通过Butelase 1进行循环细菌素的总合成
Xinya Hemu1, Yibo Qiu1, Giang K T Nguyen1
1School of Biological Sciences, Nanyang Technological University , 60 Nanyang Drive, 637551 Singapore.
Journal of the American Chemical Society
|May 21, 2016
概括
研究人员从乳酸细菌中合成了大型圆形细菌素, 它们的化学酶方法克服了合成挑战, 产生抗药性病原体的活性化合物.
科学领域:
- 生物化学
- 有机化学
- 微生物学
背景情况:
- 循环细菌素是来自乳酸细菌的大型循环,对抑制其他细菌至关重要.
- 它们的循环结构提高了食品保存的稳定性,但由于疏水性细分而使化学合成复杂化.
研究的目的:
- 为了实现三种大型圆形细菌素的总合成:AS-48,uberolysin和garvicin ML.
- 开发一种有效的化学酶策略, 克服这些复杂所带来的合成挑战.
主要方法:
- 使用微波逐步合成制备线性前体.
- 用于有效关闭骨干环的方法是使用Asn特异的布特拉酶介导循环.
- 使用标准测试来评估抗菌活性.
主要成果:
- 已经成功完成了AS-48,uberolysin和garvicin ML的总合成.
- AS-48的线性前体在100μM时没有抗菌活性.
- 宏循环AS-48对病原和耐药细菌表现出强烈的抗菌活性,具有亚微量MIC.
结论:
- 开发的化学酶策略对于合成大型复杂的循环细菌素是有效的.
- 循环化对于像AS-48这样的细菌素具有强烈的抗菌活性至关重要.
- 这项工作为生产这些有价值的抗菌剂提供了可行的途径.
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