Witry-lès-Reims, France
Witry-lès-Reims, France

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Harhar H.,Mohammed V University | Gharby S.,Mohammed V University | Monfalouti H.E.,Mohammed V University | Monfalouti H.E.,Laboratoire Of Chimie Therapeutique | And 2 more authors.
Natural Product Communications | Year: 2010

The composition of the essential oil from the fresh and dried pulp of the fruit of Argania spinosa (Skeels) L. has been studied. Camphor was the major component in both oil types, but in addition, the fresh fruit oil had significant amounts of 1,8-cineole, endo-borneol, and 2-(4-methylcyclohex-3- enyl)-propan-2-ol., and the dried pulp oil 3,5-dimethyl-4-ethylidene-cyclohex-2- ene-1-one, 1,8-cineole, and 2-methylbutanoic acid. The presence of camphor and 1,8-cineole in argan fruit essential oil suggests that it could be used locally as an insect repellent, offering an output for argan fruit pulp that is at present a waste product.


Samadi A.,Laboratorio Of Radicales Libres Y Quimica Computacional Iqog Csic | Soriano E.,Laboratorio Of Radicales Libres Y Quimica Computacional Iqog Csic | Revuelta J.,Laboratorio Of Radicales Libres Y Quimica Computacional Iqog Csic | Valderas C.,Laboratorio Of Radicales Libres Y Quimica Computacional Iqog Csic | And 11 more authors.
Bioorganic and Medicinal Chemistry | Year: 2011

The synthesis, structure, theoretical and experimental in vitro antioxidant properties using the DPPH, ORAC, and benzoic acid, as well as preliminary in vitro pharmacological activities of (Z)-α-aryl and heteroaryl N-alkyl-nitrones 6-15, 18, 19, 21, and 23, is reported. In the in vitro antioxidant activity, for the DPPH radical test, only nitrones bearing free phenol groups gave the best RSA (%) values, nitrones 13 and 14 showing the highest values in this assay. In the ORAC analysis, the most potent radical scavenger was nitrone indole 21, followed by the N-benzyl benzene-type nitrones 10 and 15. Interestingly enough, the archetypal nitrone 7 (PBN) gave a low RSA value (1.4%) in the DPPH test, or was inactive in the ORAC assay. Concerning the ability to scavenge the hydroxyl radical, all the nitrones studied proved active in this experiment, showing high values in the 94-97% range, the most potent being nitrone 14. The theoretical calculations for the prediction of the antioxidant power, and the potential of ionization confirm that nitrones 9 and 10 are among the best compounds in electron transfer processes, a result that is also in good agreement with the experimental values in the DPPH assay. The calculated energy values for the reaction of ROS (hydroxyl, peroxyl) with the nitrones predict that the most favourable adduct-spin will take place between nitrones 9, 10, and 21, a fact that would be in agreement with their experimentally observed scavenger ability. The in vitro pharmacological analysis showed that the neuroprotective profile of the target molecules was in general low, with values ranging from 0% to 18.7%, in human neuroblastoma cells stressed with a mixture of rotenone/oligomycin-A, being nitrones 18, and 6-8 the most potent, as they show values in the range 24-18.4%. © 2010 Elsevier Ltd. All rights reserved.


Harhar H.,University Mohammeddal | Gharby S.,University Mohammeddal | Gharby S.,Laboratoire Controle Qualite | Kartah B.,University Mohammeddal | And 4 more authors.
Plant Foods for Human Nutrition | Year: 2011

Virgin argan oil, which is harvested from argan fruit kernels, constitutes an alimentary source of substances of nutraceutical value. Chemical composition and oxidative stability of argan oil prepared from argan kernels roasted for different times were evaluated and compared with those of beauty argan oil that is prepared from unroasted kernels. Prolonged roasting time induced colour development and increased phosphorous content whereas fatty acid composition and tocopherol levels did not change. Oxidative stability data indicate that kernel roasting for 15 to 30min at 110°C is optimum to preserve virgin argan oil nutritive properties. © 2011 Springer Science+Business Media, LLC.


El Jaoudi R.,British Petroleum | Benziane H.,Laboratoire Of Chimie Therapeutique | Khabbal Y.,Laboratoire Of Biostatistique Et Of Recherche Medicale | Elomri N.,Hopital Militaire dInstruction Mohammed V | And 2 more authors.
Therapie | Year: 2010

Purpose. To estimate the relative frequency of reported adverse drug reactions during the malaria chemoprophylactic period of the Moroccan contingent in Democratic Republic of Congo (DRC). Methods. The transversal survey involved all military personnel of the Moroccan contingent and was carried out using a questionnaire to be filled out by a multidisciplinary medical team. It was performed in all the military sites and the advanced posts accessible during the period of the study. Results. The study involved 362 male military subjects. Ninety-four adverse drug reactions were described: neuropsychiatric (anxiety, irritability, dizziness. . . ) [n=76], digestive (anorexia, diarrhea, nausea. . . ) [n=42], cardiovascular (tachycardia, palpitation, precordialgia...) [n=5], musculoskeletal (arthralgia, cramps) [n=4], cutaneous (redness, purpura) [n=2], and other (n=13). No "unexpected" or "serious" adverse drug reaction was reported. The causality assessment score was determined in 94 cases. Two of these reports were rated "likely", 12 "possible" and 80 doubtful. More adverse drug reactions were reported by subjects having medical and paramedical functions. Conclusion. During our study, mefloquine induced adverse drug reactions in a quarter of the treated subjects. Most of the adverse drug reactions were neuropsychiatric. No "serious" adverse drug reactions were reported underlying the interest of its use, even for long-term chemoprophylaxis. © 2010 Société Française de Pharmacologie et de Thérapeutique.


