Search

Celecoxib (CEL) serves as a selective inhibitor of cyclooxygenase-2 (COX-2) used for treating conditions like rheumatoid arthritis, osteoarthritis, acute pain, and inflammation. However, its limited solubility and slow dissolution significantly restrict its wider application. This research focused on exploring eutectic mixture of celecoxib with maleic acid to enhance physico-chemical properties of the anti-inflammatory agent. The binary mixtures of celecoxib-maleic acid were prepared over the entire composition range, using the liquid-assisted grinding technique and characterized through various analysis, including differential scanning calorimetry, powder X-ray diffraction, Fourier-transform infrared spectroscopy and scanning electron microscopy. In the DSC thermograms of the binary mixtures, a eutectic reaction was observed at 108.46°C. The analysis of the phase diagram of CXB-MA binary mixtures indicated a eutectic composition at approximately 0.35 molar fraction of celecoxib. Additionally, PXRD, FTIR provided the confirmation of the eutectic mixture formation, indicated the absence of molecular interactions in the solid state. [ABSTRACT FROM AUTHOR]

The Algerian steppes face ecological imbalances due to overgrazing, cereal cultivation, and resource pressure. In response, the government implemented the "Great Works for the Development of Steppe Pastures" program in 1994, planting the nonnative Atriplex canescens, a shrub resistant to cold, drought, and salinity. However, introducing exotic plants can harm native biodiversity through allelopathy interaction. This work aims to test the allelopathic potentiel of A. canescens on the most representative North African steppe plant Macrochloa Tenacissima. Phytochemical tests are performed on the aerial parts of these two plants. Aqueous extracts are prepared from the aerial parts of A. canescens with three concentrations respectively T0 (0%), T1 (2.5%) and T2 (5%), and are applied in situ for 45 days on M. tenacissima plants. The response of M. tenacissima to the extract of A. canescens is monitored by measuring chlorophyll and proline in the fresh leaves of the target plant M. tenacissima. The results showed the presence of allopathic molecules in the aerial parts of both plants, notably Alkaloide, flavoniode, tannins, triterpnoide, Quinon and phenolic acid. The response of M. tenacissima to the application of A. canescens extract caused during the trial remarkable change in the total chlorophyll content of M. tenacissima, with reductions of 1 to 4 (mg/g FM) observed at the end of 45 days of application. The highest decrease is observed for treatment T3. After 45 days of treatment with A. canescens extract aqueous, M. tenacissima showed the highest proline accumulation 2.6 (mmol/g MF) for the treatment T3. Our findings show that A. canescens can induce physiological disruptions in M. tenacissima. [ABSTRACT FROM AUTHOR]

Cocrystallization drug/coformer and drug/drug stands as a promising method to enhance the physicochemical properties and to improve the antibacterial activity of active pharmaceutical ingredients (API). In this study the combinations metronidazole/maleic acid and metronidazole/paracetamol were prepared in the molar ratio of 1:1 via the liquidassisted grinding technique and characterized by differential scanning calorimetry (DSC), powder X-ray diffraction and scanning electron microscopy. The thermal analysis revealed the existence of an endothermic peak at the temperature of 144.93°C for the combination MTZ-MA and 130.5°C for the binary mixture MTZ-PCA. The PXRD showed the apparition of new peaks which demonstrate the formation of a novel crystalline phase. The SEM microscopy supported the results obtained through DSC and PXRD analysis. The antibacterial activity of the two combinations drug/coformer and drug/drug and the pure antibacterial agent was evaluated against aerobic and anaerobic bacterial strains. As a result, the two combinations displayed a synergistic effect. This phenomenon yields a significantly stronger therapeutic impact compared to the effect expected for the parent component. [ABSTRACT FROM AUTHOR]

The present study aimed to evaluate the antibacterial activity of the metronidazole cocrystal, an antibiotic widely used in the treatment of infectious diseases caused by anaerobic bacteria. The cocrystal was prepared by mixing metronidazole (MNZ) and nicotinamide (NIC) in a 1:1 molar ratio, using an environmentally friendly mechanical process based on liquid assisted grinding method. The MNZ-NIC cocrystal was then characterized by differential scanning calorimetry (DSC), powder X-ray diffraction and scanning electron microscopy (SEM) and tested against four aerobic and anaerobic bacterial strains: Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae and Staphylococcus aureus. The thermal analysis of MNZ-NIC cocrystal showed a single endothermic peak at 110 °C identified as the cocrystal's melting point. The SEM microscopy revealed a distinct morphology compared to the individual compound. A comparative analysis of antibacterial efficacy was conducted on MNZ drug and its cocrystal. The results demonstrated that the cocrystal displayed superior antibacterial effectiveness against Gram-negative bacteria. [ABSTRACT FROM AUTHOR]

The greatest weed management challenge is the lack of effective natural products based herbicides. Allelochemicals of plant origin can substitute synthetic chemicals as nature's own herbicide. The use of allelopathic properties of native planVcrop species offers promising opportunities for this purpose. In this study Retama raetam invasive Mediterranean plant species is selected, to test its allelopathic potential on the germination of seeds and the growth of weed seedlings of Avena sterilis, Bromus secalinus and on the wheat Triticum durum (SIMETO variety). The chemical characterization of aerial the part ofR. raetam reveals that it contains Allelochemicals compounds of flavonoids, triterpenes, alkaloids and tannins groups. Four concentration 5% (Dl), 10% (D2), 15% (D3) and control 0% (DO) of aqueous extracts of the aerial part ofR. raetam were applied in A. sterilis, B. secalinus and T durum through germination and growth bioassays in a climate-controlled incubator at a temperature 25°C. The application of these treatments revealed significant differences on the measured parameters. They showed that the germination inhibition of the two weeds increases with the increase of the concentration of aqueous extracts of R. raetam. For the two weeds, the inhibiting effect on germination is 100% with treatment D3 (15%). According to the applied concentration wheat stem length varies between 0.46 and 4.67 cm, its radicle length fluctuate between 0.09-2.41cm. The inhibition of the growth seedlings, especially on the roots ofB. secalinus weed is complete (0 cm) whatever the applied concentration of R. raetam aqueous extract. Inhibition of stem growth is noticeable in A. sterilis with treatment D3 (15%). The seedling vigor index is increasing with the decrease of concentration of aqueous extract of R. raetam. Results of this study are relatively promising in the field of biological weed control using R. raetam metabolites. [ABSTRACT FROM AUTHOR]