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Archives of pharmacal research : a publication of ... 25건

  1. [국내논문]   Synthesis, Analgesic, and Anti-Inflammatory Activities of [6-(3,5-Dimethyl-4-Chloropyrazole-1-yl)-3(2H)-Pyridazinon-2-yl]Acetamides  

    Sukuroglu, Murat (Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Gazi University ) , Caliskanergun, Burcu (Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Gazi University ) , Unlu, Serdar (Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Gazi University ) , Sahin, M.Fethi (Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Gazi University ) , Kupeli, Esra (Department of Pharmacognosy, Faculty of Pharmacy, Gazi University ) , Yesilada, Erdem (Department of Pharmacognosy, Faculty of Pharmacy, Gazi University ) , Banoglu, Erden (Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Gazi University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.28 no.5 ,pp. 509 - 517 , 2005 , 0253-6269 ,

    초록

    A series of structurally diverse amide derivatives of [6-(3,5-dimethyl-4- chloro-pyrazole-1-yl)-3(2H)-pyridazinone-2-yl]acetic acid were prepared and tested for their in vivo analgesic and anti-inflammatory activity by using p-benzoquinone-induced writhing test and carrageenan induced hind paw edema model, respectively. The analgesic and anti-inflammatory activity of the compounds, 7c, 7d and 7k were found to be equipotent to aspirin (as an analygesic) and indometacin (as an anti-inflammatory drug), respectively. The other amide derivatives generally resulted in lower activity on comparision with reference compounds.

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  2. [국내논문]   Isolation of a Natural Antioxidant, Dehydrozingerone from Zingiber officinale and Synthesis of Its Analogues for Recognition of Effective Antioxidant and Antityrosinase Agents  

    Kuo, Ping-Chung , Cherng, Ching-Yuh , Jeng, Jye-Fu , Damu, Amooru G. , Teng, Che-Ming , Lee, E-Jian , Wu, Tian-Shung
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.28 no.5 ,pp. 518 - 528 , 2005 , 0253-6269 ,

    초록

    A series of structurally diverse amide derivatives of [6-(3,5-dimethyl-4- chloro-pyrazole-1-yl)-3(2H)-pyridazinone-2-yl]acetic acid were prepared and tested for their in vivo analgesic and anti-inflammatory activity by using p-benzoquinone-induced writhing test and carrageenan induced hind paw edema model, respectively. The analgesic and anti-inflammatory activity of the compounds, 7c, 7d and 7k were found to be equipotent to aspirin (as an analygesic) and indometacin (as an anti-inflammatory drug), respectively. The other amide derivatives generally resulted in lower activity on comparision with reference compounds.

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  3. [국내논문]   Isolation of a Natural Antioxidant, Dehydrozingerone from Zingiber officinale and Synthesis of lts Analogues for Recognition of Effective Antioxidant and Antityrosinase Agents  

    Kuo, Ping-Chung (Department of Biotechnology, National Formosa University ) , Damu, Amooru G. (Department of Chemistry, National Cheng Kung University ) , Cherng, Ching-Yuh (Department of Applied Chemistry, National Chiayi University ) , Jeng, Jye-Fu (Department of Chemistry, National Cheng Kung University ) , Teng, Che-Ming (Pharmacological Institute, College of Medicine, National Taiwan University ) , Lee, E-Jian (Neurophysiology Laboratory, Neurosurgical Service, Departments of Surgery and Anesthesiology, and Institute of Biomedical Engineering, National Cheng Kung University Medical Center and Medical School ) , Wu, Tian-Shung (Department of Chemistry, National Cheng Kung University, National Research Institute of Chinese Medicine)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.28 no.5 ,pp. 518 - 528 , 2005 , 0253-6269 ,

