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Archives of pharmacal research : a publication of ... 19건

  1. [국내논문]   Evaluation of the Genetic Toxicity of Synthetic Chemicals (II), a Pyrethroid Insecticide, Fenpropathrin  

    Ryu, Jae-Chun (Toxicology Laboratory, Doping Control Center, Korea Institute of Scienece and Technology ) , Kim, Kyung-Ran (Toxicology Laboratory, Doping Control Center, Korea Institute of Scienece and Technology ) , Kim, Hyun-Joo (Toxicology Laboratory, Doping Control Center, Korea Institute of Scienece and Technology ) , Ryu, Eun-Kyoung (Toxicology Laboratory, Doping Control Center, Korea Institute of Scienece and Technology ) , Lee, Soo-Young (Toxicology Laboratory, Doping Control Center, Korea Institute of Scienece and Technology ) , Jung, Sang-Oun (Toxicology Laboratory, Doping Control Center, Korea Institute of Scienece and Technology ) , Youn, Ji-Youn (Toxicology Laboratory, Doping Control Center, Korea Institute of Scienece and Technology ) , Kim, Min-Hee (Toxicology Laboratory, Doping Control Center, Korea Institute of Scienece and Technology ) , Kwon, Oh-Seung (Toxicology Laboratory, Doping Control Center, Korea Institute of Scienece and Technology)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.19 no.4 ,pp. 251 - 257 , 1996 , 0253-6269 ,

    초록

    The detection of many synthetic chemicals used in industry that may pose a genetic hazard in our environment is subject of great concern at present. In this respect, the genetic toxicity of fenpropathrin ((RS)-.alpha.-cyano-3-phenoxybenzyl-2,2,3,3-tetramethyl cyclopropane carboxylate, CAS No.:39514-41-8), a pyrethroid insecticide, was evaluated in bacterial gene mutation system, chromosome aberration in mammalian cell system and in vivo micronucleus assay with rodents. In bacterial gene mutation assay, no mutagenicity of fenpropathrin (62- $5000\mug/plate$ ) was observed in Salmonella typhimurium TA 98, 100, 1535 and 1537 both in the absence and in the presence of S-9 metabolic activaton system. In mammalian cell system using chinese hamster lung fibroblast, no clastogenicity of fenpropathrin was also observed both in the absence and in the presence of metabolic activation system in the concentration range of $7-28\mug/ml$ . And also, in vivo micronucleus assay using mouse bone marrow cells, fenpropathrin also revealed no mutagenic potential in the dose range of 27-105 mg/kg body weight of fenpropathrin (i.p.). Consequently, no mutagenic potential of fenpropathrin was observed in vitro bacterial, mammalian mutagenicity systems and in vivo micronucleus assay in the dose ranges used in this experiment.

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  2. [국내논문]   Inhibition of Tyrosine Hydroxylase by Palmatine  

    Lee, Myung-Koo (College of Pharmacy, Chungbuk National University ) , Zhang, Yong-He (College of Pharmacy, Chungbuk National University ) , Kim, Hack-Seang (College of Pharmacy, Chungbuk National University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.19 no.4 ,pp. 258 - 260 , 1996 , 0253-6269 ,

    초록

    Palmatine, an protoberberine isoquinoline alkaloid, has been found to inhibit dopamine biosynthesis by reducing tyrosine hydroxylase (TH) activity in PC12 cells (Lee and Kim, 1996). We have therefore investigated the effects of palmatine on bovine adrenal TH. Palmatine showed a mild inhibition on bovine adrenal TH (36.4% inhibition at concentration of $200\muM$ ). Bovine adrenal TH was inhibited competitively by palmatine with a substrate L-tyrosine. The Ki value was found to be 0.67 mM. This result suggests that the inhibition of TH activity by palmatine may be partially involved in the reduction of dopamine biosynthesis in PC12 cells.

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  3. [국내논문]   In Vitro Chemosensitivity Test of SK-302B on Human Colon Carcinoma Cell Lines  

    Kim, Soo-Kie (Department of Microbiology, Wonju College of Medicine, Yonsei University ) , Ahn, Chan-Mug (Department of Basic Sciences 1,2 Institute of Basic Medical Sciences, Wonju College of Medicine, Yonsei University ) , Kim, Tae-Ue (Department of Medical Technology, College of Health Science, Yonsei University ) , Choi, Sun-Ju (Department of Microbiology ,Wonju College of Medicine, Yonsei University ) , Park, Yoon-Sun (Department of Microbiology ,Wonju College of Medicine, Yonsei University ) , Shin, Woon-Seob (Department of Microbiology ,Wonju College of Medicine, Yonsei University ) , Koh, Choon-Myung (Department of Microbiology, Wonju College of Medicine, Yonsei University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.19 no.4 ,pp. 261 - 263 , 1996 , 0253-6269 ,

