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2-(2-苯乙基)色酮衍生物:沉香(Aquilaria filaria)中具有潜力的α-葡萄糖苷酶抑制剂

2-(2-Phenylethyl)chromone derivatives: Promising α-glucosidase inhibitors in agarwood from Aquilaria filaria.

机构信息

Key Laboratory of Biology and Genetic Resources of Tropical Crops, Ministry of Agriculture, Institute of Tropical Bioscience and Biotechnology, Chinese Academy of Tropical Agricultural Sciences, Haikou, 571101, PR China; Institute of Tropical Agriculture and Forestry, Hainan University, Haikou, 570228, PR China; Hainan Engineering Research Center of Agarwood, 571101, Haikou, PR China.

Key Laboratory of Biology and Genetic Resources of Tropical Crops, Ministry of Agriculture, Institute of Tropical Bioscience and Biotechnology, Chinese Academy of Tropical Agricultural Sciences, Haikou, 571101, PR China; Hainan Engineering Research Center of Agarwood, 571101, Haikou, PR China.

出版信息

Phytochemistry. 2021 Jan;181:112578. doi: 10.1016/j.phytochem.2020.112578. Epub 2020 Nov 7.

DOI:10.1016/j.phytochem.2020.112578
PMID:33171341
Abstract

Twelve undescribed 2-(2-phenylethyl)chromone derivatives, including one pair of enantiomers, together with eleven known ones, were isolated from the EtOAc extract of agarwood originating from Aquilaria filaria. All structures were elucidated by spectroscopic (NMR, UV, IR, MS) methods and compared with reported data in literatures. Twenty-one compounds were assessed for α-glucosidase inhibitory activity, which showed inhibition of α-glucosidase with IC values ranging between 7.8 ± 0.3 to 137.7 ± 3.0 μM (Acarbose, 743.4 ± 3.3 μM; Genistein, 8.3 ± 0.1 μM). Our results expanded the structural diversity of 2-(2-phenylethyl)chromones from agarwood, and revealed the potential of 2-(2-phenylethyl)chromones as α-glucosidase inhibitors.

摘要

从沉香属Aquilaria filaria 的乙酸乙酯提取物中分离得到了 12 种未描述的 2-(2-苯乙基)色酮衍生物,包括一对对映异构体,以及 11 种已知的化合物。所有结构均通过光谱(NMR、UV、IR、MS)方法阐明,并与文献中的报道数据进行了比较。对 21 种化合物进行了α-葡萄糖苷酶抑制活性评估,结果表明这些化合物对α-葡萄糖苷酶具有抑制活性,IC 值范围在 7.8±0.3 至 137.7±3.0 μM(阿卡波糖,743.4±3.3 μM;染料木黄酮,8.3±0.1 μM)。我们的研究结果扩展了沉香属 2-(2-苯乙基)色酮的结构多样性,并揭示了 2-(2-苯乙基)色酮作为α-葡萄糖苷酶抑制剂的潜力。

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