    초록

    In the present study, the antioxidative and inhibitory activity of Zingiber officinale Rosc. Rhizomes-derived materials (on mushroom tyrosinase) were evaluated. The bioactive co mponents of Z. officinale rhizomes were characterized by spectroscopic analysis as zingerone and dehydrozingerone, which exhibited potent antioxidant and tyrosinase inhibition activities. A series of substituted dehydrozingerones [(E)-4-phenyl-3-buten-2-ones] were prepared in admirable yields by the reaction of appropriate benzaldehydes with acetone and the products were evaluated in terms of variation in the dehydrozingerone structure. The synthetic analogues were examined for their antioxidant and antityrosinase activities to probe the most potent analogue. Compound 26 inhibited Fe $^{2+}$ -induced lipid peroxidation in rat brain homogenate with an IC $_{50}$ = 6.3<T 6.3 ${\pm}$ 0.4 ${\mu}$ M. In the 1,1-diphenyl- 2-picrylhydrazyl (DPPH) radical quencher assay, compounds 2, 7, 17, 26, 28, and 29 showed radical scavenging activity equal to or higher than those of the standard antioxidants, like ${\alpha}$ -tocopherol and ascorbic acid. Compound 27 displayed superior inhibition of tyrosinase activity relative to other examined analogues. Compounds 2, 17, and 26 exhibited non-competitive inhibition against oxidation of 3,4- dihydroxyphenylalanine (L-DOPA). From the present study, it was observed that both number and position of hydroxyl groups on aromatic ring and a double bond between C-3 and C-4 played a critical role in exerting the antioxidant and antityrosinase activity.

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  4. [국내논문]   Free Radical Scavenging and Hepatoprotective Constituents from the Leaves of Juglans sinensis  

    An, Ren-Bo , Kim, Hyun-Chul , Tian, Yu-Hua , Kim, Youn-Chul
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.28 no.5 ,pp. 529 - 533 , 2005 , 0253-6269 ,

    초록

    In the present study, the antioxidative and inhibitory activity of Zingiber officinale Rosc. Rhizomes-derived materials (on mushroom tyrosinase) were evaluated. The bioactive co mponents of Z. officinale rhizomes were characterized by spectroscopic analysis as zingerone and dehydrozingerone, which exhibited potent antioxidant and tyrosinase inhibition activities. A series of substituted dehydrozingerones [(E)-4-phenyl-3-buten-2-ones] were prepared in admirable yields by the reaction of appropriate benzaldehydes with acetone and the products were evaluated in terms of variation in the dehydrozingerone structure. The synthetic analogues were examined for their antioxidant and antityrosinase activities to probe the most potent analogue. Compound 26 inhibited Fe $^{2+}$ -induced lipid peroxidation in rat brain homogenate with an IC $_{50}$ = 6.3<T 6.3 ${\pm}$ 0.4 ${\mu}$ M. In the 1,1-diphenyl- 2-picrylhydrazyl (DPPH) radical quencher assay, compounds 2, 7, 17, 26, 28, and 29 showed radical scavenging activity equal to or higher than those of the standard antioxidants, like ${\alpha}$ -tocopherol and ascorbic acid. Compound 27 displayed superior inhibition of tyrosinase activity relative to other examined analogues. Compounds 2, 17, and 26 exhibited non-competitive inhibition against oxidation of 3,4- dihydroxyphenylalanine (L-DOPA). From the present study, it was observed that both number and position of hydroxyl groups on aromatic ring and a double bond between C-3 and C-4 played a critical role in exerting the antioxidant and antityrosinase activity.

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  5. [국내논문]   Free Radica1 Scavenging and Hepatoprotective Constituents from the Leaves of Juglans sinensis   피인용횟수: 3

    An, Ren-Bo (College of Pharmacy and Phytofermentation Research Center, Wonkwang University, College of Pharmacy, Yanbian University ) , Kim, Hyun-Chul (College of Pharmacy and Phytofermentation Research Center, Wonkwang University ) , Tian, Yu-Hua (College of Pharmacy and Phytofermentation Research Center, Wonkwang University ) , Kim, Youn-Chul (College of Pharmacy and Phytofermentation Research Center, Wonkwang University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.28 no.5 ,pp. 529 - 533 , 2005 , 0253-6269 ,

