Mansour L

References (6)

Title : Novel 3-phenyl-1- (alkylphenyl)-9-oxa-4-azaphenanthren-10-ones as inhibitors of some enzymes: synthesis, characterization, biological evaluation and molecular docking studies - Salah_2022_J.Biomol.Struct.Dyn__1
Author(s) : Salah DB , Chakchouk-Mtibaa A , Mellouli L , Ghalla H , Koko W , Al-Hazmy SM , Mansour L , Al-Tamimi J , Dlala NA , Bouazizi Y , Dridi K , Hamdi N
Ref : J Biomol Struct Dyn , :1 , 2022
Abstract : A series of novel 3-phenyl-1-(alkylphenyl)-9-oxa-4-azaphenanthren-10-ones and (E)-1-phenyl-3-(aryl)prop-2-en-1-ones were synthesized and characterized by IR, (1)H NMR, (13)C spectroscopy and elemental analysis. The synthesized Compounds 5a-f were subjected to molecular docking simulation with three proteins, namely, tyrosyl-tRNA synthetase, heme oxygenase 1 and acetylcholinesterase to evaluate the antibacterial, antioxidant and acetylcholinesterase inhibition, respectively. Moreover, the docked poses of all compounds inside the proteins were subjected to further dynamic simulation through the calculation of the binding free energy using MM-GBSA analysis. Compound 5d exhibits high potential inhibition against antibacterial, antioxidant and acetylcholinesterase activities. Compounds 3d, 3f, 5a and 5d recorded an important scavenging activity in DPPH and ABTS assays. Investigation of the anti-acetylcholinesterase activity of the synthesized compounds showed that Compounds 5a and 3d are the most potent inhibitors against AchE, with percent inhibition values of 38 and 30%, respectively.Communicated by Ramaswamy H. Sarma.
ESTHER : Salah_2022_J.Biomol.Struct.Dyn__1
PubMedSearch : Salah_2022_J.Biomol.Struct.Dyn__1
PubMedID: 36082583

Title : Physiological Responses of the Bivalves Mytilus galloprovincialis and Ruditapes decussatus Following Exposure to Phenanthrene: Toxicokinetics, Dynamics and Biomarkers Study - Dellali_2022_Animals.(Basel)_13_
Author(s) : Dellali M , Mardassi K , Harrath AH , Mansour L , Pacioglu O , Aldahmash W , Nahdi S , Badraoui R , Alrefaei AF , Boufahja F
Ref : Animals (Basel) , 13 : , 2022
Abstract : The aim of the current study was to assess the multifaceted effects of the polycylic aromatic hydrocarbon phenanthrene, mainly used in the colouring, explosive, and pharmaceutical industries, on the physiology of two bivalve species with economic value as seafood, namely, the Mediterranean mussel Mytilus galloprovincyalis and the European clam Ruditapes decussatus. The current study assessed how the phenanthrene affected several biomarkers and biometric endpoints in both bivalves, based on an in vivo experiment in silico approach. The bivalves were exposed during four time slots (i.e., 7, 15, 21, and 28 days) to two concentrations of phenanthrene in water (50 microg/L and 100 microg/L). For the clam R. decussatus, an additional contamination of sediment was applied due their typical benthic lifestyle (50 microg/kg and 100 microg/kg). The phenanthrene significantly reduced the ability of bivalves to tolerate desiccation and their Median Lethal Time, and also inhibited the activity of the enzyme acetylcholinesterase in a time-dependent manner. The activity of catalase indicated that bivalves also experienced oxidative stress during the first 21 days of the experiment. The significant decline in catalase activity observed during the last week of the experiment for the mussel M. galloprovincyalis supported a depletion of enzymes caused by the phenanthrene. The phenanthrene has also toxicokinetic and toxicodynamic properties, as assessed by the in silico approach. Overall, the results obtained suggest that the bivalves Ruditapes decussatus and M. galloprovincyalis can be used as a sentinel species in monitoring studies to assess the environmental impact of phenanthene in marine ecosystems. The significance of our findings is based on the fact that in ecotoxicology, little is known about the chronic effects, the simultaneous use of multiple species as bioindicators, and the interactions molecular modelling.
ESTHER : Dellali_2022_Animals.(Basel)_13_
PubMedSearch : Dellali_2022_Animals.(Basel)_13_
PubMedID: 36611758

