell parameters, and R factors are as follows: Compound A, monoclinic, $A_{2/a}$, a= 19.074 (3), b=21.490 (3), c=15.183 (2) ${\AA};\;{\beta}$=109.67 (1) ${\AA}$; z=8; R=0.075($IF_0I>4{\sigma}(IF_0I);$ Compound B, triclinic, P$bar{1}$, a=10.776 (2), b=15.174 (4), c=10.697 (3) ${\AA};\;{\alpha}$ =126.29 (2), ${\beta}$=111.55 (2), ${\gamma}$=93.18 (2) ${\AA}$; Z=2; R=0.046($IF_0I>3{\sigma}(IF_0I);$): Compound C, triclinic, Pl, a=12.426 (2), b=13.884 (2), c=10.089 (1) ${\AA}$; ${\alpha}$=102.59 (2), ${\beta}$=110.73 (1), ${\gamma}$=53.93 (1) ${\AA}$; Z=2; R=0.074 ($IF_0I>3{\sigma}(IF_0I)$. Compounds A and C contain the well-known Anderson structure (planar structure) heteropoly oxometalate having approximate $bar{3}_m(D_{3d})$ symmetry, while compound B contains the bent structure heteropoly oxometalate having appproximate $2_{mm}(C2_v)$ symmetry. The bent structure and the planar one are geometrical isomers. These compounds are rot only novel heteroply molybdates containing platinate(IV) but also the first example of geometrical isomerism in the hexamolybdoheteropoly oxometalates. That isomerization surprisingly occurred because of the change of only 0.5 non-acidic hydrogen atom attached to the polyanion such as $[H_{3.5}{\alpha} -PtMo_6O_{24}]^{4.5-}{\to}[H_4{\beta}-PtMo_6O_{24}]^{4-}{\to}[H_{4.5}{\alpha} -PtMo_6O_{24}]^{3.5-}$. It seems that the gradual protonation of the polyanion plays an important role in that isomerism. These heteropolyanions form dimers by strong hydrogen bonds between two heteropolyanions in the respective crystal system.