Bioactive phytochemicals isolated from Akebia quinata enhances glucose-stimulated insulin secretion by inducing PDX-1
- Bioactive phytochemicals isolated from Akebia quinata enhances glucose-stimulated insulin secretion by inducing PDX-1
- 권학철; 이다해; 이진수; Jurdas Sezirahiga; 장대식; 강기성
- 으름덩굴굴; Akebia quinata; 인슐린 분비 촉진진; PDX-1; 당뇨뇨; stigmasterol-3-O-D-glucoside
- Issue Date
- VOL 9-14
- Chocolate vine (Akebia quinata) is consumed as a fruit and is also used in traditional medicine. In order to identify the bioactive components of A. quinata, a phytosterol glucoside stigmasterol-3-O-β-d-glucoside (1), three triterpenoids maslinic acid (2), scutellaric acid (3), and hederagenin (4), and three triterpenoidal saponins akebia saponin PA (5), hederacoside C (6), and hederacolchiside F (7) were isolated from a 70% EtOH extract of the fruits of A. quinata (AKQU). The chem. structures of isolates 1-7 were determined by analyzing the 1D and 2D NMR (NMR) spectroscopic data. Here, we evaluated the effects of AKQU and compounds 1-7 on insulin secretion using the INS-1 rat pancreatic β-cell line. Glucose-stimulated insulin secretion (GSIS) was evaluated in INS-1 cells using the GSIS assay. The expression levels of the proteins related to pancreatic β-cell function were detected by Western blotting. Among the isolates, stigmasterol-3-O-β-d-glucoside (1) exhibited strong GSIS activity and triggered the overexpression of pancreas/duodenum homeobox protein-1 (PDX-1), which is implicated in the regulation of pancreatic β-cell survival and function. Moreover, isolate 1 markedly induced the expression of extracellular signal-regulated protein kinases 1 and 2 (ERK1/2), insulin receptor substrate-2 (IRS-2), phosphoinositide 3-kinase (PI3K), and Akt, which regulate the transcription of PDX-1. The results of our exptl. studies indicated that stigmasterol-3-O-β-d-glucoside (1) isolated from the fruits of A. quinata can potentially enhance insulin secretion, and might alleviate the reduction in GSIS during the development of T2DM.
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