Browsing by Author "El Aouad, Noureddine"
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- Chemical composition and biological screening of the essential oils of Micromeria macrosiphon and M. arganietorum (Lamiaceae)Publication . El Yaagoubi, Mohamed; Mechqoq, Hicham; Ortiz, Sergio; Cavaleiro, Carlos; Lecsö‐Bornet, Marylin; Pereira, Catarina; Rodrigues, Maria Joao; Custódio, Luísa; El Mousadik, Abdelhamid; Picot, Laurent; Kritsanida, Marina; Msanda, Fouad; El Aouad, Noureddine; Grougnet, RaphaëlThe chemical composition and in vitro biological activities of the essential oil (EO) of Micromeria macrosiphon Coss. and M. arganietorum (J. Emb.) R. Morales, two Lamiaceae endemic to south Morocco, were investigated. GC/MS analysis resulted in the identification of 36 metabolites from the EO of M. macrosiphon, 45 from M. arganietorum. Borneol was the major metabolite in both oils and together with related derivatives such as camphor, accounted for 2/3 of the EO of M. macrosiphon, 1/3 of those of M. arganietorum. Pinene and terpinene derivatives were also present in high proportions. From a chemotaxonomic point of view, the composition of the examined samples may be related to those of other species endemic to Macaronesia. Both EOs showed significant toxicity towards liver HepG2 and melanoma B16 4A5 tumor cell lines at 100 mu g/mL; however, they were also cytotoxic towards S17 normal cell lines, with a selectivity index <1. No antibacterial activity was noticed against 52 strains at 100 mu g/mL.
- Chemical composition, antibacterial screening and cytotoxic activity of Chiliadenus antiatlanticus (Asteraceae) essential oilPublication . El Yaagoubi, Mohamed; Ortiz, Sergio; Mechqoq, Hicham; Cavaleiro, Carlos; Lecso-Bornet, Marylin; Rodrigues, Maria Joao; Custódio, Luísa; El Mousadik, Abdelhamid; Grougnet, Raphael; El Aouad, Noureddine; Msanda, Fouad; Kritsanida, MarinaThe chemical composition and in vitro antibacterial and cytotoxic activities of the essential oil (EO) of Chiliadenus antiatlanticus (Emb. & Maire) Gomiz, an asteraceous species endemic to the southwest of Morocco, were investigated. The EO yield was 1.07 +/- 0.28 %, twenty-seven metabolites were identified representing more than 96.4 % of the total composition. Camphor (35.7 %) and derivatives, borneol (4.9 %) and camphene (4.2 %) together with intermedeol (19.9 %), alpha-pinene (15.5 %) and (E)-pinocarveol (4.1 %) were the major constituents. An antibacterial activity was noticed against 24 strains (all Gram-positive) out of 71 at MICs values=100 mu g/mL. The EO also showed significant toxicity towards liver HepG2 (55.8 % of cell viability) and melanoma B16 4A5 (41.6 % of cell viability) tumor cell lines at 100 mu g/mL.
- High-content screening of natural products reveals novel nuclear export inhibitorsPublication . Cautain, Bastien; de Pedro, Nuria; Garzon, Virginia Murillo; de Escalona, Maria Munoz; Menendez, Victor Gonzalez; Tormo, Jose R.; Martin, Jesus; El Aouad, Noureddine; Reyes, Fernando; Asensio, Francisco; Genilloud, Olga; Vicente, Francisca; Link, WolfgangNatural products are considered an extremely valuable source for the discovery of new drugs against diverse pathologies. As yet, we have only explored a fraction of the diversity of bioactive compounds, and opportunities for discovering new natural products leading to new drugs are huge. In the present study, U2nesRELOC, a previously established cell-based imaging assay, was employed to screen a collection of extracts of microbial origin for nuclear export inhibition activity. The fluorescent signal of untreated U2nesRELOC cells localizes predominantly to the cytoplasm. Upon treatment with the nuclear export inhibitor leptomycin B, the fluorescent-tagged reporter proteins appear as speckles in the nucleus. A proprietary collection of extracts from fungi, actinomycetes, and unicellular bacteria that covers an uncommonly broad chemical space was used to interrogate this nuclear export assay system. A two-step image-based analysis allowed us to identify 12 extracts with biological activities that are not associated with previously known active metabolites. The fractionation and structural elucidation of active compounds revealed several chemical structures with nuclear export inhibition activity. Here we show that substrates of the nuclear export receptor CRM1, such as Rev, FOXO3a and NF-B, accumulate in the nucleus in the presence of the fungal metabolite MDN-0105 with an IC50 value of 3.4 mu M. Many important processes in tumor formation and progression, as well as in many viral infections, critically depend on the nucleocytoplasmic trafficking of proteins and RNA molecules. Therefore, the disruption of nuclear export is emerging as a novel therapeutic approach with enormous clinical potential. Our work highlights the potential of applying high-throughput phenotypic imaging on natural product extracts to identify novel nuclear export inhibitors.