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2.
Saudi Pharm J ; 32(11): 102169, 2024 Nov.
Article in English | MEDLINE | ID: mdl-39318640

ABSTRACT

The impact of Engineered nanomaterials (ENMs) (i.e., Zinc Oxide nanoparticles (ZnO NPs)) on human health has been investigated at high and unrealistic exposure levels, overlooking the potential indirect harm of subtoxic and long exposures. Therefore, this study aimed to investigate the impacts of subtoxic concentrations of zinc oxide (ZnO NPs) on breast cancer cells' response to Doxorubicin. Zinc oxide nanoparticles caused a concentration-dependent reduction of cell viability in multiple breast cancer cell lines. A subtoxic concentration of 1.56 µg/mL (i.e., no observed adverse effect level) was used in subsequent mechanistic studies. Molecularly, miRNA profiling revealed significant downregulation of 13 oncogenic miRNAs (OncomiRs) in cells exposed to the sub-toxic dose of ZnO NPs followed by doxorubicin treatment. Our comprehensive bioinformatic analysis has identified 617 target genes enriched in ten pathways, mainly regulating gene expression and transcription, cell cycle, and apoptotic cell death. Several tumor suppressor genes emerged as validated direct targets of the 13 OncomiRs, including TFDP2, YWHAG, SMAD2, SMAD4, CDKN1A, CDKN1B, BCL2L11, and TGIF2. This study insinuates the importance of miRNAs in regulating the responsiveness of cancer cells to chemotherapy. Our findings further indicate that being exposed to environmental ENMs, even at levels below toxicity, might still modulate cancer cells' response to chemotherapy, which highlights the need to reestablish endpoints of ENM exposure and toxicity in cancer patients receiving chemotherapeutics.

3.
Heliyon ; 10(16): e35621, 2024 Aug 30.
Article in English | MEDLINE | ID: mdl-39224246

ABSTRACT

Electrocardiography (ECG) is the most non-invasive diagnostic tool for cardiovascular diseases (CVDs). Automatic analysis of ECG signals assists in accurately and rapidly detecting life-threatening arrhythmias like atrioventricular blockage, atrial fibrillation, ventricular tachycardia, etc. The ECG recognition models need to utilize algorithms to detect various kinds of waveforms in the ECG and identify complicated relationships over time. However, the high variability of wave morphology among patients and noise are challenging issues. Physicians frequently utilize automated ECG abnormality recognition models to classify long-term ECG signals. Recently, deep learning (DL) models can be used to achieve enhanced ECG recognition accuracy in the healthcare decision making system. In this aspect, this study introduces an automated DL enabled ECG signal recognition (ADL-ECGSR) technique for CVD detection and classification. The ADL-ECGSR technique employs three most important subprocesses: pre-processed, feature extraction, parameter tuning, and classification. Besides, the ADL-ECGSR technique involves the design of a bidirectional long short-term memory (BiLSTM) based feature extractor, and the Adamax optimizer is utilized to optimize the trained method of the BiLSTM model. Finally, the dragonfly algorithm (DFA) with a stacked sparse autoencoder (SSAE) module is applied to recognize and classify EEG signals. An extensive range of simulations occur on benchmark PTB-XL datasets to validate the enhanced ECG recognition efficiency. The comparative analysis of the ADL-ECGSR methodology showed a remarkable performance of 91.24 % on the existing methods.

4.
ACS Sens ; 9(9): 4536-4554, 2024 Sep 27.
Article in English | MEDLINE | ID: mdl-39284075

ABSTRACT

Laser-induced graphene (LIG) and Laser-scribed graphene (LSG) are both advanced materials with significant potential in various applications, particularly in the field of sustainable sensors. The practical uses of LIG (LSG), which include gas detection, biological process monitoring, strain assessment, and environmental variable tracking, are thoroughly examined in this review paper. Its tunable characteristics distinguish LIG (LSG), which is developed from accurate laser beam modulation on polymeric substrates, and they are essential in advancing sensing technologies in many applications. The recent advances in LIG (LSG) applications include energy storage, biosensing, and electronics by steadily advancing efficiency and versatility. The remarkable flexibility of LIG (LSG) and its transformative potential in regard to sensor manufacturing and utilization are highlighted in this manuscript. Moreover, it thoroughly examines the various fabrication methods used in LIG (LSG) production, highlighting precision and adaptability. This review navigates the difficulties that are encountered in regard to implementing LIG sensors and looks ahead to future developments that will propel the industry forward. This paper provides a comprehensive summary of the latest research in LIG (LSG) and elucidates this innovative material's advanced and sustainable elements.


