Development and Evaluation of Eberconazole-Loaded Niosomes

Invasive fungal infections require a long treatment schedule; however, treatment has become more cumbersome due to the development of resistance. Most antifungal moieties show systemic toxicity upon oral administration, leading to delivery of antifungal moieties via a topical route. Eberconazole (EBZ) is a BCS class II drug that has poor solubility and high permeability. It is a broad-spectrum imidazole derivative, which acts as a both fungicidal and fungistatic drug by inhibiting ergosterol synthesis. Various topical creams of EBZ are available in the market, but the lack of a proper dosing schedule and rapid removal lead to poor bioavailability. Niosomes are vesicular carriers that can entrap both hydrophilic and lipophilic drugs. Niosomal formulations have been prepared using Span20 (nonionic surfactant) and cholesterol by thin-film hydration (TFH) technique. During preformulation studies, the purity of EBZ was ascertained using FT-IR and melting point studies, while the standard calibration curve was prepared using UV-visible spectroscopy. The prepared niosomal formulations were characterized for their morphology, entrapment efficiency, particle size, and zeta potential. The formulation has shown 86 ± 0.85% entrapment efficiency, while the noisome appeared in a ring-like structure during its microscopic evaluation. Further evaluations of in vitro and in vivo release studies will be performed in the future for its efficacy and antifungal activity

Green Synthesis of Fluorescent Carbon Dots through Solvothermal Treatment of Buchnania lanzan Leaf Extract

In the present work, we synthesized fluorescent carbon dots (CDs) through solvothermal treatment of Buchnania lanzan leaf extract at 160 °C for 4 h in an oven. Here, Buchnania lanzan leaves served as a renewable source of carbon. The obtained blackish brown CD solution was centrifuged, and the supernatant was filtered through a syringe filter (0.22 µm). Further, the CD solution was dried in a vacuum oven to obtain a powder. The synthesized CDs were characterized by different techniques including UV–visible spectroscopy, fluorescence spectroscopy, Fourier transform infrared (FTIR), zeta potential and X-ray diffraction (XRD). The as-prepared CD solution was found to be brownish colored in daylight while exhibiting green fluorescence under UV light. The UV–visible absorption spectrum displayed characteristic shoulder peaks of CDs at 257 nm and at 356 nm. In the fluorescence spectra, excitation-dependent emission behavior of the CDs was seen, which is one of the distinct characteristics of CDs. The negative zeta potential and characteristic peaks in FTIR suggested the presence of carbonyl, amine and hydroxyl functional groups on the CD surface. The XRD spectrum exhibited a broad peak at 2θ=19°, suggesting the amorphous nature of the CDs, similar to what has been reported in earlier works. As we synthesized surface-functionalized fluorescent carbon dots from a renewable and abundant precursor, this method can be highly useful in the large-scale synthesis of carbon dots with reduced costs and will find potential applications in the fields of drug delivery, bioimaging, etc

Chemical composition and antimicrobial activity of the essential oils of <i style="">Senecio rufinervis</i> DC. (Asteraceae)

44-47The chemical composition of the essential oil obtained from the leaves and roots of Senecio rufinervis DC. was analyzed by GC, GC/MS and NMR. Germacrene D was the major constituent in both the oils studied (40.19 and 24.95%, respectively). The antimicrobial activity of the oil was determined by disc diffusion method. Results showed that both the oils exhibited significant antibacterial activity

The Mycobactin Biosynthesis Pathway: A Prospective Therapeutic Target In The Battle Against Tuberculosis

The file attached to this record is the author's final peer reviewed version. The Publisher's final version can be found by following the DOI link.The alarming rise in drug-resistant clinical cases of tuberculosis (TB) has necessitated the rapid development of newer chemotherapeutic agents with novel mechanisms of action. The mycobactin biosynthesis pathway, conserved only among the mycolata family of actinobacteria, a group of intracellularly surviving bacterial pathogens that includes Mycobacterium tuberculosis, generates a salicyl-capped peptide mycobactin under ironstress conditions in host macrophages to support the iron demands of the pathogen. This in vivo essentiality makes this less explored mycobactin biosynthesis pathway a promising endogenous target for novel lead-compounds discovery. In this Perspective, we have provided an up-to-date account of drug discovery efforts targeting selected enzymes (MbtI, MbtA, MbtM, and PPTase) from the mbt gene cluster (mbtA-mbtN). Furthermore, a succinct discussion on non-specific mycobactin biosynthesis inhibitors and the Trojan horse approach adopted to impair iron metabolism in mycobacteria has also been included in this Perspectiv

