• Title/Summary/Keyword: pharmaceutical activity

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Antibacterial Activity of Zabofloxacin, a Novel Fluoroquinolone, against Gram-Positive Bacteria (그람양성세균에 대한 새로운 퀴놀론계 항균제 Zabofloxacin의 항균력)

  • Park, Hee-Soo;Jung, Sung-Ji;Jeong, Ji-Woong;Choi, Dong-Rack;Kim, Hyo-Hyun;Choi, Eung-Chil;Kwak, Jin-Hwan
    • YAKHAK HOEJI
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    • v.55 no.1
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    • pp.11-15
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    • 2011
  • Zabofloxacin is a novel broad spectrum fluoroquinolone with excellent anti-pneumococcal activity. We investigated the in vitro activity of zabofloxacin against clinical isolates of gram-positive bacteria and the in vivo activity against systemic infection in mice. Zabofloxacin was very active against gram-positive bacteria except QRSA (Quinolone-resistant S. aureus) and VRE(Vancomycin-resistant Enterococci). Especially, zabofloxacin was extremely potent against clinical isolates of Streptococci. Zabofloxacin was as active as gemifloxacin against systemic infection in mice. In view of its improved antibacterial activities against gram-positive bacteria and good pharmacokinetic profiles in animals, the clinical usefulness of zabofloxacin should be established by further studies.

Antifibrotic Activity of LCC, a Cerebroside of Lycium chinense Fruit, in Bile Duct-Ligated Rats

  • Kim, Sun-Yeou;Kim, Hong-Pyo;Yang, Hye-Kyung;Lee, Mi-Na;Ryu, Hyo-Jeong;Jang, Young-Pyo;Sung, Sang-Hyun;Kim, Young-Choong
    • Natural Product Sciences
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    • v.15 no.2
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    • pp.101-105
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    • 2009
  • We previously reported that a novel cerebroside, LCC, isolated from the fruits of Lycium chinense (Solanaceae), significantly exerted hepatoprotective activity against both the carbon tetrachloride-induced and galactosamine-induced toxicities in primary cultures of rat hepatocytes. In the present study, we further attempted to determine the effect of LCC on hepatic fibrosis in animal model. Hepatic fibrosis was induced in rats by bile duct ligation/scission (BDL) for a period of 5 weeks. Treatment of BDL rats with LCC significantly reduced collagen deposition and the activities of serum alkaline phosphatase and ${\gamma}$-glutamyl transpeptidase. In addition, the LCC treatment of BDL rats significantly preserved the decreased hepatic glutathione as well as the activities of glutathione reductase and catalase in BDL rats. From the results, it can be speculated that LCC might exert antifibrotic activity in rats with BDL, in part, through the preservation of antioxidant enzymes and hepatic glutathione.

Antimicrobial Activity and Safety Test of Mixed Plant Extracts Including Phellodendron Amurense and Eucommia Ulmides Oliv (황벽나무, 두충나무 등을 포함하는 복합수목추출물의 항균활성 및 안전성 시험)

  • Kim, Hyunwoo;Shin, Hyejin;Hwang, Danbi;Lee, Jieun;Bak, Manchun;Kim, Jinhong;Kim, Donguk
    • Korean Chemical Engineering Research
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    • v.51 no.5
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    • pp.536-539
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    • 2013
  • In this study, mixed plant extracts including Phellodendro namurense and Eucommia ulmides Oliv were tested for antimicrobial activity and safety. Antimicrobial activity was measured by disc diffusion method using normal skin flora and opportunistic microbes such as Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli and Candida albicans. As safety test, single dose oral toxicity test, single dose inhalation toxicity test and repeat dose inhalation toxicity test were done. From antimicrobial test, plant extracts showed significant antimicrobial activity Staphylococcus aureus, Pseudomonas aeruginosa, Candida albicans, however, did not indicate any antibacterial effect on Escherichia coli. From 3 kinds of safety tests, toxicity of mixed plant extracts was not observed. From experimental results, mixed plant extracts including Phellodendro namurense and Eucommia ulmides Oliv showed good potential for natural antimicrobial agent.

Synthesis and Antifungal Activities of Some Aryl (3-Methyl-Benzofuran-2-yl) Ketoximes

  • Benkli, Kadriye;Gundogdu-Karaburun, Nalan;Karaburun, Ahmet-Cagrl;Ucucu, Umit;Demirayak, Seref;Kiraz, Nuri
    • Archives of Pharmacal Research
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    • v.26 no.3
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    • pp.202-206
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    • 2003
  • In this study, some aryl (3-methyl-benzofuran-2-yl) ketoximes and their ethers and esters were synthesised. The structure elucidation of the compounds was performed by IR, $^1H-NMR$, MASS spectroscopy and elemental analyses. Antifungal activities of the compounds were examined and moderate activity was obtained.

