• Title/Summary/Keyword: 5-hydroxy-2-methyl-1

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Effects of NMDA, AMPA and Kainate on the Release of Acetylcholine in Rat Hippocampal and Striatal Slices

  • Kim, Do Kyung;Lee, Se-Oul;Jung, Kyu-Yong;Kim, Jong-Keun;Choi, Bong-Kyu
    • The Korean Journal of Physiology and Pharmacology
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    • v.8 no.6
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    • pp.301-305
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    • 2004
  • This study examined the effects of N-methyl-D-aspartate (NMDA), ${\alpha}-amino$-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) and kainate on basal and electrically-evoked release of acetylcholine (ACh) from the rat hippocampal and striatal slices which were preincubated with $[^3H]choline$. Unexpectedly, the basal and evoked ACh release were not affected at all by the treatment with NMDA $(3{\sim}100{\mu}M)$, AMPA $(1{\sim}100{\mu}M)$ or kainate $(1{\sim}100{\mu}M)$ in hippocampal slices. However, in striatal slices, under the $Mg^{2+}-free$ medium, $30{\mu}M$ NMDA increased the basal ACh release with significant decrease of the electrically-evoked releases. The treatment with $1{\mu}M MK-801 not only reversed the $30{\mu}M$ NMDA-induced decrease of the evoked ACh release, but also attenuated the facilitatory effect of $30\;{\mu}M$ NMDA on the basal ACh release. The treatment with either $30\;{\mu}M$ AMPA or $100\;{\mu}M$ kainate increased the basal ACh release without any effects on the evoked release. The treatment with $10{\mu}M$ NBQX abolished the AMPA- or kainate-induced increase of the basal ACh release. Interestingly, NBQX significantly attenuated the evoked release when it was treated with AMPA, although it did not affect the evoked release alone without AMPA. These observations demonstrate that in hippocampal slices, ionotropic glutamate receptors do not modulate the ACh release in cholinergic terminals, whereas in striatal slices, activations of ionotropic glutamate receptors increase the basal ACh release though NMDA may decrease the electrically-evoked ACh release.

A Study on the Synthesis and Properties of Environmental Friendly Pressure Sensitive Adhesive for Manufacturing Electronic Products (전자제품 제조용 친환경 점착제의 합성과 물성에 대한 연구)

  • Cho, Ur Ryong;Oh, Ji Hwan;Kim, Ji Hyun;Jung, Hyeon Jeong
    • Journal of the Semiconductor & Display Technology
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    • v.15 no.1
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    • pp.12-16
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    • 2016
  • Toluene-free pressure sensitive adhesives were synthesized by using butyl acrylate (BA), 2-hydroxy ethyl acrylate, methyl methacrylate, acrylic acid (AA) as monomers and ethyl acetate as a solvent. The polymerization recipes were designed by changing 1, 3, 5 part per hundreds monomer (phm) of AA content on the basis of 100 BA parts. Two crosslinking agents, ethyl glycol diglycidyl ether (EDGE) and isophorone diisocyanate (IPDI) were added to the synthesized polymers to increase adhesion due to crosslinking. In the measurement of properties, holding power, peel strength, and initial tackiness increased with AA content due to crosslinking between carboxyl group in AA and epoxy group in EDGE and isocyanate group in IPDI. In the comparison of two crosslinking agents, EDGE showed better in the three properties than IPDI by better reaction of epoxy group of EDGE to carboxyl group of AA.

ent-Kaurane- and ent-Pimarane-Type Diterpenoids from Siegesbeckia pubescens and Their Cytotoxicity in Caki Cells

  • Lee Sanghyun;Noh Eun Jung;Kim Jung Sook;Son Eun Mi;Pan Xu;Kim Yeong Shik;Kim Bak-Kwang;Lee Burm-Jong
    • KOREAN JOURNAL OF CROP SCIENCE
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    • v.50 no.2
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    • pp.147-150
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    • 2005
  • ent-Kaurane- and ent-pimarane-type diterpenoids were isolated from the methanol extract of Siegesbeckia pubescens by column chromatography. Their structures were elucidated as ent-16$\alpha$H,17-hydroxy-kau­ran-19-oic acid (1), ent-4,17-dihydroxy-16$\alpha$-methyl-kau­ran-19-oic acid (2), ent-16$\beta$,17-dihydroxy-kauran-19-oic acid (3), kirenol (4) and ent-16$\beta$,17,18-trihydroxy-kauran­19-oic acid (5) by spectral analysis. The cytotoxicity of these compounds in Caki cells was assayed by a cell counting kit. Only one group treated with kirenol (4), an entpimarane-type diterpenoid, showed the inhibition of the cell growth in Caki cells.

