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Archives of pharmacal research : a publication of ... 23건

  1. [국내논문]   Synthesis of Polymeric Thiazolidinediones and L-Ascorbic Acid Towards the Development of Insulin-Sensitizer  

    Lee Sun Mi (College of Pharmacy, Sookmyung Women's University ) , Jeon Raok (College of Pharmacy, Sookmyung Women's University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.28 no.4 ,pp. 377 - 381 , 2005 , 0253-6269 ,

    초록

    Polymers, containing 5-(4-O-methylacryloylbenzyl)thiazolidine-2,4-dione [MABTZD]; poly (MABTZD), poly(MABTZD-co-AA) and poly(MABTZD-co-AMAA), were prepared, and identified by FT-IR, $^1H-$ and $^{13}C-NMR$ spectra. The MABTZD unit contents in poly(MABTZD-co-AA) and poly(MABZD-co-AMAA) were 11.3 and $27.7 mol\%$ , respectively. The number average molecular weights of the polymers, as determined by GPC, ranged from 16,800 to 22,300, and with polydispersity indices of $1.2\sim1.4$ .

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  2. [국내논문]   Diastereoselective Synthesis of Unsaturated 1,4-Amino Alcohols as a Biologically Important Moiety  

    Jung Young Hoon (Organic & Medicinal Chemistry Laboratory, College of Pharmacy, Sungkyunkwan University ) , Kim Ji Duck (Organic & Medicinal Chemistry Laboratory, College of Pharmacy, Sungkyunkwan University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.28 no.4 ,pp. 382 - 390 , 2005 , 0253-6269 ,

    초록

    chial allylic ethers with a hydroxyl group attached to the $\pi-system$ and chlorosulfonyl isocyanate. The enantioselectivity of the CSI reaction with the chiral allylic and benzylic ethers was examined in various solvents and temperatures. Based on these results, it was proposed that the CSI reaction is a competitive reaction of a $S_{N}i$ (retention) and a $S_{N}1$ mechanism (racemization) according to the stability of the carbocation intermediate. This means that there is a greater proportion of retention with the less stable the carbocation intermediate and vise versa.

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  3. [국내논문]   Synthesis of 3-Alkylthio-6-Allylthiopyridazine Derivatives and Their Antihepatocarcinoma Activity   피인용횟수: 1

    Kwon Soon-Kyoung (College of Pharmacy, Duksung Women's University ) , Moon Aree (College of Pharmacy, Duksung Women's University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.28 no.4 ,pp. 391 - 394 , 2005 , 0253-6269 ,

    초록

    The allylthio group of allicin and other organosulfur compounds, isolated from garlic, is considered a pharmacophore, and a key structure component of the molecule, which affords biological activities. In the foregoing studies, various 3-alkoxy-6-allylthiopyridazine derivatives (K­compounds) were synthesized, and their biological activities tested in animals. As expected, the various derivatives showed good hepatoprotective activities on carbon tetrachloride-treated mice and aflatoxin B1-treated rats, and chemopreventive activities on hepatocarcinoma cells in rats. Other new pyridazine derivatives, with the oxygen atom at the 3-position of the 3-alkoxy­6-allylthiopyridazine displaced by sulfur (S), were synthesized, and their activities tested in vitro. Thio-K6, one of the sulfur-substituted compounds, showed better chemopreventive activity toward hepatocarcinoma cells.

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    회원님의 원문열람 권한에 따라 열람이 불가능 할 수 있으며 권한이 없는 경우 해당 사이트의 정책에 따라 회원가입 및 유료구매가 필요할 수 있습니다.이동하는 사이트에서의 모든 정보이용은 NDSL과 무관합니다.

