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Volume 31 Issue 5
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Article Navigation >  Journal of Pharmaceutical Practice and Service  > 2013  >  31(5): 359-361,365

WANG Ke-bing, ZHANG Lu-lu, CHENG Bin, LIU Hong-tao, CAO Yong-bing, JIANG Yuan-ying. The effect of butenafine on ergosterol biosynthesis in fungi by measuring incorporation of nuclide[J]. Journal of Pharmaceutical Practice and Service, 2013, 31(5): 359-361,365. doi: 10.3969/j.issn.1006-0111.2013.05.011
Citation: WANG Ke-bing, ZHANG Lu-lu, CHENG Bin, LIU Hong-tao, CAO Yong-bing, JIANG Yuan-ying. The effect of butenafine on ergosterol biosynthesis in fungi by measuring incorporation of nuclide[J]. Journal of Pharmaceutical Practice and Service, 2013, 31(5): 359-361,365. doi: 10.3969/j.issn.1006-0111.2013.05.011
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The effect of butenafine on ergosterol biosynthesis in fungi by measuring incorporation of nuclide

doi: 10.3969/j.issn.1006-0111.2013.05.011
  • 1.

    Department of pharmacy, the 169th Hospital of PLA, Hengyang 421002, China

  • 2.

    School of Pharmacy, Second Military Medical University, Shanghai 200433, China

  • 3.

    Department of Scientific Resarch, Second Military Medical University, Shanghai 200433, China

  • 4.

    Department of pharmacy, Beijing Stomatological Hospital, Capital Medical University, Beijing 100050, China

  • Received Date: 2013-03-07
  • Rev Recd Date: 2013-05-07
  • Objective To study the effect of butenafine on ergosterol biosynthesis in fungi by measuring incorporation of nuclide. Methods The inhibitory effect of butenafine on ergosterol biosynthesis in whole-cell fungi was studied by measuring the incorporation of [1-14C] acetate into nonsaponifiable lipids( NSLs), while the effect in cell-free extracts was studied by measuring the incorporation of [2-14C] mevalonate into NSLs. Results The synthesis of ergosterol in fungi was significantly decreased after butenafine treatment, whereas the level of squalene was increased. The IC50 value of butenafine on ergosterol biosynthesis was 136.19 nmol/L in whole-cell study and 203.15 nmol/L in cell-free study. Conclusion The method to measure the incorporation of [1-14C]acetate and [2-14C] mevalonate into NSLs of fungi, which could indicate the level of squalene, might be widely used to study the mechanism of inhibitor of squalene epoxidase.
  • [1] Iwatani W, Arika T, Yamaguchi H. Two mechanisms of butenafine action in Candida albicans[J]. Antimicrob Agents Chemother, 1993, 37(4): 785.
    [2] McNeely W, Spencer CM. Butenafine[J]. Drugs, 1998, 55(3):405.
    [3] 曹永兵, 孙福红. 薄层色谱扫描法检测氟康唑对真菌麦角固醇生物合成的影响[J]. 第二军医大学学报, 1999, 20(5): 312.
    [4] 曹永兵, 高平挥, 张军东, 等. 核素掺入研究氟康唑对真菌麦角甾醇生物合成的影响[J]. 第二军医大学学报, 2004, 25(7): 751.
    [5] 晏秀伟, 刘洪涛, 曹永兵, 姜远英. 同位素掺入法测定耐药白念珠菌CYP51酶活性[J]. 中国新医药. 2004, 3(6): 1.
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The effect of butenafine on ergosterol biosynthesis in fungi by measuring incorporation of nuclide

doi: 10.3969/j.issn.1006-0111.2013.05.011
  • 1. Department of pharmacy, the 169th Hospital of PLA, Hengyang 421002, China
  • 2. School of Pharmacy, Second Military Medical University, Shanghai 200433, China
  • 3. Department of Scientific Resarch, Second Military Medical University, Shanghai 200433, China
  • 4. Department of pharmacy, Beijing Stomatological Hospital, Capital Medical University, Beijing 100050, China
  • Received Date: 2013-03-07
  • Rev Recd Date: 2013-05-07

Abstract: Objective To study the effect of butenafine on ergosterol biosynthesis in fungi by measuring incorporation of nuclide. Methods The inhibitory effect of butenafine on ergosterol biosynthesis in whole-cell fungi was studied by measuring the incorporation of [1-14C] acetate into nonsaponifiable lipids( NSLs), while the effect in cell-free extracts was studied by measuring the incorporation of [2-14C] mevalonate into NSLs. Results The synthesis of ergosterol in fungi was significantly decreased after butenafine treatment, whereas the level of squalene was increased. The IC50 value of butenafine on ergosterol biosynthesis was 136.19 nmol/L in whole-cell study and 203.15 nmol/L in cell-free study. Conclusion The method to measure the incorporation of [1-14C]acetate and [2-14C] mevalonate into NSLs of fungi, which could indicate the level of squalene, might be widely used to study the mechanism of inhibitor of squalene epoxidase.

WANG Ke-bing, ZHANG Lu-lu, CHENG Bin, LIU Hong-tao, CAO Yong-bing, JIANG Yuan-ying. The effect of butenafine on ergosterol biosynthesis in fungi by measuring incorporation of nuclide[J]. Journal of Pharmaceutical Practice and Service, 2013, 31(5): 359-361,365. doi: 10.3969/j.issn.1006-0111.2013.05.011
Citation: WANG Ke-bing, ZHANG Lu-lu, CHENG Bin, LIU Hong-tao, CAO Yong-bing, JIANG Yuan-ying. The effect of butenafine on ergosterol biosynthesis in fungi by measuring incorporation of nuclide[J]. Journal of Pharmaceutical Practice and Service, 2013, 31(5): 359-361,365. doi: 10.3969/j.issn.1006-0111.2013.05.011
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