    초록

    SK-302B, an antibiotic purified from soil Streptomyces sp. 302, was structurally identified as echinomycin (C/sub 50/H/sub 66/N/sub 11/S/sub 2/). In the present experiment, the possibility of SK-302B as an anticolon cancer agent was investigated by using chemosensitivity system (MTT assay, clonogenic assay). Treatment of SK-302B on various colon cancer cell lines resulted in a significant cytotoxicity and tumor colony formation inhibition. These studies showed that SK-302B had a potent inhibition on colon cancer cells.

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

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  4. [국내논문]   Effect of Ginseng Saponin on Gap Junction Channel Reconstituted with Connexin 32  

    Hong, Eun-Jung (Department of Biochemistry, Yeungnam University ) , Huh, Keun (Department of Pharmacology, Yeungnam University ) , Rhee, Seung-Keun (Department of Biochemistry, Yeungnam University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.19 no.4 ,pp. 264 - 268 , 1996 , 0253-6269 ,

    초록

    Panax-ginseng saponin has been known to exert various pharmacological effects on cellular metabolism. This study was performed to determine the effect of ginseng saponin on gap junction channel-mediated intercellular communication, using an established in vitro system of reconstituted gap junction channels. Gap junction channels are a specialized plasma membrane fraction, which are permeable to relatively large water-soluble molecules. The sucrose permeable property of reconstituted gap junction channels was completely inhibited with 0.1 % (w/v) of ginseng saponin. We also compared the effect of ginseng saponin with that of Triton X-100, a nonionic detergent, on the same system. Triton X-100 showed significantly different effect on sucrose-permeability of gap junction channel from that was affected by ginseng saponin. The structures of liposomes containing gap junction channels was significantly destroyed by Triton X-100.

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

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  5. [국내논문]   The binding of food dyes with human serum albumin  

    Yoon, Jung-Hae , McKenzie, Duncan , Prichard, F. Elizabeth
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.19 no.4 ,pp. 269 - 274 , 1996 , 0253-6269 ,

    초록

    Panax-ginseng saponin has been known to exert various pharmacological effects on cellular metabolism. This study was performed to determine the effect of ginseng saponin on gap junction channel-mediated intercellular communication, using an established in vitro system of reconstituted gap junction channels. Gap junction channels are a specialized plasma membrane fraction, which are permeable to relatively large water-soluble molecules. The sucrose permeable property of reconstituted gap junction channels was completely inhibited with 0.1 % (w/v) of ginseng saponin. We also compared the effect of ginseng saponin with that of Triton X-100, a nonionic detergent, on the same system. Triton X-100 showed significantly different effect on sucrose-permeability of gap junction channel from that was affected by ginseng saponin. The structures of liposomes containing gap junction channels was significantly destroyed by Triton X-100.

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

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  6. [국내논문]   Identification of Certain Sequences in the 3rd Cytoplasmic Loop of$D_4$ Dopamine Receptor that Suppress the Bacterial Expression  

    Cheong, Ji-Sook (Pharmacology Laboratory, College of Pharmacy, Chonnam National University ) , Kim, Ae-Young (Pharmacology Laboratory, College of Pharmacy, Chonnam National University ) , Kim, Kyeong-Man (Pharmacology Laboratory, College of Pharmacy, Chonnam National University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.19 no.4 ,pp. 275 - 279 , 1996 , 0253-6269 ,

    초록

    To study the functional roles of dopamine receptors, we decided to raise antibodies against these proteins. To make antigen, we expressed the whole 3rd cytoplasmic loop of dopamine receptors in a fusion protein with glutathione-S-transferase (GST). $For D_2\; and\; D_3$ receptors, it was successful to express and purify fusion proteins for the whole 3rd cytoplasmic loops. However, we could not express the fusion protein for the whole 3rd cytoplasmic loop of $D_4$ dopamine receptor in the bacteria. To study the causes that prevent the bacterial expression of the GST-fusion protein of the 3rd cytoplasmic loop of $D_4$ dopamine receptor, we conducted more detailed studies on $D_4$ dopamine receptor. To locate the region which prevents bacterial expression, we made sequential constructs in the 3rd cytoplasmic loop decreasing the size step by step, and confirmed their expressions in the SDS PAGE. It was found that certain regions of 3rd cytoplasmic loop of $D_4$ dopamine receptor, located in N-terminal side of the 3rd cytoplasmic loop of $D_4$ dopamine receptor suppress the bacterial expression of fusion protein.

