Suppr超能文献

5-乙酰基-2-芳基-6-羟基苯并呋喃类化合物的合成、体外评价及针对 2 型糖尿病相关多靶点的分子对接

Synthesis, In Vitro Evaluation and Molecular Docking of the 5-Acetyl-2-aryl-6-hydroxybenzo[]furans against Multiple Targets Linked to Type 2 Diabetes.

机构信息

Department of Chemistry, University of South Africa, Private Bag X06, Florida 1710, South Africa.

Institute for Research in Molecular Medicine (INFORMM), Universiti Sains Malaysia, Penang 11800, Malaysia.

出版信息

Biomolecules. 2020 Mar 7;10(3):418. doi: 10.3390/biom10030418.

Abstract

The 5-acetyl-2-aryl-6-hydroxybenzo[]furans - have been evaluated through in vitro enzymatic assay against targets which are linked to type 2 diabetes (T2D), namely, α-glucosidase, protein tyrosine phosphatase 1B (PTP1B) and β-secretase. These compounds have also been evaluated for antioxidant activity using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) free-radical scavenging method. The most active compounds against α-glucosidase and/or PTP1B, namely, 4-fluorophenyl , 4-methoxyphenyl and 3,5-dimethoxyphenyl substituted derivatives were also evaluated for potential anti-inflammatory properties against cyclooxygenase-2 activity. The Lineweaver-Burk and Dixon plots were used to determine the type of inhibition on compounds and against α-glucosidase and PTP1B receptors. The interactions were investigated in modelled complexes against α-glucosidase and PTP1B via molecular docking.

摘要

5-乙酰基-2-芳基-6-羟基苯并[]呋喃 - 通过体外酶促测定针对与 2 型糖尿病 (T2D) 相关的靶点进行了评估,即α-葡萄糖苷酶、蛋白酪氨酸磷酸酶 1B (PTP1B) 和β-分泌酶。还使用 2,2-二苯基-1-苦基肼 (DPPH) 自由基清除法评估了这些化合物的抗氧化活性。对 α-葡萄糖苷酶和/或 PTP1B 最具活性的化合物,即 4-氟苯基、4-甲氧基苯基和 3,5-二甲氧基苯基取代的衍生物,也针对环氧化酶-2 活性的潜在抗炎特性进行了评估。Lineweaver-Burk 和 Dixon 图用于确定化合物对 α-葡萄糖苷酶和 PTP1B 受体的抑制类型。通过分子对接研究了与 α-葡萄糖苷酶和 PTP1B 的模型复合物中的相互作用。

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验