Anti-diabetic xanthones from the bark of Garcinia xanthochymus

作者：Nguyen Chi N; Trinh Binh T D; Tran Toan B; Nguyen Le Thu T; Jager Anna K; Nguyen Lien Hoa D^*

来源：Bioorganic & Medicinal Chemistry Letters, 2017, 27(15): 3301-3304.

DOI：10.1016/j.bmcl.2017.06.021

• Garcinia xanthochymus
• Structure determination
• Xanthones
• Anti-diabetic activity
• alpha-Glucosidase
• PTP1B inhibition

An ethyl acetate extract the bark of Garcinia xanthochymus exhibited strong inhibition towards alpha-glucosidase and PTP1B with IC50 values of 0.3 +/- 0.1 mu g/mL and 2.3 +/- 0.4 mu g/mL, respectively. Chemical constituents of the extract were therefore examined, and two new compounds, xanthochymusxanthones A (1) and B (2), along with ten known xanthones (3-12), were isolated. Their structures were determined using spectroscopic methods, mainly 1D and 2D NMR. Inhibitory activity of the isolated compounds was then tested, and subelliptenone F (12) showed significant effect towards alpha-glucosidase with IC50 value of 4.1 +/- 0.3 mu M (compared with acarbose, IC50 = 900.0 +/- 3.0 mu M) whilst xanthochymusxanthone B (2) exhibited remarkable activity towards PTP1B with IC50 value of 8.0 +/- 0.6 mu M (compared with RK682, IC50 = 4.4 +/- 0.3 mu M).

• 出版日期2017-8-1