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通过亲和导向分级分离从根部鉴定出的葡萄糖-6-磷酸酶和α-葡萄糖苷酶抑制剂

Glucose-6-Phosphatase and α-Glucosidase Inhibitors from Roots Identified by Affinity-Directed Fractionation.

作者信息

Rosas-Ramírez Daniel, Escandón-Rivera Sonia, Andrade-Cetto Adolfo, Arreguín-Espinosa Roberto

机构信息

Departamento de Química de Biomacromoléculas, Instituto de Química, Universidad Nacional Autónoma de México, Ciudad Universitaria, 04360 Mexico City, Mexico.

Departamento de Biología Celular, Facultad de Ciencias, Universidad Nacional Autónoma de México, Ciudad Universitaria, 04360 Mexico City, Mexico.

出版信息

Rev Bras Farmacogn. 2020;30(6):832-837. doi: 10.1007/s43450-020-00116-3. Epub 2021 Jan 7.

Abstract

UNLABELLED

The ethanol/water-soluble extracts of the roots of M. Martens & Galeotti, Smilacaceae, which have been appreciated since pre-Hispanic times and traditionally used to treat type 2 diabetes in Mexico, were fractionated by the application of the affinity-directed method to identify glucose-6-phosphatase and α-glucosidase inhibitors. Mass spectrometry was used to identify the inhibitor as free ligands after released from the enzymatic complex by denaturing acidic conditions. The affinity study led to the identification of chlorogenic acid as a glucose-6-phosphatase inhibitor, which is the most abundant metabolite present in the analyzed crude drug. In addition, the affinity studies led to the identification of a flavonolignan glycoside as an α-glucosidase inhibitor. analysis with α-glucosidase MAL12 from the yeast allowed to determine the best conformational rearrangement for the α-glucosidase inhibitors. Graphical abstract.

SUPPLEMENTARY INFORMATION

The online version contains supplementary material available at 10.1007/s43450-020-00116-3.

摘要

未标记

菝葜科植物马滕斯菝葜(M. Martens & Galeotti)的根的乙醇/水提取物自西班牙前时代就备受赞赏,在墨西哥传统上用于治疗2型糖尿病。通过应用亲和导向方法对其进行分级分离,以鉴定葡萄糖-6-磷酸酶和α-葡萄糖苷酶抑制剂。在变性酸性条件下从酶复合物中释放后,使用质谱法将抑制剂鉴定为游离配体。亲和研究导致鉴定出绿原酸为葡萄糖-6-磷酸酶抑制剂,它是所分析的粗药物中含量最丰富的代谢物。此外,亲和研究还鉴定出一种黄酮木脂素糖苷为α-葡萄糖苷酶抑制剂。用来自酵母的α-葡萄糖苷酶MAL12进行分析,有助于确定α-葡萄糖苷酶抑制剂的最佳构象重排。图形摘要。

补充信息

在线版本包含可在10.1007/s43450-020-00116-3获取的补充材料。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e86c/7790519/2933b571414b/43450_2020_116_Figa_HTML.jpg

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