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瓦尔特果实的化学成分及其对α-葡萄糖苷酶的抑制活性和胰岛素分泌作用。

The Chemical Constituents from Fruits of Walt. and Their α-Glucosidase Inhibitory Activity and Insulin Secretion Effect.

机构信息

College of Pharmacy, Yonsei Institute of Pharmaceutical Sciences, Yonsei University, Incheon 21983, Korea.

College of Korean Medicine, Gachon University, Seongnam 13120, Korea.

出版信息

Molecules. 2021 Jan 12;26(2):362. doi: 10.3390/molecules26020362.

Abstract

Catalpa pod has been used in traditional medicine for the treatment of diabetes mellitus in South America. Studies on the constituents of Catalpa species have shown that it is rich in iridoids. In the present study, three previously undescribed compounds (-), including two secoiridoid derivatives along with twelve known compounds, were isolated from the fruits of Walt. In addition, fully assigned C-NMR of 5,6-dihydroxy-7,4'-dimethoxyflavone-6--sophoroside () is reported for the first time in the present study. The structures of compounds were determined on the basis of extensive spectroscopic methods, including UV, IR, 1D, and 2D NMR, mass spectroscopy, and CD spectroscopic data. All the isolated compounds were evaluated for α-glucosidase inhibitory activity. Among the tested compounds, compounds , , and exhibited significant inhibitory activity against α-glucosidase enzyme assay. Meanwhile, the effect of compounds , , and on glucose-stimulated insulin secretion (GSIS) was measured using pancreatic β-cells. Compounds , , and exhibited non-cytotoxicity-stimulated insulin secretion in INS-1 cells. The expression levels of proteins associated with β-cell function and insulin secretion such as phosphorylation of total insulin receptor substrate-2 (IRS-2), phosphatidylinositol 3-kinase (PI3K), Akt, activated pancreatic duodenal homeobox-1 (PDX-1), and peroxisome proliferator-activated receptor-γ (PPAR-γ) were increased in INS-1 cells after treatment with compounds , , and . The findings of the present study could provide a scientific warrant for their application as a potential antidiabetic agent.

摘要

梓树在南美的传统医学中被用于治疗糖尿病。对梓属植物成分的研究表明,它富含环烯醚萜类化合物。在本研究中,从梓树的果实中分离得到了三种以前未描述的化合物(-),包括两种裂环环烯醚萜衍生物和十二种已知化合物。此外,在本研究中首次报道了 5,6-二羟基-7,4'-二甲氧基黄酮-6--槐糖苷()的完全归属 C-NMR。根据广泛的光谱方法,包括 UV、IR、1D 和 2D NMR、质谱和 CD 光谱数据,确定了化合物的结构。所有分离得到的化合物均进行了α-葡萄糖苷酶抑制活性评估。在所测试的化合物中,化合物 、 、和 对α-葡萄糖苷酶酶抑制活性有显著抑制作用。同时,采用胰腺β细胞测定了化合物 、 、和 对葡萄糖刺激胰岛素分泌(GSIS)的影响。化合物 、 、和 对 INS-1 细胞无细胞毒性刺激胰岛素分泌。化合物 、 、和 处理后,与β细胞功能和胰岛素分泌相关的蛋白如总胰岛素受体底物-2(IRS-2)、磷酸肌醇 3-激酶(PI3K)、Akt、激活的胰腺十二指肠同源盒-1(PDX-1)和过氧化物酶体增殖物激活受体-γ(PPAR-γ)的表达水平增加。本研究的结果可为将其作为潜在的抗糖尿病药物应用提供科学依据。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a7ad/7826643/77e48dc877de/molecules-26-00362-g001.jpg

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