微生物对抗结核病剂黄的糖化
1Department of Biological Engineering, Utah State University, 4105 Old Main Hill, Logan, UT 84322-4105, USA.
Journal of bioscience and bioengineering
|September 24, 2023
概括
研究人员开发了黄的水溶性糖化物,一种具有抗结核活性的化合物. 这些新型衍生品显示出增强的溶解性,为开发新的抗结核药物来对抗耐药菌株提供了有前途的战略.
科学领域:
- 生物化学 生物化学
- 微生物学 微生物学
- 药用化学 医学化学
背景情况:
- 黄素具有健康益处,包括抗氧化和抗炎性质,用于营养品和药品中.
- 纤维状真菌,如Aspergillus candidus,产生生物活性黄素,如黄,它表现出抗真菌和抗结核 (抗结核病) 活动.
- 黄的低水溶性限制了其生物可用性,需要制定策略来改善其用于治疗的物理化学性质.
研究的目的:
- 开发新的水溶性黄衍生物,以应对耐药结核病的挑战.
- 通过糖化,增强黄的极性和生物可用性.
主要方法:
- 优化发酵和净化过程,以增加阿斯伯吉卢斯候选菌NRRL 5214.4中黄的产量.
- 通过使用Streptomyces chromofuscus ATCC 49982和Beauveria bassiana ATCC 7159进行微生物糖化,生产了两个黄糖化物,即黄-5-O-β-d-glucuronopyranoside (1) 和黄-7-O-4′′-O-methyl-β-d-glucopyranoside (2).
- 量化了母化合物及其糖基化衍生物的水溶性.
主要成果:
- 在A. candidus.中显著增加了黄的产生.
- 与原始化合物相比,成功合成了两种新型黄糖化物,明显提高了水溶性.
- 黄-5-O-β-d-glucuronopyranoside (1) 的溶解度为117.86 ± 4.81 mg/L,而黄-7-O-4′′-O-methyl-β-d-glucopyranoside (2) 的溶解度为124.34 ± 9.13 mg/L,而黄的溶解度为4.38 ± 0.54 mg/L.
结论:
- 甘化是一种有效的方法,可以提高黄的水溶性和物理化学性质.
- 开发的水溶性黄糖化物代表了开发抗耐药结核病新型治疗剂的有希望的候选人.
- 这项研究提出了一个可行的策略,用于为抗结核病药物发现创造改进的黄衍生物.
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