Note O.P.,CNRS Laboratory for Therapeutic Innovation | Note O.P.,University of Yaounde I | Simo L.,CNRS Laboratory for Therapeutic Innovation | Simo L.,University of Yaounde I | And 6 more authors.
Phytochemistry Letters | Year: 2016

As part of our search of new apoptosis-inducing triterpenoid saponins from Cameroonian Albizia genus, phytochemical investigation of the roots of Albizia zygia led to the isolation of two new oleanane-type saponins, named zygiaosides A–B (1–2), together with two known saponins, coriarioside A (3) and lebbeckoside A (4). Their structures were established on the basis of extensive 1D and 2D NMR (1H, 13C NMR, DEPT, COSY, HSQC-TOCSY, NOESY, HSQC and HMBC) and HRESIMS studies, and by chemical evidence. The apoptotic effect of saponins 1–2 was evaluated on the A431 human epidermoid cancer cell. Cytometric analyses showed that saponins 1–2 induced apoptosis of human epidermoid cancer cell (A341) in a dose-dependent manner. © 2016


Verones V.,Laboratoire Of Chimie Therapeutique | Flouquet N.,Laboratoire Of Chimie Therapeutique | Farce A.,Laboratoire Of Chimie Therapeutique | Carato P.,Laboratoire Of Chimie Therapeutique | And 4 more authors.
European Journal of Medicinal Chemistry | Year: 2010

The synthesis of new 4-amino-tetrahydroquinazolino[3,2-e]purine derivatives along with their activity in cell-free enzymatic assays on Src is reported. Some compounds emerged as moderately active inhibitors of the enzyme and showed antiproliferative effects on the murine leukemia L1210 cell line. Docking studies have been also performed to analyze the binding mode of compounds under study and to identify the structural determinants of their interaction. Therefore, this study provides a new promising scaffold with moderate enzymatic inhibitory activities for further development of new anticancer drugs targeting Src tyrosine kinase. © 2010 Elsevier Masson SAS. All rights reserved.


PubMed | University of Yaounde I, Laboratoire Of Chimie Therapeutique and CNRS Laboratory for Therapeutic Innovation
Type: | Journal: Fitoterapia | Year: 2016

As part of our search of new bioactive saponins from Cameroonian medicinal plants, phytochemical investigation of the roots of Albizia glaberrima led to the isolation of three new oleanane-type saponins, named glaberrimosides A-C (1-3). Their structures were established by direct interpretation of their spectral data, mainly HRESIMS, 1D NMR (1H, 13C NMR, and DEPT) and 2D NMR (COSY, ROESY, HSQC and HMBC) as 3-O-[-L-arabinopyranosyl-(1 6)-[-D-glucopyranosyl-(1 2)]--D-glucopyranosyl]-28-O-[-D-glucopyranosyl-(1 6)-[-d-glucopyranosyl-(1 2)]--D-glucopyranosyl]-oleanolic acid (1), 3-O-[-L-arabinopyranosyl-(1 6)-[-D-glucopyranosyl-(1 2)]--D-glucopyranosyl]-28-O-[-D-glucopyranosyl-(1 6)--D-glucopyranosyl]-oleanolic acid (2), and 3-O-[-D-glucopyranosyl-(12)--D-glucopyranosyl]-28-O-[-D-glucopyranosyl-(1 6)-[-D-fucopyranosyl-(1 2)]--D-glucopyranosyl]-oleanolic acid (3). The pro-apoptotic effect of the three saponins was evaluated on three human cell lines (pancreatic carcinoma AsPC-1, hematopoietic monocytic THP-1, and human fibroblast cell line BJ). Saponins 1-3 specifically induced apoptosis of pancreatic carcinoma cell (AsPC-1) in a dose-dependent manner. More interestingly, there were inactive on monocytic (THP-1) and normal human fibroblast (BJ) cell lines.


Garofalo A.,University of Lille Nord de France | Goossens L.,University of Lille Nord de France | Six P.,University of Lille Nord de France | Lemoine A.,University of Lille Nord de France | And 4 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2011

Three series of 6,7-dimethoxyquinazoline derivatives substituted in the 4-position by aniline, N-methylaniline and aryloxy entities, targeting EGFR and VEGFR-2 tyrosine kinases, were designed and synthesized. Pharmacological activities of these compounds have been evaluated for their enzymatic inhibition of VEGFR-2 and EGFR and for their antiproliferative activities on various cancer cell lines. We have studied the impact of the variation in the 4-position substitution of the quinazoline core. Substitution by aryloxy groups led to new compounds which are selective inhibitors of VEGFR-2 enzyme with IC50 values in the nanomolar range in vitro. © 2011 Elsevier Ltd. All rights reserved.


PubMed | Laboratoire Of Chimie Therapeutique
Type: Journal Article | Journal: European journal of medicinal chemistry | Year: 2010

The synthesis of new 4-amino-tetrahydroquinazolino[3,2-e]purine derivatives along with their activity in cell-free enzymatic assays on Src is reported. Some compounds emerged as moderately active inhibitors of the enzyme and showed antiproliferative effects on the murine leukemia L1210 cell line. Docking studies have been also performed to analyze the binding mode of compounds under study and to identify the structural determinants of their interaction. Therefore, this study provides a new promising scaffold with moderate enzymatic inhibitory activities for further development of new anticancer drugs targeting Src tyrosine kinase.

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