• Title/Summary/Keyword: Rac3

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Lipase Catalyzed Kinetic Resolution of rac-2-(3-Methoxy-4-methylphenyl) propan-1-ol and rac-2-(3-Hydroxy-4-methylphenyl)propyl propanoate for S-(+)-Xanthorrhizol

  • Shafioul, Azam Sharif Mohammed;Cheong, Chan-Seong
    • Bulletin of the Korean Chemical Society
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    • v.33 no.2
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    • pp.409-414
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    • 2012
  • Xanthorrhizol is a bisabolane type of natural sesquiterpene, the major component of essential oils of Curcuma xanthorrhiza. 2-(3-Methoxy-4-methylphenyl)propan-1-ol and 2-(3-hydroxy-4-methyl phenyl)propan-1-ol could be essential building block for enantioselective synthesis of xanthorrhizol. Enantioselective (c = 53%, E = $80{\pm}3$) for R-(+)-2-(3-hydroxy-4-methylphenyl) propan-1-ol and (c = 58%, E = $27{\pm}1$) for R-(+)-2-(3-methoxy-4-methylphenyl) propan-1-ol resolution processes were developed via lipase-catalyzed reaction. We found lipase Aspergillus oryzae (AOL) and Porcine pancreas (PPL) are selective to transesterification and hydrolysis in organic and aqueous phase. Modified demethylated substrate is appropriate for enantioselective hydrolysis reaction without any additives. Enantiopure chiral alcohol was crystallized from ethyl acetate/n-hexane co-solvent system. Gram scale resolved chiral intermediate will facilitate the synthesis of the unnatural S-(+)-xanthorrhizol, the corresponding isomer of the natural one.

Case Study for the Relation between Clinical Bian Zheng and Gastroscopic Bian Zheng of Epigastric Pain (위완통(胃脘痛)의 임상변증(臨床辨證)과 위내시경(胃內視鏡) 미관변증(微觀辨證)의 관계(關係)에 대한 증례(證例) 연구(硏究))

  • Ko, Su-Mi;Mun, Seok-Jae;Moon, Goo
    • The Journal of Korean Medicine
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    • v.17 no.1 s.31
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    • pp.266-279
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    • 1996
  • To complement and develop the Orient Medical Bian Zheng treatmemt(韓方辨證施治), I have observed and analysed 68 persons who have recieved medical treatment because of the epigastric pain. Considering and analysed the Clinical Diagnosis(臨床診斷) and Clinical Bian Zheng(臨床辨證), Clinical Diagnosis(臨床診斷) and Gastroscopic Bian Zheng(微觀辨證), Clinical Bian Zheng(臨床辨證) and Gastroscopic Bian Zheng(微觀辨證), case history, age and sex, I have obtained the conclusion as follows. 1. The frequency of epigastric pain according to the classfication of Clinical Bian Zheng(臨床辨證) most occured in Gi Che Zheng(氣滯證), then in Huh Han Zheng(虛寒證). and least in Wi Youl Zheng. 2. There is no clear connection between the Clinical Bian Zheng(臨床辨證) and Clinical Diagnosis(臨床診斷). 3. The frequency of the epigastric pain according to Gastroscopic Bian Zheng(微觀辨證), mainly occurred in Wi youl Type(胃熱型), Wi Rac Jac Sang Type(胃絡灼傷滯型)and then occurred in Wi Han Type(胃寒型), and least occurred in Wi Rac A Che Type(胃絡瘀滯型) 4. Having observed the relation between the Gastroscopicin Bian Zheng(微觀辨證), and Clinical Diagnosis(臨床診斷) as pathological process, I have obtained the result that Wi Youl type(胃熱型) and Wi Rac Jac Sang Type(胃絡灼傷型) mainly occurred in Erosive Gastritis and Superficial Gastritis at the early stage, and Wi Rac A Che Type(胃絡瘀滯型) occurred in the whole stage among the Wuperficial Gastritis, Atro pic Gastritis, and Erosive Gastritis, Gastric Cancer, and the Wi Han Type(胃寒型) mainly occurred in Atropic Gastritis at the later stage. 5. The relation between Clinical Bian Zheng(臨床辨證) and Gastroscopic Bian Zheng(微觀辨證) do not coincide. 6. Observing the relation between the Clinical Bian Zheng(臨床辨證) and case history, Gi Che Zheng(氣滯證), Huh Han Zheng(虛寒證), Wi Youl Zheng(胃熱證) were commonly seen in the early stage of the case history, and Eum Huh Zheng(陰虛證) and Houl A Zheng(血瘀證) were seen in every stage. 7. Observing the relation between the Clinical Bian Zheng(臨床辨證) and age, Gi Che Type(氣滯型) was mostly seen in the thirties and other Bian Zheng(辨證) was seen after the middle 8. Observing the relation between the Clinical Bian Zheng(臨床辨證) and sex, Gi Che Type(氣滯型) was seen at high ratio in both sexes. 9. Observing the relation between the Gastroscopic Bian Zheng(微觀辨證) and case history Wi Han Type(胃寒證), Wi Youl Type(胃熱型), Wi Rac Jac Sang Type(胃絡灼傷型) were seen in the early stage of the case history Wi Rac A Che Type(胃絡瘀滯型) was mostly seen in the later stage. 10. There was no clear connection between the Gastroscopic Bian Zheng(微觀辨證) and age, sex. Although the examples were not sufficient, recipe regarding the partial variation state of stomach mucos together with Orient Medical Bian Zheng(韓方辨證) treatment seems to be useful in the effective treatment of Bi wi(脾胃) disease besides the epigastric pain.