SELEX based aptamers with diagnostic and entry inhibitor therapeutic potential for SARS-CoV-2

Abstract Frequent mutation and variable immunological protection against vaccination is a common feature for COVID-19 pandemic. Early detection and confinement remain key to controlling further spread of infection. In response, we have developed an aptamer-based system that possesses both diagnostic and therapeutic potential towards the virus. A random aptamer library (~ 1017 molecules) was screened using systematic evolution of ligands by exponential enrichment (SELEX) and aptamer R was identified as a potent binder for the SARS-CoV-2 spike receptor binding domain (RBD) using in vitro binding assay. Using a pseudotyped viral entry assay we have shown that aptamer R specifically inhibited the entry of a SARS-CoV-2 pseudotyped virus in HEK293T-ACE2 cells but did not inhibit the entry of a Vesicular Stomatitis Virus (VSV) glycoprotein (G) pseudotyped virus, hence establishing its specificity towards SARS-CoV-2 spike protein. The antiviral potential of aptamers R and J (same central sequence as R but lacking flanked primer regions) was tested and showed 95.4% and 82.5% inhibition, respectively, against the SARS-CoV-2 virus. Finally, intermolecular interactions between the aptamers and the RBD domain were analyzed using in silico docking and molecular dynamics simulations that provided additional insight into the binding and inhibitory action of aptamers R and J

c-Phycocyanin primed silver nano conjugates: Studies on red blood cell stress resilience mechanism

In this study, we have synthesized cPC functionalized hybrid Ag nanoparticles (AgcPCNPs) by employing a green chemistry approach. This study also entails an in-depth understanding of different biochemical interaction between synthesized AgcPCNPs with whole blood and hemoglobin (Hbc). The cPC primed on the surface of the AgNPs reduced the hemolysis and lipid oxidation. A variation in the K+ concentrations and were observed. Additionally, molecular docking technique did not indicate significant changes in the protein structures. Finally, the AgcPCNPS enhanced the cellular migration of fibroblast. [Display omitted] •Synthesis and characterization of silver core CPC capped nanoparticles.•cPC conjugation reverses blood cell stress phenomenon by AgNPs.•AgcPC nanoparticles enhanced migration of fibroblasts. Green synthesis of metal-encased nutraceutical nano-hybrids has been a target for research over the last few years. In the present investigation, we have reported temperature dependent facile synthesis of silver nanoparticles using FDA approved c phycocyanin (cPC). The cPC conjugated silver nanoparticles (AgcPCNPs) were characterized by TEM, Zeta Potential, UV–vis, XPS, FTIR, and CD Spectroscopy. The temperature optimization studies suggested the synthesis of stable AgcPCNPs at 40 °C while at higher temperature system shows aggregated appearance. Molecular docking studies predicted the exclusive interaction of C, D, I, and J chains of cPC with the surface of AgNPs. Moreover, AgcPCNPs significantly (p < 0.1 %) counteract the toxic nature of AgNPs on red blood cell by measuring parameters like total RBC count, % hemolysis, % hematocrit, coagulation time, pH, electrolyte concentrations and degree of blood cell lipid peroxidation by the anti-oxidation mechanism. Skin fibroblast in vitro cell migration result suggeststhat AgcPCNPs enhanced the degree of cell movement towards the wound area. Data obtained collectively demonstrate that AgcPCNPs can be a better agent in the dermal wound healing with reduced toxicity with the bi-phasic advantage of cPC as a wound healer and Ag nano-metal as an anti-bacterial agent

Sinteza, antibakterijsko i potencijalno anti-HIV djelovanje nekoliko novih analoga imidazola

A series of 1-(2-methyl-4-nitro-imidazol-1-yl)-3-arylamino-propan-2-ones (2a-e), 2-methyl-5-nitro-1-{2-[arylmethoxy]ethyl}-1H- imidazoles (5a-d), and N-(3-hydroxyphenyl)-2-(substituted imidazol-1-yl)alkanamides (8a-e) were synthesized with the aim to develop novel imidazole analogs with broad-spectrum chemotherapeutic properties. Title compounds were evaluated for their anti-HIV and antibacterial activities.Sintetizirana je serija 1-(2-metil-4-nitro-imidazol-1-il)-3-arilamino-propan-2-ona (2a-e), 2-metil-5-nitro-1-{2-[arilmetoksi]etil}-1H- imidazola (5a-d) i N-(3-hidroksifenil)-2-(supstituiranih imidazol-1-il)alkanamida (8a-e) s ciljem dobivanja novih derivata imidazola sa širokim kemoterapijskim svojstvima. Navedeni spojevi ispitani su na anti-HIV i antibakterijsko djelovanje