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Pimarane Diterpenoids from the Seeds of Caesalpinia minax as PTP1B Inhibitors and Insulin Sensitizers.

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 2?-hydroxy-7-oxo-pimara-8(9),15-diene (1) and 19-hydroxy-2?-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 ?M. 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.

SUBMITTER: Xu Y 

PROVIDER: S-EPMC7587383 | biostudies-literature | 2020 Oct

REPOSITORIES: biostudies-literature

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Pimarane Diterpenoids from the Seeds of <i>Caesalpinia minax</i> as PTP1B Inhibitors and Insulin Sensitizers.

Xu Yunshao Y   Feng Zheling Z   Zhang Tian T   Lv Peng P   Cao Jun J   Li Dan D   Peng Cheng C   Lin Ligen L  

Molecules (Basel, Switzerland) 20201013 20

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 (<b>1</b>) and 19-hydroxy-2α-acetoxy-7-oxo-pimara-8(9),15-diene (<b>2</b>), were isolated from the seeds of <i>Caesalpinia minax</i>. Their structures were determined by extensive analysis of NMR and HR-ESIMS data, and their absolute configurations were  ...[more]

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