查看更多>>摘要：Nano delivery systems, polymeric micelles represent one of the most promising delivery platforms for therapeutic compounds. It has shown that a poorly soluble molecule which has high potency and remarkable toxicity can be encapsulated with the polymeric micelle. There are various poorly soluble drugs used in micellar preparations, mostly for their anti-cancer activity. Drugs in the inner core protect the drug from degradation and allow drug accumulation in the tumour site in the case of cancer treatment. Block copolymers are chosen based on the physicochemical characteristics of medicinal drugs. The amphiphilic block copolymer structure has both lipophilic and hydrophilic blocks, which enclose tiny hydrophobic molecules. It is a targeted drug delivery method because of its high effectiveness for drug retention in tissue, prevention of enzymes from degradation, and improvement of the cellular absorption mechanism. In an experimental environment, variations in temperature and solvent polarity stimulate copolymer micelle self-assembly. This is a thermodynamically guided procedure in which self-assembly happens by converting polymeric micelles. These aggregates go from a non-equilibrium to a thermodynamically equilibrium state, and they stay stable for a long time. The balance of thermodynamic and kinetic forces is critical in micelles selfassembly because the kinetic process predicts assembly behaviour and hierarchical structure. The purpose of this special issue is to provide an updated overview ofmicelles, a number of polymers and drugs commonly used in micellar preparation and their application.
查看更多>>摘要：The endophytic microbiota is considered to be one of the consistent and noble souce of potential and unique natural amalgams. These natural amalgams carry diverse pharmaceutical significance which the reason for their importance among research fields.The diversity of plants carries much more diversity of the endophytes as their mutual parts where both are benefited from each other. The current work deals with the isolation of the endophytic fungus from Tinospora cordifolia, for which the leaves wereused after the surface sterilization, followed by the production of secondary metabolite by the endophytic isolates through submerged fermentation technique. The produced metabolite was extracted by liquid-liquid extraction technique, which was furtherused for evaluating its antifungal potential against Candida albicans and the obtained results show their considerable potential. The GC-MS profiling of secondary metabolite was conducted to determine the presence of some bioactive compounds in them, andas a result, some potential compounds detected are Levoglucosenone, Silanediol, Nonane, D-Allose, 5-Hydroxymethylfurfural. Since these compounds are biologically important in various aspects which gives the diversified application to the secondary metabolites. The study concludes the potential of secondary metabolites from endophytic fungus of Tinospora cordifolia and further investigation can be approached on determining the same from other plants, and also evaluating another bioactive potential of secondary metabolites.
查看更多>>摘要：Ras is a small G protein known as a central regulator of cellular signal transduction that induces processes, such as cell division, transcription. The hypervariable region (HVR) is one of the functional parts of this G protein, which induces multimerization and interaction between Ras and the plasma membrane. We introduced two highly different in polarity photochromic SH group-reactive azobenzene derivatives, N-4-phenyl-azophenyl maleimide (PAM) and 4-chloroacetoamido-4-sulfo-azobenzene (CASAB), into three cysteine residues in HVR to control Ras GTPase using light. PAM stoichiometrically reacted with the SH group of cysteine residues and induced multimerization. The mutants modified with PAM exhibited reversible changes in GTPase activity accelerated by the guanine nucleotide exchange factor and GTPase activating protein and multimerization accompanied by cis- and trans-photoisomerization upon ultraviolet and visible light irradiation. CASAB was incorporated into two of the three cysteine residuesin HVR but did not induce multimerization. The H-Ras GTPase modified with CASAB was photo controlled more effectively than PAM-H-Ras. In this study, we revealed that the incorporation of azobenzene derivatives into the functional site of HVR enables photo reversible control of Ras function. Our findings may contribute to the development of a method to control functional biomolecules with physiologically important roles.
查看更多>>摘要：Although the cause of Alzheimer’s disease is unknown, most experts feel that the disease is caused by a combination of circumstances rather than a single cause. Age, gene polymorphism, diabetes, and other conditions are all risk factors for Alzheimer’s disease. Given the importance of gene polymorphism in different diseases, we intended to find out the association of APOE gene polymorphism with Alzheimer’s risk in the Kashmiri population. Out of 300 patients who were referred to the memory clinicof the hospital, we conducted the study on 59 clinically confirmed Alzheimer’s patients and 52 age and ethnicity-matched healthy controls found in a community survey. Our data revealed a statistically significant association of s4 variant genotype of the APOE gene with AD susceptibility in the Kashmiri population. The current study’s findings provided insight into the role of APOE polymorphisms in Alzheimer’s disease susceptibility. The identified susceptibility variant may become a marker genotype for AD.
