Synthesis and Activity of New Schiff Bases of Furocoumarin

Heterocyclic communications

article

Huijun Xie¹  Chao Niu¹  Zeyang Chao¹  Nuramina Mamat¹  Haji Akber Aisa¹ 

[1] State Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization and Key Laboratory of Plant Resources and Chemistry of Arid Zone, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences;University of Chinese Academy of Sciences;Ltd.

关键词: vitiligo;    furocoumarin;    melanin synthesis;    anti-bacterial activity;    SAR;   

DOI  :  10.1515/hc-2020-0115

学科分类：内科医学

来源: De Gruyter

【 摘 要 】

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.

【 授权许可】

CC BY|CC BY-NC-ND