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

Total Phenolic Contents and Antioxidant Capacity of Aqueous Extract from Pituranthos scoparius (Coss. & Dur.) Growing in Algeria

This study aims to estimate the total phenolics, flavonoids and tannins contents then to investigate both in vitro antioxidant capacity models of aqueous extract (AqE) from the stems of Pituranthos scoparius, growing in Algeria. Total polyphenol contents were determined using Folin Ciocalteu's reagent; flavonoids were quantified employing the AlCl3 and method tannins using haemoglobin precipitation test. The in vitro antioxidant property was assessed by DPPH-scavenging radical and lipid peroxidation assays. The results revealed that aqueous extract presented a high total phenolic and tannins contents with values of 150.89 ± 0.68 mg GAE (gallic acid equivalent)/g and 71.24 ± 0.09 mg TAE (tannic acid equivalent)/g dry extract, respectively. This extract show an essential effect toward DPPH-scavenging assay and lipid peroxidation inhibition with 96.19 ± 0.00 µg/mL, 91.53 ± 0.98 %, respectively. This study indicates that the aqueous extract from Pituranthos sciparius has potent antioxidant effects and may prove to be of latent health benefit as well as supplementary sources for natural antioxidants drugs. Keywords: Pituranthos scoparius, aqueous extract, antioxidant activity, phenolic compounds

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

In Silico, in Vitro and in vivo Ecotoxicology and Biodegradability Evaluations of Bioactive Schiff Base Ligand

Bioactive Schiff base ligand, 2-[(1E)-N-{2-[(2-{(Z)-[1-(2 hydroxyphenyl)ethylidene]amino} ethyl)amino]ethyl}ethanimidoyl]phenol was selected for in silico, in vitro and in vivo ecotoxicological and biodegradability studies. In vivo and in vitro ecotoxicological evaluations were estimated by the use of snails (Eobania vermiculata) and microorganisms’ bacteria and fungus respectively. In silico ecotoxicological and biodegradability predictions were carried out online computer software programs such as Pro Tox, Pred-skin, Endocrine Disruptor Knowledge Base (EDKB) and UM-BBD. The obtained results from in vivo bioassays showed moderate toxicity of the ligand at the high concentration (1000 µg/mL) with mortality percent value of 35%. For in vitro evaluations, results showed negative effect against bacteria and fungus. In silico predictions, results showed low toxicity with high LD50 of 4340 mg/kg, no toxic targets and low probability to bind with the majority of endocrine receptors with docking ranging between -7.4 and -8.9. In addition, the results from Human skin sensitization and Murine local lymph node assay indicate sensitizer effect of the ligand. For biodegradability prediction, the results indicate the ability of microorganism to degrade the ligand with no-toxic resultant products. We conclude the possibility to using the ligand without risks from environment and human health.                      

Fractionation, Phytochemical Screening and Free Radical Scavenging Capacity of Different Sub-Fractions from Pituranthos scoparius Roots

The purpose of this study was to prepare three sub-fractions from Pituranthos scoparius roots (PSR), characterize their phytochemicals contents and to investigate their free radical scavenging activity by 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) and hydroxyl scavenging activities. Tannins, flavonoids, steroids, and other bioactive compounds were found in the different sub-fractions. The Ethyle acetate extract (EAE) and chloroform extract (ChE) exhibited the highest antioxidant activity using ABTS (17.8 ± 0.87 µg/mL and 18.15 ± 0.68 µg/mL), respectively. Whereas, Crude extract (CrE) have been presented strong hydroxyl scavenging activity (14.9 ± 0.8 µg/mL). This study indicates that PSR extracts has potent free radical scavenging, and may prove to be of potential health benefit as well as additional resources for natural antioxidants. Keywords: Medicinal plant; phytochemical screening; sub-fractions, free radical scavenging

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

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

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