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从何首乌中分离得到的二苯乙烯苷及其体外 PTP1B 抑制活性。

Multiflorumisides HK, stilbene glucosides isolated from Polygonum multiflorum and their in vitro PTP1B inhibitory activities.

机构信息

National Institutes for Food and Drug Control, Beijing 100050, China.

Institute of Materia Medica, Chinese Academy of Medical Sciences and Pekin Union Medical College, Beijing 100050, China.

出版信息

Fitoterapia. 2020 Oct;146:104703. doi: 10.1016/j.fitote.2020.104703. Epub 2020 Aug 20.

Abstract

A phytochemical study on a 70% EtOH extract of dried roots of Polygonum multiflorum resulted in the isolation of four undescribed stilbene glucosides, namely multiflorumisides HK (1-4). The structures of the natural products were elucidated by 1D and 2D nuclear magnetic resonance (NMR) as well as mass spectroscopy analyses. Among them, multiflorumiside J (3) and multiflorumiside K (4) belong to rare tetramer stilbene glucosides. Moreover, the in vitro inhibitory activities against protein tyrosine phosphatase 1B (PTP1B) were evaluated and the putative biosynthetic pathway was proposed. Notably, compounds 1-4 showed the inhibitory activity against PTP1B with the IC values of 1.2, 1.7, 1.5 and 4.6 μm, respectively. Based on the obtained results, stilbene glucosides could be the potential PTP1B inhibitors of P. multiflorum.

摘要

从何首乌 70%乙醇提取物中分离得到四种新的二苯乙烯葡萄糖苷,即何首乌二苯乙烯葡萄糖苷 HK(1-4)。通过一维和二维核磁共振(NMR)以及质谱分析确定了天然产物的结构。其中,何首乌二苯乙烯葡萄糖苷 J(3)和何首乌二苯乙烯葡萄糖苷 K(4)属于罕见的四聚体二苯乙烯葡萄糖苷。此外,还评价了它们对蛋白酪氨酸磷酸酶 1B(PTP1B)的体外抑制活性,并提出了可能的生物合成途径。值得注意的是,化合物 1-4 对 PTP1B 的抑制活性的 IC50 值分别为 1.2、1.7、1.5 和 4.6μm。基于实验结果,二苯乙烯葡萄糖苷可能是何首乌中潜在的 PTP1B 抑制剂。

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