Polyphenol Contents and Antioxidant Activity of Ethanolic and Aqueous Algerian Propolis Extracts (Region of Serdj el ghoul)

Aqueous and ethanolic extracts (EAP and EEP) of propolis sample collected from Serdj El Ghoul, region of Sétif (east of Algeria), were prepared and evaluated to identify their biological activities. Total phenolic contents were determined using Folin-Ciocalteu reagent and found to be 164,690 ± 0,044 (EAP), 155,078 ± 0,176 mg cafeic acid equivalent/ g of propolis. Flavonoids were evaluated by AlCl3 method and shown to be 9,839± 0,006 (EAP), 55,758 ± 0,128 (EEP) mg quercetin equivalent/ g of propolis. The free radical scavenging potential of the extracts was determined by the DPPH method, the IC50 are estimated at 0.0865 (BHT), 0.0223 (EAP), 0.0194 (EEP) mg/mL. We can conclude that propolis contains molecules that are considered first class of antioxidants and can be used for therapeutic applications, knowing that antioxidants contribute very effectively to disease prevention such as cancer, and cardiovascular disease. Keywords: Propolis, aqueous extract, ethanolic extract, Antioxidan

Evaluation of isoniazid-oxidative reactions in mice model

In this study the anti-tubercular drug; isoniazid (INH) was investigated for their adverse effect; the oxidative stress. This effect was evaluated by using mice model, at the dose of 151 mg/kg.  We found that oxidative stress induced by INH is associated with lipid peroxidation expressed by the increase in the level of MDA from 76.9 ± 1.74 to 79.61 ± 2.67 nmol/g tissue. The oxidative stress of INH is accompanied by a decrease in reduced GSH level (from 79.9 ± 12 μmol / mg  to 68.48 ± 4.28 μmol / mg compared to of the control group). After treatment with INH at 151 mg/kg, a decrease in CAT activities occurred compared to control (2.53 ± 0.39 U/mg Pr vs 5.07 ± 0.73 U/mg Pr). Keywords: isoniazid, oxidative stress, MDA, GSH, CA

Synthesis, Characterization, Hydrolytic Cleavage, and Biological Activity Studies of 2-[(1e)-N-{2-[(2-{(Z)-[1-(2-Hydroxyphenyl)Ethylidene] Amino}Ethyl)Amino]Ethyl}Ethanimidoyl]Phenol

A Schiff base ligand 2-[(1E)-N-{2-[(2-{(Z)-[1-(2-hydroxyphenyl) ethylidene] amino}ethyl)amino]ethyl} ethanimidoyl]phenol L was hydrolyzed by copper cation which lead to formation of 8,8-dichloro-2H,3H,5H,6H-1,3-diaza-2-cupracyclopenta[1,3-a]1,3-diaza-2-cupracyclopentane hydrate (Complex), characterized by UV, IR, Powder XRD and by elemental analysis. In vitro antioxidant and anticoagulant, activities of L were evaluated. Antioxidant potential of L was assessed by DPPH scavenging, β-carotene bleaching test, hydroxyl radical scavenging method, ABTS radical scavenging test, and by reducing power test. In vitro anticoagulant effect of L at the 84 µg/mL; showed the maximum prolongation of plasma recalcification time which is comparable with that of the anticoagulant drug; heparin. In conclusion, results of the present investigation indicate that the ligand L can be a potential anticoagulant agent. Keywords: Schiff base; Antioxidant; Free radicals; Anticoagulant

Synthesis, Characterization, in vivo acute toxicity and superoxide anion scavenging evaluation of new isatin-hydrazone

A new isatin-hydrazone (I); N'-[(E)-(5-bromo-1H- indol-3-yl) methylidene] pyridine-4-carbohydrazide  was prepared from the condensation reaction of 5-bromo-1H-indole-3-carbaldehyde and the anti-tubercular drug; isoniazid, in the presence of acetic acid. The obtained hydrazone was identified and characterized by physico-chemical techniques such as melting point, IR, NMR, and mass spectroscopy. In addition, the acute toxicity was evaluated using mice. The antioxidant of I was evaluated against superoxide anion radical.  Our biological results indicate low toxicity of I at the high dose of 1000 mg/kg, and high superoxide anion scavenging effect with inhibition percentage of 82.57 % and IC50 138.78 µg/mL. Keyword: hydrazone, toxicity, antioxidant, superoxide anio

Skin Sensitization Calculation, Topical anti-inflammatory effect and DFT Study of New Indole-Hydrazone