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  7. [국내논문]   Preparation and in Vitro Release of Melatonin-Loaded Multivalent Cationic Alginate Beads  

    Lee, Beom-Jin (College of Pharmacy, Kangwon National University ) , Min, Geun-Hong (College of Pharmacy, Kangwon National University ) , Kim, Tae-Wan (College of Pharmacy, Kangwon National University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.19 no.4 ,pp. 280 - 285 , 1996 , 0253-6269 ,

    초록

    The sustained release dosage form which delivers melatonin (MT) in a circadian fashion over 8 h is of clinical value for those who have disordered circadian rhythms because of its short halflife. The purpose of this study was to evaluate the gelling properties and release characteristics of alginate beads varying multivalent cationic species $(Al^{+++}, \; Ba^{++}, \; Ca^{++}, \; Mg^{++}, \; Fe^{+++}, \; Zn^{++})$ . The surface morphologies of Ca- and Ba-alginate beads were also studied using scanning electron microscope (SEM). MT, an indole amide pineal hormone was used as a model drug. The $Ca^{++}, \; Ba^{++}, \; Zn^{++}, \; Al^{++}\; and\; Fe^{+++}\; ions\; except\; Mg^{++}$ induced gelling of sodium alginate. The strength of multivalent cationic alginate beads was as follows: $Al^{+++}\llFe^{+++} the induced hydrogel beads were very fragile and less spherical. Fe-alginate beads were also fragile but stronger compared to Al-alginate beads. Ba-alginate beads had a similar gelling strength but was less spherical when compared to Ca-alginate beads. Zn-alginate beads were weaker than Ca- and Ba-alginate beads. Very crude and rough crystals of Ba- and Ca-alginate beads at higher magnifications were observed. However, the type and shape of rough crystals of Ba- and Ca-alginate beads were quite different. No significant differences in release profiles from MT-loaded multivalent cationic alginate beads were observed in the gastric fluid. Most drugs were continuously released upto 80% for 5 h, mainly governed by the passive diffusion without swelling and disintegrating the alginate beads. In the intestinal fluid, there was a significant difference iq the release profiles of MT-loaded multivalent cationic alginate beads. The release rate of Ca-alginate beads was faster when compared to other multivalent cationic alginate beads and was completed for 3 h. Ba-alginate beads had a very long lag time (7 h) and then rapidly released thereafter. MT was continuously released from Feand Zn-alginate beads with initial burstout release. It is assumed that the different release rofiles of multivalent cationic alginate beads resulted from forces of swelling and disintegration of alginate beads in addition to passive diffusion, depending on types of multivalent ions, gelling strength and drug solubility. It was estimated that 0.2M $CaCl_2$ concentration was optimal in terms of trapping efficiency of MT and gelling strength of Ca-alginate beads. In the gastric fluid, Ca-alginate beads gelled at 0.2 M $CaCl_2$ concentration had higher bead strength, resulting in the most retarded release when compared to other concentrations. In the intestinal fluid, the decreased release of Ca-alginate beads prepared at 0.2 M $CaCl_2$ concentration was also observed. However, release profiles of Ca-alginate beads were quite similar regardless of $CaCl_2$ concentration. Either too low or high $CaCl_2$ concentrations may not be useful for gelling and curing of alginate beads. Optimal $CaCl_2$ concentrations must be decided in terms of trapping efficiency and release and profiles of drug followed by curing time and gelling strength of alginate beads.

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

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  8. [국내논문]   Cytotoxicity of a Novel Biphenolic Compound, Bis(2-hydroxy-3-tert-butyl-5-methylphenyl)methane against Human Tumor Cells In vitro  

    Choi, Sang-Un (Pharmaceutical Screening Team, Korea Research Institute of Chemical Technology ) , Kim, Kwang-Hee (Pharmaceutical Screening Team, Korea Research Institute of Chemical Technology ) , Kim, Nam-Young (Pharmaceutical Screening Team, Korea Research Institute of Chemical Technology ) , Choi, Eun-Jung (Pharmaceutical Screening Team, Korea Research Institute of Chemical Technology ) , Lee, Chong-Ock (Pharmaceutical Screening Team, Korea Research Institute of Chemical Technology ) , Son, Kwang-Hee (Bioproducts Research Group, Korea Research Institute of Bioscience and Technology, KIST ) , Kim, Sung-Uk (Bioproducts Research Group, Korea Research Institute of Bioscience and Technology, KIST ) , Bok, Song-Hae (Bioproducts Research Group, Korea Research Institute of Bioscience and Technology, KIST ) , Kim, Young-Kook (Bioproducts Research Group, Korea Research Institute of Bioscience and Technology, KIST)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.19 no.4 ,pp. 286 - 291 , 1996 , 0253-6269 ,

