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Synthesis and Activity of New Schiff Bases of Furocoumarin
Heterocyclic Communications ( IF 2.3 ) Pub Date : 2020-12-31 , DOI: 10.1515/hc-2020-0115
Huijun Xie 1, 2 , Chao Niu 1, 2, 3 , Zeyang Chao 1 , Nuramina Mamat 1 , Haji Akber Aisa 1, 2
Affiliation  

Abstract Furocoumarins, such as 8-MOP, are the most common medications used to relieve the symptoms of vitiligo clinically. Some furocoumarins also showed excellent performance in an anti-bacterial assay. This paper describes the synthesis of a series of novel Schiff bases (6a-6k), and their promotion in melanogenesis and anti-bacterial properties were studied in vitro. The pigment production of B16 cells and bacterial inhibition ring assay were applied for the bioactivity of 6a-6k. According to the results, a stronger promotion on pigment content was observed, when six compounds co-cultured with cells, compared with positive control (8-MOP). Significantly, compound 6k (237%) as the most active was found to increase the amount of melanin more than 1.7 times compared with 8-MOP activation rate (136%). All the compounds could moderately retard C. albicans growth. Interestingly, aldehyde 5, which possessed a broader antibacterial spectrum, showed the highest inhibition against C. albicans as well and much better than the positive control (Amphotericin B). Studies of 6k in animal models of vitiligo and related molecular mechanism are presently under way, with the aim of discovering an anti-vitiligo leading compound.

中文翻译:

呋喃香豆素新席夫碱的合成及活性

摘要 呋喃香豆素,如8-MOP,是临床上最常用的缓解白癜风症状的药物。一些呋喃香豆素在抗菌试验中也表现出优异的性能。本文描述了一系列新型希夫碱 (6a-6k) 的合成,并在体外研究了它们在黑色素生成和抗菌特性中的促进作用。6a-6k的生物活性应用B16细胞的色素产生和细菌抑制环测定。根据结果​​,与阳性对照 (8-MOP) 相比,当六种化合物与细胞共培养时,观察到对色素含量有更强的促进作用。值得注意的是,与 8-MOP 激活率 (136%) 相比,最活跃的化合物 6k (237%) 使黑色素的数量增加了 1.7 倍以上。所有化合物都可以适度延迟 C. 白色念珠菌的生长。有趣的是,醛 5 具有更广的抗菌谱,对白色念珠菌的抑制作用也最高,并且比阳性对照(两性霉素 B)好得多。目前正在进行白斑病动物模型中的6k及其相关分子机制的研究,目的是发现抗白斑病的先导化合物。
更新日期:2020-12-31
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