Title : Acute toxicity and biomarker responses in Gammarus locusta amphipods exposed to copper, cadmium, and the organochlorine insecticide dieldrin - Dellali_2021_Environ.Sci.Pollut.Res.Int_28_36523
Author(s) : Dellali M , Douggui A , Harrath AH , Mansour L , Alwasel S , Beyrem H , Gyedu-Ababio T , Rohal-Lupher M , Boufahja F
Ref : Environ Sci Pollut Res Int , 28 :36523 , 2021
Abstract : The toxicity of copper, cadmium, and dieldrin in adult Gammarus locusta (a marine amphipod) is currently unclear. Thus, G. locusta from the North Lake of Tunis were subjected to acute toxicity tests to assess LC50s at 48-96 h and to biomarker response tests through the assessment of catalase and acetylcholinesterase activities and malondialdehyde levels. The present study demonstrated the abilities of a chlorinated hydrocarbon pesticide (dieldrin) induce to oxidative stress and neurotoxicity. The comparison of metal toxicity showed that G. locusta was more sensitive to cadmium than copper. The three stressors caused significant inductions of all three biomarkers in a concentration-dependent manner. Catalase induction was dependent on exposure duration for all pollutants, while only copper led to increased malondialdehyde with longer exposure times. Catalase induction and malondialdehyde increase appeared to be sex dependent for all three pollutants. The neurotoxic effects of the pollutants were concentration dependent according to inhibition of acetylcholinesterase activity. In conclusion, catalase, malondialdehyde, and acetylcholinesterase are efficient biomarkers of copper, cadmium, and dieldrin in G. locusta.
ESTHER : Dellali_2021_Environ.Sci.Pollut.Res.Int_28_36523
PubMedSearch : Dellali_2021_Environ.Sci.Pollut.Res.Int_28_36523
PubMedID: 33694119

Title : Anti-tyrosinase, anti-cholinesterase and cytotoxic activities of extracts and phytochemicals from the Tunisian Citharexylum spinosum L.: Molecular docking and SAR analysis - Saidi_2020_Bioorg.Chem_102_104093
Author(s) : Saidi I , Nimbarte VD , Schwalbe H , Waffo-Teguo P , Harrath AH , Mansour L , Alwasel S , Ben Jannet H
Ref : Bioorg Chem , 102 :104093 , 2020
Abstract : Previously phytochemical investigations carried out on the flowers and trunk bark extracts of Citharexylum spinosum L. tree, allowed the isolation of twenty molecules belonging to several families of natural substances [triterpene acids, iridoid glycosides, phenylethanoid glycosides, 8,3'-neolignan glycosides, together with other phenolic compounds]. In the present work, a biological evaluation (anti-tyrosinase, anticholinesterase and cytotoxic activities) was performed on the prepared extracts and the isolated secondary metabolites. The results showed that the EtOAc extract of the trunk bark displayed the highest anti-tyrosinase effect with a percent inhibition of 55.0 +/- 1.8% at a concentration of 100 mug/mL. The highest anticholinesterase activity was presented by the same extract with an IC(50) value of 99.97 +/- 3.01 mug/mL. The EtOAc extract of flowers and that of the trunk bark displayed the best cytotoxic property with IC(50) values of 96.00 +/- 2.85 and 88.75 +/- 2.00 mug/mL, respectively, against the human cervical cancer cell line (HeLa), and IC(50) values of 188.23 +/- 3.88 and 197.00 +/- 4.25 mug/mL, respectively, against the human lung cancer (A549) cell lines. Biological investigation of the pure compounds showed that the two 8,3'-neolignan glycosides, plucheosides D(1)-D(2), generate the highest anti-tyrosinase potency with a percent inhibition of 61.4 +/- 2.0 and 79.5 +/- 2.3%, respectively, at a concentration of 100 muM. The iridoid glycosides exhibited a significant anticholinesterase activity with IC(50) values ranging from 17.19 +/- 1.02 to 52.24 +/- 2.50 muM. Triterpene pentacyclic acids and iridoid glycosides exerted encouraging cytotoxic effects against HeLa with IC(50) values ranging from 9.00 +/- 1.10 to 25.00 +/- 1.00 muM. The study of the structure-activity relationship (SAR) has been sufficiently and widely discussed. The natural compounds that exhibited the significant bioactivities were docked.
ESTHER : Saidi_2020_Bioorg.Chem_102_104093
PubMedSearch : Saidi_2020_Bioorg.Chem_102_104093
PubMedID: 32717693