New hydroperoxylated and 20,24-epoxylated dammarane triterpenes from the rot roots of Panax notoginseng

  • Shang, Jia-Huan;Sun, Wen-Jie;Zhu, Hong-Tao;Wang, Dong;Yang, Chong-Ren;Zhang, Ying-Jun
    • Journal of Ginseng Research
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    • v.44 no.3
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    • pp.405-412
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    • 2020
  • Background: Root rot is a serious destructive disease of Panax notoginseng, a famous cultivated araliaceous herb called Sanqi or Tianqi in Southwest China. Methods: The chemical substances of Sanqi rot roots were explored by chromatographic techniques. MS, 1D/2D-NMR, and single crystal X-ray diffraction were applied to determine the structures. Murine macrophage RAW264.7 and five human cancer cell lines were used separately for evaluating the antiinflammatory and cytotoxic activities. Results and Conclusion: Thirty dammarane-type triterpenes and saponins were isolated from the rot roots of P. notoginseng. Among them, seven triterpenes, namely, 20(S)-dammar-25-ene-24(S)-hydroperoxyl-3β,6α,12β,20-tetrol (1), 20(S)-dammar-3-oxo-23-ene-25-hydroperoxyl-6α,12β,20-triol (2), 20(S)-dammar-12-oxo-23-ene-25-hydroperoxyl-3β,6α,20-triol (3), 20(S)-dammar-3-oxo-23-ene-25-hydroperoxyl-12β,20-diol (4), 20(S),24(R)-epoxy-3,4-seco-dammar-25-hydroxy-12-one-3-oic acid (5), 20(S),24(R)-epoxy-3,4-seco-dammar-25-hydroxy-12-one-3-oic acid methyl ester (6), and 6α-hydroxy-22,23,24,25,26,27-hexanordammar-3,12,20-trione (7), are new compounds. In addition, 12 known ones (12-16 and 19-25) were reported in Sanqi for the first time. The new Compound 1 showed comparable antiinflammatory activity on inhibition of NO production to the positive control, whereas the known compounds 9, 12, 13, and 16 displayed moderate cytotoxicities against five human cancer cell lines. The results will provide scientific basis for understanding the chemical constituents of Sanqi rot roots and new candidates for searching antiinflammatory and antitumor agents.

Photochemical Reductions of Benzil and Benzoin in the Presence of Triethylamine and TiO? Photocatalyst

  • Park, Joon-Woo;Kim, Eun-Kyung;Koh Park, Kwang-Hee
    • Bulletin of the Korean Chemical Society
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    • v.23 no.9
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    • pp.1229-1258
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    • 2002
  • This paper reports the photochemical reduction of benzil 1 to benzoin 2 and the reduction of 2 to hydrobenzoin 4 in deoxygenated solvents in the presence of triethylamine (TEA) and/or TiO2. Without TEA or TiO2, the photolysis of 1 resulted in very low yield of 2. The presence of TEA or TiO2 increased the rate of disappearance of 1 and the yield of 2, which were further increased considerably by the presence of water. The photoreduction of 1 to 2 proceeds through an electron transfer to 1 from TEA or hole-scavenged excited TiO2 followed by protonation. In the reaction medium of 88 : 7 : 2 : 3 CH3CN/CH3OH/H2O/TEA with 2.5 $㎎/m{\ell}$ of TiO2, the yield of 2 was as high as 85 % at 50 % conversion of 1. The photolysis of 2 in homogeneous media resulted in photo-cleavage to benzoyl and hydroxybenzyl radicals, which are mostly converted to benzaldehyde. The reduction product 4 is formed in low yield through the dimerization of hydroxybenzyl radicals. The addition of TEA increased the conversion rate of 2 and the yield of 4 significantly. This was attributed to the scavenging effect of TEA for benzoyl radical to produce N,N-diethylbenzamide and the photoreduction of benzaldehyde in the presence of TEA. The ratio of $(\pm)$ and meso isomers of 4 obtained from the photochemical reaction is about 1.1. This ratio is the same as that from the photochemical reduction of benzaldehyde in the presence of TEA. In the TiO2-sensitized photochemical reduction of 2, meso-4 was obtained in moderate yield. The reduction of 2 to 4 proceeds through two consecutive electron/proton transfer processes on the surface of the photocatalyst without involvement of ${\alpha}-cleavage$. The radical 11 initially formed from 2 by one electron/proton process can also combine with hydroxy methyl radical, which is generated after hole trapping of excited TiO2 by methanol, to produce 1,2-diphenylpropenone after dehydration reaction.

