Serrulatane diterpenoids from the leaves of Eremophila glabra and their potential as antihyperglycemic drug leads.

Phytochemistry

Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, DK-2100, Copenhagen, Denmark. Electronic address:

Published: April 2022

AI Article Synopsis

  • Eremophila is a genus of desert plants from Australia used for traditional medicinal purposes by Aboriginal people.
  • The leaf resin of Eremophila glabra has been found to inhibit certain enzymes important in glucose metabolism, with specific inhibitory concentrations measured.
  • Seven new compounds, called eremoglabrane A-G, were isolated along with nine previously known compounds, with some of the new diterpenoids also exhibiting enzyme-inhibitory activity.

Article Abstract

Eremophila (Scrophulariaceae) is a genus of Australian desert plants, which have been used by Australian Aboriginal people for various medicinal purposes. Crude extracts of the leaf resin of Eremophila glabra (R.Br.) Ostenf. showed α-glucosidase and protein tyrosine phosphatase 1B (PTP1B) inhibitory activity with IC values of 19.3 ± 1.2 μg/mL and 11.8 ± 2.1 μg/mL, respectively. Dual α-glucosidase/PTP1B high-resolution inhibition profiling combined with HPLC-PDA-HRMS and NMR were used to isolate and identify the compounds providing these activities. This resulted in isolation of seven undescribed serrulatane diterpenoids, eremoglabrane A-G, together with nine previously identified serrulatane diterpenoids and flavonoids. Three of the serrulatane diterpenoids showed PTP1B inhibitory activities with IC values from 63.8 ± 5.8 μM to 104.5 ± 25.9 μM.

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http://dx.doi.org/10.1016/j.phytochem.2021.113072DOI Listing

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