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通过气相色谱-质谱法量化埃尔戈斯特生物合成中的异类化合物
Maximilian Liebl1, Ludwig Huber1, Hesham Elsaman2
1Department of Pharmacy, Center for Drug Research, Ludwig-Maximilians University, 81377 Munich, Germany.
Journal of fungi (Basel, Switzerland)
|July 28, 2023
概括
一种新的全细胞查试验通过分析真菌细胞中的异oprenoid 模式来识别抗真菌药物标. 这种方法有助于发现抑制必要的ergosterol生物合成酶的化合物.
科学领域:
- 生物化学 生物化学
- 菌类学 菌类学是指菌类学.
- 药理学 药理学是指药理学的学科.
背景情况:
- 厄戈斯特醇途径对真菌细胞活力至关重要,也是抗真菌药物开发的关键目标.
- 现有的选方法需要改进,以识别异oprenoid生物合成酶的抑制剂.
研究的目的:
- 开发和验证一种全细胞查试验,用于识别厄戈斯特生物合成的抑制剂.
- 分析真菌细胞中的异oprenoid 形状,以确定受抑制的酶.
主要方法:
- 机械溶解 *Aspergillus fumigatus* 和 *Saccharomyces cerevisiae* 的细胞.
- 酶去化异烯酸铁酸盐,然后进行提取和GC-MS分析.
- 使用特比纳治疗和基因敲除菌株 (*erg9*, *erg1*) 的验证.
主要成果:
- 该试验成功地确定了特定的异oprenoid积累模式,表明了酶抑制.
- *erg9*下调导致了法内索尔,格拉尼尔格拉尼奥尔和异二醇的积累.
- 降低erg1表达和terbinafine治疗增加了素水平,在erg9下调期间在介质中检测到farnesyl pyrophosphate.
结论:
- 开发的全细胞检测方法对选潜在的针对异oprenoid生物合成的抗真菌化合物有效.
- 该方法提供了一种可靠的方式来识别埃尔戈斯特路径内的受抑制酶.
- 这种测定有助于发现新型抗真菌药物,通过表征化合物与真菌酶的相互作用.
关键词:
亚斯伯吉拉斯烟虫 (Aspergillus fumigatus) 是一种有毒的植物.在GC-MS中使用GC-MS.erg1 erg1 erg1 erg1 erg1 erg1 erg1 erg1 erg1 erg1 erg1 erg1erg9 erg9 erg9 的意思是什么意思埃尔戈斯特醇生物合成法恩索尔 (Farnesol) 是一个农场.这是异oprenoids.特尔比纳非因 (terbinafine) 是一种药物.更多相关视频
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