Potential of Polygonum cuspidatum root as an antidiabetic food: Dual high-resolution α-glucosidase and PTP1B inhibition profiling combined with HPLC-HRMS and NMR for identification of antidiabetic constituents

Yong Zhao; Martin Xiaoyong Chen; Kenneth Thermann Kongstad; Anna K Jäger; Dan Stærk

doi:10.1021/acs.jafc.7b01353

Potential of Polygonum cuspidatum root as an antidiabetic food: Dual high-resolution α-glucosidase and PTP1B inhibition profiling combined with HPLC-HRMS and NMR for identification of antidiabetic constituents

Yong Zhao, Martin Xiaoyong Chen, Kenneth Thermann Kongstad, Anna K Jäger, Dan Stærk

31 Citations (Scopus)

Abstract

The worldwide increasing incidence of type 2 diabetes has fueled an intensified search for food and herbal remedies with preventive and/or therapeutic properties. Polygonum cuspidatum Siebold & Zucc. (Polygonaceae) is used as a functional food in Japan and South Korea, and it is also a well-known traditional antidiabetic herb used in China. In this study, dual high-resolution α-glucosidase and protein-tyrosine phosphatase 1B (PTP1B) inhibition profiling was used for the identification of individual antidiabetic constituents directly from the crude ethyl acetate extract and fractions of P. cuspidatum. Subsequent preparative-scale HPLC was used to isolate a series of α-glucosidase inhibitors, which after HPLC-HRMS and NMR analysis were identified as procyanidin B2 3,3″-O-digallate (3) and (-)-epicatechin gallate (5) with IC₅₀ values of 0.42 ± 0.02 and 0.48 ± 0.0004 μM, respectively, as well as a series of stilbene analogues with IC₅₀ value in the range from 6.05 ± 0.05 to 116.10 ± 2.04 μM. In addition, (trans)-emodin-physcion bianthrone (15b) and (cis)-emodin-physcion bianthrone (15c) were identified as potent PTP1B inhibitors with IC₅₀ values of 2.77 ± 1.23 and 7.29 ± 2.32 μM, respectively. These findings show that P. cuspidatum is a potential functional food for management of type 2 diabetes.

Original language	English
Journal	Journal of Agricultural and Food Chemistry
Volume	65
Pages (from-to)	4421-4427
ISSN	0021-8561
DOIs	https://doi.org/10.1021/acs.jafc.7b01353
Publication status	Published - 7 Jun 2017

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Zhao, Y., Chen, M. X., Kongstad, K. T., Jäger, A. K., & Stærk, D. (2017). Potential of Polygonum cuspidatum root as an antidiabetic food: Dual high-resolution α-glucosidase and PTP1B inhibition profiling combined with HPLC-HRMS and NMR for identification of antidiabetic constituents. Journal of Agricultural and Food Chemistry, 65, 4421-4427. https://doi.org/10.1021/acs.jafc.7b01353

Potential of Polygonum cuspidatum root as an antidiabetic food: Dual high-resolution α-glucosidase and PTP1B inhibition profiling combined with HPLC-HRMS and NMR for identification of antidiabetic constituents. / Zhao, Yong; Chen, Martin Xiaoyong; Kongstad, Kenneth Thermann et al.
In: Journal of Agricultural and Food Chemistry, Vol. 65, 07.06.2017, p. 4421-4427.

Research output: Contribution to journal › Journal article › Research › peer-review

Zhao, Y, Chen, MX, Kongstad, KT, Jäger, AK & Stærk, D 2017, 'Potential of Polygonum cuspidatum root as an antidiabetic food: Dual high-resolution α-glucosidase and PTP1B inhibition profiling combined with HPLC-HRMS and NMR for identification of antidiabetic constituents', Journal of Agricultural and Food Chemistry, vol. 65, pp. 4421-4427. https://doi.org/10.1021/acs.jafc.7b01353

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abstract = "The worldwide increasing incidence of type 2 diabetes has fueled an intensified search for food and herbal remedies with preventive and/or therapeutic properties. Polygonum cuspidatum Siebold & Zucc. (Polygonaceae) is used as a functional food in Japan and South Korea, and it is also a well-known traditional antidiabetic herb used in China. In this study, dual high-resolution α-glucosidase and protein-tyrosine phosphatase 1B (PTP1B) inhibition profiling was used for the identification of individual antidiabetic constituents directly from the crude ethyl acetate extract and fractions of P. cuspidatum. Subsequent preparative-scale HPLC was used to isolate a series of α-glucosidase inhibitors, which after HPLC-HRMS and NMR analysis were identified as procyanidin B2 3,3″-O-digallate (3) and (-)-epicatechin gallate (5) with IC50 values of 0.42 ± 0.02 and 0.48 ± 0.0004 μM, respectively, as well as a series of stilbene analogues with IC50 value in the range from 6.05 ± 0.05 to 116.10 ± 2.04 μM. In addition, (trans)-emodin-physcion bianthrone (15b) and (cis)-emodin-physcion bianthrone (15c) were identified as potent PTP1B inhibitors with IC50 values of 2.77 ± 1.23 and 7.29 ± 2.32 μM, respectively. These findings show that P. cuspidatum is a potential functional food for management of type 2 diabetes.",

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AB - The worldwide increasing incidence of type 2 diabetes has fueled an intensified search for food and herbal remedies with preventive and/or therapeutic properties. Polygonum cuspidatum Siebold & Zucc. (Polygonaceae) is used as a functional food in Japan and South Korea, and it is also a well-known traditional antidiabetic herb used in China. In this study, dual high-resolution α-glucosidase and protein-tyrosine phosphatase 1B (PTP1B) inhibition profiling was used for the identification of individual antidiabetic constituents directly from the crude ethyl acetate extract and fractions of P. cuspidatum. Subsequent preparative-scale HPLC was used to isolate a series of α-glucosidase inhibitors, which after HPLC-HRMS and NMR analysis were identified as procyanidin B2 3,3″-O-digallate (3) and (-)-epicatechin gallate (5) with IC50 values of 0.42 ± 0.02 and 0.48 ± 0.0004 μM, respectively, as well as a series of stilbene analogues with IC50 value in the range from 6.05 ± 0.05 to 116.10 ± 2.04 μM. In addition, (trans)-emodin-physcion bianthrone (15b) and (cis)-emodin-physcion bianthrone (15c) were identified as potent PTP1B inhibitors with IC50 values of 2.77 ± 1.23 and 7.29 ± 2.32 μM, respectively. These findings show that P. cuspidatum is a potential functional food for management of type 2 diabetes.

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