Evidence for the anti-inflammatory activity of Bupleurum marginatum (Apiaceae) extracts using in vitro and in vivo experiments supported by virtual screening

Objectives To explore the potential anti-inflammatory activity of Bupleurum marginatum extracts using in vitro and in vivo studies supported by virtual screening. Methods Antioxidant activity was assessed using the DPPH˙ and inhibition of 2-deoxyribose degradation assays. Anti-inflammatory activity...

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Main Authors: Ashour, Mohamed L. (Author) , Youssef, Fadia S. (Author) , Gad, Haidy A. (Author) , Readi, Mahmoud Zaki el (Author) , Bouzabata, Amel (Author) , Abuzeid, Riham M. (Author) , Sobeh, Mansour (Author) , Wink, Michael (Author)
Format: Article (Journal)
Language:English
Published: 03 April 2018
In: Journal of pharmacy and pharmacology
Year: 2018, Volume: 70, Issue: 7, Pages: 952-963
ISSN:2042-7158
DOI:10.1111/jphp.12904
Online Access:Verlag, lizenzpflichtig, Volltext: https://doi.org/10.1111/jphp.12904
Verlag, lizenzpflichtig, Volltext: https://onlinelibrary.wiley.com/doi/abs/10.1111/jphp.12904
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Author Notes:Mohamed L. Ashour, Fadia S. Youssef, Haidy A. Gad, Mahmoud Z. El‐Readi, Amel Bouzabata, Riham M. Abuzeid, Mansour Sobeh, and Michael Wink

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520 |a Objectives To explore the potential anti-inflammatory activity of Bupleurum marginatum extracts using in vitro and in vivo studies supported by virtual screening. Methods Antioxidant activity was assessed using the DPPH˙ and inhibition of 2-deoxyribose degradation assays. Anti-inflammatory activity was determined in vitro by measuring the suppression of prostaglandin E2 release (PGE2) in pancreatic cancer cells (MIA-PaCa-2) and the inhibition of 5-lipoxygenase whereas the rat paw oedema was used in vivo. The major constituents were docked in 5-lipoxygenase and cyclooxygenase-II active sites. Key findings Methanol and dichloromethane (DCM) extracts showed IC50 of 46.99 and 162.99 μg/ml in the DPPH˙, 1.52 and 2.12 μg/ml in inhibition of 2-deoxyribose degradation assays, respectively. They reduced PGE2 release by 41.33 and 52.85% at 25 μg/ml and inhibited 5-lipoxygenase with IC50 of 45.28 and 25.92 μg/ml, respectively. 50 and 70% reduction in the diameter of the carrageenan-induced rat paws with methanol and DCM extracts, respectively, with a marked decline in the inflammation score was observed. Rutin, a predominating compound, showed a strong interaction with the key amino acids in 5-LOX active site with interaction energy of −74.59 kcal/mol. Conclusions Our study provides evidence for an interesting anti-inflammatory activity of B. marginatum aerial parts offering a natural anti-inflammatory agent. 
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