    초록

    In the course of searching for hepatoprotective agents from natural products, six compounds were isolated from the MeOH extract of the leaves of Juglans sinensis, as guid ed by their DPPH free radical scavenging activity. The structures were determined as juglanoside B (1), quercetin 3-O- ${\alpha}$ -L-arabinofuranoside (avicularin, 2), quercetin 3-O- ${\alpha}$ -L-arabinopyranoside (guaijaverin,3), quercetin 3-O- ${\alpha}$ -L-rhamnopyranoside (quercitrin,4), (+)-catechin (5) and quercetin 3-O- ${\beta}$ - D-galactopyranoside (hyperin,6). Compounds 2-6 showed significant DPPH free radical scavenging effects. An evaluation for the hepatoprotective activity of the isolated compounds on drug-induced cytotoxicity was conducted, and compounds 1, 2, and 5 showed protective effects against nitrofurantoin-induced cytotoxicity, and compound 5 also exhibited a moderate protective effect on amiodarone-induced cytotoxicity in Hep G2 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.

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

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  6. [국내논문]   In Vitro Free Radical and ONOO- Scavengers from Sophora flavescens   피인용횟수: 7

    Jung, Hee-Jin (Faculty of Food Science and Biotechnology, Pukyong National University ) , Kang, Sam-Sik (Natural Products Research Institute, Seoul National University ) , Hyun, Sook-Kyung (Faculty of Food Science and Biotechnology, Pukyong National University ) , Choi, Jae-Sue (Faculty of Food Science and Biotechnology, Pukyong National University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.28 no.5 ,pp. 534 - 540 , 2005 , 0253-6269 ,

    초록

    Activity-guided fractionation of the CH $_2Cl_2$ -soluble fraction of the roots of Sophora flavescens furnished five 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scaveng ers: trans-hexadecyl ferulic acid (1) cis-octadecyl ferulic acid (2), trans-hexadecyl sinapic acid (3), (-)-4-hydroxy-3-methoxy-(6aR,11aR)-8, 9-methylenedioxypterocarpan (4) and desmethylanhydroicaritin (8), along with nine known inactive compounds: (-)-maackiain (5), xanthohumol (6), formononetin (7), (2S)-2'-methoxykurarinone (9), (2S)-3 ${\beta}$ ,7,4'-trihydroxy-5-methoxy-8-( ${\gamma},{\gamma}$ - imethylallyl )-flavanone (10), (2S)-7,4'-dihydroxy-5-methoxy-8- ( ${\gamma},{\gamma}$ -dimethylallyl ) -flavanone (11), umbelliferone (12), kuraridin (13), and trifolirhizin (14). Compounds 1-4 and 8 exhibited DPPH free radical scavenging effects at IC $_{50}$ values of 33.01 ${\pm}$ 0.20, 57.06 ${\pm}$ 0.16, 39.84 ${\pm}$ 0.36, 35.83 ${\pm}$ 0.47, and 18.11 ${\pm}$ 0.04 ${\mu}$ M, respectively. L-Ascorbic acid, when used as a positive control, exhibited an IC $_{50}$ value of 7.39 ${\pm}$ 0.01 ${\mu}$ M. Compounds 1-4 and 8 also appeared to exert significant scavenging effects on authentic ONOO-, with IC $_{50}$ values of 5.76 ${\pm}$ 1.19, 15.06 ${\pm}$ 1.64, 8.17 ${\pm}$ 4.97, 1.95 ${\pm}$ 0.29 and 4.06 ${\pm}$ 2.41 ${\mu}$ M, respectively. Penicillamine (IC $_{50}$ = 2.36 2.36 ${\pm}$ 0.79 ${\mu}$ M) was used as a positive control. In addition, compounds 2,4,6,8, and 10 were isolated from this plant for the first time.

