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26 result(s) for "Metouekel, Amira"
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Efficacy of various extracting solvents on phytochemical composition, and biological properties of Mentha longifolia L. leaf extracts
The current work attempts to explore the influence of three extraction solvents on phytochemical composition, content of polyphenols, antioxidant potential, and antibacterial capacity of hydroethanolic, acetonic, and aqueous extracts from Moroccan Mentha longifolia leaves. To achieve this goal, the chemical composition was identified using an HPLC–DAD examination. The contents of polyphenols were assessed, while the total antioxidant capacity (TAC), the DPPH test, and the reducing power test (RP) were utilized to determine antioxidant capacity. To assess the antibacterial activity, the microdilution technique was carried out to calculate the minimum inhibitory (MIC) and minimum bactericidal concentrations (MBC) of extracts against four nosocomial bacteria ( Bacillus cereus , Pseudomonas aeruginosa , Escherichia coli , S taphylococcus aureus ). Additionally, the antibacterial and antioxidant activities of all tested extracts were examined in silico against the proteins NADPH oxidase and Bacillus cereus phospholipase C. Study reveals that M. longifolia extracts contain high phenolic and flavonoids. Additionally, the hydroethanolic extract contained the highest amounts of phenolic and flavonoid content, with values of 23.52 ± 0.14 mg Gallic acid equivalent/g dry weight and 17.62 ± 0.36 mg Quercetin Equivalent/g dry weight, respectively compared to the other two extracts. The same extract showed the best antioxidant capacity (IC 50  = 39 µg/mL ± 0.00), and the higher RP (EC 50 of 0.261 ± 0.00 mg/mL), compared to the acetonic and aqueous extract regarding these tests. Furthermore, the hydroethanolic and acetonic extracts expressed the highest TAC (74.40 ± 1.34, and 52.40 ± 0.20 mg EAA/g DW respectively), compared with the aqueous extract. Regarding antibacterial activity, the MIC value ranges between 1.17 and 12.50 mg/mL. The in-silico results showed that the antibacterial activity of all extracts is principally attributed to kaempferol and ferulic acid, while antioxidant capacity is attributed to ferulic acid.
Fabrication and evaluation of solidified nanoemulsion designs for systemic delivery of atorvastatin through the lung
To improve the solubility of atorvastatin and overcome the stability issues of liquid nanoemulsion, the current study aimed to synthesize solidified SNEDDS particles with aerodynamic diameter of ≤ 3 μm. The simple and chitosan-decorated liquid SNEDDS were dried by spray drying method and evaluated for their physicochemical properties, release characteristics and aerodynamic performance. A single dose pharmacokinetic study was performed in rabbits to establish the therapeutic performance of solidified nanoemulsion with respect to LIPITOR. The liquid SNEDDS were efficiently dried with pectin (1% w/w). The chitosan decorated solidified SNEDDS (SF10) have small particle size (2.02 μm), higher tapped density (0.733 g/cm 3 ) and smooth surface as compared to uncoated solidified SNEDDS (SF8). The chitosan coated SNEDDS had higher drug content and significantly lower roughness than uncoated SNEDDS (student t-test; p  ≤ 0.01). The uncoated SNEDDS exhibited significantly higher burst drug release as compared to the chitosan coated SNEDDS due to the porous structure, amorphous nature and small size of its associated nanoemulsion. The solidified nanoemulsion had relatively lower MMAD (1.0 to 1.5 μm) that supports higher FPF values of 45–54% for the uncoated SNEDDS and chitosan coated SNEDDS, respectively. The pharmacokinetic study revealed that the solidified SNEDDS are superior with respect to its bioavailability being 1.5 times higher than LIPITOR.
