Identification of α-glucosidase inhibitors in Machilus litseifolia by combined use of high-resolution α-glucosidase inhibition profiling and HPLC-PDA-HRMS-SPE-NMR
Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › fagfællebedømt
Standard
Identification of α-glucosidase inhibitors in Machilus litseifolia by combined use of high-resolution α-glucosidase inhibition profiling and HPLC-PDA-HRMS-SPE-NMR. / Li, Tuo; Kongstad, Kenneth Thermann; Stærk, Dan.
I: Journal of Natural Products, Bind 82, 2019, s. 249-258.Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › fagfællebedømt
Harvard
APA
Vancouver
Author
Bibtex
}
RIS
TY - JOUR
T1 - Identification of α-glucosidase inhibitors in Machilus litseifolia by combined use of high-resolution α-glucosidase inhibition profiling and HPLC-PDA-HRMS-SPE-NMR
AU - Li, Tuo
AU - Kongstad, Kenneth Thermann
AU - Stærk, Dan
PY - 2019
Y1 - 2019
N2 - Type 2 diabetes is a chronic multifactorial disease affecting more than 425 million people worldwide, and new selective α-glucosidase inhibitors with fewer side effects are urgently needed. In this study, a crude ethyl acetate extract of Machilus litseifolia was fractionated by solid-phase extraction using C18 cartridges to give a fraction enriched in α-glucosidase inhibitors. Subsequent microfractionation and bioassaying of the eluate by high-performance liquid chromatography (HPLC) using a complementary pentafluorophenyl column allowed construction of a high-resolution α-glucosidase inhibition profile (biochromatogram). This was used to target high-performance liquid chromatography – photodiode array detection – high-resolution mass spectrometry – solid-phase extraction – nuclear magnetic resonance spectroscopy (HPLC-PDA-HRMS-SPE-NMR) analysis towards α-glucosidase inhibitors. This led to the identification of 13 di-coumaroylated flavonol rhamnosides, of which seven (8, 10, 12a, 12b, 16, 17, and 18) are reported for the first time, and two lignans, of which one (5) is reported for the first time. IC50 values of isolated compounds towards α-glucosidase range from 5.9 to 35.3 μM, which is 8 to 91 times lower than the IC50 value of 266 μM measured for the reference compound acarbose.
AB - Type 2 diabetes is a chronic multifactorial disease affecting more than 425 million people worldwide, and new selective α-glucosidase inhibitors with fewer side effects are urgently needed. In this study, a crude ethyl acetate extract of Machilus litseifolia was fractionated by solid-phase extraction using C18 cartridges to give a fraction enriched in α-glucosidase inhibitors. Subsequent microfractionation and bioassaying of the eluate by high-performance liquid chromatography (HPLC) using a complementary pentafluorophenyl column allowed construction of a high-resolution α-glucosidase inhibition profile (biochromatogram). This was used to target high-performance liquid chromatography – photodiode array detection – high-resolution mass spectrometry – solid-phase extraction – nuclear magnetic resonance spectroscopy (HPLC-PDA-HRMS-SPE-NMR) analysis towards α-glucosidase inhibitors. This led to the identification of 13 di-coumaroylated flavonol rhamnosides, of which seven (8, 10, 12a, 12b, 16, 17, and 18) are reported for the first time, and two lignans, of which one (5) is reported for the first time. IC50 values of isolated compounds towards α-glucosidase range from 5.9 to 35.3 μM, which is 8 to 91 times lower than the IC50 value of 266 μM measured for the reference compound acarbose.
U2 - 10.1021/acs.jnatprod.8b00609
DO - 10.1021/acs.jnatprod.8b00609
M3 - Journal article
C2 - 30668111
VL - 82
SP - 249
EP - 258
JO - Journal of Natural Products
JF - Journal of Natural Products
SN - 0163-3864
ER -
ID: 210989341