A Benzimidazolium-Based Organic Cage with Antimicrobial Activity
A Benzimidazolium-Based Organic Cage with Antimicrobial Activity
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DOI：
10.3390/chemistry4030061
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发表时间：
2022-09-01
影响因子：
2.1
通讯作者：
Amendola, Valeria
中科院分区：
文献类型：
--
作者：
La Cognata, Sonia;Armentano, Donatella;Amendola, Valeria
考虑到（苯并）咪唑类药物的广泛兴趣，我们在这里报告我们的研究苯并咪唑类有机笼作为潜在的抗菌和抗真菌剂。对人源细胞系SH-SY 5 Y的细胞毒性研究表明，在研究浓度下，融合器无细胞毒性。阴离子结合研究表明，笼可以结合阴离子（氯离子和硝酸根，特别是）在有机溶剂和20%v的D2 O/CD 3CN混合物。笼也被测试为阴离子载体，显示出弱的，但可测量的跨LUVs囊泡的氯化物和硝酸盐的运输。尽管如此，所述化合物对金黄色葡萄球菌（革兰氏阳性菌）具有抗微生物活性。这可能是作为阴离子载体和抗微生物剂研究的第一个有机笼。
Considering the wide interest in (benz)imidazolium-based drugs, we here report our study on a benzimidazolium-based organic cage as potential antimicrobial and antifungal agent. Cytotoxicity studies on a human derived cell line, SH-SY5Y, showed that the cage is not cytotoxic at all at the investigated concentrations. Anion binding studies demonstrated that the cage can bind anions (chloride and nitrate, in particular) both in organic solvent and 20%v D2O/CD3CN mixture. The cage was also tested as anionophore, showing a weak but measurable transport of chloride and nitrate across LUVs vesicles. Nonetheless, the compounds have antimicrobial activity towards Staphylococcus aureus (Gram-positive bacteria). This is probably the first organic cage studied as anionophore and antimicrobial agent.