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SHR Neuro Cancer Cardio Lipid Metab Microb

Liu, X; Latkolik, S; Atanasov, AG; Kunert, O; Pferschy-Wenzig, EM; Heiss, EH; Malainer, C; Schinkovitz, A; Kollroser, M; Dirsch, VM; Bauer, R.
Bupleurum chinense Roots: a Bioactivity-Guided Approach toward Saponin-Type NF-κB Inhibitors.
Planta Med. 2017; 83(14-15):1242-1250 Doi: 10.1055/s-0043-118226 [OPEN ACCESS]
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Co-authors Med Uni Graz: Kollroser Manfred
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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. Georg Thieme Verlag KG Stuttgart · New York.
Find related publications in this database (using NLM MeSH Indexing): Anti-Inflammatory Agents - chemistry; Anti-Inflammatory Agents - isolation & purification; Anti-Inflammatory Agents - pharmacology; Bupleurum - chemistry; Inhibitory Concentration 50 -; Lysophosphatidylcholines -; Medicine, Traditional -; Methanol -; Methylene Chloride -; NF-kappa B - antagonists & inhibitors; Oleanolic Acid - analogs & derivatives; Oleanolic Acid - chemistry; Oleanolic Acid - isolation & purification; Oleanolic Acid - pharmacology; Plant Roots - chemistry; Sapogenins - chemistry; Sapogenins - isolation & purification; Sapogenins - pharmacology; Saponins - chemistry; Saponins - isolation & purification; Saponins - pharmacology; Signal Transduction - drug effects
Find related publications in this database (Keywords): Bupleurum chinense; Apiaceae; NF-kappa B; saponin; polyacetylene; lysophosphatidylcholine