Design, synthesis and biological evaluation of alginate oligosaccharide derivatives

IF 2.5 4区 医学 Q3 CHEMISTRY, MEDICINAL
Wenkang Guo , Manchun Chen , Changjie Zou , Weizhi Liu , Weidong Wang , Heyong Gao
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Abstract

To discover new potential drug for acute kidney injury (AKI), a series of novel alginate oligosaccharide derivatives were synthesized and characterized by the spectroscopic analysis. By using the controlled experimental method, the target compounds were evaluated preliminarily for therapeutic activity in AKI. The results demonstrated that compounds 2a, 2b, 2c and 3b exhibited notable inhibitory activity against the expression of related proteins at 250 μg/ml in vitro. Furthermore, the in vivo activity of 2a and 2b was found to be comparable to that of the trisaccharide (AOSC).

Abstract Image

海藻酸寡糖衍生物的设计、合成和生物学评价。
为了发现治疗急性肾损伤(AKI)的新药,研究人员合成了一系列新型海藻酸寡糖衍生物,并通过光谱分析对其进行了表征。通过对照实验法,初步评价了目标化合物对 AKI 的治疗活性。结果表明,化合物 2a、2b、2c 和 3b 在 250 μg/ml 的体外浓度下对相关蛋白的表达具有显著的抑制活性。此外,还发现 2a 和 2b 的体内活性与三糖(AOSC)相当。
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来源期刊
CiteScore
5.70
自引率
3.70%
发文量
463
审稿时长
27 days
期刊介绍: Bioorganic & Medicinal Chemistry Letters presents preliminary experimental or theoretical research results of outstanding significance and timeliness on all aspects of science at the interface of chemistry and biology and on major advances in drug design and development. The journal publishes articles in the form of communications reporting experimental or theoretical results of special interest, and strives to provide maximum dissemination to a large, international audience.
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