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Bupleurum chinense Roots: a Bioactivity-Guided Approach toward Saponin-Type NF-κB Inhibitors.

Authors
  • Liu, Xin1
  • Latkolik, Simone2
  • Atanasov, Atanas G2, 3
  • Kunert, Olaf4
  • Pferschy-Wenzig, Eva-Maria1
  • Heiss, Elke H2
  • Malainer, Clemens2
  • Schinkovitz, Andreas1
  • Kollroser, Manfred5
  • Dirsch, Verena M2
  • Bauer, Rudolf1
  • 1 Institute of Pharmaceutical Sciences, Department of Pharmacognosy, University of Graz, Austria. , (Austria)
  • 2 Department of Pharmacognosy, University of Vienna, Austria. , (Austria)
  • 3 Institute of Genetics and Animal Breeding of the Polish Academy of Sciences, Jastrzebiec, Poland. , (Poland)
  • 4 Institute of Pharmaceutical Sciences, Department of Pharmaceutical Chemistry, University of Graz, Austria. , (Austria)
  • 5 Institute of Forensic Medicine, Medical University of Graz, Austria. , (Austria)
Type
Published Article
Journal
Planta Medica
Publisher
Georg Thieme Verlag KG
Publication Date
Oct 01, 2017
Volume
83
Issue
14-15
Pages
1242–1250
Identifiers
DOI: 10.1055/s-0043-118226
PMID: 28902374
Source
Medline
License
Unknown

Abstract

The roots of Bupleurum chinense have a long history in traditional medicine to treat infectious diseases and inflammatory disorders. Two major compounds, saikosaponins A and D, were reported to exert potent anti-inflammatory activity by inhibiting NF-κB. In the present study, we isolated new saikosaponin analogues from the roots of B. chinese interfering with NF-κB activity in vitro. The methanol-soluble fraction of the dichloromethane extract of Radix Bupleuri was subjected to activity-guided isolation yielding 18 compounds, including triterpenoids and polyacetylenes. Their structures were determined by spectroscopic methods as saikogenin D (1), prosaikogenin D (2), saikosaponins B2 (3), W (4), B1 (5), Y (6), D (7), A (8), E (9), B4 (10), B3 (11), and T (12), saikodiyne A (13), D (14), E (15) and F (16), falcarindiol (17), and 1-linoleoyl-sn-glycero-3-phosphorylcholine (18). Among them, 4, 15, and 16 are new compounds, whereas 6, previously described as a semi-synthetic compound, is isolated from a natural source for the first time, and 13-17 are the first reports of polyacetylenes from this plant. Nine saponins/triterpenoids were tested for inhibition of NF-κB signaling in a cell-based NF-κB-dependent luciferase reporter gene model in vitro. Five of them (1, 2, 4, 6, and 8) showed strong (> 50%, at 30 µM) NF-κB inhibition, but also varying degrees of cytotoxicity, with compounds 1 and 4 (showing no significant cytotoxicity) presenting IC50 values of 14.0 µM and 14.1 µM in the cell-based assay, respectively.

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