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.2021.113072 | DOI Listing |
J Nat Prod
April 2023
Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark.
Extracts of subsp. showed α-glucosidase and PTP1B inhibitory activity with IC values of 19.6 and 13.
View Article and Find Full Text PDFAnal Chem
March 2023
Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, Copenhagen DK-2100, Denmark.
Discovery of sustainable and benign-by-design drugs to combat emerging health pandemics calls for new analytical technologies to explore the chemical and pharmacological properties of Nature's unique chemical space. Here, we present a new analytical technology workflow, polypharmacology-labeled molecular networking (PLMN), where merged positive and negative ionization tandem mass spectrometry-based molecular networking is linked with data from polypharmacological high-resolution inhibition profiling for easy and fast identification of individual bioactive constituents in complex extracts. The crude extract of was subjected to PLMN analysis for the identification of antihyperglycemic and antibacterial constituents.
View Article and Find Full Text PDFJ Nat Prod
March 2023
Griffith Institute for Drug Discovery, School of Environment and Science, Griffith University, Brisbane, QLD 4111, Australia.
The known -derived diterpenoid 3,7,8-trihydroxyserrulat-14-en-19-oic acid () was targeted for large-scale purification, as this bioactive plant compound has proven to be an attractive scaffold for semisynthetic studies and subsequent library generation. Compound was converted to a selectively protected trimethyl derivative, 3-hydroxy-7,8-dimethoxyserrulat-14-en-19-oic acid methyl ester (), using simple and rapid methylation conditions. The resulting scaffold was reacted with a diverse series of commercially available isocyanates to generate an 11-membered carbamate-based library.
View Article and Find Full Text PDFMolecules
November 2022
Ecole De Biologie Industrielle, 95800 Cergy, France.
The genus (family Scrophulariaceae) consists of approximately 200 species that are widely distributed in the semi-arid and arid regions of Australia. Multiple spp. are used as traditional medicines by the First Australians in the areas in which they grow.
View Article and Find Full Text PDFPhytochemistry
November 2022
Department of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, DK-2100, Copenhagen, Denmark. Electronic address:
The plant genus Eremophila is endemic to Australia and widespread in arid regions. Root bark extract of Eremophila longifolia (R.Br.
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