Solanum elaeagnifolium Var. Obtusifolium (Dunal) Dunal: Antioxidant, Antibacterial, and Antifungal Activities of Polyphenol-Rich Extracts Chemically Characterized by Use of In Vitro and In Silico Approaches
The present work was designed to study the chemical composition and the antioxidant and antimicrobial properties of fruits (SFr) and leaf (SF) extracts from Solanum elaeagnifolium var. obtusifolium (Dunal) Dunal (S. elaeagnifolium). The chemical composition was determined using HPLC-DAD analysis. Colorimetric methods were used to determine polyphenols and flavonoids. Antioxidant capacity was assessed with DPPH, TAC, and FRAP assays. Antimicrobial activity was assessed using disk diffusion and microdilution assays against two Gram (+) bacteria (Staphylococcus aureus ATCC-6633 and Bacillus subtilis DSM-6333) and two Gram (-) bacteria (Escherichia coli K-12 and Proteus mirabilis ATCC-29906), while the antifungal effect was tested vs. Candida albicans ATCC-1023. By use of in silico studies, the antioxidant and antimicrobial properties of the studied extracts were also investigated. HPLC analysis showed that both fruits and leaf extracts from S. elaeagnifolium were rich in luteolin, quercetin, gallic acid, and naringenin. Both SFr and SF generated good antioxidant activity, with IC50 values of 35.15 ± 6.09 μg/mL and 132.46 ± 11.73 μg/mL, respectively. The EC50 of SFr and SF was 35.15 ± 6.09 μg/mL and 132.46 ± 11.73 μg/mL, respectively. SFr and SF also showed a good total antioxidant capacity of 939.66 ± 5.01 μg AAE/and 890.1 ± 7.76 μg AAE/g, respectively. SFr had important antibacterial activity vs. all tested strains—most notably B. subtilis DSM-6333 and E. coli, with MICs values of 2.5 ± 0.00 mg/mL and 2.50 ± 0.00 mg/mL, respectively. SFr demonstrated potent antifungal activity against C. albicans, with an inhibition diameter of 9.00 ± 0.50 mm and an MIC of 0.31 ± 0.00 mg/mL. The in silico approach showed that all compounds detected in SFr and SF had high activity (between −5.368 and 8.416 kcal/mol) against the receptors studied, including NADPH oxidase, human acetylcholinesterase, and beta-ketoacyl-[acyl carrier protein] synthase.
Characterization and safety evaluation of highly swellable polymeric nanomatrices for enhanced solubility of acyclovir
Solubility is one of the most important factors for therapeutic agents to show significant pharmacological response. Drugs that suffer from poor aqueous solubility are not absorbed in significant concentrations and hence their bioavailability is compromised and effectiveness of the drug is disrupted. In order to achieve the maximum absorption and significant bioavailability, solubility of the drug has to be enhanced. For this purpose, nanomatrices were formulated by free radical polymerization technique in order to enhance the solubility of acyclovir. The formulated nanomatrices were structurally characterized by Fourier Transform Infrared Spectroscopy (FTIR), Scanning Electron Microscopy (SEM), Powder X-ray Diffraction (PXRD) and Particle Size Analysis. For in-vitro characterization, sol-gel fraction, swelling, in-vitro drug release and solubility studies of the formulated nanomatrices were carried out. Toxicity study was also performed in rabbits in order to access the biocompatibility of the formulated system with biological systems. According to FTIR spectroscopy, the unloaded and drug loaded nanomatrices were having specific functional groups of the individual components. According to SEM, the formulated nanomatrices were feasible for efficient loading of the drug while PXRD confirmed amorphous nature of the formulated nanomatrices. Average particle size of the formulated nanomatrices was 282.4 ± 09.43 nm, confirming the nano-sized particles. According to swelling and drug release studies, it was observed that nanomatrices showed pH responsiveness and showed enhanced swelling and drug release in pH 6.8 as compared to pH 1.2. The optimized formulation showed a significant increase in the solubility of the drug as compared to the drug alone while toxicity study confirmed the biocompatibility of the system with the biological systems. Statistical analysis was also applied to determine the level of significance.
Formulation of pH responsive polymeric hydrogels for prolonged delivery of famciclovir with biosafety evaluation
Recent study aimed to fabricate pH responsive, intelligent, Pluronic F127 based polymeric system for controlled delivery of Famciclovir. Nine formulations were developed through free radical polymerization. Polymeric system exhibited pH dependent swelling by showing higher degree of swelling in simulated intestinal fluid of pH 7.4 while negligible swelling in simulated gastric fluid of pH 1.2. Drug loading increased with increase in percent water content. Famciclovir loading percent was found in range of 60.892% to 73.741%. In FTIR spectra, characteristic peaks were achieved confirming the successful grafting of drug in polymeric system. PXRD results demonstrated the conversion of crystalline nature of Famciclovir into an amorphous one in the loaded hydrogel. SEM confirmed the porous nature of hydrogel. Famciclovir loaded hydrogel showed superior thermal behavior as compared to the drug alone. In vitro Famciclovir release studies unveiled small quantity of drug release in simulated gastric fluid (25.55–34.89%) while maximal release in simulated intestinal fluid (90.12–99.13%) for 36 h was documented thereby confirming pH regulated release. Application of DD solver revealed that PLMA hydrogels followed zero order while First order was being followed by Famciclovir marketed tablet. No toxicity signs were observed in rabbits establishing the biosafety of system. Hence, the results suggest that Pluronic based polymeric system can act as promising carrier for controlled, site specific delivery of Famciclovir in intestine for prolonged period thereby reducing its dosing frequency and minimizing gastric side effects for treating Herpes and Varicella zoster infections.