Subject(s)
Biosensing Techniques , Graphite , Lasers , Graphite/chemistry , Biosensing Techniques/methods , Humans
5.
Headache ; 2024 Sep 09.
Article in English | MEDLINE | ID: mdl-39248024

ABSTRACT

BACKGROUND: Fasting headaches frequently occur during the first few days of Ramadan, and treatment is challenging because of fasting. OBJECTIVE: This study aimed to evaluate the effect of extended-release paracetamol on preventing fasting headaches. METHODS: A randomized, open-label clinical trial investigated the efficacy of extended-release paracetamol at a daily dose of 1330 mg in preventing fasting headache. Adults aged 18 years and older were recruited through the Clinical Trial Unit at the King Saud University Medical City. The eligible participants in the study fasted 13.5 h daily during the first week of Ramadan. Participants in the treatment and control arms were followed up to investigate the occurrence, severity, and timing of headache symptoms via self-reporting using a standardized headache diary scale with a daily online link or phone call. The primary outcome was the frequency of headache episodes while fasting during the first week of Ramadan. RESULTS: A total of 238 participants were enrolled and randomized. Of these, 173 followed the protocol (80 treated, 93 control) for at least the first day and were included in the analysis. Most participants were young and healthy, with a mean age of 32.2 ± 10.2 years. More men were included in the study (102/173; 59.0%), a small proportion of participants were smokers (31/173; 17.9%), and almost all participants reported being coffee drinkers (165/173; 95.4%); nonetheless, these characteristics were evenly distributed between the two groups in the study. The overall incidence of headache episodes was 33.0% (57/173) on day 1 and decreased to 11.3% (18/159) on day 7. On average over the 7 days, no significant effect was observed for the treatment on the incidence of headache, as the findings from the generalized estimating equation model indicated (ß = -0.398, p = 0.084; odds ratio = 0.67, 95% confidence interval [CI] 0.42-1.06). Moreover, there was initially no significant difference in the incidence of headache episodes between the treatment and control groups. However, the treatment group had significantly fewer headache episodes during fasting than the control group on day 3 (4/72 [5.6%] vs. 15/91 [16.5%], p = 0.031; relative risk [RR] = 0.34, 95% CI 0.12-0.97) and day 6 (5/69 [7.2%] vs. 20/90 [22.2%], p = 0.010; RR = 0.33, 95% CI 0.13-0.82). No adverse effects were observed during the study period. CONCLUSION: No significant differences were observed in the occurrence of fasting headaches between the two groups on most days during the study period. Additional studies are required to address fasting headaches during the first week of Ramadan.

6.
Environ Monit Assess ; 196(10): 946, 2024 Sep 18.
Article in English | MEDLINE | ID: mdl-39289191

ABSTRACT

Inorganic arsenic (As), a known carcinogen and major contaminant in drinking water, affects over 140 million people globally, with levels exceeding the World Health Organization's (WHO) guidelines of 10 µg L-1. Developing innovative technologies for effluent handling and decontaminating polluted water is critical. This paper summarizes the fundamental characteristics of chitosan-embedded composites for As adsorption from water. The primary challenge in selectively removing As ions is the presence of phosphate, which is chemically similar to As(V). This study evaluates and summarizes innovative As adsorbents based on chitosan and its composite modifications, focusing on factors influencing their adsorption affinity. The kinetics, isotherms, column models, and thermodynamic aspects of the sorption processes were also explored. Finally, the adsorption process and implications of functionalized chitosan for wastewater treatment were analyzed. There have been minimal developments in water disinfection using metal-biopolymer composites for environmental purposes. This field of study offers numerous research opportunities to expand the use of biopolymer composites as detoxifying materials and to gain deeper insights into the foundations of biopolymer composite adsorbents, which merit further investigation to enhance adsorbent stability.