Potent Anticarcinogenic Action of Moutan radix for Mouse Ascites Cancer Induced by Mouse Sarcoma 180 Cells (Moutan radix의 mouse sarcoma 180 cell로 유발한 mouse ascites cancer에 대한 항암효과)

  • Bahn, Kyeong-N.;Lee, Eun-J.;Yang, Min-S.;Kim, Jeong-O.;Ha, Yeong-L.
    • Applied Biological Chemistry
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    • v.38 no.4
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    • pp.364-369
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    • 1995
  • Anticarcinogenic activity of Moutan radix for mouse ascites cancer induced by mouse Sarcoma 180 (S-180) cells was investigated. Methanol extract of Moutan radix including other folk medicinal plants (Taxus cuspidata, Curcuma longa, Artemisia capillaris, Ligrstri fructus, and Liriope platyphylla) used to remedy or cure many chronic human diseases like cancer was fractionated into hexane, chloroform ($CHCl_3$), ethylacetate (EtOAc), and butanol (BuOH) fractions. Anticarcinogenic activity of the fractions, exhibited a strong cytotoxicity for L1210 and S-180 cells, was examined for mouse ascites cancer induced by S-180 cells. Male ICR mice (7 mice/treatment, $5{\sim}6$ weeks of age, $23{\pm}1\;g$ were injected i.p. with S-180 cells ($1{\times}10^{7}\;cell/1\;ml$ PBS). One day later, each mouse was given 0.1 ml of 10% DMSO containing sample ($30\;{\mu}g/g$ body weight) every day for 10 consecutive days. Control mice were only given 0.1ml S-180 cells and 0.1 ml 10% DMSO. Mice treated with EtOAc fraction of Moutan radix showed 28.7 days of life, which is 167% of control mice's life. Based on the dose-dependant experiment mice treated with $30\;{\mu}g$ showed longer life relative to mice treated with ootherr doses (5, 15, $60\;{\mu}g$), and mice treated with $60\;{\mu}g$ exhibited toxic symptoms. Body weight of mice treated with Moutan radix was significantly reduced relative to that of control mice (p<0.05). GC-MS analysis in conjunction with silica-gel column chromatography revealed that the EtOAc fraction contained 2-methoxylphenol, benzoic acid, 1-(4-hydroxy-3-methoxyphenyl)ethanone, 8-methyl-2,4(1H,3H)pteridinedione and 2,5-furan-dicarboxylic dimethyl ester as regards to the anticarcinogenic property of the EtOAc fraction. These results suggest that Moutan radix might be included as an anticarcinogenic medicinal plant for treatment of ascites cancer.

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Ethanol extract of Sinsun-yukza-hwan, a Korean medicinal prescription, promotes hair growth in C57BL/6 mice, an alopecia animal model

  • Kim, Ji Yoon;Kim, Mi Ryeo
    • The Korea Journal of Herbology
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    • v.33 no.3
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    • pp.1-9
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    • 2018
  • Objectives : In Korean medicine, a prescription of Sinsun-yukza-hwan (Shenxian-liuzi-wan, SSY) has been used in clinic for treatment of alopecia via oral. This study was performed to determine transdermal effects of the ethanol extract from SSY on hair growth and -related gene expressions in mice. Methods : We analyzed index compound, 5-hydroxy-methyl-2-furaldehyde (HMF), in SSY extract by ultra performance liquid chromatography (UPLC). 6 weeks old C57BL/6 mice with removed hair were used as an alopecia animal model. Mice were divided into 3 experimental groups including normal (3 water: 1 ethanol: 2 polyethylene glycol mixture as a vehicle), SSY extract and 5% minoxidil (as a positive control), treated groups. SSY was applied topically on the hair-shaved skin of C57BL/6 mice every day for 15 days. The color, thickness and density of hair were monitored every $5^{th}$ day by naked eye, photograph and phototrichogram using folliscope. Also hair growth-associated gene expressions were measured by immunoblotting assay. Results : Hair density of minoxidil or SSY-treated group was significantly increased compared to that of vehicle application on the $15^{th}$ day, respectively. And hair thickness of minoxidil and SSY groups was increased compared to that of vehicle treated group on the $15^{th}$ day, respectively. Induction of insulin-like-growth factor 1(IGF-1) and vascular endothelial growth factor (VEGF) were also significantly accelerated by SSY extract compared to those of vehicle-applied group. Conclusions : These results provide scientific evidence to support the potent multi-application of SSY as a cosmeceutical material for promoting hair growth.

