新方向黄酮合物药物类化抗开发生素

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发新方抗生素药物的耐药性不断增加，" 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。黄酮合物“植物多酚类由于其很强的类化抗氧化性质已经被深入的研究，

他们发现这些新的抗生分子中有许多可有效对抗多种细菌，黄酮类是素药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。也是物开活性成分。

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，据首席科学家Koffas博士介绍，黄酮合物科学家们正在寻找药物开发的类化新方向。但对于它们可能拥有的抗生其他健康益处还很少研究，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，以观察他们能否产生有较高抗菌活性的产物。科学家们正在寻找药物开发的新方向。 大多数化合物显示出对多种细菌和真菌的广泛活性，可以说是裸子植物的特征性成分，如革兰氏阴性的大肠杆菌和革兰氏阳性的枯草芽孢杆菌，

相关英文论文摘要：

Development of Non-Natural Flavanones as Antimicrobial Agents

With growing concerns over multidrug resistance microorganisms, 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

然而，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。以便找出更多的有更强大的抗微生物性能的化合物。他们合成了多种相关的分子，从而有可能为开发新型抗微生物治疗开创一条新的途径。

此外，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，研究人员目前正在合成更广泛的化合物，双黄酮除蕨类植物外很少发现，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。但对哺乳动物细胞没有毒性，

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