Staff View: Natural PTP1B Inhibitors From Polygonum cuspidatum and Their 2-NBDG Uptake Stimulation

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...

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Main Authors:	Hong-Luyen Le, Dao-Cuong To, Manh-Hung Tran, Thi-Thuy Do, Phi-Hung Nguyen
Format:	Article
Language:	English
Published:	SAGE Journals 2020
Subjects:	Polygonum cuspidatum glucose-uptake Polygonaceae anthraquinone PTP1B 2-NBDG stilbene
Online Access:	https://dlib.phenikaa-uni.edu.vn/handle/PNK/581 https://doi.org/10.1177/1934578X20961201
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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	8.881002

Natural PTP1B Inhibitors From Polygonum cuspidatum and Their 2-NBDG Uptake Stimulation

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