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  4. [국내논문]   Antiinflammatory Constituents from the Roots of Smilax bockii warb.   피인용횟수: 1

    Xu Jing (Research Department of Natural Medicine, Shenyang Pharmaceutical University ) , Li Xian (Research Department of Natural Medicine, Shenyang Pharmaceutical University ) , Zhang Peng (Research Department of Natural Medicine, Shenyang Pharmaceutical University ) , Li Zhan-Lin (Research Department of Natural Medicine, Shenyang Pharmaceutical University ) , Wang Yi (Research Department of Natural Medicine, Shenyang Pharmaceutical University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.28 no.4 ,pp. 395 - 399 , 2005 , 0253-6269 ,

    초록

    From $70\%$ ethanol extract of the roots of Smilax bockii warb., seven flavonoids, kaempferol (1), $kaempferol-7-O-\beta-D-glucopyranoside$ (2), quercetin (3), isorhamnetin (4), (+)-dihydro­kaempferol (5), engeletin (6), isoengeletin (7), and $n-butyl-\beta-D-fructopyranoside$ (8), caffeic acid n-butyl ester (9) were isolated and identified by means of chemical and spectroscopic. Compounds 2, 4, and 6-9 were isolated for the first time from the roots of S. bockii and compounds 2, 8, and 9 were firstly isolated from the genus Smilax. In addition, using the SEAP (Secreted alkaline phosphatase) assay system, we investigated the in vitro anti-inflammatory activity of the $70\%$ ethanol extract of the roots of S. bockii, which showed moderate activity in inhibiting $TNF-\alpha-induced NF-{\kappa}B$ activation with an $IC_{50}$ value of $166.6 {\mu}g/mL$ .

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  5. [국내논문]   Monoamine Oxidase Inhibitory Naphthoquinones from the Roots of Lithospermum erythrorhizon   피인용횟수: 1

    Choi Woo Hoi (College of Pharmacy, Chungbuk National University ) , Hong Seong Su (College of Pharmacy, Chungbuk National University ) , Lee Seon A (College of Pharmacy, Chungbuk National University ) , Han Xiang Hua (College of Pharmacy, Chungbuk National University ) , Lee Kyong Soon (College of Pharmacy, Chungbuk National University ) , Lee Myung Koo (College of Pharmacy, Chungbuk National University, Research Center for Biore-source and Health, Chungbuk National University ) , Hwang Bang Yeon (College of Pharmacy, Chungbuk National University ) , Ro Jai Seup (College of Pharmacy, Chungbuk National University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.28 no.4 ,pp. 400 - 404 , 2005 , 0253-6269 ,

    초록

    Activity-guided fractionation of a hexane-soluble extract of the roots of Lithospermum erythrorhizon, using a mouse brain monoamine oxidase (MAO) inhibition assay, led to the isolation of two known naphthoquinones, acetylshikonin and shikonin, and a furylhydroquinone, shikonofuran E. These compounds were shown to inhibit MAO with $IC_{50}$ values of 10.0, 13.3, and $59.1 {\mu}M$ , respectively. Although no specificity for MAO-A and MAO-B was shown by acetylshikonin and shikonin, a Lineweaver-Burk plot analysis indicated that the inhibition was competitive for both MAO-A and MAO-B activity.

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  6. [국내논문]   Sensitization of Vanilloid Receptor Involves an Increase in the Phosphorylated Form of the Channel  

    Lee Soon-Youl (Department of Genomic Engineering, Genetic Informatics Center, GRRC ) , Lee Jae-Hag (Department of Food and Nutrition, Seoil College ) , Kang Kwon Kyoo (Department of Horticulture, Hankyong National University ) , Hwang Sue-Yun (Graduate School of Bio & Information Technology, Hankyong National University ) , Choi Kang Duk (Graduate School of Bio & Information Technology, Hankyong National University ) , Oh Uhtaek (The Sensory Research Center, National Creative Research Initiatives, College of Pharmacy, Seoul National University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.28 no.4 ,pp. 405 - 412 , 2005 , 0253-6269 ,

