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一些新型苔色酸酯和与黑茶渍素相关的缩酚酸作为α-葡萄糖苷酶抑制剂的合成。

Synthesis of some novel orsellinates and lecanoric acid related depsides as -glucosidase inhibitors.

作者信息

Rama Krishna Boddu, Ramakrishna Sistla, Rajendra Sangaraju, Madhusudana Kuncha, Mallavadhani Uppuluri Venkata

机构信息

Natural Products Chemistry Division, CSIR-Indian Institute of Chemical Technology , Hyderabad 500007 , India.

Academy of Scientific and Innovative Research (AcSIR), CSIR-Indian Institute of Chemical Technology , Hyderabad 500007 , India.

出版信息

J Asian Nat Prod Res. 2019 Oct;21(10):1013-1027. doi: 10.1080/10286020.2018.1490274. Epub 2018 Jul 3.

DOI:10.1080/10286020.2018.1490274
PMID:29968482
Abstract

Sixteen novel orsellinic esters () along with four lecanoric acid related depsides (3) were synthesized and confirmed their structures by spectroscopic data (H, C & HRMS). The synthesized compounds were evaluated for their -glucosidase () inhibitory potential. Among the tested compounds, (IC: 140.9 μM) and (IC: 203.9 μM) displayed potent α-glucosidase inhibitory activity and found more active than the standard drug acarbose (IC: 686.6 μM). Both the test compounds were subjected to antihyperglycemic activity using sucrose loaded model in Wistar rats and found compound exhibited significant reduction in glucose levels.

摘要

合成了16种新型苔色酸酯()以及4种与黑茶渍素相关的缩酚酸(3),并通过光谱数据(H、C和HRMS)确认了它们的结构。对合成的化合物进行了α-葡萄糖苷酶()抑制潜力的评估。在测试的化合物中,(IC:140.9 μM)和(IC:203.9 μM)表现出较强的α-葡萄糖苷酶抑制活性,且比标准药物阿卡波糖(IC:686.6 μM)更具活性。使用Wistar大鼠的蔗糖负荷模型对这两种测试化合物进行了抗高血糖活性研究,发现化合物使血糖水平显著降低。

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