A new indol-hydrazone (IH); N'-[(E)-(5-bromo-1H- indol-3-yl) methylidene] pyridine-4-carbohydrazide was selected for theoretical and experimental studies. Molecular structure proprieties were investigated using density functional theory (DFT) via B3LYP/6-31G (d,p), skin sensitization prediction was carried out using Pred Skin software program. The obtained results demonstrate the reactivity of IH with Energy gap (Δ) of 0.0579 a.u, low sensitizer effect towards human skin with probability of 60 %, and an excellent topical anti-inflammatory effect against xylen-induced ear odema in mice model with inhibition percentages of 81.48%. Keyword: Hydrazone, skin sensitization, Topical, Anti-inflammatory

Topical Anti-inflammatory evaluation of new hydrazone: 4-chloro-3-nitrobenzylidene) isonicotinohydrazide

The anti-inflammatory effects of the investigated compounds; Isoniazid, hydrazone, and Indomethacin were evaluated in this study. The experiment was performed using xylene induced topical ear edema method in mice model, at the dose of (0.5 mg/ear). Results showed that the compounds; Isoniazid, hydrazone, and Indomethacin exerted 85, 90 and 89% of inhibition percentages, respectively. The effect of hydrazone was statistically similar to the effect of indomethacin which is a standard anti-inflammatory drug. Keywords: inflammation, hydrazone, ear edema, topical

Synthesis, Characterisation and Analgesic Activity of Diethylenediamine Copper Complex

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In Silico Toxicological, Anti-Tubercular Effect Evaluation And In Vitro Marine Pathogenic Bacteria Inhibition of N-[(3-Chloro-4-Nitro-Phenyl)Methyleneamino]Pyridine-4-Carboxamidine

The hydrazone; N-[(3-chloro-4-nitro-phenyl) methyleneamino] pyridine-4-carboxamidine (H) was selected for in silico toxicological and in vitro bactericidal studies. Toxicological investigation was carried out using software program, such as eMolTox and Gusar, for the toxic substructure determination, and acute rat toxicity prediction respectively. In vitro bactericidal effect evaluation was investigated using tow marine pathogenic bacteria; Vibrio anguillarum and Photobacterium damselae. Computational results determinate toxicophores of (H), which are nitro-aromatic part, hydrazine group, and quaternary carbon, were predicted as responsible for Idiosyncratic toxicity metabolic activation, covalent bond with DNA, and hepatotoxicity respectively. In addition, the predicted LD50 of (H) are 1086, 244, 1816, and 823.40 mg/kg in intraperitenial, intravenous, oral and subcutaneous administration respectively. For bactericidal results, H exhibited an excellent effect with inhibition percentages of 98.65 and 98.83% at the concentrations of 1000 and 500 µg/mL against Vibrio anguillarum respectively, the same effect was demonstrated against Photobacterium damselae with inhibition percentages of 97.74 and 97.98 % at the same concentrations. For anti-tubercular effect prediction, results revealed that H has an excellent effect with probability percentage of 84.6%.   Keyword: Hydrazone, toxicophore, LD50, Anti-tubercular, Vibrio anguillarum, Photobacterium damselae.    &nbsp

Chemical composition and antibacterial activity of Algerian propolis against fish pathogenic bacteria

Five different varieties of propolis from four sites from Sétif region (East of Algeria) (Babor, Setif; Ain-Abbassa and El-Hamma), and one site from the center of Algeria (Tizi-Ouzou) were chemically analysed by gas chromatography-mass spectrometry. One hundred and two compounds were identified including aromatic acids, linear hydrocarbons and their acids, terpenes and alcaloïdes. Furthermore, the in vitro bacteriostatic and bactericidal activities of the aqueous extracts were evaluated against one Gram positive (Bacillus subtilis, used as probiotics in aquaculture) and two Gram negative (Vibrio anguillarum and Vibrio harveyi, pathogenic for fish) bacteria. The obtained results showed that all aqueous extracts of propolis inhibit the growth of B. Subtilis while the growth inhibition of fish pathogens was achieved when using higher propolis concentrations. These antibacterial properties would warrant further studies on the clinical applications of propolis in aquaculture field. Keywords: Bactericidal activity; Chemical characterization; Propolis; Vibrio

Bioefficacy of Azadirachtin in Controlling Culex pipiens pipiens (Diptera: Culicidae)

Abstract Azadirachtin was tested for its effects against First P P and second instars larvae of mosquito Culex pipiens pipiens (Diptera: Culicidae), laboratory reared larvae were exposed to 0.125 ; 0.250; 0.500 and 0.750 mg/ L of azadirachtin in laboratory of biology animal application, biology Department , university of Badji Mokhtar, Annaba, Algeria