    초록

    A vanilloid receptor (VR1, now known as TRPV1) is an ion channel activated by vanilloids, including capsaicin (CAP) and resiniferatoxin (RTX), which are pungent ingredients of plants. Putative endogenous activators (anandamide and metabolites of arachidonic acid) are weak activators of VR1 compared to capsaicin and RTX, and the concentrations of the physiological condition of those activators are not sufficient to induce significant activation of VR1. One way to overcome the weak activation of endogenous activators would be the sensitization of VR1, with the phosphorylation of the channel being one possibility. The phosphorylation of VR1 by several kinases has been reported, mostly by indirect evidence. Here, using an in vivo phosphorylation method, the VR1 channel was shown to be sensitized by phosphorylation of the channel itself by multiple pathways involving PKA, PKC and acid. Also, in sensitizing VR1, BK appeared to show activation of PKC for the sensitization of VR1 by phosphorylation of the channel.

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    NDSL에서는 해당 원문을 복사서비스하고 있습니다. 아래의 원문복사신청 또는 장바구니담기를 통하여 원문복사서비스 이용이 가능합니다.

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  7. [국내논문]   Effect of calmodulin on ginseng saponin-induced Ca2+-Activated CI-channel activation inXenopus laevis oocytes  

    Lee, Jun-Ho , Jeong, Sang-Min , Lee, Byung-Hwan , Kim, Jong-Hoon , Ko, Sung-Ryong , Kim, Seung-Hwan , Lee, Sang-Mok , Nah, Seung-Yeol
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.28 no.4 ,pp. 413 - 420 , 2005 , 0253-6269 ,

    초록

    A vanilloid receptor (VR1, now known as TRPV1) is an ion channel activated by vanilloids, including capsaicin (CAP) and resiniferatoxin (RTX), which are pungent ingredients of plants. Putative endogenous activators (anandamide and metabolites of arachidonic acid) are weak activators of VR1 compared to capsaicin and RTX, and the concentrations of the physiological condition of those activators are not sufficient to induce significant activation of VR1. One way to overcome the weak activation of endogenous activators would be the sensitization of VR1, with the phosphorylation of the channel being one possibility. The phosphorylation of VR1 by several kinases has been reported, mostly by indirect evidence. Here, using an in vivo phosphorylation method, the VR1 channel was shown to be sensitized by phosphorylation of the channel itself by multiple pathways involving PKA, PKC and acid. Also, in sensitizing VR1, BK appeared to show activation of PKC for the sensitization of VR1 by phosphorylation of the channel.

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    회원님의 원문열람 권한에 따라 열람이 불가능 할 수 있으며 권한이 없는 경우 해당 사이트의 정책에 따라 회원가입 및 유료구매가 필요할 수 있습니다.이동하는 사이트에서의 모든 정보이용은 NDSL과 무관합니다.

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  8. [국내논문]   Effect of Calmodulin on Ginseng Saponin-Induced $Ca^{2+}$-Activated $Cl^{-}$ Channel Activation in Xenopus laevis Oocytes   피인용횟수: 1

    Lee Jun-Ho (Research Laboratory for the Study of Ginseng Signal Transduction and Department of Physiology, College of Veterinary Medicine, Konkuk University ) , Jeong Sang-Min (Research Laboratory for the Study of Ginseng Signal Transduction and Department of Physiology, College of Veterinary Medicine, Konkuk University ) , Lee Byung-Hwan (Research Laboratory for the Study of Ginseng Signal Transduction and Department of Physiology, College of Veterinary Medicine, Konkuk University ) , Kim Jong-Hoon (Research Laboratory for the Study of Ginseng Signal Transduction and Department of Physiology, College of Veterinary Medicine, Konkuk University ) , Ko Sung-Ryong (KT & G Central Research Institute ) , Kim Seung-Hwan (Department of Exercise Science, College of Natural Science, Chungbuk National University ) , Lee Sang-Mok (Research Laboratory for the Study of Ginseng Signal Transduction and Department of Physiology, College of Veterinary Medicine, Konkuk University ) , Nah Seung-Yeol (Research Laboratory for the Study of Ginseng Signal Transduction and Department of Physiology, College of Veterinary Medicine, Konkuk Univ)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.28 no.4 ,pp. 413 - 420 , 2005 , 0253-6269 ,

