Physiological microspecies-constrained docking links UHPLC–MS/MS fingerprints to multi-target COX-1/COX-2/5-LOX inhibition by an ultrasound extract of Ziziphus lotus fruits

Ziziphus lotus (L.) Desf. fruits are traditionally used against inflammatory disorders, yet the bioactive phytochemical forms present at physiological pH are rarely considered in molecular docking, leading to misleading target–ligand hypotheses. Here, an ultrasound-assisted hydroethanolic extraction was optimized to obtain a phenolic-rich extract (yield 47.03 ± 2.26%; TPC 19.72 mg GAE g−1; TFC 9.30 mg QE g−1). UHPLC-MS/MS revealed rutin (42.05% AUC), delphinidin-3-rutinoside (21.30% AUC) and kaempferol glycosides (8.47% AUC) as major constituents. The extract inhibited 5-lipoxygenase, COX-1 and COX-2 with IC50 values of 158.35 ± 5.33, 89.78 ± 1.63 and 92.96 ± 2.22 µg mL−1, respectively. To address a key gap in in silico anti-inflammatory studies, we implemented pH-aware microspecies selection: dominant protonation states at pH 7.4 were predicted and docked into 5-LOX and COX isoforms. Rutin and delphinidin-3-rutinoside showed the most favorable binding energies (≈−8.2 and −8.1 kcal mol−1) with stable hydrogen-bond and π-interactions, supporting multi-target inhibition. This integrated pH-constrained workflow strengthens the translation of docking to biologically relevant chemical space.

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Publication Details

Journal
Moroccan Journal of chemistry
Published
2026-02-23
DOI
https://doi.org/10.48317/imist.prsm/morjchem-v14i2.64815
Primary Topic
Ziziphus Jujuba Studies and Applications
Type
article
Field-Weighted Citation Impact
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article

Physiological microspecies-constrained docking links UHPLC–MS/MS fingerprints to multi-target COX-1/COX-2/5-LOX inhibition by an ultrasound extract of Ziziphus lotus fruits

E.B. Maarouf, Abdessadek Rahimi, Raffaele Conte, Abdessamad Benabbou et al.
Moroccan Journal of chemistry
Ziziphus Jujuba Studies and Applications
article

Physiological microspecies-constrained docking links UHPLC–MS/MS fingerprints to multi-target COX-1/COX-2/5-LOX inhibition by an ultrasound extract of Ziziphus lotus fruits

E.B. Maarouf, Abdessadek Rahimi, Raffaele Conte, Abdessamad Benabbou, Oussama Khibech, M. Mimouni, A. Elbouzidi, M. Addi, A. Duong, M. Bouhchich, A. Challioui
article en

Abstract

Ziziphus lotus (L.) Desf. fruits are traditionally used against inflammatory disorders, yet the bioactive phytochemical forms present at physiological pH are rarely considered in molecular docking, leading to misleading target–ligand hypotheses. Here, an ultrasound-assisted hydroethanolic extraction was optimized to obtain a phenolic-rich extract (yield 47.03 ± 2.26%; TPC 19.72 mg GAE g−1; TFC 9.30 mg QE g−1). UHPLC-MS/MS revealed rutin (42.05% AUC), delphinidin-3-rutinoside (21.30% AUC) and kaempferol glycosides (8.47% AUC) as major constituents. The extract inhibited 5-lipoxygenase, COX-1 and COX-2 with IC50 values of 158.35 ± 5.33, 89.78 ± 1.63 and 92.96 ± 2.22 µg mL−1, respectively. To address a key gap in in silico anti-inflammatory studies, we implemented pH-aware microspecies selection: dominant protonation states at pH 7.4 were predicted and docked into 5-LOX and COX isoforms. Rutin and delphinidin-3-rutinoside showed the most favorable binding energies (≈−8.2 and −8.1 kcal mol−1) with stable hydrogen-bond and π-interactions, supporting multi-target inhibition. This integrated pH-constrained workflow strengthens the translation of docking to biologically relevant chemical space.

Moroccan Journal of chemistry
Mohammed V University (MA), Laboratoire de Glycochimie, des Antimicrobiens et des Agroressources (FR), Mohamed I University (MA), National Research Council (IT), Université de Picardie Jules Verne (FR)
Openalex Percentile: Top 18%
Ziziphus Jujuba Studies and Applications
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