Subject(s)
Arsenic , Chitosan , Iron , Water Pollutants, Chemical , Water Purification , Chitosan/chemistry , Arsenic/analysis , Arsenic/chemistry , Adsorption , Water Pollutants, Chemical/analysis , Water Pollutants, Chemical/chemistry , Water Purification/methods , Iron/chemistry , Polymers/chemistry
7.
Chemosphere ; 364: 143050, 2024 Sep.
Article in English | MEDLINE | ID: mdl-39121967

ABSTRACT

4-aminophenol (AP), an aromatic phenolic compound, is commonly found in commercial products that eventually enter and pollute environmental water sources. The precise detection and quantification of AP in environmental samples are critical for comprehensively assessing contamination levels, safeguarding public health, and formulating effective remediation strategies. In the shed of light, this work proposes an electrochemical sensing platform for detecting and quantifying AP using Araucaria heterophylla biomass-derived activated carbon (AH-AC) prepared via the SC-CO2 pathway. To evaluate the significance of SC-CO2-mediated chemical activation (SC-AHAC), a comparative study with conventional activation methods (C-AHAC) was also conducted. The physical characterizations such as structural, morphological, optical, and elemental analysis demonstrate the greater ID/IG value and enhanced surface functionalities of SC-AHAC than C-AHAC. The obtained lower empirical factor (R) value of 1.89 for SC-AHAC suggests increased disorder and a higher presence of single-layer amorphous carbon compared to C-AHAC (2.03). In the electrochemical analysis, the active surface area of the SC-AHAC modified electrode (0.069 cm2) is higher than that of the C-AHAC modified electrode (0.061 cm2), demonstrating the significance of SC-CO2 activation. Further, the quantitative analysis on SC-AHAC@SPCE resulted in a sensitivity of 3.225 µA µM-1 cm-2 with the detection limit and quantification limit of 2.13 and 7.11 nM L-1, respectively, in the linear range of 0.01-582.5 µM L-1 at the oxidation potential of 0.13V. This suggests that the prepared SC-AHAC could be a promising electrocatalyst for AP detection in the environmental and healthcare sectors.


Subject(s)
Biomass , Carbon Dioxide , Carbon , Phenols , Water Pollutants, Chemical , Carbon Dioxide/analysis , Carbon Dioxide/chemistry , Phenols/analysis , Carbon/chemistry , Porosity , Water Pollutants, Chemical/analysis , Tracheophyta/chemistry , Electrochemical Techniques/methods , Charcoal/chemistry
8.
RSC Adv ; 14(30): 21682-21691, 2024 Jul 05.
Article in English | MEDLINE | ID: mdl-38979467

ABSTRACT

High concentrations of deferasirox (DFX) in living organisms cause hepatic, gastric and renal malfunctions. Therefore, it is significant to establish an accurate and efficient approach for the detection of deferasirox (DFX) to protect public health. Herein, we synthesized a thiourea-based diphenylacetamide probe MPT for the effective sensing of deferasirox through the fluorescence quenching phenomenon. The designed probe MPT shows a fluorescence quenching response toward deferasirox (DFX) through photo-induced electron transfer (PET). Furthermore, DFT studies were performed to support the experimental results. 1H-NMR titration experiment was used to explore the interaction type between probe MPT and DFX. The existence of non-covalent interactions was verified with spectroscopic studies that were assisted by NCI studies, QTAIM and SAPT0 analysis. Dynamic light scattering (DLS) analysis and scanning electron microscopy (SEM) were used to investigate the complexation of probe MPT with DFX. Moreover, the on-site solution phase and solid-state detection of DFX by probe MPT are executed. Additionally, the practical applications of probe MPT to sense DFX were also revealed in human plasma as well as in artificial urine samples.