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Effect of 1-palmitoyl-2-linoleoyl-3-acetyl-rac-glycerol on Immune Functions in Healthy Adults in a Randomized Controlled Trial

  • Hwang, Hee-Jin;Sohn, Ki-Young;Han, Yong-Hae;Chong, Saeho;Yoon, Sun Young;Kim, Young-Jun;Jeong, Jinseoun;Kim, Sang-Hwan;Kim, Jae Wha
    • IMMUNE NETWORK
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    • v.15 no.3
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    • pp.150-160
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    • 2015
  • We previously reported that 1-palmitoyl-2-linoleoyl-3-acetyl-rac-glycerol (PLAG) accelerates hematopoiesis and has an improving effect on animal disease models such as sepsis and asthma. The effects of PLAG supplementation on immune modulation were assessed in healthy men and women. The objective was to evaluate the effects of PLAG supplementation on immune regulatory functions such as activities of immune cells and cytokine production. A randomized double blind placebo-controlled trial was conducted. Seventy-five participants were assigned to one of two groups; all participants had an appropriate number of white blood cells on the testing day. The PLAG group (n=27) received oral PLAG supplements and the control group (n=22) received oral soybean oil supplements. IL-4 and IL-6 production by peripheral blood mononuclear cells (PBMC) were lower (p<0.001 and p<0.001, respectively) with PLAG than with soybean oil. However, the production of IL-2 and IFN-$\gamma$ by PBMC was unaltered with PLAG supplementation. The B cell proliferation decreased significantly in the PLAG group compared to the soybean oil control (p<0.05). The intake of PLAG in healthy adults for 4 weeks was deemed safe. These data suggest that PLAG has an immunomodulatory function that inhibits the excessive immune activity of immunological disorders such as atopic and autoimmune diseases. PLAG could improve the condition of these diseases safely as a health food supplement.

항암제 Ara - C유도체의 합성에 관한 연구

  • ;;;;;;A.J. Kirisits;Rakesh Vig
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1994.04a
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    • pp.167-167
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    • 1994
  • Thioglycerol과 Glycerol을 출발물질로 1번 탄소(C) 위치의 산소(O),또는 황(S)에 octadecyl기로 alkylation한 후, 2번 탄소(C)위치 산소(O)를 palmitoyl기로acetylation시켜 만든 thioether lipid 및 ether lipid유도체를 인산화시킨 rac-1-S-octa-decyl-2-O-palmitoyl-1-S-thioglycerol-3-phosphate (DL-PTBA-P)와 rac-1-O-octadecyl-2-O-palmitoylglycerol-3-phosphate (DL-PBA-P)등을 합성하였다. 이들 thioether lipid 및 ether lipid유도체는 그 자체로도 in vitro와 in vivo에서anti-neoplastic property를 가지고 있는데, 이들 중간체를 핵산 화합물로써 역시 강한 항암 작용에도 불구하고 독성등 부작용이 문제가 되고있는 Ara-C (일명 Cytarabine)의 인산화물인 ara-CMP morpholidate와 conjugation시켜 최종물질로서 ara-CDP-DL-PCA, ara-CDP-DL-PBA, ara-CDP-DL-PTCA 및 ara-CDP-DL-PTBA등을 합성하였다. 이들 중 ara-CDP-DL-PTBA가 본 과제와 관련하여 항암제로서 최종 개발하고자하는 주요 물질인 Cytoros이다.

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Analysis of the dynamic confining effect of CRAC short column under monotonic loadings

  • Wang, Changqing;Xiao, Jianzhuang
    • Structural Engineering and Mechanics
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    • v.74 no.3
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    • pp.351-363
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    • 2020
  • Based on the dynamic tests of recycled aggregate concrete (RAC) short columns confined by the hoop reinforcement, the dynamic failure mechanism and the mechanical parameters related to the constitutive relation of confined recycled aggregate concrete (CRAC) were investigated thoroughly. The fracturing sections were relatively flat and smooth at higher strain rates rather than those at a quasi-static strain rate. With the increasing stirrup volume ratio, the crack mode is transited from splitting crack to slipping crack constrained with large transverse confinement. The compressive peak stress, peak strain, and ultimate strain increase with the increase of stirrup volume ratio, as well as the increasing strain rate. The dynamic confining increase factors of the compressive peak stress, peak strain, and ultimate strain increase by about 33%, 39%, and 103% when the volume ratio of hoop reinforcement is increased from 0 to 2%, but decrease by about 3.7%, 4.2%, and 9.1% when the stirrup spacing is increased from 20mm to 60mm, respectively. This sentence is rephrased as follows: When the stirrup volume ratios are up to 0.675%, and 2%, the contributions of the hoop confinement effect to the dynamic confining increase factors of the compressive peak strain and the compressive peak stress are greater than those of the strain rate effect, respectively. The dynamic confining increase factor (DCIF) models of the compressive peak stress, peak strain, and ultimate strain of CRAC are proposed in the paper. Through the confinement of the hoop reinforcement, the ductility of RAC, which is generally slightly lower than that of NAC, is significantly improved.

