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Pimarane diterpenoids from the seeds of caesalpinia minax as PTP1B inhibitors and insulin sensitizers
Xu,Yunshao1; Feng,Zheling1; Zhang,Tian1; Lv,Peng1; Cao,Jun1; Li,Dan2; Peng,Cheng2; Lin,Ligen1,2
2020-10-13
Source PublicationMolecules
Volume25Issue:20
Abstract

Protein-tyrosine phosphatase 1B (PTP1B) has been considered as a promising target for treating insulin resistance. In searching for naturally occurring PTB1B antagonists, two new pimarane diterpenoids, named 2α-hydroxy-7-oxo-pimara-8(9),15-diene (1) and 19-hydroxy-2α-acetoxy-7-oxo-pimara-8(9),15-diene (2), were isolated from the seeds of Caesalpinia minax. Their structures were determined by extensive analysis of NMR and HR-ESIMS data, and their absolute configurations were determined by electronic circular dichroism (ECD) spectra. Compound 1 was disclosed as a competitive inhibitor of PTP1B with an IC50 (the half-maximal inhibitory concentration) value of 19.44 ± 2.39 µM and a Ki (inhibition constant) value of 13.69 ± 2.72 μM. Moreover, compound 1 dose-dependently promoted insulin-stimulated glucose uptake in C2C12 myotubes through activating insulin signaling pathway. Compound 1 might be further developed as an insulin sensitizer.

KeywordGlucose Uptake Pimarane Diterpenoids Caesalpinia Minax Ptp1b
DOI10.3390/molecules25204674
URLView the original
Indexed BySCIE
Language英語English
WOS Research AreaBiochemistry & Molecular Biology ; Chemistry
WOS SubjectBiochemistry & Molecular Biology ; Chemistry, Multidisciplinary
WOS IDWOS:000585515000001
Scopus ID2-s2.0-85092521049
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Cited Times [WOS]:4   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Corresponding AuthorLin,Ligen
Affiliation1.State Key Laboratory of Quality Research in Chinese Medicine,Institute of Chinese Medical Sciences,University of Macau,Macao SAR,999078,Macao
2.State Key Laboratory of Southwestern Characteristic Chinese Medicine Resources,School of Pharmacy,Chengdu University of Traditional Chinese Medicine,Chengdu,610075,China
First Author AffilicationInstitute of Chinese Medical Sciences
Corresponding Author AffilicationInstitute of Chinese Medical Sciences
Recommended Citation
GB/T 7714
Xu,Yunshao,Feng,Zheling,Zhang,Tian,et al. Pimarane diterpenoids from the seeds of caesalpinia minax as PTP1B inhibitors and insulin sensitizers[J]. Molecules,2020,25(20).
APA Xu,Yunshao,Feng,Zheling,Zhang,Tian,Lv,Peng,Cao,Jun,Li,Dan,Peng,Cheng,&Lin,Ligen.(2020).Pimarane diterpenoids from the seeds of caesalpinia minax as PTP1B inhibitors and insulin sensitizers.Molecules,25(20).
MLA Xu,Yunshao,et al."Pimarane diterpenoids from the seeds of caesalpinia minax as PTP1B inhibitors and insulin sensitizers".Molecules 25.20(2020).
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