9.
Dalton Trans ; 53(30): 12410-12433, 2024 Jul 30.
Article in English | MEDLINE | ID: mdl-38952249

ABSTRACT

Due to their distinctive security characteristics, all-solid-state batteries are seen as a potential technology for the upcoming era of energy storage. The flexibility of nanomaterials shows enormous potential for the advancement of all-solid-state batteries' exceptional power and energy storage capacities. These batteries might be applied in many areas such as large-scale energy storage for power grids, as well as in the creation of foldable and flexible electronics, and portable gadgets. The most difficult aspect of creating a comprehensive nanoscale all-solid-state battery assembly is the task of decreasing the particle size of the solid electrolyte while maintaining its excellent ionic conductivity. Materials possessing nanoscale structural features and a substantial electrochemically active surface area have the potential to significantly enhance power characteristics and the cycle life. This might bring about substantial changes to existing energy storage models. The primary objective of this research is to summarize the latest advancements in utilizing nanomaterials for energy harvesting in various all-solid-state battery assemblies. This study examines the most complex solid-solid interfaces of all-solid-state batteries, as well as feasible methods for implementing nanomaterials in such interfaces. Currently, there is significant attention on the necessity to develop electrode-solid electrolyte interfaces that exhibit nanoscale particle articulation and other characteristics related to the behavior of lithium ions.

10.
Macromol Rapid Commun ; : e2400258, 2024 Jul 17.
Article in English | MEDLINE | ID: mdl-39018482

ABSTRACT

This study explores the synthesis and characterization of superabsorbent hydrogels derived from chemically modified gum Arabic, designed for controlled folic acid release. The synthesis involves a two-step process: carboxymethylation followed by grafting with 2-hydroxyethyl methacrylate via gamma irradiation. The resulting hydrogels exhibit enhanced mechanical strength and controlled diffusivity, essential for nutrient delivery systems. Key factors such as copolymer composition and irradiation dose are investigated, affecting the synthesis process. Systematic studies of swelling behaviors reveal that the hydrogel achieves a maximum swelling of 888.1% at 40 °C. The hydrogels are loaded with folic acid, and in vitro, sustained release profiles are examined under various pH conditions. The maximum release of 83.3% is observed after 24 h at pH 7.0, following a Korsmeyer-Peppas release mechanism. Different characterization techniques, confirm the successful synthesis and unique properties of the superabsorbent hydrogels. Rheological behavior analysis, scanning electron microscopy, and biocompatibility assessments provide a comprehensive understanding of the hydrogel structures. Gamma irradiation ensures a homogeneous network structure, crucial for optimal swelling behavior and mechanical properties. This research highlights the potential of eco-friendly biopolymer hydrogels in precise drug delivery applications, leveraging the safety and process control benefits of gamma irradiation.

11.
Proteomics Clin Appl ; : e202400018, 2024 Jun 24.
Article in English | MEDLINE | ID: mdl-38923810

ABSTRACT

PURPOSE: Diabetic kidney disease (DKD) is a serious complication of diabetes mellitus and a leading cause of chronic kidney disease and end-stage renal disease. One potential mechanism underlying cellular dysfunction contributing to kidney disease is aberrant protein post-translational modifications. Lysine acetylation is associated with cellular metabolic flux and is thought to be altered in patients with diabetes and dysfunctional renal metabolism. EXPERIMENTAL DESIGN: A novel extraction and LC-MS/MS approach was adapted to quantify sites of lysine acetylation from formalin-fixed paraffin-embedded (FFPE) kidney tissue and from patients with DKD and non-diabetic donors (n = 5 and n = 7, respectively). RESULTS: Analysis of FFPE tissues identified 840 total proteins, with 225 of those significantly changing in patients with DKD. Acetylomic analysis quantified 289 acetylated peptides, with 69 of those significantly changing. Pathways impacted in DKD patients revealed numerous metabolic pathways, specifically mitochondrial function, oxidative phosphorylation, and sirtuin signaling. Differential protein acetylation in DKD patients impacted sirtuin signaling, valine, leucine, and isoleucine degradation, lactate metabolism, oxidative phosphorylation, and ketogenesis. CONCLUSIONS AND CLINICAL RELEVANCE: A quantitative acetylomics platform was developed for protein biomarker discovery in formalin-fixed and paraffin-embedded biopsies of kidney transplant patients suffering from DKD.