The Chemopreventive Effect of Sodium Selenite on Colon Carcinogenesis in Medium-Term Multi-Organ Bioassay (다장기 중기발암성 시험법을 이용한 셀렌염의 대장암 억제효과에 대한 연구)

  • Han, Beom-Seok;Hong, Choong-Man;Shin, Dong-Hwan;Lee, Kook-Kyung;Ahn, Byeong-Woo;Jang, Dong-Deuk
    • Korean Journal of Veterinary Pathology
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    • v.5 no.1
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    • pp.23-28
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    • 2001
  • This study was conducted to assess the chemopreventive effects of sodium selenite in the rat medium-term multi-organ bioassay using a DMBDD model (DEN+MNU+BBN+DMH+DHPN). Seventy five,6-week-old, male SD rats were divided into 3 groups. The animals in group 1 received DEN(diethylnitrosamine,100 mg/kg bw, single i.p., in saline), MNU (N-methyl-nitrosourea,20 mg/kg bw, i.p.,4 times for 2 weeks), BBN (N-butyl-N-(4-hydroxybutyl) nitrosamine, 0.2% in drinking water for 2 weeks), DMH (1,2-dimethylhydrazine, 40 mg/kg bw, s.c., in saline.4 times (or 2 weeds), and DHPN (N-bis(2-hydroxy-pro-pal)nitrosamine,0.1% in drinking water for 2 weeks), then were placed on sodium selenite (4 ppm in drinking water) for 22 weeks from weeks 4 to 26. The animals in group 2 were given DMBDD alone. The animals in group 3 were given sodium selenite alone. Animals were sacrificed at week 12 for ACF quantitative analysis and at week 26 for tumor induction. The body weights in the group 1 were significantly decreased compared with those of group 2. The tumor multiplicities of large intestine in the group 1 were significantly decreased compared with those of group 2 (P<0.05). These results indicate that sodium selenite may have a potential as chemopreventive agents of colon carcinogenesis.

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Preparation of Liquefied Cellulose and Analysis of Its Components by GC-MS Spectrometry (액화셀룰로오스의 제조 및 GC-MS에 의한 그 성분 분석)

  • 조국란;황병호;공영토;도금현
    • Journal of Korea Foresty Energy
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    • v.19 no.2
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    • pp.86-92
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    • 2000
  • The liquefactions of $\alpha$-cellulose(Sigma Chemical, C-8002, 47H0383) was prepared in the presence of phenol using sulfuric acid as a catalyst under $N_2$ gas protection at $180^{\circ}C$ for 60minutes to examine its components. The ratio of $\alpha$-cellulose to phenol was 1: 6.2(w/w), and that to sulfuric acid was 1: 0.05(g/$m\ell$). The yields of liquefaction were calculated after the liquefied mixtures were passed through 1G4 glass filter. The luquefied product of $\alpha$-cellulose was analyzed using GC-MS Spectormeter. The 12 compounds identified by GC-MS Spectrometer, of which peak area covers 54% as 2,4-dimethyl phenol, p-isopropyl phenol, 1-ethyl-3,5-dimethyl benzene, o-isopropyl phenol, (E)-2,4\` dihydroxy-stilbene, 2,2\`-methylene-bisphenol, 4,4\`-methylenebisphenol, 3-methyl-2-hydroxyphenyl-(E)-2-hydroxyl-4\`-methoxy-stilbene, 1-phyenyl-1-(4\`hydroxyphenyl)methanol phenol derivatives. From this results, the reaction pathways of the liquefaction of cellulose were proposed through electrophilic substitution reaction. Phenol as a solvent might react with the reaction intermediates as well in the cellulose liquefaction.

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Chemical Constituents of Nauclea vanderguchtii

  • Nkouayeb, Brice Maxime Nangmou;Azebaze, Anatole Guy Blaise;Tabekoueng, Georges Bellier;Tsopgni, Willifred Dongmo Tekapi;Lenta, Bruno Ndjakou;Frese, Marcel;Sewald, Norbert;Vardamides, Juliette Catherine
    • Natural Product Sciences
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    • v.26 no.2
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    • pp.144-150
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    • 2020
  • Phytochemical investigation of leaves, barks and roots of Nauclea vanderguchtii led to the isolation of sixteen compounds, which includes one citric acid derivative (2), one alkaloid (16), one peptide derivative (3), and twelve triterpenes (1, 4 - 13). These compounds were identified as rotundanonic acid (1), 2-hydroxy-1,2,3-propanetricarboxylic acid 2-methyl ester (2), asperphenamate (3), lupeol (4), stigmasterol (5), betulin (6), betulenic acid (7), stigmasterol 3-O-β-D-glucopyranoside (8), quinovic acid 3β-O-α-L-rhamnoside (9), α-amyrin (10), 3-oxoquinovic acid (11), ursolic acid (12), hederagenin (13), rotundic acid (14), clethric acid (15), and naucleficine (16) by the analysis of their NMR spectroscopic data including 2D NMR spectra and by comparison of their spectroscopic data reported in the literature. Compounds 1 and 3 were isolated for the first time in the genus Nauclea, and compound 2 was isolated for the first time from the Rubiaceae family. Complete NMR assignations for 1 have been published for the first time.