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