Anthony Taghogho EduviereEmuesiri Goodies MokeAdrian Itivere Omogbiya
9页
查看更多>>摘要：Disruption of the active phase of sleep alters the physiological homeostasis of the body and results in oxidative breakdown which may trigger a wide array of defects. The central nervous system and the metabolic system are some of the most affected systems as described in several literatures. Some plant based compounds with antioxidant property have been previously described in the abrogation of the deleterious effects of active sleep disruption. One of such compounds is quercetin. This study was premeditated to expatiate on the probable neuroprotective effect of quercetin on mice exposed to 72hr active sleep disruption. Mice were allotted into five treatment groups (n = 6): group 1 served as control, group 2 received 10 mL/kg vehicle, groups 3 and4 received 25 and 50 mg/kg quercetin respectively, and group 5 received 50 mg/kg astaxanthin. Treatment lasted for 7 days while groups 2-5 were exposed to the sleep deprivation protocol starting from day 4. Behavioural tests followed by biochemical assays and histopathological changes in the prefrontal cortex were evaluated. Data were analysed by ANOVA set at p<0.05 significance. The results revealed that quercetin, in both doses, significantly amplified memory performance, attenuated depression-like behaviour, replenished catalase and superoxide dismutase, attenuated nitric oxide levels in brain and liver of mice when compared to control group and protected against loss of prefrontal cortex neurons. In conclusion, quercetin possesses protective effects against sleep deprivation-induced brain damage.
查看更多>>摘要：Generally, synthesis and encapsulation process improve therapeutic value of nano encapsulated drugs. The silver nanoparticles (AgNPs) biosynthesized from Ziziphus nummularia leaves and encapsulated with polyvinyl pyrrolidone (PVP) polymer as antibacterial agents, due to its high bioavailability, better encapsulation and less toxic properties. The nanoparticles (AgNPs) biosynthesized from Ziziphus nummularia leaves and capped with polyvinyl pyrrolidone (PVP) polymer, The acquired AgNPs and polymeric functionalized AgNPs were fully characterised by the UV- Visible spectroscopy , Transmission electron microscopy (TEM), X-Ray diffraction pattern (XRD) and Fourier transform infrared spectroscopy (FTIR). The crystalline Ag NPs and Polymer Functionalized AgNPs have a face-centered cubic structure with an average size of 9.20 nm, according to X-ray Diffraction spectroscopy. Fourier Transform Infrared spectroscopy revealed that biomolecules such as proteins are incapable of reducing metal ions and the formation of an encapsulating layer in terms of metal ions. High-Resolution transmission electron microscopy revealed that Polymer functionalized AgNPs ranged in size of 10 nm. AgNPs and Polymer functionalized AgNPs showed effective antimicrobial and antioxidant activity. The biosynthesized monodisperse silver nanoparticles and encapsulated silver nanoparticles demonstrated better antimicrobial and antioxidant activity which can be used in various biomedical applications.
查看更多>>摘要：Shigellosis is a serious public health issue. Millions of people suffer from this deadly food and water borne disease each year. The main manifestations of affected persons are bloody diarrhea with excessive dehydration. The causative agent of this disease is the bacteria Shigella spp. which has four serogroups. Though Shigella flexneri and Shigella dysenteriae are the dominant serogroups in developing countries, reports of other serogroups, namely Shigella boydii and Shigella sonnei, in the food contaminations are available. There are seasonal variations of Shigella infection throughout the world. In Asian subcontinent, monsoon and post monsoon times are the ideal for infection. The transmission of the bacteria in human is usually caused by feco-oral route or by contaminated food and water. There are several groups of antibiotics like foscomycin, macrolide, amiglycoside, tetracycline etc. which were used before. But they are now become useless as Shigella spp. is getting resistant against those drugs. The quinolone groups of antibiotics like ciprofloxacin, ofloxacin, norflxacin, ceftriaxone etc. are the important drugs for the cure of the disease shigellosis but prevalence of drug resistant strains of Shigella spp. against those drugs are a greatconcern nowadays. The occurrence of plasmid mediated quinolone resistance genes (PMQR), efflux pump proteins and effective mutations at drug binding region of gyrA etc. are the major mechanisms for the development of drug resistance.
