2-(2-Phenylethyl)chromone derivatives in artificial agarwood from Aquilaria sinensis

Fitoterapia. 2016 Apr:110:38-43. doi: 10.1016/j.fitote.2016.01.011. Epub 2016 Jan 16.

Abstract

Seven new 2-(2-phenylethyl)chromone derivatives (1-7) including a chlorinated one (4), together with eight known ones (8-15), were isolated from the EtOAc extract of artificial agarwood originating from Aquilaria sinensis (Lour.) Gilg. All structures including the absolute configurations were unambiguously elucidated by spectroscopic (NMR, UV, IR, MS) methods, Mosher's method, and comparison with reported data in the literatures. Among those, compounds 8, 12, and 14 exhibited significant inhibition against α-glucosidase in vitro with IC50 values of 0.15, 0.05, and 0.09 mM, respectively (with acarbose as the positive control; IC50: 0.98 mM). In addition, compounds 3, 9, 11, and 14 showed weak inhibitory activity against AChE; and compounds 12 and 13 displayed weak cytotoxicity against human gastric cell line (SGC-7901) among three types of tested human cancer cell lines (BEL-7402, K562, and SGC-7901).

Keywords: 2-(2-Phenylethyl)chromone; Agarwood; Aquilaria sinensis; Biological activity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents, Phytogenic / chemistry
  • Antineoplastic Agents, Phytogenic / isolation & purification
  • Cell Line, Tumor
  • Cholinesterase Inhibitors / chemistry
  • Cholinesterase Inhibitors / isolation & purification
  • Flavonoids / chemistry*
  • Flavonoids / isolation & purification
  • Glycoside Hydrolase Inhibitors / chemistry
  • Glycoside Hydrolase Inhibitors / isolation & purification
  • Humans
  • Inhibitory Concentration 50
  • Molecular Structure
  • Plant Extracts / chemistry
  • Thymelaeaceae / chemistry*
  • Wood / chemistry
  • alpha-Glucosidases

Substances

  • Antineoplastic Agents, Phytogenic
  • Cholinesterase Inhibitors
  • Flavonoids
  • Glycoside Hydrolase Inhibitors
  • Plant Extracts
  • 2-(2-phenylethyl)chromone
  • alpha-Glucosidases