Unraveling the complexity of complex mixtures by combining high-resolution pharmacological, analytical and spectroscopic techniques: Antidiabetic constituents in Chinese medicinal plants

Yong Zhao; Kenneth Thermann Kongstad; Yueqiu Liu; Chenhua He; Dan Stærk

doi:10.1039/c8fd00223a

Unraveling the complexity of complex mixtures by combining high-resolution pharmacological, analytical and spectroscopic techniques: Antidiabetic constituents in Chinese medicinal plants

Yong Zhao, Kenneth Thermann Kongstad, Yueqiu Liu, Chenhua He, Dan Stærk

5 Citations (Scopus)

Abstract

Medicinal plants have been widely used as (poly)pharmacological remedies and constitute a rich source for antidiabetic drug discovery. In the present study, forty medicinal plant samples collected in China were tested for inhibitory activity against α-glucosidase, α-amylase, and protein-tyrosine phosphatase 1B (PTP1B). Crude ethyl acetate extracts of Dioscorea bulbifera L., Boehmeria nivea Gaudich, Tinospora sagittata Gagnep. and Persicaria bistorta (L.) Samp. showed dual inhibitory activity towards α-glucosidase and PTP1B, and were chosen for further investigation. Subsequent dual high-resolution α-glucosidase/PTP1B profiling or triple high-resolution
α-glucosidase/α-amylase/PTP1B profiling combined with HPLC-HRMS and NMR spectroscopy led to the identification of 28 metabolites with one or more bioactivities. Among these, three new phenanthrenes were identified from D. bulbifera, including one new biphenanthrene (10) exhibiting promising dual inhibitory activity towards α-glucosidase and PTP1B with IC₅₀ values of 2.08 ± 0.19 and 3.36 ± 0.25 μM, respectively. Two triterpenoids and one fatty acid from B. nivea and T. sagittata as well as some commercially available fatty acids showed strong PTP1B inhibitory activity with IC₅₀ values in the range of 4.89 ± 0.38 to 53.77 ± 4.20 μM.

Original language	English
Journal	Faraday Discussions
Volume	218
Pages (from-to)	202-218
ISSN	1359-6640
DOIs	https://doi.org/10.1039/c8fd00223a
Publication status	Published - 2019

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Unraveling the complexity of complex mixtures by combining high-resolution pharmacological, analytical and spectroscopic techniques: Antidiabetic constituents in Chinese medicinal plants. / Zhao, Yong ; Kongstad, Kenneth Thermann; Liu, Yueqiu et al.

In: Faraday Discussions, Vol. 218, 2019, p. 202-218.

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

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title = "Unraveling the complexity of complex mixtures by combining high-resolution pharmacological, analytical and spectroscopic techniques: Antidiabetic constituents in Chinese medicinal plants",

abstract = "Medicinal plants have been widely used as (poly)pharmacological remedies and constitute a rich source for antidiabetic drug discovery. In the present study, forty medicinal plant samples collected in China were tested for inhibitory activity against α-glucosidase, α-amylase, and protein-tyrosine phosphatase 1B (PTP1B). Crude ethyl acetate extracts of Dioscorea bulbifera L., Boehmeria nivea Gaudich, Tinospora sagittata Gagnep. and Persicaria bistorta (L.) Samp. showed dual inhibitory activity towards α-glucosidase and PTP1B, and were chosen for further investigation. Subsequent dual high-resolution α-glucosidase/PTP1B profiling or triple high-resolutionα-glucosidase/α-amylase/PTP1B profiling combined with HPLC-HRMS and NMR spectroscopy led to the identification of 28 metabolites with one or more bioactivities. Among these, three new phenanthrenes were identified from D. bulbifera, including one new biphenanthrene (10) exhibiting promising dual inhibitory activity towards α-glucosidase and PTP1B with IC50 values of 2.08 ± 0.19 and 3.36 ± 0.25 μM, respectively. Two triterpenoids and one fatty acid from B. nivea and T. sagittata as well as some commercially available fatty acids showed strong PTP1B inhibitory activity with IC50 values in the range of 4.89 ± 0.38 to 53.77 ± 4.20 μM.",

author = "Yong Zhao and Kongstad, {Kenneth Thermann} and Yueqiu Liu and Chenhua He and Dan St{\ae}rk",

