Drug-Initiated Synthesis of Cladribine-Based Polymer Prodrug Nanoparticles: Biological Evaluation and Structure Activity Relationships

International audienceBy using two reversible deactivation radical polymerization techniques, either nitroxide-mediated polymerization or reversible addition-fragmentation chain transfer polymerization, the "drug-initiated" approach was applied to cladribine (CdA) as an anticancer drug to synthesize small libraries of well-defined and self-stabilized CdA-based polymer prodrug nanoparticles, differing from the nature and the molar mass of the grown polymer, and the nature of the linker between CdA and the polymer, thus allowing structure-cytotoxicity relationships to be determined. Their biological evaluation was investigated in vitro on L1210 cancer cells. The preparation of fluorescent CdA-based nanoparticles with excellent imaging ability was also reported by applying the "drug-initiated" approach to an aggregation-induced emission-active dye

Distribution of phenolic compounds within seed and seedlings of two Vicia faba cvs differing in their seed tannin content, and study of their seed and root phenolic exudations

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Composition and antimicrobial activity of the essential oil from Algerian Warionia saharae Benth. & Hook.

International audienceThe essential oil of aerial parts of Warionia saharae was obtained by hydrodistillation and analyzed by gas chromatography/flame ionization detector (GC/FID), GC/mass spectrometry (GC/MS) and 13C nuclear magnetic resonance (NMR). In total, forty-three constituents, mainly oxygenated mono- and sesquiterpenes, were identified representing 89.2% of the total oil. Sixteen samples of essential oil of W. saharae collected in three locations exhibited similar chemical compositions showing a chemical homogeneity. The essential oil showed poor antifungal activity against filamentous fungi, Alternaria alternata, Cladosporium herbarum, Fusarium oxysporum and Aspergillus flavus with minimum inhibitory concentration (MIC) values between 4 and 8 μL/mL

Antimicrobial Activity of Ammodaucus leucotrichus Fruit Oil from Algerian Sahara

International audienceThree fruit oil samples of Ammodaucus leucotrichus Cosson & Durieu from Algerian Sahara were obtained by hydrodistillation and analyzed by GC(RI), GC-MS and 13C NMR spectroscopy. The main compounds were perillaldehyde (87.0-87.9%) and limonene (7.4-8.2%). The antimicrobial effect of the essential oil was evaluated against bacteria, yeasts and filamentous fungi. High antibacterial activity was observed against Escherichia coli, Staphylococcus aureus, Enterobacter cloaceae, Bacillus cereus and Salmonella typhimurium, with MIC values between 0.5-1.0 μL/mL. Fungal strains were also sensitive to the essential oil (MIC values: 0.25-0.75 μL/mL).The most potent activity was observed against the filamentous fungi, Fusarium oxysporum and Aspergillus flavus (0.25-0.50 μL/mL)

GC/MS analysis, and antioxidant and antimicrobial activities of alkaloids extracted by polar and apolar solvents from the stems of Anabasis articulata

Anabasis articulata is a plant widely used in popular medicine to treat several pathologies in Algerian Sahara, such as diabetes. It is also associated with two other plants to cure certain types of cancer. Few research studies have been conducted on phytochemical analysis and in vivo biological activities of this species. However, no report is available on chemical elucidation of alkaloids and their antioxidant and antimicrobial properties. This study aims to characterise alkaloids in A. articulata stems and to evaluate their antioxidant and antimicrobial effects. Alkaloids extraction was carried out using polar (E1; E2.1; E2.2) and apolar solvents (E3), while chemical characterisation was performed by GC/MS. In vitro antioxidant activity was assessed by tree tests: total antioxidant capacity (TAC), DPPH scavenging assay and β-carotene–linoleate inhibition. For antimicrobial activity, eight different microorganisms were tested. The results suggest that E2.2 extract had the highest TAC value (14.742 ± 0.224 mg AAE/g DM), but E3 extract presented the highest DPPH scavenging activity (EC50 = 1.242 ± 0.168 mg/mL) and a strong β-carotene–linoleate inhibition (EC50 = 0.943 ± 0.027 mg/mL). In addition, E3 extract had the strongest inhibitory effects against all tested microorganisms and produced inhibition zones ranging between 9 and 20 mm, while the MICs of this extract ranged from 0.781 to >100 mg/mL and the MBCs ranged between 1.562 and >100 mg/mL. Forty-nine compounds belonging to 16 families, namely cyclopeptide alkaloids, steroid alkaloids, quinoline alkaloids, camptothecin alkaloids, quinazoline alkaloids, quinazoline alkaloids, isoquinoline alkaloids, isoquinolone alkaloids, indole alkaloids, terpene indole alkaloids, pyridine/pyrrolidine alkaloids, piperidine alkaloids, pyrrolizidine alkaloids, purine alkaloids, acridone alkaloids, benzazonine alkaloids and homolycorine-type Amaryllidaceae alkaloids were identified. Therefore, A. articulata can be considered as a source of antioxidant and antimicrobial agents

Fatty acid composition and antioxidant activity of Pistacia lentiscus L. fruit fatty oil from Algeria

The current study was carried out to investigate the chemical composition of Pistacia lentiscus fruit fatty oil by HPLC–DAD and GC analysis. The quantification of phenolic content and DPPH radical scavenging capacity of this oil were furthermore evaluated. The results showed that the oil has the highest phenolic content (810 mg GAE/kg oil). The capacity to scavenge DPPH radical was admissible (EC50 = 20.619 ± 0.312 mg/mL), compared to the butylated hydroxyanisole (BHA) (0.012 ± 0.0001 mg/mL). The main fatty acids where oleic, palmitic, linoleic, palmitoleic and stearic acids which have specific carbon number and their values in percentage are C18:1 n-9 (50.02 ± 0.55%), C16:0 (24.83 ± 1.25%), C18:2 n-6 (17.24 ± 0.10%), C16:1 n-7(1.55 ± 0.09%) and C18:0 (1.08 ± 0.02%), respectively. The analyses showed concentrations of approximately 26% of saturated fatty acids, 52% of monounsaturated and 18% of polyunsaturated

Valorization of Algerian Saffron: Stigmas and Flowers as Source of Bioactive Compounds

Purpose: Saffron is widely used for its medicinal and culinary properties. Its stigmas are the most expensive part comparing with the flowers that are discarded during production. For that, the objective of this work was to determine the phytocomplex of stigma and flower material (except stigma) of saffron from Algeria. Crocin, picrocrocin and safranal contents were quantified to classify its quality according to ISO/TS 3632 standards. The antioxidant and antimicrobial properties of extracts were also investigated. Methods: Crocins, total phenolic content, flavonoids, phenolic acids, and anthocyanins were detected and quantified by HPLC-DAD and spectrophotometric analyses. The antioxidant potential was evaluated by 4 in vitro assays. The antimicrobial activity against seven bacteria and two strains of Candida albicans was also evaluated. Results: The results revealed that the chromatographic analysis showed the presence of 20 phenolic acids and flavonoids in the plant samples, with the highest concentrations in stigmas. Crocin derivatives were found only in stigmas, except that trans-crocetin (β-D-gentiobiosyl) which was present also in flower material. The highest total phenolic, total flavonoid and total flavonol contents were observed in stigmas and the highest level of anthocyanins and hydrolysable and condensed tannins in flowers. This extract showed a stronger protection effect from β-carotene bleaching and a higher TAC. The both extracts had some antimicrobial effect. Conclusions: These results point out that flower material could be considered as natural bioresource of polyphenolic compounds, with higher biological activities which remain to be exploited. Graphic Abstract: [Figure not available: see fulltext.