12.
Dalton Trans ; 53(26): 10770-10804, 2024 Jul 02.
Article in English | MEDLINE | ID: mdl-38859722

ABSTRACT

Prussian blue and Prussian blue analogues have attracted increasing attention as versatile framework materials with a wide range of applications in catalysis, energy conversion and storage, and biomedical and environmental fields. In terms of energy storage and conversion, Prussian blue-based materials have emerged as suitable candidates of growing interest for the fabrication of batteries and supercapacitors. Their outstanding electrochemical features such as fast charge-discharge rates, high capacity and prolonged cycling life make them favorable for energy storage application. Furthermore, Prussian blue and its analogues as rechargeable battery anodes can advance significantly by the precise control of their structure, morphology, and composition at the nanoscale. Their tunable structural and electronic properties enable the detection of many types of analytes with high sensitivity and specificity, and thus, they are ideal materials for the development of sensors for environmental detection, disease trend monitoring, and industrial safety. Additionally, Prussian blue-based catalysts display excellent photocatalytic performance for the degradation of pollutants and generation of hydrogen. Specifically, their excellent light capturing and charge separation capabilities make them stand out in photocatalytic processes, providing a sustainable option for environmental remediation and renewable energy production. Besides, Prussian blue coatings have been studied particularly for corrosion protection, forming stable and protective layers on metal surfaces, which extend the lifespan of infrastructural materials in harsh environments. Prussian blue and its analogues are highly valuable materials in healthcare fields such as imaging, drug delivery and theranostics because they are biocompatible and their further functionalization is possible. Overall, this review demonstrates that Prussian blue and related framework materials are versatile and capable of addressing many technical challenges in various fields ranging from power generation to healthcare and environmental management.

13.
Sci Rep ; 14(1): 13032, 2024 06 06.
Article in English | MEDLINE | ID: mdl-38844676

ABSTRACT

Green products such as plant tints are becoming more and more well-known worldwide due to their superior biological and ayurvedic properties. In this work, colorant from Amba Haldi (Curcuma aromatica) was isolated using microwave (MW), and bio-mordants were added to produce colorfast shades. Response surface methodology was used to develop a central composite design (CCD), which maximizes coloring variables statistically. The findings from 32 series of experiments show that excellent color depth (K/S = 12.595) was established onto MW-treated silk fabric (RS = 4 min) by employing 65 mL of radiated aqueous extract (RE = 4 min) of 5 pH cutting-edge the existence of 1.5 g/100 mL used sodium chloride at 75 °C for 45 min. It was discovered that acacia (keekar) extract (1%), pomegranate extract (2%), and pistachio extract (1.5%) were present before coloring by the use of bio-mordants. On the other hand, upon dyeing, acacia extract (1.5%), pomegranate extract (1.5%), and pistachio extract (2%) have all shown extremely strong colorfast colors. Comparatively, before dyeing, salts of Al3+ (1.5%), Fe2+ (2%), and TA (1.5%) gave good results; after dyeing, salts of Al3+ (1%) and Fe2+ (1.5%) and TA (2%) gave good results. When applied to silk fabric, MW radiation has increased the production of dyes recovered from rhizomes. Additionally, the right amount of chemical and biological mordants have been added, resulting in color fastness ratings ranging from outstanding to good. Therefore, the natural color extracted from Amba Haldi can be a sustainable option for the dyeing of silk fabric in the textile dyeing and finishing industries.


Subject(s)
Coloring Agents , Curcuma , Plant Extracts , Rhizome , Silk , Curcuma/chemistry , Rhizome/chemistry , Coloring Agents/chemistry , Plant Extracts/chemistry , Silk/chemistry , Microwaves , Color , Green Chemistry Technology/methods
14.
Clin Lab ; 70(6)2024 Jun 01.
Article in English | MEDLINE | ID: mdl-38868887