    초록

    Phenolic compounds are prevalent as toxins or environmental pollutants, but they are also widely used as drugs for various purpose including anticancer agent. A novel biphenolic compound, bis(2-hydroxy-3-tert-butyl-5-methylphenyl)methane (GERI-BPO02-A) was isolated from the fermentation broth of Aspergillus fumigatus F93 previously, and it has revealed cytotoxicity against human solid tumor cells. Its effective doses that cause 50% inhibition of cell growth in vitro against non-small cell lung cancer cell A549, ovarian cancer cell SK-OV-3, skin cancer cell SK-MEL-2 and central nerve system cancer cell XF498 were 8.24, 10.60, 8.83, $9.85\mug/ml$ respectively. GERI-BPO02-A has also revealed cytotoxicity against P-glycoproteinexpressed human colon cancer cell HCT15 and its multidrug-resistant subline HCT15/CL02, and its cytotoxicity was not affected by P-glycoprotein. We have also tested cytotoxicities of structurally related compounds of GERI-BPO02-A such as diphenylmethane, 1,1-bis(3,4dimethylphenyl)ethane, 2,2-diphenylpropane, 2-benzylpyridine, 3-benzylpyridine, $4,4^I-di-tert-butylphenyl$ , bibenzyl, $2,2^I-dimethylbibenzyl$ , cis-stilbene, trans-stilbene, 3-tert-butyl-4-hydroxy-5-methylphenyisulfide, sulfadiazine and sulfisomidine for studying of structure and activity relationship, and from these data we could suppose that hydroxyl group of GERI-BPO02A conducted important role in its cytotoxicity.

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  9. [국내논문]   Metabolism of glycyrrhizin and baicalin by human intestinal bacteria  

    Kim, Dong-Hyun (College of Pharmacy, Kyung-Hee University ) , Jang, Il-Sung (College of Pharmacy, Kyung-Hee University ) , Lee, Hyeong-Kyu (Korean Research Institute of Bioscience and Biotechnology,KIST ) , Jung, Eun-Ah (College of Pharmacy, Kyung-Hee University ) , Lee, Kyeu-Yup (College of Pharmacy, Kyung-Hee University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.19 no.4 ,pp. 292 - 296 , 1996 , 0253-6269 ,

    초록

    By human intestinal bacteria, glycyrrhizin (18 ${\beta}$ -glycyrrhetic acid ${beta}$ -D-glucuronyl. ${\alpha}$ -D-glucuronic acid, GL) and baicalin (baicalein ${\beta}$ -D-glucuronic acid) were metabolized to glycyrrhetinic acid and baicalin, respectively. However, . ${\alpha}$ -glucuronidase of Bacteroides JY-6 isolated from human intestinal bacteria hydrolyzed GL or 18. ${\beta}$ -glycyrrhetinic acid .. ${\alpha}$ -D-glucuronic acid to 18 ${\beta}$ -glycyrrhetic acid but did not baicalin. However, E. coli ${\beta}$ -glucironidase from human intestinal bacteria hydrolyzed baicalin to baicalein, but did not GL. ${\beta}$ -Glucuronidase of mammalian tissues hydrolyzed both GL and baicalin.

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

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  10. [국내논문]   Pharmacokinetics of talniflumate, a prodrug of niflumic acid, following oral administration to man  

    Kim, Hyun-Ji (Department of Pharmaceutics, College of Pharmacy, Seoul National University ) , Han, Yong-Hae (Department of Pharmaceutics, College of Pharmacy, Seoul National University ) , Chung, Suk-Jaeng (Department of Pharmaceutics, College of Pharmacy, Seoul National University ) , Lee, Min-Hwa (Department of Pharmaceutics, College of Pharmacy, Seoul National University ) , Shim, Chang-Koo (Department of Pharmaceutics, College of Pharmacy, Seoul National University)
    Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea v.19 no.4 ,pp. 297 - 301 , 1996 , 0253-6269 ,

    초록

    Plasma profile of niflumic acid following oral administration of talniflumate tablets (Somalgen) was compared to that of niflumic acid tablets in man. Plasma niflumic acid was assayed by HPLC method. Plasma niflumic acid profile from the tainiflumate tablets was similar to that from the niflumic acid tablets resulting in no differences in $AUC, C_max, t_max$ and MRT. It demonstrates that talniflumate is a prodrug of niflumic acid, and undergoes extensive first-pass biotransformation to niflumic acid. However, plasma niflumic acid concentration at 30 min after tainiflumate dosing was significantly (p

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