Department of Medicine, Karolinska University Hospital, Huddinge, 14186, Stockholm, Sweden.
J Appl Microbiol. 2009 Feb;106(2):624-33. doi: 10.1111/j.1365-2672.2008.04035.x.
To prepare 1,5-anhydro-d-fructose (AF) derivatives, test their microbial inhibition spectrum, and to further examine the most effective AF derivative against Pseudomonas aeruginosa and malignant blood cell lines.
Microthecin and nine other AF derivatives were synthesized from AF. The 10 compounds were tested in vitro against Gram-positive (GP) and Gram-negative (GN) bacteria, yeasts and moulds using a well diffusion method and in a Bioscreen growth analyser. Of the test compounds, microthecin exhibited the most significant antibacterial activity at 100-2000 ppm against both GP and GN bacteria, including Ps. aeruginosa. Further tests with three malignant blood cell lines (Mutu, Ramos, Raji) and one normal cell line indicated that microthecin was a cell toxin, with a cell mortality >85% at 50 ppm. The other nine AF derivatives demonstrated low or no antimicrobial activity.
Microthecin was active 100-2000 ppm against GP and GN bacteria including Ps. aeruginosa, but was inactive against yeasts and moulds. Microthecin was also a cytotoxin to some mammalian cell lines.
Microthecin might have potential for development as a novel drug against Ps. aeruginosa and to target cancer cells. It might also be developed as a food processing aid to control bacterial growth.
制备 1,5-脱水-D-呋喃果糖(AF)衍生物,测试其对微生物的抑制谱,并进一步研究对铜绿假单胞菌和恶性血癌细胞系最有效的 AF 衍生物。
从 AF 合成了微曲菌素和其他 9 种 AF 衍生物。使用平板扩散法和 Bioscreen 生长分析仪,将这 10 种化合物在体外测试对革兰氏阳性(GP)和革兰氏阴性(GN)细菌、酵母和霉菌的抑制活性。在 100-2000ppm 浓度下,微曲菌素对 GP 和 GN 细菌(包括铜绿假单胞菌)均表现出最显著的抗菌活性。对三种恶性血癌细胞系(Mutu、Ramos、Raji)和一种正常细胞系的进一步测试表明,微曲菌素是一种细胞毒素,在 50ppm 时细胞死亡率>85%。其他 9 种 AF 衍生物表现出低抗菌活性或无抗菌活性。
微曲菌素对 GP 和 GN 细菌(包括铜绿假单胞菌)的活性为 100-2000ppm,但对酵母和霉菌无活性。微曲菌素对一些哺乳动物细胞系也是细胞毒素。
微曲菌素可能有潜力开发为一种新型抗铜绿假单胞菌药物,并针对癌细胞。它也可能被开发为一种食品加工助剂,以控制细菌生长。