Department of Biological Engineering, Graduate School of Science and Engineering, Yamagata University, Yonezawa 992-8510, Japan.
Faculty of Pharmaceutical Science, Mukogawa Women's University, Nishinomiya 663-8179, Japan.
Molecules. 2022 Feb 10;27(4):1191. doi: 10.3390/molecules27041191.
The burkholdines are a family of cyclic lipopeptides reported to exhibit antifungal activity. We synthesized a series of 18 burkholdine analogues in good yield by conventional Fmoc-SPPS followed by cyclization with DIPCI/HOBt in the solution phase. Although none of the synthesized peptides exhibited antifungal activity, several did potentiate the antibiotic effect of the antibiotic G418, including the Thr-bearing Bk analogue () and the tartaramide-bearing Bk analogue (). This work exemplifies the potential of burkholdine analogues as potentiating agents.
伯克霍尔德菌素是一类具有抗真菌活性的环脂肽。我们通过常规的 Fmoc-SPPS 合成了一系列 18 个伯克霍尔德菌素类似物，然后在溶液相中用 DIPCI/HOBt 进行环化反应。虽然合成的肽都没有抗真菌活性，但有几个能够增强抗生素 G418 的作用，包括含有 Thr 的伯克霍尔德菌素类似物 () 和含有酒石酰胺的伯克霍尔德菌素类似物 ()。这项工作说明了伯克霍尔德菌素类似物作为增效剂的潜力。
