Active components with inhibitory activities on IFN-γ/STAT1 and IL-6/STAT3 signaling pathways from Caulis Trachelospermi

  • Molecules. 2014 Aug 5;19(8):11560-71. doi: 10.3390/molecules190811560.
Xiao-Ting Liu  1 ,  Zhe-Xing Wang  1 ,  Yu Yang  2 ,  Lin Wang  2 ,  Ruo-Feng Sun  2 ,  Yi-Min Zhao  2 ,  Neng-Jiang Yu  3
Affiliations
  • 1. School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, China.
  • 2. Beijing Institute of Pharmacology and Toxicology, Beijing 100850, China.
  • 3. Beijing Institute of Pharmacology and Toxicology, Beijing 100850, China. [email protected].
PMID: 25100250 DOI: 10.3390/molecules190811560
Abstract

Initial investigation for new active herbal extract with inhibiting activity on JAK/STAT signaling pathway revealed that the extract of Caulis Trachelospermi, which was separated by 80% alcohol extraction and subsequent HP-20 macroporous resin column chromatography, was founded to strongly inhibit IFN-γ-induced STAT1-responsive luciferase activity (IFN-γ/STAT1) with IC50 value of 2.43 μg/mL as well as inhibiting IL-6-induced STAT3-responsive luciferase activity (IL-6/STAT3) with IC50 value of 1.38 μg/mL. Subsequent study on its active components led to the isolation and identification of two new dibenzylbutyrolactone Lignans named 4-demethyltraxillaside (1) and nortrachelogenin 4-O-β-D-glucopyranoside (2), together with six known compounds. The lignan compounds 1-4 together with Other lignan compounds isolated in previous study were tested the activities on IFN-γ/STAT1 and IL-6/STAT3 pathways. The following result showed that the main components trachelogenin and arctigenin had corresponding activities on IFN-γ/STAT1 pathway with IC50 values of 3.14 μM and 9.46 μM as well as trachelogenin, arctigenin and matairesinol strongly inhibiting IL-6/STAT3 pathway with IC50 values of 3.63 μM, 6.47 μM and 2.92 μM, respectively.

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