Anti-inflammatory and healing effect of leaf-flower mixture extract of Cytisus triflorus L

Objective: The present study aims to study the anti-inflammatory and healing effects of the crude leaf and flower mixture extract of Cytisus triflorus L., known in Algeria as Igoulli. Methodology and results: The method consists of studying the anti-inflammatory effect by measuring the diameter of edema of the paw of rats that received carrageenan. In addition, 2 cm diameter circular incision wounds were made in rats to evaluate the healing activity of the crude leaf and flower mixture extract of Cytisus triflorus L. at doses of 200 mg/kg and 400 mg/kg. The anti-inflammatory effect of C. triflorus showed that E.Br at the dose 400 mg has the higher activity, which induces a significant decrease in the thickness of the rat paw from the second hour, its effects being similar to those of Diclofenac. The percentages of inhibition of edema at 4 h and 6 h are 80.05 and 88.56% for E.Br and Diclofenac respectively. With respect to healing activity, the results show that after 18 days, complete healing was achieved with almost two concentrations of crude C. triflorus, tissue remodeling and reoccurrence of hair was observed at level of scars. Conclusion: The results of the study show that the leaf extract and flower extract of Cytisus triflorus L. has healing and anti-inflammatory properties that could justify the use of this plant in traditional medicine against inflammatory diseases. Keywords: Cytisus triflorus, anti-inflammatory, healing activity

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

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

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

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

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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Effect of Thymoquinone as Prophylactic Treatment Against CCl4-Induced Hepatotoxicity on Antioxidants Status

Objective: The present study aims to study the effect of thymoquinone as prophylactic treatment against CCl4-induced hepatotoxicity on antioxidants status. Methodology: Hepatotoxicity was induced in rats by intraperitoneal administration of 3 ml/kg, 1:1 (V/V) mixture of CCl4 and olive oil after treatment for 7 days with TQ, using two doses. The method consists of studying the antioxidant effect of thymoquinone pretreatment by measuring superoxide dismutase (SOD) and catalase (CAT) activities, with reduced glutathione level in both plasma and liver homogenate. Results: The results revealed that hepatotoxicity is accompanied by significant decrease (p ≤ 0.01) of SOD and CAT activities with GSH level, in both plasma and liver homogenate. While prophylactic treatment using TQ at doses of 02.5 and 05 mg/kg increase significantly the status of the antioxidants, as dose dependent manner, in both plasma and liver homogenate.  Conclusion: The results of this study show that thymoquinone has an antioxidant effect when it used as prophylactic treatment against CCl4-induced hepatotoxicity. Keywords: Thymoquinone, hepatotoxicity, CCl4, prophylactic and antioxidant