Naphthopyrone Glucosides from the Seeds of Cassia tora with Inhibitory Activity on Advanced Glycation End Products (AGEs) Formation

  • Lee, Ga-Young;Jang, Dae-Sik;Lee, Yun-Mi;Kim, Jong-Min;Kim, Jin-Sook
    • Archives of Pharmacal Research
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    • v.29 no.7
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    • pp.587-590
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    • 2006
  • Three naphthopyrone glucosides, cassiaside (1), $rubrofusarin-6-O-{\beta}-D-gentiobioside$ (2), and $toralactone-9-O-{\beta}-D-gentiobioside$ (3), were isolated from the BuOH-soluble extract of the seeds of Cassia tora as active constituents, using an in vitro bioassay based on the inhibition of advanced glycation end products (AGEs) to monitor chromatographic fractionation. The structures of 1-3 were determined by spectroscopic data interpretation, particularly by extensive 1D and 2D NMR studies. All the isolates (1-3) were evaluated for the inhibitory activity on AGEs formation in vitro.

Estrogenic Activity of Furanocoumarins Isolated from Angelica dahurica

  • Piao, Xiang-Lan;Yoo, Hye-Hyun;Kim, Hyun-Young;Kang, Tak-Lim;Hwang, Gwi-Seo;Park, Jeong-Hill
    • Archives of Pharmacal Research
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    • v.29 no.9
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    • pp.741-745
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    • 2006
  • In our efforts to discover novel phytoestrogens to treat menopausal symptoms, eleven furanocoumarins were isolated from Angelica dahurica and tested for their estrogenic activity on the Ishikawa cell line. Among the compounds tested, 9-hydroxy-4-methoxypsoralen and alloisoimperatorin showed strong abilities to induce alkaline phosphatase (AP) with $EC_{50}$ values of 1.1 and $0.8\;{\mu}g/mL$, respectively, whereas the other nine furanocoumarins were weakly or only slightly active.

Thiadiazole Derivatives as Potential Anticonvulsant Agents

  • Mullick, Pooja;Khan, Suroor A.;Verma, Surajpal;Alam, Ozair
    • Bulletin of the Korean Chemical Society
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    • v.32 no.3
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    • pp.1011-1016
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    • 2011
  • A series of thiadiazole derivatives were synthesized with differently substituted benzoic acids which were cyclized to give differently substituted thiazolidin-4-one. Elemental analysis, IR, $^1H$ NMR, $^{13}C$ NMR and mass spectral data confirmed the structure of the synthesized compounds. The derivatives of these moieties were evaluated for anticonvulsant activity by MES model and neurotoxicity by rotarod method. The synthesized compounds showed good potential for anticonvulsant activity besides this, the compounds also showed neurotoxic effect. It was observed that compounds with $OCH_3$ at 3, 4 position of phenyl ring [5(a-l)] showed less protection against convulsions as compared to compounds having unsubstituted phenyl ring [4(a-l)].

Evaluation of Anti-inflammatory Activity of Asparagus racemosus Willd. (Liliaceae) root extract

  • Mandal, Subhash C.;Maiti, B.C.;Maity, Tapan K.;Pal, M.;Saha, B.P.
    • Natural Product Sciences
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    • v.4 no.4
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    • pp.230-233
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    • 1998
  • The methanol extract of Asparagus racemosus root was evaluated for its anti-inflammatory activity on carrageenin and serotonin-induced rat hind paw oedema models. The extract (200 and 400 mg/kg) showed maximum inhibition of oedema of 18.6% and 33.7% at 3 h with carrageenin and 22.2% and 40.5% at 5 h with serotonin-induced rat paw oedema respectively. The experimental models tested, where the effect produced by the extract was compared to that of phenylbutazone, a prototype non-steroidal anti-inflammatory drug.

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Inhibition of Aromatase Activity by Flavonoids

  • Jeong, Hyeh-Jean;Shin, Young-Geun;Kim, Il-Hyuk;Pezzuto, John-M.
    • Archives of Pharmacal Research
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    • v.22 no.3
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    • pp.309-312
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    • 1999
  • In searching for potent cancer chemopreventive agents from synthetic or natural products, 28 randomly selected flavonoids were screened for inhibitory effects against partially purified aromatase prepared form human placenta. Over 50% of the flavonoids significantly inhibited aromatase activity, with greatest activity being demonstrated with apigenin $(IC_{50}: 0.9{\mu}/mL)$, chrysin $(IC_{50}: 1.1{\mu}/mL)$ , and hesperetin $(IC_{50}:1.0{\mu}/mL)$.

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A long duration of anticoagulant activity of acharan sulfate in vivo

  • Li, Da-Wei;Lee, In-Sun;Toshihiko Toida;Kim, Yeong-Shik
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.98.2-99
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    • 2003
  • Introduction: We previously reported that a new glycosaminoglycan, acharan sulfate (AS) from the African giant snail Achatina fulica showed anticoagulation activity in vitro, but it was much less than that of heparin. In the present study, the anticoagulant activity of AS was investigated in vivo. Methods: AS and heparin were administered to rats in various concentrations and anticoagulant activities were measured. Both were also compared in thrombin-induced Results: Intravenous administration of acharan sulfate prolonged the coltting time (APTT) in mice and rats in a dose-dependent manner. (omitted)

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