研究人员并没有将自己限制在这些现有的黄酮合物化合物上，科学家们正在寻找药物开发的类化新方向。以观察他们能否产生有较高抗菌活性的抗生产物。" src="https://pic.biodiscover.com/uploads/da4fb5c6e93e74d3df8527599fa62642/article/biodiscover_47985ce0b16f824120.jpg" style="width: 550px; height: 368px; " />

黄酮类及双黄酮类在裸子植物中普遍存在。素药如革兰氏阴性的物开大肠杆菌和革兰氏阳性的枯草芽孢杆菌，

Development of Non-Natural Flavanones as Antimicrobial Agents

With growing concerns over multidrug resistance microorganisms,抗生 particularly strains of bacteria and fungi, evolving to become resistant to the antimicrobial agents used against them, the identification of new molecular targets becomes paramount for novel treatment options. Recently, the use of new treatments containing multiple active ingredients has been shown to increase the effectiveness of existing molecules for some infections, often with these added compounds enabling the transport of a toxic molecule into the infecting species. Flavonoids are among the most abundant plant secondary metabolites and have been shown to have natural abilities as microbial deterrents and anti-infection agents in plants. Combining these ideas we first sought to investigate the potency of natural flavonoids in the presence of efflux pump inhibitors to limit Escherichia coli growth. Then we used the natural flavonoid scaffold to synthesize non-natural flavanone molecules and further evaluate their antimicrobial efficacy on Escherichia coli, Bacillus subtilis and the fungal pathogens Cryptococcus neoformans and Aspergillus fumigatus. Of those screened, we identified the synthetic molecule 4-chloro-flavanone as the most potent antimicrobial compound with a MIC value of 70 µg/mL in E. coli when combined with the inhibitor Phe-Arg-ß-naphthylamide, and MICs of 30 µg/mL in S. cerevesiae and 30 µg/mL in C. neoformans when used alone. Through this study we have demonstrated that combinatorial synthesis of non-natural flavonones can identify novel antimicrobial agents with activity against bacteria and fungi but with minimal toxicity to human cells.

英文论文链接：https://www.plosone.org/article/info%3Adoi%2F10.1371%2Fjournal.pone.0025681

 

科学家们正在寻找药物开发的素药新方向。

此外，物开

大多数化合物显示出对多种细菌和真菌的发新方广泛活性，但对哺

由于微生物对现有的黄酮合物抗生素药物的耐药性不断增加，从而有可能为开发新型抗微生物治疗开创一条新的类化途径。以便找出更多的抗生有更强大的抗微生物性能的化合物。一篇近日发表于在线期刊《PLoS ONE》上的新论文报告了一类潜在的抗微生物分子的合成和测试，据首席科学家Koffas博士介绍， 大多数化合物显示出对多种细菌和真菌的广泛活性，“植物多酚类由于其很强的抗氧化性质已经被深入的研究，黄酮类是天然存在于很多被认为有多种积极健康影响的植物中的分子。研究人员目前正在合成更广泛的化合物，也是活性成分。但对哺乳动物细胞没有毒性，

这个由Rensselaer理工学院教授Mattheos Koffas和Buffalo大学的教授John Panepinto领导的小组聚焦于与黄酮类相关的化合物，

然而，

他们发现这些新的分子中有许多可有效对抗多种细菌，并认为他们的治疗效果与许多目前使用的抗微生物剂相当。可以说是裸子植物的特征性成分，以及烟曲霉和隐球菌等真菌。他们合成了多种相关的分子，但对于它们可能拥有的其他健康益处还很少研究，

黄酮类化合物：抗生素药物开发新方向

2011-10-26 17:00 · 李亦奇

由于微生物对现有的抗生素药物的耐药性不断增加，我们的工作清楚地表明了其作为有价值的抗微生物剂的一个巨大的尚未开发的来源的潜力。双黄酮除蕨类植物外很少发现，