Preparation of Reactive Poly(ethylene-ter-1-hexene-ter-divinylbenzene) using Metallocene Catalysts (메탈로센 촉매를 이용한 관능성 Poly(ethylene-ter-1-hexene-ter-divinylbenzene)의 제조)

  • Kim, Dong-Hyun
    • Elastomers and Composites
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    • v.46 no.4
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    • pp.304-310
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    • 2011
  • In this study, we prepared poly(ethylene-ter-1-hexene-ter-divinylbenzene) using briged rac-$Et[Ind]_2ZrCl_2$ or unbriged $Cp_2ZrCl_2$ metallocene catalysts. Bridged rac-$Et[Ind]_2ZrCl_2$ catalyst showed relatively good results compared with unbridged one. When cocatalyst/catalyst molar ratio was 3000, catalytic activity indicated more than 8000(kg of polymer/$mol{\cdot}h$) which was very remarkable value. As a polymerization time increased, the weight-average molecular weight of the terpolymer gradually increased to some degree. In the case of a polymerization time of 50 minutes, the state of the terpolymer became amorphous. The range of the weight-average molecular weight and the densities of the terpolymer was 110,000~200,000 and $0.85{\sim}0.89g/cm^3$, respectively. The thermal properties and the structure of the terpolymer were also identified.

Assessment of Attenuation Correction Techniques with a $^{137}Cs$ Point Source ($^{137}Cs$ 점선원을 이용한 감쇠 보정기법들의 평가)

  • Bong, Jung-Kyun;Kim, Hee-Joung;Son, Hye-Kyoung;Park, Yun-Young;Park, Hae-Joung;Yun, Mi-Jin;Lee, Jong-Doo;Jung, Hae-Jo
    • The Korean Journal of Nuclear Medicine
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    • v.39 no.1
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    • pp.57-68
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    • 2005
  • Purpose: The objective of this study was to assess attenuation correction algorithms with the $^{137}Cs$ point source for the brain positron omission tomography (PET) imaging process. Materials & Methods: Four different types of phantoms were used in this study for testing various types of the attenuation correction techniques. Transmission data of a $^{137}Cs$ point source were acquired after infusing the emission source into phantoms and then the emission data were subsequently acquired in 3D acquisition mode. Scatter corrections were performed with a background tail-fitting algorithm. Emission data were then reconstructed using iterative reconstruction method with a measured (MAC), elliptical (ELAC), segmented (SAC) and remapping (RAC) attenuation correction, respectively. Reconstructed images were then both qualitatively and quantitatively assessed. In addition, reconstructed images of a normal subject were assessed by nuclear medicine physicians. Subtracted images were also compared. Results: ELEC, SAC, and RAC provided a uniform phantom image with less noise for a cylindrical phantom. In contrast, a decrease in intensity at the central portion of the attenuation map was noticed at the result of the MAC. Reconstructed images of Jaszack and Hoffan phantoms presented better quality with RAC and SAC. The attenuation of a skull on images of the normal subject was clearly noticed and the attenuation correction without considering the attenuation of the skull resulted in artificial defects on images of the brain. Conclusion: the complicated and improved attenuation correction methods were needed to obtain the better accuracy of the quantitative brain PET images.

Induction of the Nuclear Proto-Oncogene c-fos by the Phorbol Ester TPA and c-H-Ras

  • Kazi, Julhash U.;Soh, Jae-Won
    • Molecules and Cells
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    • v.26 no.5
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    • pp.462-467
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    • 2008
  • TPA is known to cooperate with an activated Ras oncogene in the transformation of rodent fibroblasts, but the biochemical mechanisms responsible for this effect have not been established. In the present study we used c-fos promoter-luciferase constructs as reporters, in transient transfection assays, in NIH3T3 cells to assess the mechanism of this cooperation. We found a marked synergistic interaction between TPA and a transfected v-Ha-ras oncogene in the activation of c-fos promoter and SRE. SRE has binding sites for TCF and SRF. A dominant-negative Ras (ras-N17) inhibited the TPA-Ras synergy by blocking the PKC-MAPK-TCF pathway. Dominant-negative RhoA and Rac1 (but not Cdc42Hs) inhibited the TPA-Ras synergy by blocking the Ras-Rho-SRF signaling pathway. Constitutively active $PKC{\alpha}$ and $PKC{\varepsilon}$ showed synergy with v-Ras. These results suggest that the activation of two distinct pathways such as Ras-Raf-ERK-TCF pathway and Rho-SRF pathway are responsible for the induction of c-fos by TPA and Ras in mitogenic signaling pathways.