Chemical Profiling, Analgesic and Anti-Inflammatory Activities of Farsetia aegyptia and Zilla spinosa: Integrated In Vitro, In Vivo, and In Silico Studies

TL;DR

This study explores the anti-inflammatory and pain-relieving properties of two plants, Farsetia aegyptia and Zilla spinosa, using various models and identifies key compounds responsible for these effects.

Contribution

The study integrates in vitro, in vivo, and in silico methods to identify novel anti-inflammatory compounds in two understudied plant species.

Findings

Aqueous extracts of both plants showed strong anti-inflammatory activity in animal models.

Quercetin 3-[rhamnosyl-(1->2)-rhamnosyl-(1->6)-glucoside] exhibited the best docking score against 5-lipoxygenase.

Both extracts significantly inhibited lipoxygenase with low IC50 values.

Abstract

Plants are a rich source of active metabolites that have been used to treat inflammation troubles. The current study aimed to identify the analgesic and anti-inflammatory compounds in Farsetia aegyptia and Zilla spinosa extracts. The anti-inflammatory activity was evaluated using the xylene-induced ear edema model in mice and the carrageenan-induced paw edema model in Wistar rats. Additionally, both central and peripheral analgesic effects were assessed in mice. The anti-lipoxygenase activity was examined through an in vitro enzyme inhibition assay. The phytochemical composition of the bioactive extracts was characterized using High-Resolution Liquid Chromatography–Mass Spectrometry (HR-LCMS). The aqueous extracts of both species exhibited the strongest anti-inflammatory activity. The F. aegyptia extract showed inhibition percentages of 51.82% at 6.25 mg/kg and 51.14% at 0.78 mg/kg, while the Z. spinosa extract yielded 65.05% inhibition at 12.5 mg/kg and 56.14% at 1.56 mg/kg in the paw and ear edema models, respectively. These extracts also demonstrated significant analgesic activity and inhibited lipoxygenase, with IC50 values of 0.063 mg/mL for F. aegyptia and 0.072 mg/mL for Z. spinosa. HR-LCMS analysis revealed that the main constituent in Fa was malic acid (18.83%), while retronecine (19.03%) was the primary compound in Z. spinosa. Quercetin 3-[rhamnosyl-(1->2)-rhamnosyl-(1->6)-glucoside] was detected in both extracts with important proportions 7.87% in F. aegyptia and 8.29% in Z. spinosa and displayed the best docking score of −9.2 kcal/mol against the 5-lipoxygenase receptor (PDB: 3V99) in molecular docking studies. Overall, these findings indicate that F. aegyptia and Z. spinosa have significant potential as sources of novel anti-inflammatory agents.

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