ABSTRACT

BACKGROUND: Polycythemia is a common medical problem, frequently acquired and reactive to secondary conditions. High-altitude-associated hypoxia contributes to the greater prevalence of polycythemia at altitude. Primary clonal polycythemia vera (PV), even though it is rare, requires a different therapeutic approach. Suspicion of PV usually drives the diagnostic workup of polycythemia. METHODS: In this retrospective lab record study, we collected all JAK2 tests requested over a three-year period. We analyzed requests that were made for the evaluation of polycythemia. Complete blood count (CBC) and imaging of the abdomen were collected. RESULTS: Out of 208 total requests, 136 were for the purpose of polycythemia evaluation. JAK2 mutation was positive (confirming the presence of PV) in 22 (16.7%) cases. PV patients have the usual demographics reported elsewhere. Additionally, PV patients exhibit distinct hemogram results featuring leukocytosis, thrombocytosis, and hypochromic microcytic red blood cells (RBCs) related to the associated iron deficiency. CONCLUSIONS: Many patients with polycythemia at altitude might be unnecessarily considered for an evaluation of PV, if hemoglobin/hematocrit is the sole deciding criterion. PV patients have a distinct CBC pattern that can be exploited to better select patients with polycythemia for further evaluation and thus reduce unnecessary workups.


Subject(s)
Altitude , Janus Kinase 2 , Polycythemia Vera , Humans , Polycythemia Vera/diagnosis , Polycythemia Vera/genetics , Polycythemia Vera/blood , Retrospective Studies , Female , Male , Middle Aged , Janus Kinase 2/genetics , Adult , Blood Cell Count , Aged , Mutation , Polycythemia/diagnosis , Polycythemia/blood
15.
Chem Asian J ; 19(17): e202400391, 2024 Sep 02.
Article in English | MEDLINE | ID: mdl-38825568

ABSTRACT

Direct installation of key functionalities in a molecule through C-H bond activation is one of the thrust areas as well as challenging task in organic synthesis. Particularly, introduction of chlorine in a molecule imparts additional benefits for further functionalizations as well as improves the electronic behaviour such as lipophilicity and polarity towards drug development process. The chlorinated molecules have also been established as efficient biologically relevant scaffolds. Current manuscript has been focused on the direct installation of the chlorine atom at various aromatic and aliphatic positions to produce functional molecules. The key highlight of the manuscript belongs to the site selectivity (regioselectivity) for the installation of chlorine functionality. Manuscript describes the advanced methods developed for the direct C-H chlorination reactions and further simplified for the chlorination reactions at various positions including aromatic (o-, m-, and p-), benzylic, heteroaromatic, and aliphatic positions. Directing groups (DGs) and the coordination with the catalyst is the key for the enhancement of regioselectivities during direct C-H chlorination reactions.

16.
Mar Pollut Bull ; 203: 116415, 2024 Jun.
Article in English | MEDLINE | ID: mdl-38723552

ABSTRACT

This study assessed the occurrence, origins, and potential risks of emerging perfluoroalkyl acids (PFAAs) for the first time in drinking water resources of Khyber Pakhtunkhwa, Pakistan. In total, 13 perfluoroalkyl carboxylic acids (PFCAs) with carbon (C) chains C4-C18 and 4 perfluoroalkyl sulfonates (PFSAs) with C chains C4-C10 were tested in both surface and ground drinking water samples using a high-performance liquid chromatography system (HPLC) equipped with an Agilent 6460 Triple Quadrupole liquid chromatography-mass spectrometry (LC-MS) system. The concentrations of ∑PFCAs, ∑PFSAs, and ∑PFAAs in drinking water ranged from 1.46 to 72.85, 0.30-8.03, and 1.76-80.88 ng/L, respectively. Perfluorobutanoic acid (PFBA), perfluorohexanoic acid (PFHxA), and perfluoropentanoic acid (PFPeA) were the dominant analytes in surface water followed by ground water, while the concentration of perfluorobutane sulfonate (PFBS), perfluorooctanoic acid (PFOA), perfluoroheptanoic acid (PFHpA), perfluorooctane sulfonate (PFOS), perfluorohexane sulfonate (PFHxS), perfluorononanoic acid (PFNA), perfluorodecanoic acid (PFDA), perfluoroundecanoic acid (PFUnDA), and perfluorododecanoic acid (PFDoDA) were greater than long-chain PFOA and PFOS. The correlation statistics, which showed a strong correlation (p < 0.05) between the PFAA analytes, potentially indicated the fate of PFAAs in the area's drinking water sources, whereas the hierarchical cluster analysis (HCA) and principal component analysis (PCA) statistics identified industrial, domestic, agricultural, and commercial applications as potential point and non-point sources of PFAA contamination in the area. From risk perspectives, the overall PFAA toxicity in water resources was within the ecological health risk thresholds, where for the human population the hazard quotient (HQ) values of individual PFAAs were < 1, indicating no risk from the drinking water sources; however, the hazard index (HI) from the ∑PFAAs should not be underestimated, as it may significantly result in potential chronic toxicity to exposed adults, followed by children.


