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

Malene Johanne Petersen; Chao Liang; Louise Kjaerulff; Chi Ndi; Susan Semple; Bevan Buirchell; Sonia Coriani; Birger Lindberg Møller; Dan Stærk

doi:10.1016/j.phytochem.2021.113072

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

Malene Johanne Petersen, Chao Liang, Louise Kjaerulff, Chi Ndi, Susan Semple, Bevan Buirchell, Sonia Coriani, Birger Lindberg Møller, Dan Stærk

Research output: Contribution to journal › Journal article › Research › peer-review

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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 IC50 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 IC50 values from 63.8 ± 5.8 μM to 104.5 ± 25.9 μM.

Original language	English
Article number	113072
Journal	Phytochemistry
Volume	196
Number of pages	11
ISSN	0031-9422
DOIs	https://doi.org/10.1016/j.phytochem.2021.113072
Publication status	Published - 2022

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Serrulatane diterpenoids from the leaves of Eremophila glabra and their potential as antihyperglycemic drug leads. / Petersen, Malene Johanne; Liang, Chao ; Kjaerulff, Louise; Ndi, Chi; Semple, Susan; Buirchell, Bevan; Coriani, Sonia; Møller, Birger Lindberg ; Stærk, Dan.

In: Phytochemistry, Vol. 196, 113072, 2022.

Research output: Contribution to journal › Journal article › Research › peer-review

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title = "Serrulatane diterpenoids from the leaves of Eremophila glabra and their potential as antihyperglycemic drug leads",

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 IC50 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 IC50 values from 63.8 ± 5.8 μM to 104.5 ± 25.9 μM.",

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AU - Petersen, Malene Johanne

AU - Liang, Chao

AU - Kjaerulff, Louise

AU - Ndi, Chi

AU - Semple, Susan

AU - Buirchell, Bevan

AU - Coriani, Sonia

AU - Møller, Birger Lindberg

AU - Stærk, Dan

PY - 2022

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N2 - 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 IC50 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 IC50 values from 63.8 ± 5.8 μM to 104.5 ± 25.9 μM.

AB - 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 IC50 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 IC50 values from 63.8 ± 5.8 μM to 104.5 ± 25.9 μM.

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DO - 10.1016/j.phytochem.2021.113072

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JF - Phytochemistry

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