Cheminformatics-aided discovery of potential allosteric site modulators of ubiquitin-specific protease 7
Ubiquitin-specific peptidase 7 (USP7) is a deubiquitinating enzyme that mediates the stability and activity of numerous proteins. At basal expression levels, USP7 stabilizes p53 protein, even in the presence of excess MDM2. However, its overexpression leads to the deubiquitination of MDM2 at a rate faster than p53, leading to p53 degradation and pro-tumorigenic roles. Consequently, it is an attractive target for anticancer drug discovery via the modulation of its allosteric site from which the protein is activated. In this study, molecular modeling techniques and cheminformatics approaches were employed to unravel the potential of eighty compounds to serve as its allosteric site modulators. The compounds were initially subjected to virtual screening. Subsequently, the binding free energies of the top four compounds with the highest binding affinities were calculated, and their drug-likeness, and pharmacokinetic and toxicity profiles were evaluated. Ultimately, the complexes of the protein and hit compounds were subjected to a 100 nanoseconds (ns) molecular dynamics simulation. The results of the study revealed eight compounds from the compound library with docking scores ranging from − 7.491 to -11.43 kcal/mol, compared to P217564, which exhibited a docking score of -5.671 kcal/mol. The top four compounds with the highest affinities possessed drug-like properties, and good pharmacokinetic and toxicity profiles, and their predicted inhibitory potentials showed they will be effective at minimal concentration. Also, molecular dynamics simulation confirmed the stability of the protein-ligand complexes. Conclusively, the compounds identified in this study are worthy of further evaluation for the development of allosteric site modulators of USP7.
Pharmaceutical properties and phytochemical characterization of Juniperus thurifera degraded species in high mountains
This study evaluates the antioxidant and antimicrobial activities of HPLC-characterized extracts from Juniperus thurifera (L.) leaf extract (ELJT), bark extract (EBJT), and fruit extract (ESJT). The HPLC analysis of the hydroethanol extract of EBJT identified several key constituents, notably urocanic acid. In terms of antioxidant potential, the DPPH assay showed that both the EBJT and ESJT extracts had significant free radical scavenging activity. The IC 50 values for EBJT and ESJT were 43 µg/mL and 77 µg/mL, respectively. These values indicate that EBJT has a stronger capacity to neutralize free radicals compared to ESJT. For comparison, the positive control (BHT) showed a significantly lower IC 50 , underscoring the fact that while the extracts exhibit antioxidant activity, their effectiveness is still relatively weaker than that of BHT. In the FRAP assay, the EC 50 values for EBJT and ESJT were 256 µg/mL and 261 µg/mL, respectively, indicating similar antioxidant efficacy between the two extracts. Again, both extracts show antioxidant potential, but still fall short of the control’s activity. The extracts exhibited significant antibacterial activity against S. aureus , E. coli , B. subtilis , and P. mirabilis , with ELJT displaying the strongest effect, characterized by large inhibition zones and low MIC values. This highlights the superior antibacterial potential of the leaf extract compared to the bark and fruit extracts. Regarding antifungal activity, EBJT demonstrated notable efficacy against A. niger , A. flavus , and F. oxysporum , with substantial inhibition zones and relatively low MIC values. Against C. albicans , all extracts showed significant inhibition, with EBJT exhibiting the highest inhibition zone (29.5 mm) and a MIC of 65.29 µL/mL. The J. thurifera extracts, especially ELJT, show promising antioxidant and antimicrobial activities, though less effective than positive controls. Despite this, they remain valuable sources of bioactive compounds for further study and potential applications.
