NDLI: Identification of PTP1B and α-Glucosidase Inhibitory Serrulatanes from Eremophila spp. by Combined use of Dual High-Resolution PTP1B and α-Glucosidase Inhibition Profiling and HPLC-HRMS-SPE-NMR.

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Identification of PTP1B and α-Glucosidase Inhibitory Serrulatanes from Eremophila spp. by Combined use of Dual High-Resolution PTP1B and α-Glucosidase Inhibition Profiling and HPLC-HRMS-SPE-NMR.

Content Provider	Semantic Scholar
Author	Wubshet, Sileshi Gizachew Tahtah, Yousof Heskes, Allison Maree Kongstad, Kenneth Thermann Pateraki, Irini Hamberger, Bjoern Møller, Birger Lindberg Staerk, Dan
Copyright Year	2016
Abstract	According to the International Diabetes Federation, type 2 diabetes (T2D) has reached epidemic proportions, affecting more than 382 million people worldwide. Inhibition of protein tyrosine phosphatase-1B (PTP1B) and α-glucosidase is a recognized therapeutic approach for management of T2D and its associated complications. The lack of clinical drugs targeting PTP1B and side effects of the existing α-glucosidase drugs, emphasize the need for new drug leads for these T2D targets. In the present work, dual high-resolution PTP1B and α-glucosidase inhibition profiles of Eremophila gibbosa, E. glabra, and E. aff. drummondii "Kalgoorlie" were used for pinpointing α-glucosidase and/or PTP1B inhibitory constituents directly from the crude extracts. A subsequent targeted high-performance liquid chromatography-high-resolution mass spectrometry-solid-phase extraction-nuclear magnetic resonance spectroscopy (HPLC-HRMS-SPE-NMR) analysis and preparative-scale HPLC isolation led to identification of 21 metabolites from the three species, of which 16 were serrulatane-type diterpenoids (12 new) associated with either α-glucosidase and/or PTP1B inhibition. This is the first report of serrulatane-type diterpenoids as potential α-glucosidase and/or PTP1B inhibitors.
File Format	PDF HTM / HTML
DOI	10.1021/acs.jnatprod.5b01128
PubMed reference number	26960032
Journal	Medline
Volume Number	79
Issue Number	4
Alternate Webpage(s)	http://pdf-s3.xuebalib.com:1262/2otdTkBYfhy.pdf
Alternate Webpage(s)	https://doi.org/10.1021/acs.jnatprod.5b01128
Journal	Journal of natural products
Language	English
Access Restriction	Open
Content Type	Text
Resource Type	Article

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