Natural PTP1B Inhibitors From Polygonum cuspidatum and Their 2-NBDG Uptake Stimulation
Ten active principles (compounds 1-10) have been isolated following protein tyrosine phosphatase 1B (PTP1B) assay-guided fractionation of the methanol extract of the root of Polygonum cuspidatum. The chemical structures of the compounds were characterized mainly by nuclear magnetic resonance (NMR) s...
Lưu vào:
Tác giả chính: | , , , , |
---|---|
Định dạng: | Bài Báo |
Ngôn ngữ: | English |
Nhà xuất bản: |
SAGE Journals
2020
|
Chủ đề: | |
Truy cập trực tuyến: | https://dlib.phenikaa-uni.edu.vn/handle/PNK/581 https://doi.org/10.1177/1934578X20961201 |
Từ khóa: |
Thêm từ khóa
Không có từ khóa, Hãy là người đầu tiên đánh dấu biểu ghi này!
|
id |
oai:localhost:PNK-581 |
---|---|
record_format |
dspace |
spelling |
oai:localhost:PNK-5812022-08-17T05:54:38Z Natural PTP1B Inhibitors From Polygonum cuspidatum and Their 2-NBDG Uptake Stimulation Hong-Luyen Le Dao-Cuong To Manh-Hung Tran Thi-Thuy Do Phi-Hung Nguyen Polygonum cuspidatum glucose-uptake Polygonaceae anthraquinone PTP1B 2-NBDG stilbene Ten active principles (compounds 1-10) have been isolated following protein tyrosine phosphatase 1B (PTP1B) assay-guided fractionation of the methanol extract of the root of Polygonum cuspidatum. The chemical structures of the compounds were characterized mainly by nuclear magnetic resonance (NMR) spectroscopic and physicochemical data. This is the first time that 9,10-anthraquinones (compounds 5-6) have been isolated from P. cuspidatum, and this is the first record of compound 9 from the genus Polygonum. Except for compound 4, all the isolates showed potential inhibitory activity against PTP1B with half-maximal inhibitory concentration IC50 values ranging from 6.3 to 28.9 µM. Furthermore, a kinetic study indicated mixed-competitive inhibition with PTP1B for compounds 2 and 9 and noncompetitive inhibition for compounds 3 and 6. In addition, compounds 2, 3, 6, and 9 also induced the 2-deoxy-2-[(7-nitro-2,1,3-benzoxadiazol-4-yl) amino]-d-glucose uptake stimulation in 3T3-L1 adipocytes at concentrations of 10 and 5 µM. Taken together, the results reveal that P. cuspidatum could be a new source of natural compounds for further research and development of antidiabetic agents. 2020-10-13T03:57:34Z 2020-10-13T03:57:34Z 2020 Article https://dlib.phenikaa-uni.edu.vn/handle/PNK/581 https://doi.org/10.1177/1934578X20961201 en application/pdf SAGE Journals |
institution |
Digital Phenikaa |
collection |
Digital Phenikaa |
language |
English |
topic |
Polygonum cuspidatum glucose-uptake Polygonaceae anthraquinone PTP1B 2-NBDG stilbene |
spellingShingle |
Polygonum cuspidatum glucose-uptake Polygonaceae anthraquinone PTP1B 2-NBDG stilbene Hong-Luyen Le Dao-Cuong To Manh-Hung Tran Thi-Thuy Do Phi-Hung Nguyen Natural PTP1B Inhibitors From Polygonum cuspidatum and Their 2-NBDG Uptake Stimulation |
description |
Ten active principles (compounds 1-10) have been isolated following protein tyrosine phosphatase 1B (PTP1B) assay-guided fractionation of the methanol extract of the root of Polygonum cuspidatum. The chemical structures of the compounds were characterized mainly by nuclear magnetic resonance (NMR) spectroscopic and physicochemical data. This is the first time that 9,10-anthraquinones (compounds 5-6) have been isolated from P. cuspidatum, and this is the first record of compound 9 from the genus Polygonum. Except for compound 4, all the isolates showed potential inhibitory activity against PTP1B with half-maximal inhibitory concentration IC50 values ranging from 6.3 to 28.9 µM. Furthermore, a kinetic study indicated mixed-competitive inhibition with PTP1B for compounds 2 and 9 and noncompetitive inhibition for compounds 3 and 6. In addition, compounds 2, 3, 6, and 9 also induced the 2-deoxy-2-[(7-nitro-2,1,3-benzoxadiazol-4-yl) amino]-d-glucose uptake stimulation in 3T3-L1 adipocytes at concentrations of 10 and 5 µM. Taken together, the results reveal that P. cuspidatum could be a new source of natural compounds for further research and development of antidiabetic agents. |
format |
Article |
author |
Hong-Luyen Le Dao-Cuong To Manh-Hung Tran Thi-Thuy Do Phi-Hung Nguyen |
author_facet |
Hong-Luyen Le Dao-Cuong To Manh-Hung Tran Thi-Thuy Do Phi-Hung Nguyen |
author_sort |
Hong-Luyen Le |
title |
Natural PTP1B Inhibitors From Polygonum cuspidatum and Their 2-NBDG Uptake Stimulation |
title_short |
Natural PTP1B Inhibitors From Polygonum cuspidatum and Their 2-NBDG Uptake Stimulation |
title_full |
Natural PTP1B Inhibitors From Polygonum cuspidatum and Their 2-NBDG Uptake Stimulation |
title_fullStr |
Natural PTP1B Inhibitors From Polygonum cuspidatum and Their 2-NBDG Uptake Stimulation |
title_full_unstemmed |
Natural PTP1B Inhibitors From Polygonum cuspidatum and Their 2-NBDG Uptake Stimulation |
title_sort |
natural ptp1b inhibitors from polygonum cuspidatum and their 2-nbdg uptake stimulation |
publisher |
SAGE Journals |
publishDate |
2020 |
url |
https://dlib.phenikaa-uni.edu.vn/handle/PNK/581 https://doi.org/10.1177/1934578X20961201 |
_version_ |
1751856283268415488 |
score |
8.891787 |