2(5H)-Furanone sesquiterpenes from Eremophila bignoniiflora: High-resolution inhibition profiling and PTP1B inhibitory activity
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2(5H)-Furanone sesquiterpenes from Eremophila bignoniiflora : High-resolution inhibition profiling and PTP1B inhibitory activity. / Zhao, Yong; Kjaerulff, Louise; Kongstad, Kenneth Thermann; Heskes, Allison Maree; Møller, Birger Lindberg; Stærk, Dan.
In: Phytochemistry, Vol. 166, 112054, 2019, p. 1-8.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - 2(5H)-Furanone sesquiterpenes from Eremophila bignoniiflora
T2 - High-resolution inhibition profiling and PTP1B inhibitory activity
AU - Zhao, Yong
AU - Kjaerulff, Louise
AU - Kongstad, Kenneth Thermann
AU - Heskes, Allison Maree
AU - Møller, Birger Lindberg
AU - Stærk, Dan
PY - 2019
Y1 - 2019
N2 - Eremophila bignoniiflora is a shrub distributed throughout inland northern and eastern Australia, and it has been used in several medicinal applications by some Australian Aboriginal people. In our continued search for anti-diabetic constituents from natural resources, the crude ethyl acetate extract of E. bignoniiflora was found to have protein-tyrosine phosphatase 1B (PTP1B) inhibitory activity with an IC50 value of 23.9 ± 1.9 μg/mL. High-resolution PTP1B inhibition profiling combined with HRMS and NMR were subsequently used to investigate the individual compounds responsible for the observed bioactivity of the crude extract. This led to identification of five undescribed 2(5H)-furanone sesquiterpenes, together with 13 flavonoids and phenolic compounds. Dose-response curves of the isolated compounds revealed that two 2(5H)-furanone sesquiterpene cinnamates and three flavonoids exhibited moderate PTP1B inhibitory activity with IC50 values from 41.4 ± 1.4 to 154.5 ± 8.9 μM.
AB - Eremophila bignoniiflora is a shrub distributed throughout inland northern and eastern Australia, and it has been used in several medicinal applications by some Australian Aboriginal people. In our continued search for anti-diabetic constituents from natural resources, the crude ethyl acetate extract of E. bignoniiflora was found to have protein-tyrosine phosphatase 1B (PTP1B) inhibitory activity with an IC50 value of 23.9 ± 1.9 μg/mL. High-resolution PTP1B inhibition profiling combined with HRMS and NMR were subsequently used to investigate the individual compounds responsible for the observed bioactivity of the crude extract. This led to identification of five undescribed 2(5H)-furanone sesquiterpenes, together with 13 flavonoids and phenolic compounds. Dose-response curves of the isolated compounds revealed that two 2(5H)-furanone sesquiterpene cinnamates and three flavonoids exhibited moderate PTP1B inhibitory activity with IC50 values from 41.4 ± 1.4 to 154.5 ± 8.9 μM.
U2 - 10.1016/j.phytochem.2019.112054
DO - 10.1016/j.phytochem.2019.112054
M3 - Journal article
C2 - 31284174
VL - 166
SP - 1
EP - 8
JO - Phytochemistry
JF - Phytochemistry
SN - 0031-9422
M1 - 112054
ER -
ID: 217384706