ABSTRACT
Objectives: Lichens are complex symbiotic organisms that generate various bioactive compounds with significant therapeutic value. We investigated the chemical composition and bioactivity of the acetone extract of the Algerian lichen Physconia venusta (Ach.) poet. Materials and Methods: Phytochemical screening was performed using gas chromatography-mass spectrometry (GC-MS). The antibacterial activity was assessed against Escherichia coli, Pseudomonas aeruginosa, Salmonella enteritidis, Salmonella typhi, Staphylococcus aureus, Listeria monocytogenes, and Bacillus subtilis using an agar diffusion test with the determination of the minimal inhibition concentration (MIC), while the antioxidant activity was determined using different chemical methods (DPPH, ABTS, CUPRAC, reducing power, superoxide anion scavenging, ß-carotene bleaching, and metal chelate). In addition, cytotoxic activity was tested using Artemia salina (Brine shrimp) bioassay. Results: The studied extract exhibited intense antibacterial activity against E. coli and S. aureus with inhibition diameters of 28 ± 0.01 and 22 ± 0.01 mm, respectively, with a MIC value of 6.25 mg/mL and a selectivity index of 2.8. The obtained extract showed different antioxidant trends depending on the selected assay. GC-MS analysis revealed many secondary metabolites. Conclusion: P. venusta, a type of lichen, is a potential source of bioactive substances that could be used in pharmaceuticals.
ABSTRACT
AIM AND OBJECTIVE: The excessive consumption of alcohol and the installation of dependence is, in most cases, facilitated by favorable psychological factors that trigger and maintain the behavior of consumers. Examples more frequently encountered in individuals having difficulty with alcohol are, in particular: one or more anxiety disorders, deficits in the capacities to manage stress and anxiety. The main objective of this work was to study in vivo the anti-addiction effect and hepatotoxicity of tow baclofen analogues complexed with ß-Cyclodextrin (ßCD) on an alcohol-dependent rat model. MATERIALS AND METHODS: The synthesis of two analogues, ABF1 and ABF2, close to baclofen was reported. The structural determination of the two compounds was confirmed by NMR and IR analysis. The complexation of analogues with ß-Cyclodextrin (ßCD) was performed in water at room temperature (25 °C). The interactions of ABF with ß-Cyclodextrin, and the stability constant (Ka) of the inclusion complex formed between them were investigated by using UV-visible spectroscopy. The biological effects of baclofen and the two analogues on alcohol dependence were studied in wistar rats. The anti-addiction effect of the analogues was tested by measuring the alcohol intake and the variation of the animal behaviour. The toxicity of the compounds was also analysed on liver injury markers. RESULTS: The amino-3-phenylbutanoic acid (ABF1) and 3,4,5-trihydroxy-N-(methyl-2-acetate) benzamide (ABF2) were synthesized. The complexation of both analogues of baclofen (BF) with ß-cyclodextrin (ßCD) (ABF- ßCD) was realized and confirmed by the stability constant of the inclusion complex (Ka) and Job's method. The evaluation of anti-addiction activity in vivo showed that ABF1-ßCD inhibits the consumption of alcohol at doses equivalent to those of baclofen. Both baclofen analogues have shown an anxiolytic effect. Regarding the toxicity of the two compounds, our results showed that ABF1-ßCD has less toxic effect than baclofen; it reduces the activity of ALT and AST enzymes. Histologically, ABF1-ßCD has no effect on the liver structure and has a protective effect against lesions alcohol-induced liver disease. CONCLUSION: Therefore, it can be suggested that ABF1 analogue combined with ß-Cyclodextrin can be used as a treatment for alcohol dependence. Further clinical works are needed to confirm its effectiveness.
