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1.
J Fluoresc ; 2023 Oct 13.
Article in English | MEDLINE | ID: mdl-37831354

ABSTRACT

The development of a simple, biocompatible, pH sensor with a wide range of detection, using a single fluorescent probe is highly important in the medical field for the early detection of diseases related to the pH change of tissues and body fluids. For this purpose, europium-doped fluorapatite (FAP: Eu) nanoparticles were synthesized using the coprecipitation method. Doping with the rare earth element europium (Eu) makes the non-luminescent phosphate mineral fluorapatite, luminescent. The luminous response of the sample upon dissolution in hydrochloric acid (HCl), in highly acidic to weakly basic media, makes it a potential pH sensor. A linear variation was observed with an increase in pH, in both the total intensity of emission and the R-value or the asymmetry ratio. The ratiometric pH sensing enabled by the variation in R-value makes the sensor independent of external factors. The structural, optical, and photoluminescent (PL) lifetime analysis suggests a particle size-dependent pH sensing mechanism with the changes in the coordinated water molecules around the Eu3+ ion in the nanoparticle. Given its exceptional biocompatibility and pH-dependent fluorescence intensity for a wide range of pH from 0.83 to 8.97, the probe can be used as a potential candidate for pH sensing of biological fluid.

2.
J Fluoresc ; 33(5): 2023-2039, 2023 Sep.
Article in English | MEDLINE | ID: mdl-36971980

ABSTRACT

1,3,4-Oxadiazole pharmacophore is still considered a viable biologically active scaffold for the synthesis of more effectual and broad-spectrum antimicrobial agents. Therefore, the present study is based on five 1,3,4-oxadiazole target structures, viz., CAROT, CAROP, CARON (D-A-D-A systems) and NOPON and BOPOB (D-A-D-A-D systems) bearing various bioactive heterocyclic moieties relevant to potential biological activities. Three of the compounds, CARON, NOPON and BOPOB were assessed in-vitro for their efficacy as antimicrobial agents against gram positive (Staphylococcus aureus and Bacillus cereus) and gram negative (Escherichia coli and Klebsiella pneumonia) bacteria; and two fungi, Aspergillus niger and Candida albicans; also, as an anti-tuberculosis agent against Mycobacterium tuberculosis. Most of the tested compounds displayed promising antimicrobial activity, especially CARON which was then analyzed for the minimum inhibitory concentration (MIC) studies. Similarly, NOPON portrayed the highest anti-TB activity among the studied compounds. Consequently, to justify the detected anti-TB activity of these compounds and to recognize the binding mode and important interactions between the compounds and the ligand binding site of the potential target, these compounds were docked into the active binding site of cytochrome P450 CYP121 enzyme of Mycobacterium tuberculosis, 3G5H. The docking results were in good agreement with the result of in-vitro studies. In addition, all the five compounds were tested for their cell viability and have been investigated for cell labeling applications. To conclude, one of the target compounds, CAROT was used for the selective recognition of cyanide ion by 'turn-off' fluorescent sensing technique. The entire sensing activity was examined by spectrofluorometric method and MALDI spectral studies. The limit of detection obtained was 0.14 µM.


Subject(s)
Anti-Infective Agents , Anti-Infective Agents/pharmacology , Anti-Infective Agents/chemistry , Oxadiazoles/pharmacology , Fungi , Bacteria , Microbial Sensitivity Tests , Anti-Bacterial Agents/chemistry , Structure-Activity Relationship , Antifungal Agents/chemistry
3.
J Fluoresc ; 31(6): 1927-1936, 2021 Nov.
Article in English | MEDLINE | ID: mdl-34546470

ABSTRACT

Hen's eggshell, a biological waste product, was turned into a cell imaging probe: europium doped hydroxyapatite (HAp: Eu) nanoparticle using hydrothermal method. Luminescence of the synthesized nanoparticle was studied for various doping concentrations of the lanthanide ion europium (Eu3+). Eu doped HAp showed a hexagonal crystal structure and rod-shaped morphology. Well-defined emission peaks of europium, corresponding to the substitution of Eu3+ at the Ca2+(I) site of HAp, were confirmed from the samples' photoluminescence (PL) spectra. Good biocompatibility up to 500 µg/mL of the samples indicates their potential applications in bioimaging. Synthesized nanoparticles were internalized and used for in vitro imaging of the PC12 cells without any surface modification. The materials' use as a potential in vivo imaging agent is proposed from the haemolysis study.


Subject(s)
Durapatite/chemistry , Egg Shell/chemistry , Europium/chemistry , Nanoparticles/chemistry , Optical Imaging , Animals , Cell Line, Tumor , Chickens , Humans , Rats
5.
Mol Neurobiol ; 2023 Nov 21.
Article in English | MEDLINE | ID: mdl-37987958

ABSTRACT

Therapeutic options to contain seizures, a transitional stage of many neuropathologies, are limited due to the blood-brain barrier (BBB). Herbal nanoparticle formulations can be employed to enhance seizure prognosis. Bacoside A (BM3) and bacopaside I (BM4) were isolated from Bacopa monnieri and synthesized as nanoparticles (BM3NP and BM4NP, respectively) for an effective delivery system to alleviate seizures and associated conditions. After physicochemical characterization, cell viability was assessed on mouse neuronal stem cells (mNSC) and neuroblastoma cells (N2a). Thereafter, anti-seizure effects, mitochondrial membrane potential (MMP), apoptosis, immunostaining and epileptic marker mRNA expression were determined in vitro. The seizure-induced changes in the cortical electroencephalogram (EEG), electromyography (EMG), Non-Rapid Eye Movement (NREM) and Rapid Eye Movement (REM) sleep were monitored in vivo in a kainic acid (KA)-induced rat seizure model. The sizes of BM3NPs and BM4NPs were 165.5 nm and 689.6 nm, respectively. They were biocompatible and also aided in neuroplasticity in mNSC. BM3NPs and BM4NPs depicted more than 50% cell viability in N2a cells, with IC50 values of 1609 and 2962 µg/mL, respectively. Similarly, these nanoparticles reduced the cytotoxicity of N2a cells upon KA treatment. Nanoparticles decreased the expression of epileptic markers like fractalkine, HMGB1, FOXO3a and pro-inflammatory cytokines (P < 0.05). They protected neurons from apoptosis and restored MMP. After administration of BM3NPs and BM4NPs, KA-treated rats attained a significant reduction in the epileptic spikes, sleep latency and an increase in NREM sleep duration. Results indicate the potential of BM3NPs and BM4NPs in neutralizing the KA-induced excitotoxic seizures in neurons.

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