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@article{1396414,
author = {Hošek, Jan and Šebrlová, Kristýna and Kaucká, Petra and Peš, Ondřej and Táborská, Eva},
article_location = {Brno},
article_number = {3},
doi = {http://dx.doi.org/10.2754/avb201786030223},
keywords = {Cyclooxygenase; cytotoxicity; inflammation; TNF-alpha.},
language = {eng},
issn = {0001-7213},
journal = {Acta Veterinaria Brno},
title = {The capability of minor quaternary benzophenanthridine alkaloids to inhibit TNF-alpha secretion and cyclooxygenase activity},
volume = {86},
year = {2017}
}
TY - JOUR
ID - 1396414
AU - Hošek, Jan - Šebrlová, Kristýna - Kaucká, Petra - Peš, Ondřej - Táborská, Eva
PY - 2017
TI - The capability of minor quaternary benzophenanthridine alkaloids to inhibit TNF-alpha secretion and cyclooxygenase activity
JF - Acta Veterinaria Brno
VL - 86
IS - 3
SP - 223-230
EP - 223-230
PB - Veterinární a farmaceutická univerzita Brno
SN - 00017213
KW - Cyclooxygenase
KW - cytotoxicity
KW - inflammation
KW - TNF-alpha.
N2 - 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 alpha (TNF-alpha) 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-alpha. 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.
ER -
HOŠEK, Jan, Kristýna ŠEBRLOVÁ, Petra KAUCKÁ, Ondřej PEŠ and Eva TÁBORSKÁ. The capability of minor quaternary benzophenanthridine alkaloids to inhibit TNF-alpha secretion and cyclooxygenase activity. \textit{Acta Veterinaria Brno}. Brno: Veterinární a farmaceutická univerzita Brno, 2017, vol.~86, No~3, p.~223-230. ISSN~0001-7213. Available from: https://dx.doi.org/10.2754/avb201786030223.
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