Subject(s)
Drinking Water , Environmental Monitoring , Fluorocarbons , Water Pollutants, Chemical , Fluorocarbons/analysis , Drinking Water/chemistry , Water Pollutants, Chemical/analysis , Risk Assessment , Pakistan , Alkanesulfonic Acids/analysis , Humans , Environmental Exposure/statistics & numerical data , Multivariate Analysis
17.
RSC Adv ; 14(24): 17245-17260, 2024 May 22.
Article in English | MEDLINE | ID: mdl-38808237

ABSTRACT

A simple synthetic method was performed to design a novel series of polycyclic systems consisting of carbazole-thiazolidinone-chromone hybrids 4a-e and carbazole-thiazolidinone-pyrazole hybrids 5a-e in excellent yields. The methodology depended on the one-pot four-component reaction of 3-amino-9-ethylcarbazole, substituted isothiocyanates, ethyl bromoacetate and 6-methyl-3-formylchromone in ethanol under ultrasound waves at 50 °C to give the carbazole-thiazolidinone-chromone hybrids 4a-e. The latter isolated products were treated with hydrazine hydrate in ethanol under ultrasound waves at 50 °C affording the corresponding carbazole-thiazolidinone-pyrazole hybrids 5a-e. Spectral and analytical data confirmed the structures of all the synthesized compounds. The target compounds were screened for their in vitro anticancer activities against HCT116, PC3 and HepG2 cancer cell lines using the standard SRB method. Fortunately, both compounds 5dand5e were the most active against all cancer cell lines compared with doxorubicin and can be promising anticancer agents. Both bioactive products 5band5e were studied by the molecular docking to see how they bind with VEGFR-2 receptor. The results indicated that those compounds exhibited high affinities towards VEGFR-2 and established remarkably similar interactions to those of the powerful VEGFR-2-KDR.

18.
Int J Pharm ; 658: 124206, 2024 Jun 10.
Article in English | MEDLINE | ID: mdl-38734276

ABSTRACT

The constraints associated with current cancer therapies have inspired scientists to develop advanced, precise, and safe drug delivery methods. These delivery systems boost treatment effectiveness, minimize harm to healthy cells, and combat cancer recurrence. To design advanced drug delivery vehicle with these character, in the present manuscript, we have designed a self-healing and injectable hybrid hydrogel through synergistically interacting metal organic framework, CuBTC with the poly(vinyl alcohol) (PVA). This hybrid hydrogel acts as a localized drug delivery system and was used to encapsulate and release the anticancer drug 5-Fluorouracil selectively at the targeted site in response to the physiological pH. The hydrogel was formed through transforming the gaussian coil like matrix of PVA-CuBTC into a three-dimensional network of hydrogel upon the addition of crosslinker; borax. The biocompatible character of the hydrogel was confirmed through cell viability test. The biocompatible hybrid hydrogel then was used to encapsulate and studied for the pH responsive release behavior of the anti-cancer drug, 5-FU. The in vitro cytotoxicity of the drug-loaded hydrogel was evaluated against MCF-7 and HeLa cells. The study confirms that the hybrid hydrogel is effective for targeted and sustained release of anticancer drugs at cancer sites.