Title : A Palladium Catalyst System for the Efficient Cross-Coupling Reaction of Aryl Bromides and Chlorides with Phenylboronic Acid: Synthesis and Biological Activity Evaluation - Lamia_2017_Molecules_22_
Author(s) : Lamia B , Chakchouk-Mtibaa A , Hallouma B , Mansour L , Mellouli L , Ozdemir I , Yasar S , Hamdi N
Ref : Molecules , 22 : , 2017
Abstract : New benzimidazolium salts 1a-c and their palladium bis-N-heterocyclic carbene complexes 2a-c and palladium PEPPSI-type complexes 3a-c were designed, synthesized and structurally characterized by NMR (1H and 13C), IR, DART-TOF mass spectrometry and elemental analysis. Then these complexes 2-3 were employed in the Suzuki-Miyaura cross-coupling reaction of substituted arenes with phenylboronic acid under mild conditions in toluene and DMF/H2O (1/1) to afford functionalized biaryl derivatives in good to excellent yields. The antibacterial activity of palladium bis-N-heterocyclic carbene complexes 2a-c and palladium PEPPSI-type complexes 3a-c was measured by disc diffusion method against Gram positive and Gram negative bacteria. Compounds 2a, 2c and 3a-c exhibited potential antibacterial activity against four bacterial species among the five used indicator cells. The product 2b inhibits the growth of the all five tested microorganisms. Moreover, the antioxidant activity determination of these complexes 2-3, using 2.2-diphenyl-1-picrylhydrazyl (DPPH) as a reagent, showed that compounds 2a-c and 3b possess DPPH antiradical activity. The higher antioxidant activity was obtained from the product 2b which has radical scavenging activity comparable to that of the two used positive controls (gallic acid "GA" and tutylatedhydroxytoluene "BHT"). Investigation of the anti-acetylcholinesterase activity of the studied complexes showed that compounds 2b, 3a, and 3b exhibited moderate activity at 100 mug/mL and product 2b is the most active.
ESTHER : Lamia_2017_Molecules_22_
PubMedSearch : Lamia_2017_Molecules_22_
PubMedID: 28272376

Title : Exome sequencing links corticospinal motor neuron disease to common neurodegenerative disorders - Novarino_2014_Science_343_506
Author(s) : Novarino G , Fenstermaker AG , Zaki MS , Hofree M , Silhavy JL , Heiberg AD , Abdellateef M , Rosti B , Scott E , Mansour L , Masri A , Kayserili H , Al-Aama JY , Abdel-Salam GMH , Karminejad A , Kara M , Kara B , Bozorgmehri B , Ben-Omran T , Mojahedi F , El Din Mahmoud IG , Bouslam N , Bouhouche A , Benomar A , Hanein S , Raymond L , Forlani S , Mascaro M , Selim L , Shehata N , Al-Allawi N , Bindu PS , Azam M , Gunel M , Caglayan A , Bilguvar K , Tolun A , Issa MY , Schroth J , Spencer EG , Rosti RO , Akizu N , Vaux KK , Johansen A , Koh AA , Megahed H , Durr A , Brice A , Stevanin G , Gabriel SB , Ideker T , Gleeson JG
Ref : Science , 343 :506 , 2014
Abstract : Hereditary spastic paraplegias (HSPs) are neurodegenerative motor neuron diseases characterized by progressive age-dependent loss of corticospinal motor tract function. Although the genetic basis is partly understood, only a fraction of cases can receive a genetic diagnosis, and a global view of HSP is lacking. By using whole-exome sequencing in combination with network analysis, we identified 18 previously unknown putative HSP genes and validated nearly all of these genes functionally or genetically. The pathways highlighted by these mutations link HSP to cellular transport, nucleotide metabolism, and synapse and axon development. Network analysis revealed a host of further candidate genes, of which three were mutated in our cohort. Our analysis links HSP to other neurodegenerative disorders and can facilitate gene discovery and mechanistic understanding of disease.
ESTHER : Novarino_2014_Science_343_506
PubMedSearch : Novarino_2014_Science_343_506
PubMedID: 24482476