• Title/Summary/Keyword: Mollugin

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Mollugin-mediated Inhibition of Proinflammatory Biomarkers in Lipopolysaccharide-stimulated RAW264.7 Cells

  • Kim, Jin-Kyung;Park, Geun-Mook;Jun, Jong-Gab
    • Biomedical Science Letters
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    • v.18 no.4
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    • pp.338-344
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    • 2012
  • Mollugin is the active compound of Rubia cordifolia, a well known herb widely used in alternative medicines for the treatment of various inflammatory diseases including arthritis and uteritis. In the present study, we investigated the anti-inflammatory effects of mollugin in lipopolysaccharide (LPS)-stimulated RAW264.7 murine macrophage cells. Treatment with mollugin significantly inhibited LPS-induced release of nitric oxide, prostaglandin $E_2$, and inflammatory cytokines, such as tumor necrosis factor-${\alpha}$ and interleukin-6. In addition, mollugin suppressed LPS-induced nuclear factor-kappa B (NF-${\kappa}B$) transcriptional activity. These results suggest that mollugin inhibits LPS-induced expression of inflammatory molecules via NF-${\kappa}B$, at least in part, and indicate the potential value of mollugin as a valuable new drug candidate for the treatment of various inflammatory diseases.

Effects of Mollugin on Hepatic Cytochrome P450 in Male ICR Mice as Determined by Liquid Chromatography/Tandem Mass Spectrometry

  • Song, Min;Hong, Miri;Choi, Hyun Gyu;Jahng, Yurngdong;Lee, Seung Ho;Lee, Sangkyu
    • Mass Spectrometry Letters
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    • v.3 no.4
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    • pp.104-107
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    • 2012
  • Mollugin isolated from Rubia cordifolia is known to have anti-inflammatory, anti-cancer, and anti-viral activities. In the present study, a cocktail probe assay and LC-MS/MS were used to investigate the modulating effect of mollugin on cytochrome P450 (CYP) enzymes in male ICR mice. After mollugin was orally administrated to mice at the 20, 40, or 80 mg/kg for 3 days, the activities of CYP in hepatic S-9 fractions were investigated. Unlike the selective inhibitory effect of mollugin on CYP1A2-catalyzed phenacetin O-deethylation in vitro, mollugin only significantly inhibited the activity of CYP2E1-catalyzed chlorzoxazone 6-hydroxylase in vivo. The activities of other CYPs were only slightly altered by mollugin. The results of this study suggest that mollugin might cause herb-drug interactions via the selective inhibition of CYP2E1 in vivo.

Facile Synthesis of Mollugin by Kinetic Control and anti-HCV (Hepatitis C Virus) Activity of Its Analogues

  • Choi, Da Hye;Lee, Na Ri;Kim, Cheol Gi;Kim, Jong Woo;Lee, Sang Wook;Jun, Jong-Gab
    • Bulletin of the Korean Chemical Society
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    • v.35 no.11
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    • pp.3232-3238
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    • 2014
  • Mollugin has been reported to have various biological activities including antineoplastic, antitumor, antiviral against the hepatitis B virus, anti-aging and antimutagenic activities. An effective and concise synthesis of mollugin in two steps including kinetic control from the cheap starting material 1,4-naphthoquinone has been introduced, and mollugin derivatives thus prepared are screened for their inhibition ability against the hepatitis C virus (HCV) and the dihydrobenzochromene structure might be an additional anti-HCV agent as a new leading compound.

Concise Synthesis of Biologically Interesting Mollugin and Its Analogues

  • Lee, Yong-Rok;Wang, Xue;Kim, Yun-Mi;Shim, Jae-Jin;Kim, Byung-Nam;Han, Do-Hung
    • Bulletin of the Korean Chemical Society
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    • v.28 no.10
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    • pp.1735-1738
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    • 2007
  • The synthesis of naturally occurring mollugin and its analogues, 3,4-dihydromollugin, cis-3,4-dihydroxy-3,4- dihydromollugin, and trans-3,4-dihydroxy-3,4-dihydromollugin was achieved starting from 1,4-dihydroxynaphthalene- 2-carboxylic acid. The key reaction is an electrocyclization for pyranyl ring formation in the presence of PhB(OH)2/AcOH.