Subject(s)
Breast Neoplasms , Cell Survival , Drug Delivery Systems , Drug Liberation , Fluorouracil , Hydrogels , Metal-Organic Frameworks , Polyvinyl Alcohol , Humans , Fluorouracil/administration & dosage , Fluorouracil/chemistry , Fluorouracil/pharmacology , Breast Neoplasms/drug therapy , MCF-7 Cells , HeLa Cells , Cell Survival/drug effects , Hydrogels/chemistry , Female , Metal-Organic Frameworks/chemistry , Polyvinyl Alcohol/chemistry , Drug Delivery Systems/methods , Hydrogen-Ion Concentration , Drug Carriers/chemistry , Antimetabolites, Antineoplastic/administration & dosage , Antimetabolites, Antineoplastic/chemistry , Antimetabolites, Antineoplastic/pharmacology , Antineoplastic Agents/administration & dosage , Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology
19.
Spectrochim Acta A Mol Biomol Spectrosc ; 314: 124224, 2024 Jun 05.
Article in English | MEDLINE | ID: mdl-38574611

ABSTRACT

Overuse of doxycycline (DOXY) can cause serious problems to human health, environment and food quality. So, it is essential to develop a new sensing methodology that is both sensitive and selective for the quantitative detection of DOXY. In our current research, we synthesized a simple fluorescent probe 4,4'-bis(benzyloxy)-1,1'-biphenyl (BBP) for the highly selective detection of doxycycline by through fluorescence spectroscopy. The probe BBP displayed ultra-sensitivity towards doxycycline due to Forster resonance energy transfer (FRET). Fluorescence spectroscopy, density functional theory (DFT), 1H NMR titration, UV-Vis, and Job's plot were used to confirm the sensing mechanism. The charge transfer between the probe and analyte was further examined qualitatively by electron density differences (EDD) and quantitively by natural bond orbital (NBO) analyses. Whereas the non-covalent nature of probe BBP towards DOXY was verified by theoretical non-covalent interaction (NCI) analysis as along with Bader's quantum theory of atoms in molecules (QTAIM) analysis. Furthermore, probe BBP was also practically employed for the detection of doxycycline in fish samples, pharmaceutical wastewater and blood samples.


Subject(s)
Doxycycline , Fluorescent Dyes , Animals , Humans , Fluorescent Dyes/chemistry , Spectrometry, Fluorescence/methods , Fluorescence Resonance Energy Transfer , Magnetic Resonance Spectroscopy
20.
Int J Biol Macromol ; 267(Pt 1): 131388, 2024 May.
Article in English | MEDLINE | ID: mdl-38608982

ABSTRACT

We developed a facile method for the fabrication of a biodegradable delivery system composed of two blocks: curdlan and curcumin. This was achieved by chemical functionalization of curdlan through tosylation, amination followed by complexation with curcumin. A comprehensive evaluation of structural characterization and component stability showed that cur-cum complex exhibited better anticancer properties with enhanced thermal properties. The cur-cum complex shows pH sensitive sustained release behaviour with higher release at acidic pH and kinetic data of drug release follows the Korsmeyer-Peppas model. The cur-cum complex has ability to block the proliferation of the MCF-7 cell line as revealed by MTT assay which showed increased toxicity of cur-cum complex against these cell lines. The results obtained from western blot analysis demonstrated that the co-administration of cur and cum effectively induced apoptosis in MCF-7 cells. This effect was observed by a considerable upregulation of the Bcl-2/Bax ratio, a decline in mRNA expression of LDHA, level of lactate and LDH activity. The results clearly depict the role of functionalized curdlan as efficient carrier for curcumin delivery with prolonged, sustained release and enhanced bioavailability, thereby improving the overall anticancer activity.


Subject(s)
Apoptosis , Breast Neoplasms , Curcumin , Drug Liberation , beta-Glucans , Curcumin/pharmacology , Curcumin/chemistry , Curcumin/administration & dosage , beta-Glucans/chemistry , beta-Glucans/pharmacology , Humans , Breast Neoplasms/drug therapy , Breast Neoplasms/pathology , Breast Neoplasms/metabolism , MCF-7 Cells , Female , Apoptosis/drug effects , Antineoplastic Agents/pharmacology , Antineoplastic Agents/chemistry , Drug Carriers/chemistry , Drug Delivery Systems , Cell Proliferation/drug effects , Hydrogen-Ion Concentration
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