    초록

    We previously demonstrated the ability of ginseng saponins (active ingredients of Panax ginseng) to enhance $Ca^{2+}$ -activated $Cl^{-}$ current. The mechanism for this ginseng saponin-induced enhancement was proposed to be the release of $Ca^{2+}$ from $IP_{3}-sensitive$ intracellular stores through the activation of PTX-insensitive $G\alpha_{q/11}$ proteins and PLC pathway. Recent studies have shown that calmodulin (CaM) regulates $IP_{3}$ receptor-mediated $Ca^{2+}$ release in both $Ca^{2+}-dependent$ and -independent manner. In the present study, we have investigated the effects of CaM on ginseng saponin-induced $Ca^{2+}$ -activated $Cl^{-}$ current responses in Xenopus oocytes. Intraoocyte injection of CaM inhibited ginseng saponin-induced $Ca^{2+}$ -activated $Cl^{-}$ current enhancement, whereas co-injection of calmidazolium, a CaM antagonist, with CaM blocked CaM action. The inhibitory effect of CaM on ginseng saponin-induced $Ca^{2+}$ -activated $Cl^{-}$ current enhancement was dose- and time-dependent, with an $IC_{50} of 14.9\pm3.5 {\mu}M$ . The inhibitory effect of CaM on saponin's activity was maximal after 6 h of intraoocyte injection of CaM, and after 48 h the activity of saponin recovered to control level. The half-recovery time was calculated to be $16.7\pm4.3 h$ . Intraoocyte injection of CaM inhibited $Ca^{2+}$ -induced $Ca^{2+}$ -activated $Cl^{-}$ current enhancement and also attenuated $IP_{3}$ -induced $Ca^{2+}$ -activated $Cl^{-}$ current enhancement. $Ca^{2+}$ /CaM kinase II inhibitor did not inhibit CaM-caused attenuation of ginseng saponin-induced $Ca^{2+}$ -activated $Cl^{-}$ current enhancement. These results suggest that CaM regulates ginseng saponin effect on $Ca^{2+}$ -activated $Cl^{-}$ current enhancement via $Ca^{2+}$ -independent manner.

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    NDSL에서는 해당 원문을 복사서비스하고 있습니다. 아래의 원문복사신청 또는 장바구니담기를 통하여 원문복사서비스 이용이 가능합니다.

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  9. [국내논문]   Reabsorption of Neutral Amino Acids Mediated by Amino Acid Transporter LAT2 and TAT1 in The Basolateral Membrane of Proximal Tubule  

    Park Sun Young (Department of Pediatrics, Kwangju Christian Hospital ) , Kim Jong-Keun (Department of Pharmacology, Chonnam National University Medical School ) , Kim In Jin (Department of Oral Physiology, Chosun University College of Dentistry ) , Choi Bong Kyu (Department of Pharmacology, Wonkwang University School of Medicine ) , Jung Kyu Yong (Department of Pharmacology, Wonkwang University School of Medicine ) , Lee Seoul (Department of Pharmacology, Wonkwang University School of Medicine ) , Park Kyung Jin (Department of Oral Physiology, Chosun University College of Dentistry ) , Chairoungdua Arthit (Department of Pharmacology and Toxicology, Kyorin University School of Medicine ) , Kanai Yoshikatsu (Department of Pharmacology and Toxicology, Kyorin University School of Medicine ) , Endou Hitoshi (Department of Pharmacology and Toxicology, Kyorin University School of Medicine ) , Kim Do Kyung (Department of Oral Physiology, Chosun University College of Dentistry)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.28 no.4 ,pp. 421 - 432 , 2005 , 0253-6269 ,