Najwa Menwer AlharbiAmjad Khalid AlharthiAishah Ahmed Alsamadani
14页
查看更多>>摘要：This study aimed to investigate a method to manage antimicrobial resistance (AMR) issues by exploring soil microorganisms that are capable of producing bioactive compounds. Eight different types of soil were selected from three locations to screen, isolate, and identify microorganisms that are capable of producing antimicrobial compounds. The multi-drug resistant strains are Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli, and Candida albicans were selected for primary and secondary screening using the crowded plate method and the agar well diffusion method. Inhibition zones were measured, and data were assessed using statistical tests to check for normality and differences between parametric variables and nonparametric data. This was followed by biochemical characterization, DNA isolation, and polymerase chain reaction (PCR). Molecular identification was performed using 16S rRNA amplification and sequencing. Here, 86 isolates containing bacteria and fungi were successfully extracted from soil samples. Further, 49 of 86 microbes showed possible antimicrobial activity, but only 12 isolates resulted in distinct inhibition zones with the selected multi-drug resistant strains. The following different taxa were identified: Firmicutes (nine strains), Proteobacteria (one strain), Actinobacteria (one strain), and Azotobacter (one strain). Species are represented in a phylogenetic tree, which was constructed using the unweighted pair-group method with arithmetic mean (UPGMA) method. The evolutionary distances were computed using the Maximum Composite Likelihood method. The identified microorganisms showed antimicrobial activity, confirming that soil microorganisms have great potential to address AMR issues.
查看更多>>摘要：Microspheres, a potential drug delivery approach, has opened a new era for attaining versatile release patterns needed. By optimizing the formulation variables, they can be prepared to obtain targeted release, immediate release, sustained release patterns. The release of the active drug material depends upon a number of formulation parameters such as polymers, stirring speed (rpm), methodology, surfactants, etc. Fexofenadine hydrochloride (HCl) is a second generation antihistamine. Our present research has explored the effects of using different rpm (600- 1000 rpm) in preparing fexofenadine hydrochloride (HCl) microspheres by emulsion solvent evaporation method. The formulation is aimed to provide sustained release for the required long period witha high margin of safety. We used a blended mixture of Hydroxy Propyl Methyl Cellulose (HPMC) K 100 MCR and Eudragit RL100 polymers to have sustained-release microspheres. The impact of different rpm on Yield, drug encapsulation efficiency, flow properties, and dissolution pattern were appraised. We observed the release of the drug for 10 hours in phosphate buffer (pH 6.8) and evaluated the drug release spectrophotometrically. Our study finds that the release of fexofenadine HCl from the microspheres wassignificantly increased with drug loading. We found the dosage forms to follow Higuchi release kinetics and Hixson-Crowell release kinetics the most, indicating successful achievement of sustained-release pattern in the dosage form. The change in drug release rate was statistically significant for variation in the stirring rate. We found that 600 rpm was the most optimized stirring rate for preparing microspheres in the emulsion solvent evaporation method.
查看更多>>摘要：Beauty salons may draw in customers with glamour; however, they could also be considered a major health issue. They can cause the spread of bacterial and fungal infections. The purpose of this research was to identify pathogenic microbes from beauty salon tools. Microorganisms from contaminated salon tools and cosmetic products were isolated using various selective media. Microbial isolates were identified based on their molecular and biochemical characteristics. The most common bacterial species isolated were Staphylococcus aureus, Staphylococcus epidermidis, Staphylococcus equorum, Microbacterium spp., Bacillus siamensis, Bacillus subtilis, Sphingomonas aeria, Macrococcus spp., Microbacterium oxydans, Brachybacterium spp., Micrococcus luteus, andBrachybacterium nesterenkovii. Fungal isolates included Penicillium spp., Aspergillus niger, Purpureocillium lilacium, and Aspergillus flavus. Overall, Staphylococcus spp. and A. niger were the most common organisms isolated from the samples. The presence of potential pathogens indicates that the tools used in salons have not been adequately sterilized and the high risk of diseases spread.
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