Journal
PHYTOCHEMISTRY
Volume 166, Issue -, Pages -Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.phytochem.2019.112054
Keywords
Eremophila bignoniiflora (Benth.) F.Muell. (Scrophulariaceae); Furanone sesquiterpene; High-resolution inhibition profiling; Protein-tyrosine phosphatase 1B
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Funding
- Danish Agency for Science, Technology and Innovation via the National Research Infrastructure funds
- Novo Nordisk Foundation [NNF160C0021616]
- Carlsberg Foundation
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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. bignoniifiora was found to have protein-tyrosine phosphatase 1B (PTP1B) inhibitory activity with an IC50 value of 23.9 +/- 1.9 mu g/mL. High-resolution PTP1B inhibition profiling combined with FIRMS 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 mu M.
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