    초록

    In order to understand the renal reabsorption mechanism of neutral amino acids via amino acid transporters, we have isolated human L-type amino acid transporter 2 (hLAT2) and human T-type amino acid transporter 1 (hTAT1) in human, then, we have examined and compared the gene structures, the functional characterizations and the localization in human kidney. Northern blot analysis showed that hLAT2 mRNA was expressed at high levels in the heart, brain, placenta, kidney, spleen, prostate, testis, ovary, lymph node and the fetal liver. The hTAT1 mRNA was detected at high levels in the heart, placenta, liver, skeletal muscle, kidney, pancreas, spleen, thymus and prostate. Immunohistochemical analysis on the human kidney revealed that the hLAT2 and hTAT1 proteins coexist in the basolateral membrane of the renal proximal tubules. The hLAT2 transports all neutral amino acids and hTAT1 transports aromatic amino acids. The basolateral location of the hLAT2 and hTAT1 proteins in the renal proximal tubule as well as the amino acid transport activity of hLAT2 and hTAT1 suggests that these transporters contribute to the renal reabsorption of neutral and aromatic amino acids in the basolateral domain of epithelial proximal tubule cells, respectively. Therefore, LAT2 and TAT1 play essential roles in the reabsorption of neutral amino acids from the epithelial cells to the blood stream in the kidney. Because LAT2 and TAT1 are essential to the efficient absorption of neutral amino acids from the kidney, their defects might be involved in the pathogenesis of disorders caused by a disruption in amino acid absorption such as blue diaper syndrome.

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    NDSL에서는 해당 원문을 복사서비스하고 있습니다. 아래의 원문복사신청 또는 장바구니담기를 통하여 원문복사서비스 이용이 가능합니다.

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  10. [국내논문]   Temperature Effect on the Functional Expression of Human Cytochromes P450 2A6 and 2E1 in Escherichia coli  

    Yim Sung-Kun (School of Biological Sciences and Technology, Chonnam National University ) , Ahn Taeho (Department of Biochemistry, College of Veterinary Medicine, Chonnam National University ) , Jung Heung-Chae (The National Research Laboratory of Microbial Display, GenoFocus, Inc., and Laboratory of Microbial Function, Korea Research Institute of Bioscience and Biotechnology ) , Pan Jae-Gu (The National Research Laboratory of Microbial Display, GenoFocus, Inc., and Laboratory of Microbial Function, Korea Research Institute of Bioscience and Biotechnology ) , Yun Chul-Ho (School of Biological Sciences and Technology, Chonnam National University, Hormone Research Institute, Chonnam National University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.28 no.4 ,pp. 433 - 437 , 2005 , 0253-6269 ,

    초록

    Human cytochromes P450 (GYP) 2A6 and 2E1 are of great interest because of their important roles in the oxidation of numerous drugs and carcinogens. Bacterial expression systems, especially Escherichia coli cells, have been widely used for the production of various GYP enzymes in order to obtain high yield of proteins. The expression methods usually employ longer culture time (30-72 h) at lower temperature (usually under $30^{\circ}C$ ). Expression levels of GYPs 2A6 and 2E1 at $37^{\circ}C$ were compared to those at $28^{\circ}C$ , which is a usual temperature used in most bacterial expression systems for human GYP expression. Within 18 h the expression levels of GYPs 2A6 and 2E1 reached up to 360 and 560 nmol per liter culture at $37^{\circ}C$ , respectively, which are compatible with those of 36 h culture at $28^{\circ}C$ . The activities of GYPs expressed at $37^{\circ}C$ were also comparable to those expressed at $28^{\circ}C$ . The present over-expression system can be useful for rapid production of large amounts of active human GYPs 2A6 and 2E1 in E. coli.

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