The capability of minor quaternary benzophenanthridine alkaloids to inhibit TNF-α secretion and cyclooxygenase activity

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Quaternary benzophenanthridine alkaloids are known to have a wide range of biological effects, including antimicrobial, antifungal, anti-inflammatory, and antitumour activities. However, only sanguinarine and chelerythrine have been studied intensively. The aim of this study was to evaluate the anti-inflammatory potential of the five minor quaternary benzophenanthridine alkaloids sanguilutine, sanguirubine, chelirubine, chelilutine, and macarpine in vitro and to compare them with more thoroughly studied sanguinarine and chelerythrine. Before making cell-based assays, the cytotoxicity of the alkaloids was evaluated. The anti-inflammatory potential of the chosen alkaloids was evaluated as for their ability to modulate the lipopolysaccharide-induced secretion of tumour necrosis factor α (TNF-α) in the macrophage-like cell line THP-1. The cyclooxygenase (COX)-1 and COX-2 inhibitory activities were also measured. The results indicate that the presence of a methylenedioxy ring attached at carbon (C)7-C8 is important for reducing the secretion of TNF-α. Interestingly, this effect did not show a simple dependence on concentration. The selected alkaloids showed little or no anti-COX activity. The results obtained from the present experiments may provide additional information useful in understanding the structure-to-activity relationship of the quaternary benzophenanthridine alkaloids. The anti-inflammatory potential and the cytotoxic effect are driven by the presence of a methylenedioxy ring attached at C7-C8 and C2-C3, respectively. … full description

Bibliographic Details

Main Author:

Jan Hošek, 1983 únor 19.-

Other Authors:

Kristýna Šebrlová, Petra Kaucká, Ondřej Peš , Eva Táborská, 1951-

Document Type:

Articles

Published in:

Acta veterinaria. -- ISSN 0001-7213. -- Roč. 86, č. 3 (2017), s. 223-230

Subjects:

DRUG PLANTS

PAPAVERACEAE

ALKALOIDS

Cytotoxicity

BIOLOGICAL PROPERTIES

MEDICINAL PROPERTIES

ANTIINFLAMMATORY AGENTS

CELL CULTURE

MACROPHAGES

Tumour necrosis factor

LIPOPOLYSACCHARIDES

CYTOKINES

ENZYME INHIBITORS

IN VITRO EXPERIMENTATION

léčivé rostliny

mákovité

alkaloidy

cytotoxicita

biologické vlastnosti

léčivé vlastnosti

protizánětlivé přípravky

buněčná kultura

makrofágy

faktor nekrotizující nádorové buňky

lipopolysacharidy

cytokiny

inhibitory enzymů

pokusy in vitro

Macleaya microcarpa > Dicranostigma lactucoides > Sanguinaria canadensis > krevnice kanadská > Stylophorum lasiocarpum > benzofenanthridin > sanguilutin > sanguirubin > chelirubin > chelilutin > makarpin > protizánětlivé účinky > cyklooxygenáza-1 > cyklooxygenáza-2 > methylenedioxy ring

Item Description:

2 grafy, 1 schéma, 2 tabulky

Physical Description:

Ilustrace

Bibliography:

Literatura na s. 229-230