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  7. [국내논문]   Ergosterol Peroxide from Flowers of Erigeron annuus L.as an Anti-Atherosclerosis Agent   피인용횟수: 6

    Kim, Dong-Hyun (Graduate School of Biotechnology & Plant Metabolism Research Center, Kyung Hee University ) , Jung, Sung-Je (Graduate School of Biotechnology & Plant Metabolism Research Center, Kyung Hee University ) , Chung, In-Sik (Graduate School of Biotechnology & Plant Metabolism Research Center, Kyung Hee University ) , Lee, Youn-Hyung (Graduate School of Biotechnology & Plant Metabolism Research Center, Kyung Hee University ) , Kim, Dae-Keun (Department of Pharmacy, Woosuk University ) , Kim, Sung-Hoon (Graduate School of East-West Medical Science, Kyung-Hee University ) , Kwon, Byoung-Mog (Korea Research Institute of Bioscience and Biotechnology ) , Jeong, Tae-Sook (Korea Research Institute of Bioscience and Biotechnology ) , Park, Mi-Hyun (Erom Life Co. Ltd. ) , Seoung, Nak-Sul (National Institute of Crop Science, RDA ) , Baek, Nam-In (Graduate School of Biotechnology & Plant Metabolism Research Center, Kyung Hee University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.28 no.5 ,pp. 541 - 545 , 2005 , 0253-6269 ,

    초록

    Flowers of Erigeron annuus L. were extracted with 80% aqueous MeOH, and the concentrated extract was partitioned with EtOAc, n-BuOH, and H $_2$ O. Repeated silica gel and OD S column chromatography of the EtOAc fraction led to the isolation of a sterol, through activityguided fractionation, using ACAT inhibitory activity measurements. From the physico-chemical data, including NMR, MS, and IR, the chemical structure of the compound was determined to be an ergosterol peroxide (1), which has been isolated for the first time from this plant. This compound exhibited hACAT-1 and Lp-PLA $_2$ inhibitory effects, with inhibitory values of 51.6 ${\pm}$ 0.9 and 51 .7 ${\pm}$ 1.2%, at a treatment concentration of 0.23 mM.

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  8. [국내논문]   Potentially Cytotoxic Triterpenoids from the Root Bark of Siphonodon celastrineus Griff.  

    Niampoka, Chokchai (Department of Pharmaceutical Botany, Faculty of Pharmaceutical Sciences, Chulalongkorn University ) , Suttisri, Rutt (Department of Pharmaceutical Botany, Faculty of Pharmaceutical Sciences, Chulalongkorn University ) , Bavovada, Rapepol (Department of Pharmaceutical Botany, Faculty of Pharmaceutical Sciences, Chulalongkorn University ) , Takayama, Hiromitsu (Faculty of Pharmaceutical Sciences, Chiba University ) , Aimi, Norio (Faculty of Pharmaceutical Sciences, Chiba University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.28 no.5 ,pp. 546 - 549 , 2005 , 0253-6269 ,

    초록

    A new oleanane-triterpene, 3 ${\beta}$ -acetoxy-11 ${\alpha}$ -benzoyloxy-13 ${\beta}$ -hydroxyolean-1 2-one (1), was isolated along with a known quinone-methide triterpene, pristimerin (2), from the root bark of Siphonodon celastrinneus Griff., a Thai medicinal plant of the family Celastraceae. Their structures were determined based on spectroscopic analysis.

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

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  9. [국내논문]   Triterpenoids from the Flower of Campsis grandiflora K. Schum. As Human Acyl-CoA: Cholesterol Acyltransferase Inhibitors   피인용횟수: 5

