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准备和生物活性 isoperrottetin A 和它的盐衍生物的酸盐

Mário Markuliak¹, Dominika Kos², Veronika Vojáčková³

¹Department of Chemical Theory of Drugs, Faculty of Pharmacy, Comenius University Bratislava, Kalinčiakova 8, 83104 Bratislava, Slovakia.

European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences

|June 13, 2025

概括

从肝化合物中提取的新盐显示出强大的抗菌活性,对抗MRSA和VRE等耐药菌株. 这些新型微生物杀伤剂为治疗具有挑战性的感染提供了有希望的替代方案.

科学领域:

自然产品化学自然产品化学
药用化学医学化学
微生物学微生物学

背景情况:

抗生素耐药性构成了全球严重的健康威胁,需要开发新型抗菌剂.
鼻腔感染往往会带来治疗挑战,推动人们寻找新的治疗化合物.
肝是具有潜在生物活性的独特 bis ((bibenzyl) 化合物的来源.

研究的目的:

为了合成和评估一系列来自bis ((bibenzyl) isoperrottetin A的盐的抗菌性质.
研究这些新型化合物对一系列临床相关细菌的抗菌疗效,包括耐药菌株.
探索合成化合物的更广泛的生物活动,例如对细胞呼吸和细胞毒性的影响.

主要方法:

采用了涉及乌尔曼和维蒂格反应的八步合成方法,制备了十种盐.
使用最小杀菌度 (MBC) 测试对抗格兰阳性 (黄金葡萄球菌,白菌) 和格兰阴性 (大肠杆菌, Pseudomonas aeruginosa, Klebsiella pneumoniae) 细菌进行抗菌活性评估.
还对Mycobacterium smegmatis和Mycobacterium marinum进行了活性测试,对黑色素瘤,视网膜和上皮细胞进行了细胞毒性评估.

主要成果:

几种合成的盐表现出显著的抗菌活性,大多数衍生品的性能优于母化合物异罗丁A.
化合物4P (5,5',5'',5'''-[1,7(1),4,5(1,3) -四二甲-1³,4⁴,5⁶,8³-四二甲{oxy) ]四甲5-[oxo-P,P,P-triphenylpentane-1-phosphonium) tetrabromide) 显示出强烈的活性,MBC值<1μM对甲素敏感/耐药的金黄色菌和对香素敏感/耐药的E. faecalis.
化合物4P在MBC值显示出有利的安全性,而不会损害细胞壁,还抑制了细胞呼吸,并对测试的细胞系表现出细胞毒性.

结论:

用酸化学修饰bis (((bibenzyls) 产生强大的微生物杀伤性化合物.
这些来自肝的新型盐显示出作为对敏感和耐药细菌菌株的治疗剂的巨大潜力.
这些发现强调了天然产品的价值,作为开发打击抗微生物药物耐药性的新策略的来源.

关键词:

具有抗菌活性,具有抗菌活性.比亚利斯的比亚利斯布里奥菲特 (Bryophytes) 是一种植物.细胞毒性活动的细胞毒性.酸盐是一种酸盐.聚醇是一种多醇.维蒂格的反应反应.

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