• 제목/요약/키워드: ergosterol derivative

검색결과 4건 처리시간 0.02초

Ergosteryl Myristate, a New Ergosterol Derivative from Unidentified Marine Algicolous Fungus

  • Lee, Dong-Ick;Choi, Jin-Souk;Yang, Mi-Rim;Lee, Won-Kap;Kim, Dong-Soo;Choi, Hong-Dae;Son, Byeng-Wha
    • Natural Product Sciences
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    • 제5권2호
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    • pp.93-96
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    • 1999
  • A new ergosteryl myristate (1) and ergosterol (2) have been isolated from the organic extract of the mycelium of unidentified marine algicolous fungus, isolate MF001. The structure of a new compound was assigned on the basis of comprehensive spectroscopic analyses and chemical synthesis.

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Synthesis of Ergosterol and 5,6-Dihydroergosterol Glycosides and Their Inhibitory Activities on Lipopolysaccharide-Induced Nitric Oxide Production

  • Park, HoonGyu;Lee, Tae Hoon;Chang, Fei;Kwon, Hyun Ji;Kim, Jiyoung;Kim, Hakwon
    • Bulletin of the Korean Chemical Society
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    • 제34권5호
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    • pp.1339-1344
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    • 2013
  • We have synthesized several glycosyl ergosterols and 5,6-dihydroergosterols (DHE) and examined their effects on production of nitric oxide (NO) and iNOS protein expression in LPS-treated RAW264.7 macrophage cells. Our results showed that DHE derivatives inhibited production of NO and iNOS protein expression more strongly than ergosterol derivative. Especially, DHE-Glc exhibited most potent inhibitory activity without cytotoxicity up to the concentration of $100{\mu}M$.

Anti-Candida Activity of YH-1715R, a New Triazole Derivative

  • Park, Kang-Sik;Kang, Heui-Il;Lee, Jong-Wook;Paik, Young-Ki
    • Journal of Microbiology and Biotechnology
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    • 제14권4호
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    • pp.693-697
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    • 2004
  • YH-1715R, (2R,3R)-2-(2,4-difluorophenyl)-3-(3-methoxy-1,2,4-isothiazol-3-yl-thio)-1-( 1H-1,2,4-triazol-l-yl)-2-butanol, a new triazole derivative obtained by the structural modification of fluconazole, was found to exhibit potent anti-Candida activity against a wide variety of Candida albicans (C. albicans) (MIC: 0.4-12.5 mg/l). To investigate the mode of action of YH-1715R, its effect on ergosterol biosynthesis in cell-free extracts and whole cells of C. albicans was examined. The inhibitory activity of YH-1715R was approximately ten-fold higher than that of fluconazole. To determine the primary action mechanism of YH-1715R, its inhibitory activity against lanosterol $14\alpha$-demethylase (14$\alpha$-DM), a major target for azole, was measured using gas-liquid chromatography. YH-1715R and fluconazole were found to inhibit 14a-DM with an $IC_{50}$ of 0.015 $\mu$M and 0.01$8\mu$M, respectively, plus the mode of inhibition of YH-1715R and fluconozole was noncompetitive with a $K_i$ of 0.0533$\mu$M and 0.0975$\mu$M.

낙엽송층버섯으로부터 Ergosterol 유도체의 분리 및 RAW 264.7 세포주의 Nitric Oxide 생성 저해활성 (Inhibition of Nitric Oxide Synthesis by Ergosterol Derivative from Phellinus pini in LPS-Activated RAW 264.7 Cells)

  • 장현진;양기숙
    • 약학회지
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    • 제50권6호
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    • pp.367-371
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    • 2006
  • Phellinus pini (Hymenocaetaceae) has been used for the immunomodulating activity hypolipidemic effect, gastric cancer non-insulin dependant diabetes, diarrhea, and menstrual irregularity. From the screening of each fraction for the inhibitory activity of NO production in lipopolysaccaride (LPS) activated RAW 264.7 cells, methanol extract of Phellinus pini and hexane soluble fraction exhibited inhibition of NO production compared with LPS control without toxicity. The hexane soluble fraction showed dose dependent inhibition of NO production. According to activity guided fractionation, the active hexane fr. was repeatedly chromatographed over silica gel, ergosta-4,6,8(14),22- tetraen-3-one was isolated. The compound inhibited NOS activation (IC$_{50}$ = 29.7 uM) and NO production of activated macrophage at 30 uM.