    Kim, Dong-Hyun (Graduate School of Biotechnology & Plant Metabolism Research Center, Kyung Hee University ) , Han, Kyung-Min (Graduate School of Biotechnology & Plant Metabolism Research Center, Kyung Hee University ) , Chung, In-Sik (Graduate School of Biotechnology & Plant Metabolism Research Center, Kyung Hee University ) , Kim, Dae-Keun (Department of Pharmacy, Woosuk University ) , Kim, Sung-Hoon (Graduate School of East-West Medical Science, Kyung Hee University ) , Kwon, Byoung-Mog (Korea Research Institute of Bioscience and Biotechnology ) , Jeong, Tae-Sook (Korea Research Institute of Bioscience and Biotechnology ) , Park, Mi-Hyun (Erom life Co. Ltd. ) , Ahn, Eun-Mi (Scigenic Co. Led. ) , Baek, Nam-In (Graduate School of Biotechnology & Plant Metabolism Research Center, Kyung Hee University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.28 no.5 ,pp. 550 - 556 , 2005 , 0253-6269 ,

    초록

    The flower of Campsis grandiflora K. Schum. Was extracted with 80% aqueous MeOH, and the concentrated extract was partitioned with EtOAc, n-BuOH and H $_2$ O. From the EtO Ac fraction, seven triterpenoids were isolated through the repeated silica gel, ODS column chromatographies and preparative HPLC. From the result of physico- chemical data including NMR, MS and IR, the chemical structures of the compounds were determined as 3 ${\beta}$ -hydroxyolean-12-en-28-oic acid (oleanolic acid, 1), 3 ${\beta}$ -hydroxyurs-12-en-28-oic acid (ursolic acid, 2), 3 ${\beta}$ -hydroxyurs-12-en-28-al (ursolic aldehyde, 3), 2 ${\alpha}$ ,3 ${\beta}$ -dihydroxyolean-12-en-28-oic acid (maslinic acid, 4), 2 ${\alpha}$ ,3 ${\beta}$ -dihydroxyurs-12-en-28-oic acid (corosolic acid, 5), 3 ${\beta}$ ,23-dihydroxyurs-12- en-28-oic acid (23-hydroxyursolic acid ,6) and 2 ${\alpha}$ ,3 ${\beta}$ ,23-trihydroxyolean-12-en-28- oic acid (arjunolic acid, 7). These teriterpenoids were isolated for the first time from this plant. Also, compounds 4, 5, 6, and 7 revealed relatively high hACAT-1 inhibitory activity with the value of 46.2 ${\pm}$ 1.1, 46.7 ${\pm}$ 0.9, 41.5 ${\pm}$ 1.3 and 60.8 ${\pm}$ 1.1% at the concentration of 100 ${\mu}$ g/mL, respectively.

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  10. [국내논문]   Fungicidal Effect of Resveratrol on Human Infectious Fungi   피인용횟수: 2

    Jung, Hyun-Jun (Department of Microbiology, College of Natural Sciences, Kyungpook National University ) , Hwang, In-Ah (Department of Microbiology, College of Natural Sciences, Kyungpook National University ) , Sung, Woo-Sang (Department of Microbiology, College of Natural Sciences, Kyungpook National University ) , Kang, Hyun-Gu (Department of Microbiology, College of Natural Sciences, Kyungpook National University ) , Kang, Beom-Sik (School of Life Science, College of Natural Sciences, Kyungpook National University ) , Seu, Young-Bae (Department of Microbiology, College of Natural Sciences, Kyungpook National University ) , Lee, Dong-Gun (Department of Microbiology, College of Natural Sciences, Kyungpook National University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.28 no.5 ,pp. 557 - 560 , 2005 , 0253-6269 ,

    초록

    Resveratrol, a phenolic antioxidant found in grapes, has been known to mediate various biological activities on the human body. In the present study, we tested the antifungal a ctivity of resveratrol against human pathogenic fungi before carrying out further studies to elucidate the antifungal mechanism(s) of resveratrol. Resveratrol displayed potent antifungal activity against human pathogenic fungi at concentration levels of 10-20 ${\mu}g$ /mL. Furthermore, time-kill curve exhibited fungicidal effect of resveratrol on C. albicans, but the compound had no hemolytic activity against human erythrocytes. The destruction of C. albicans cells by resveratrol was confirmed by scanning electron microscopy. These results suggest that resveratrol could be employed as a therapeutic agent to treat fungal infections of humans.

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