Genetic characterization and phylogenetic analysis of common house crows (Corvus splendens)
The Common House Crow ( Corvus splendens ) exhibits remarkable ecological adaptability, enabling its rapid expansion across continents. However, despite its wide distribution, there is a need for genetic studies to clarify its evolutionary history and population structure. This research employs DNA barcoding, focusing on the mitochondrial gene cytochrome oxidase subunit I ( Cox1 ), which is effective for species identification and phylogenetic analysis. Blood samples were collected from 70 C. splendens specimens across seven cities in Punjab, Pakistan: Lahore, Kasur, Sialkot, Narowal, Pakpattan, Gujranwala, and Bahawalpur. Genomic DNA extraction was performed, and a partial sequence of the COX1 gene was amplified using PCR techniques. Sequencing of the Cox1 marker from 10 randomly selected specimens revealed nine distinct genetic variants. Interspecific analysis positioned our C. splendens sequences alongside various Corvus species available in GenBank, while intraspecific analysis identified a total of 15 genetic variants. These variants showed nucleotide identity rates ranging from 98.7 to 99.8%, with genetic distances between 0.002 and 0.013. The analysis indicated that the C. splendens group consists of a single heterogeneous clade with variants from multiple countries, including Pakistan, Tanzania, Nepal, South Africa, Malaysia, Sri Lanka, Bangladesh, Kenya, Australia, and Singapore. This study significantly enhances our understanding of genetic diversity and evolutionary relationships within C. splendens populations, highlighting the necessity of genetic research to inform conservation strategies. Further research employing advanced molecular techniques and broader geographic sampling is essential to assess the genetic diversity and population dynamics of this adaptable species.
Fabrication and in vitro evaluation of pH/thermo dual responsive hydrogels as controlled ibuprofen sodium in situ depot
Ibuprofen sodium (IBP) is a commonly used NSAID for multiple pain conditions. However, despite its extensive use, it is associated with multiple GIT adverse effects after oral administration. In the present study, we have fabricated thermoresponsive gel depot using Poly (N-vinylcaprolactam) and sodium alginate as polymers. The designed formulations are intended to be used as IBP depot after being administered subcutaneously. The sol-gel phase transition temperature and gelation time of gel samples were optimized by tube inversion, rheological exploration and optical transmittances. Temperature sweep experiments confirmed that optimized gel samples have sol-gel transition between 32°C and 37°C. Swelling and in vitro drug release displayed that optimized gels have maximum swelling and IBP release at pH 7.4 and at 35°C confirming their pH/thermo sensitivity. The degradation profile of hydrogels displayed controlled degradation for 6 days that with increasing contents. MTT assay showed L929 cells displayed more than 90% cell viability against blank and IBP-loaded PNVCL/NaAlg hydrogels at optimized concentrations. Fourier transform infrared spectroscopy confirmed the polymer blend hydrogels structure formation. Thermogravimetric analysis confirmed the presence of thermoresponsive moieties and thermal stability of polymer blend hydrogel sample. While scanning electron microscopy showed that hydrogel has channels in structure that might facilitate the diffusion of solvent. Results concluded that PNVCL/NaAlg hydrogels can be utilized as IBP sustained depot following subcutaneous application invivo and GIT adverse effects could be avoided associated with its oral administration.
Influence of the seasons on the chemical composition and biological properties of pistacia lentiscus L. essential oil in the mediterranean region
Medicinal plants are effective in treating many infections. Pistacia lentiscus L., whose oil is recognized for its biological properties, is attracting growing interest in medical research. These biological properties are due to their chemical composition (CC), which various conditions, like climate, can affect. P. lentiscus EOs biological properties from December, May, and August were investigated in vitro; gas chromatography-mass spectrometry (GC-MS) helped analyse their CC. Autodock Vina was used for molecular docking and SwissADME was used for ADMET analysis. The Eos of P. lentiscus leaves collected in December showed a remarkable presence of β-caryophyllene and β -myrcene. May Eos, α -pinene dominated, while August Eos, β -pinene, and D-limonene were predominant. The biological activity of Eos from P. lentiscus collected in August was highest compared to other periods. During this time (August), the leave’s Eos showed significant antibacterial, antioxidant, and anti-inflammatory activity. The computational molecular docking and ADMET results align with experimental evidence, lending scientific validation to the traditional medicinal uses of the plants from which these compounds were derived. These results provide valuable information on the seasonal dynamics of the CC of P. lentiscus Eos and underline the importance of taking environmental factors into account in studies of metabolite biosynthesis.