Active Components with Inhibitory Activities on IFN-γ/STAT1 and IL-6/STAT3 Signaling Pathways from Caulis Trachelospermi

Molecules

Xiao-Ting Liu¹  Zhe-Xing Wang¹  Yu Yang²  Lin Wang²  Ruo-Feng Sun²  Yi-Min Zhao² 

[1] School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, China;Beijing Institute of Pharmacology and Toxicology, Beijing 100850, China

关键词: Caulis Trachelospermi;    4-demethyltraxillaside;    nortrachelogenin 4-O-β-d-glucopyranoside;    JAK/STAT signaling pathway;   

DOI  :  10.3390/molecules190811560

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
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