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T1 - Unraveling the complexity of complex mixtures by combining high-resolution pharmacological, analytical and spectroscopic techniques: Antidiabetic constituents in Chinese medicinal plants

AU - Zhao, Yong

AU - Kongstad, Kenneth Thermann

AU - Liu, Yueqiu

AU - He, Chenhua

AU - Stærk, Dan

PY - 2019

Y1 - 2019

N2 - Medicinal plants have been widely used as (poly)pharmacological remedies and constitute a rich source for antidiabetic drug discovery. In the present study, forty medicinal plant samples collected in China were tested for inhibitory activity against α-glucosidase, α-amylase, and protein-tyrosine phosphatase 1B (PTP1B). Crude ethyl acetate extracts of Dioscorea bulbifera L., Boehmeria nivea Gaudich, Tinospora sagittata Gagnep. and Persicaria bistorta (L.) Samp. showed dual inhibitory activity towards α-glucosidase and PTP1B, and were chosen for further investigation. Subsequent dual high-resolution α-glucosidase/PTP1B profiling or triple high-resolutionα-glucosidase/α-amylase/PTP1B profiling combined with HPLC-HRMS and NMR spectroscopy led to the identification of 28 metabolites with one or more bioactivities. Among these, three new phenanthrenes were identified from D. bulbifera, including one new biphenanthrene (10) exhibiting promising dual inhibitory activity towards α-glucosidase and PTP1B with IC50 values of 2.08 ± 0.19 and 3.36 ± 0.25 μM, respectively. Two triterpenoids and one fatty acid from B. nivea and T. sagittata as well as some commercially available fatty acids showed strong PTP1B inhibitory activity with IC50 values in the range of 4.89 ± 0.38 to 53.77 ± 4.20 μM.

AB - Medicinal plants have been widely used as (poly)pharmacological remedies and constitute a rich source for antidiabetic drug discovery. In the present study, forty medicinal plant samples collected in China were tested for inhibitory activity against α-glucosidase, α-amylase, and protein-tyrosine phosphatase 1B (PTP1B). Crude ethyl acetate extracts of Dioscorea bulbifera L., Boehmeria nivea Gaudich, Tinospora sagittata Gagnep. and Persicaria bistorta (L.) Samp. showed dual inhibitory activity towards α-glucosidase and PTP1B, and were chosen for further investigation. Subsequent dual high-resolution α-glucosidase/PTP1B profiling or triple high-resolutionα-glucosidase/α-amylase/PTP1B profiling combined with HPLC-HRMS and NMR spectroscopy led to the identification of 28 metabolites with one or more bioactivities. Among these, three new phenanthrenes were identified from D. bulbifera, including one new biphenanthrene (10) exhibiting promising dual inhibitory activity towards α-glucosidase and PTP1B with IC50 values of 2.08 ± 0.19 and 3.36 ± 0.25 μM, respectively. Two triterpenoids and one fatty acid from B. nivea and T. sagittata as well as some commercially available fatty acids showed strong PTP1B inhibitory activity with IC50 values in the range of 4.89 ± 0.38 to 53.77 ± 4.20 μM.

U2 - 10.1039/c8fd00223a

DO - 10.1039/c8fd00223a

M3 - Journal article

SN - 1359-6640

VL - 218

SP - 202

EP - 218

JO - Faraday Discussions

JF - Faraday Discussions

ER -

Unraveling the complexity of complex mixtures by combining high-resolution pharmacological, analytical and spectroscopic techniques: Antidiabetic constituents in Chinese medicinal plants

Abstract

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