核素掺入研究布替萘芬对真菌麦角甾醇生物合成的影响

王科兵; 张璐璐; 程滨; 刘洪涛; 曹永兵; 姜远英

doi:10.3969/j.issn.1006-0111.2013.05.011

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核素掺入研究布替萘芬对真菌麦角甾醇生物合成的影响

王科兵, 张璐璐, 程滨, 刘洪涛, 曹永兵, 姜远英

文章导航 > 药学实践与服务 > 2013 > 31(5): 359-361,365

王科兵, 张璐璐, 程滨, 刘洪涛, 曹永兵, 姜远英. 核素掺入研究布替萘芬对真菌麦角甾醇生物合成的影响[J]. 药学实践与服务, 2013, 31(5): 359-361,365. doi: 10.3969/j.issn.1006-0111.2013.05.011

引用本文:

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

核素掺入研究布替萘芬对真菌麦角甾醇生物合成的影响

doi: 10.3969/j.issn.1006-0111.2013.05.011

1.
解放军第169医院药械科, 湖南衡阳 421001
2.
第二军医大学药学院, 上海 200433
3.
第二军医大学科研部, 上海 200433
4.
首都医科大学附属北京口腔医院药剂科, 北京 100050

基金项目: 国家自然科学基金(81273556).

The effect of butenafine on ergosterol biosynthesis in fungi by measuring incorporation of nuclide

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

摘要: 目的研究抗真菌药物布替萘芬对真菌麦角甾醇生物合成的影响。方法通过真菌活细胞[1-¹⁴C]乙酸钠掺入和离细胞液[2-¹⁴C]甲羟戊酸掺入实验,考察布替萘芬对真菌麦角甾醇生物合成的影响。结果布替萘芬能使真菌中麦角甾醇的合成减少,而增加角鲨烯的含量,两种方法测得布替萘芬对真菌细胞麦角甾醇生物合成的IC₅₀分别为136.19 nmol/L和203.15 nmol/L。结论布替萘芬为角鲨烯环氧化酶抑制剂,核素掺入法能定量考察布替萘芬对角鲨烯环氧化酶的抑制活性,且效果优于薄层色谱扫描法。
- 布替萘芬 /
- 麦角甾醇 /
- 角鲨烯环氧化酶 /
- 核素掺入 /
- 液体闪烁计数
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.
- butenafine /
- ergosterol /
- squalene epoxidase /
- fluid flash counter /

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核素掺入研究布替萘芬对真菌麦角甾醇生物合成的影响

doi: 10.3969/j.issn.1006-0111.2013.05.011

1. 解放军第169医院药械科, 湖南衡阳 421001

2. 第二军医大学药学院, 上海 200433

3. 第二军医大学科研部, 上海 200433

4. 首都医科大学附属北京口腔医院药剂科, 北京 100050

基金项目: 国家自然科学基金(81273556).

收稿日期: 2013-03-07
修回日期: 2013-05-07

关键词:

摘要: 目的研究抗真菌药物布替萘芬对真菌麦角甾醇生物合成的影响。方法通过真菌活细胞[1-¹⁴C]乙酸钠掺入和离细胞液[2-¹⁴C]甲羟戊酸掺入实验,考察布替萘芬对真菌麦角甾醇生物合成的影响。结果布替萘芬能使真菌中麦角甾醇的合成减少,而增加角鲨烯的含量,两种方法测得布替萘芬对真菌细胞麦角甾醇生物合成的IC₅₀分别为136.19 nmol/L和203.15 nmol/L。结论布替萘芬为角鲨烯环氧化酶抑制剂,核素掺入法能定量考察布替萘芬对角鲨烯环氧化酶的抑制活性,且效果优于薄层色谱扫描法。

English Abstract

The effect of butenafine on ergosterol biosynthesis in fungi by measuring incorporation of nuclide

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

Keywords:

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.

引用本文:

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