• Title/Summary/Keyword: pharmaceutical activity

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Synthesis of Dithiolopyrrolone Derivatives and Their Leukocyte-Increasing Activities

  • Li, Chungang;Sun, Yiping;Wang, Guoping;Tan, Xiangduan
    • Bulletin of the Korean Chemical Society
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    • v.35 no.12
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    • pp.3489-3494
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    • 2014
  • In search of new antileukopenia agents, twenty dithiolopyrrolone derivatives were synthesized and evaluated for their leukocyte-increasing activities in normal mice. Among the synthesized compounds 4-23, compounds 5 and 6 showed significant leukocyte-increasing activity ( p < 0.01), and compounds 4, 9 and 16 had a moderate effect ( p < 0.05). Compound 5 also displayed stronger leukocyte-increasing activity than that of the positive recombinant human granulocyte colony stimulating factor (rhG-CSF). Above all, compound 5 would be a potential antileukopenia agent which deserved further research.

Biotransformation of Rosamicin Antibiotic into 10,11-Dihydrorosamicin with Enhanced In Vitro Antibacterial Activity Against MRSA

  • Nguyen, Lan Huong;Nguyen, Huu Hoang;Shrestha, Anil;Sohng, Jae Kyung;Yoon, Yeo Joon;Park, Je Won
    • Journal of Microbiology and Biotechnology
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    • v.24 no.1
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    • pp.44-47
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    • 2014
  • A biotransformation approach using microbes as biocatalysts can be an efficient tool for the targeted modification of existing antibiotic chemical scaffolds to create previously uncharacterized therapeutic agents. By employing a recombinant Streptomyces venezuelae strain as a microbial catalyst, a reduced macrolide, 10,11-dihydrorosamicin, was created from rosamicin macrolide. Its chemical structure was spectroscopically elucidated, and the new rosamicin analog showed 2-4-fold higher antibacterial activity against two strains of methicillin-resistant Staphylococcus aureus compared with its parent rosamicin. This kind of biocatalytic approach is able to expand existing antibiotic entities and can also provide more diverse therapeutic resources.

A New Potent Angiogenesis Inhibitor, FR-118487

  • Otsuka, Takanao;Ohkawa, Takehiko;Shibata, Toshihiro;Oku, Teruo;Okuhara, Masakuni;Terano, Hiroshi;Kohsaka, Masanobu;Imanaka, Hiroshi
    • Journal of Microbiology and Biotechnology
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    • v.1 no.3
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    • pp.163-168
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    • 1991
  • A new angiogenesis inhibitor, FR-118487 was obtained by chemical modification of FR-111142 which was isolated from the fermentation products of Scolecobasidium arenarium F-2015. The antiangiogenic activity of FR-118487 was compared with that of the parent compound, FR-111142. In the endothelial cell proliferation test in vitro and the angiogenesis in the chick embryo chorioal-lantoic membrane assay, FR-118487 had about 5∼10 times stronger antiangiogenic activities than FR-111142. In addition, FR-118487 inhibited the angiogenesis in the rabbit corneal assay and suppressed the solid tumor growth in mice. These findings showed that FR-118487 would be a unique antiangiogenic agent with promising antitumor activity.

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Antihepatotoxic Activity of Cassia tora Leaf Extract

  • Maity, Tapan K.;Mandal, Subhash C.;Pal, M.;Saha, B.P.
    • Natural Product Sciences
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    • v.4 no.4
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    • pp.226-229
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    • 1998
  • Methanolic extract of Cassia tora leaves was evaluated for its hepatoprotective activity in rats by inducing hepatotoxicity with paracetamol (acute model). The extract at a dose of 400 mg/kg orally exhibited significant protective effect by lowering the serum levels of transaminase (SGOT and SGPT), bilirubin, and alkaline phosphatase (ALP). The effects produced were comparable to that of a standard hepatoprotective agent.

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Antioxidative and antigenotoxic activity of vegetable and fruit extracts

  • Heo, Chan;Lee, Seung-Chul;Kim, Hyun-Pyo;Heo, Moon-Young
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.110.2-110.2
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    • 2003
  • The ethanol extracts of mixed vegetables (Bioactive V, BV), mixed fruits (Bioactive F, BF) and its liquid formulation (Chungpae Plus$\circledR$) were evaluated for their antioxidative and antigenotoxic activity. They were shown to possess the significant free radical scavenging effect against l,l-diphenyl-2-picryl hydrazine (DPPH) radical generation and were revealed to show the inhibitory effect of lipid peroxidation as measured by malondialdehyde (MDA) formation. (omitted)

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Synthesis of Certain 6-(Arylthio)uracils and Related Derivatives as Potential Antiviral Agents

  • El-Emam, Ali A.;Massoud, Mohamed A.M.;El-Bendary, Eman R.;El-Sayed, Magda A.
    • Bulletin of the Korean Chemical Society
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    • v.25 no.7
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    • pp.991-996
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    • 2004
  • New series of 6-(arylthio)uracils, 6-(4-substituted-1-piperazinyl)uracils, 2,4,5-trioxo-1H,3H-benzothiopyrano[2,3-d]pyrimidine and 5-aryl-2,4-dioxo-1H,3H-pyrimido[5,4-f]benzo[1,4]thiazepines have been prepared and screened for their in vitro activity against herpes simplex-1 virus (HSV-1) and human immunodeficiency virus-1 (HIV-1). The in vitro cytotoxic activity was also evaluated. The results of biological testing revealed that compound 5b showed marginal activity against HSV-1, while compounds 5b and 5f exhibited marginal activity against HIV-1. The rest of the tested compounds were found devoid of antiviral activity against both HSV-1 and HIV-1.

An Ellagic Acid Rhamnoside from the Roots of Potentilla discolor with Protein Glycation and Rat Lens Aldose Reductase Inhibitory Activity

  • Jang, Dae-Sik;Yoo, Nam-Hee;Kim, Jong-Min;Lee, Yun-Mi;Yoo, Jeong-Lim;Kim, Young-Sook;Kim, Jin-Sook
    • Natural Product Sciences
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    • v.13 no.2
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    • pp.160-163
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    • 2007
  • Four glycosides, rosamultin (1), tetracentronside B (2), 4-O-methylellagic acid 3-O-${\alpha}$-$_L$-rhamnopyranoside (3), and vanillic acid 4-O-${\beta}$-$_L$-glucopyranoside (4), isolated from the roots extract of Potentilla discolor, were subjected to in vitro bioassays to evaluate the inhibitory activity on advanced glycation end products (AGEs) formation and rat lens aldose reductase (RLAR). Compound 3 exhibited a significant inhibitory activity against both AGEs formation and RLAR with IC$_{50}$ values of 79.5 and 8.03 ${\mu}$M, respectively. All the compounds (1-4) were isolated for the first time from this plant.