Chemical constituents isolated from Actinidia polygama and their α-glucosidase inhibitory activity and insulin secretion effect

[Display omitted] •13 compounds, including three new monoterpenoids (1–3) and two hydroxycinnamoyl triterpenoids (4–5), were identified in Actinidia polygama.•Three new monoterpenoids (1–3) were identified by analyzing spectroscopic and chiroptical data.•3-O-coumaroylmaslinic acid (4) and jacoumaric...

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Veröffentlicht in:Bioorganic chemistry 2023-05, Vol.134, p.106466-106466, Article 106466
Hauptverfasser: Hwang, Hoseong, Lee, Dahae, Son, Jong Dai, Baek, Jong Gwon, Lee, Hyeon-Seong, Park, InWha, Kim, Dong Hoon, Lee, Soon Kwang, Kim, Won Kyu, Kwon, Hak Cheol, Kang, Ki Sung, Kwon, Jaeyoung
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Sprache:eng
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Zusammenfassung:[Display omitted] •13 compounds, including three new monoterpenoids (1–3) and two hydroxycinnamoyl triterpenoids (4–5), were identified in Actinidia polygama.•Three new monoterpenoids (1–3) were identified by analyzing spectroscopic and chiroptical data.•3-O-coumaroylmaslinic acid (4) and jacoumaric acid (5) exhibited α-glucosidase inhibitory activity.•3-O-coumaroylmaslinic acid (4) and jacoumaric acid (5) induced glucose‐stimulated insulin secretion activity in rat INS-1 pancreatic β-cells.•3-O-coumaroylmaslinic acid (4) and jacoumaric acid (5) increased IRS-2, PI3K, Akt, PDX-1, and PPAR-γ expression. Actinidia polygama has been used as a traditional medicine for treating various diseases. In the present study, 13 compounds, including three new monoterpenoids (1–3), were isolated from the leaves of A. polygama to investigate the bioactive constituents of the plant. The structures were characterized by analyzing spectroscopic and chiroptical data. These compounds were preliminarily screened for their ability to increase insulin secretion levels after glucose stimulation. Of these, 3-O-coumaroylmaslinic acid (4) and jacoumaric acid (5) showed activity. In further biological studies, these compounds exhibited increased glucose‐stimulated insulin secretion (GSIS) activity without cytotoxicity in rat INS-1 pancreatic β-cells as well as α-glucosidase inhibitory activity. Furthermore, both compounds increased insulin receptor substrate-2 (IRS-2), phosphatidylinositol 3-kinase (PI3K), protein kinase B (Akt), pancreatic and duodenal homeobox-1 (PDX-1), and peroxisome proliferator-activated receptor-γ (PPAR-γ) expression. Hence, these compounds may be developed as potential antidiabetic agents.
ISSN:0045-2068
1090-2120
DOI:10.1016/j.bioorg.2023.106466