Unraveling the complexity of complex mixtures by combining high-resolution pharmacological, analytical and spectroscopic techniques: Antidiabetic constituents in Chinese medicinal plants
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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; He, Chenhua; Stærk, Dan.
I: Faraday Discussions, Bind 218, 2019, s. 202-218.Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › fagfællebedømt
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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
VL - 218
SP - 202
EP - 218
JO - Faraday Discussions
JF - Faraday Discussions
SN - 1359-6640
ER -
ID: 209810415