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INTRODUCTION: This study explores the under-investigated area of obesity-related discrimination and stigmatization across different countries, specifically comparing Spain (Europe) and Egypt (Middle East). METHODS: We conducted a cross-sectional observational study involving 2,090 participants from both countries. Participants completed three well-validated questionnaires to assess their attitudes towards obesity, experiences of weight-related stigma, and internalization of weight bias: Antifat Attitudes Scale (AFA), Stigmatizing Situations Inventory (SSI), and Weight Bias Internalization Scale (WBIS). Participants were categorized into four groups based on BMI and history bariatric surgery. RESULTS: Egyptian participants [BMI = 30.2±6.7 kg/m2 (range: 18.5 to 69.0 kg/m2)] showed significantly higher aversion towards obesity, as indicated by higher AFA score, compared to their Spanish counterparts [BMI = 35.4±10.1 kg/m2 (18.5 to 71,9 kg/m2)]. In contrast, Spanish participants reported higher levels of weight bias internalization with increasing BMI, while in Egypt, this association was negative. The association of bariatric surgery on stigma reduction also differed between the countries. Multivariate analysis revealed that residing in Egypt was an independent risk factor for higher scores in AFA and WBIS (Odds Ratio 8.20 [95% confidence interval: 6.78 to 9.62], p<0.001 and OR 6.28 [95% CI: 4.78 to 7.78], p<0.001; respectively). In contrast, Spaniards experienced more stigmatizing situations than Egyptians [OR -2.54 (95% CI: 6.78 to 9.62), p<0.001]. CONCLUSION: Our study underscore the complex and diverse nature of obesity-related attitudes across cultures. Understanding these cultural differences is crucial for developing effective, culturally sensitive strategies to tackle weight stigma. This research opens avenues for further studies and interventions tailored to cultural contexts.
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The current study aimed to explore the genotoxic impacts of the insecticide acetamiprid (ACP) on the myocardium and assess the ameliorative role of resveratrol (RSV). Male rats (10/group) were treated via oral route for 90 days: control; ACP (25â¯mg/kg); RSV (20â¯mg/kg); ACP+RSV. Peripheral blood micronucleus test, oxidative stress analysis, comet assay, 8-hydroxydeoxyguanosine and gene expression assessment were performed. The findings revealed that ACP has myocardial genotoxic effects, as demonstrated by increased micronucleus and 8-hydroxydeoxyguanosine formation and increased all comet parameters. Oxidative stress analysis demonstrated that ACP elevated H2O2 and NO levels while decreasing catalase and GST activities. Acetamiprid dysregulated the expression of genes related to oxidative stress and DNA damage response. However, RSV co-treatment resulted in significant protection against these genotoxic impacts. Resveratrol reduced DNA damage and restored the oxidative balance in the myocardium. Moreover, RSV modulated the Nrf2/HO-1 and Atm/P53 pathways, potentiating antioxidant defense and DNA repair.
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Nucleophosmin (NPM1) is a key nucleolar protein released from the nucleolus in response to stress stimuli. NPM1 functions as a stress regulator with nucleic acid and protein chaperone activities, rapidly shuttling between the nucleus and cytoplasm. NPM1 is ubiquitously expressed in tissues and can be found in the nucleolus, nucleoplasm, cytoplasm, and extracellular environment. It plays a central role in various biological processes such as ribosome biogenesis, cell cycle regulation, cell proliferation, DNA damage repair, and apoptosis. In addition, it is highly expressed in cancer cells and solid tumors, and its mutation is a major cause of acute myeloid leukemia (AML). This review focuses on NPM1's structural features, functional diversity, subcellular distribution, and role in stress modulation.
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Nucléolo Celular , Proteínas Nucleares , Nucleofosmina , Estrés Fisiológico , Humanos , Proteínas Nucleares/metabolismo , Nucléolo Celular/metabolismo , Animales , Fosfoproteínas/metabolismoRESUMEN
The novelty of this study lies in demonstrating a new approach to control wilt diseases using Jania ethyl acetate extract. In the current investigation, the potential impacts of Jania sp. ethyl acetate extract (JE) on Tomato Fusarium oxysporum wilt (FOW) have been studied. The in vitro antifungal potential of JE against F. oxysporum (FO) was examined. GC-MS investigation of the JE revealed that, the compounds possessing fungicidal action were Phenol,2-methoxy-4-(2-propenyl)-,acetate, Eugenol, Caryophyllene oxide, Isoespintanol, Cadinene, Caryophylla-4(12),8(13)-dien-5à-ol and Copaen. Jania sp. ethyl acetate extract exhibited strong antifungal potential against FO, achieving a 20 mmzone of inhibition. In the experiment, two different methods were applied: soil irrigation (SI) and foliar application (FS) of JE. The results showed that both treatments reduced disease index present DIP by 20.83% and 33.33% respectively. The findings indicated that during FOW, proline, phenolics, and the antioxidant enzymes activity increased, while growth and photosynthetic pigments decreased. The morphological features, photosynthetic pigments, total phenol content, and antioxidant enzyme activity of infected plants improved when JE was applied through soil or foliar methods. It is interesting to note that the application of JE had a substantially less negative effect on the isozymes peroxidase and polyphenol oxidase in tomato plants, compared to FOW. These reactions differed depending on whether JE was applied foliarly or via the soil. Finally, the use of Jania sp. could be utilized commercially as an ecologically acceptable method to protect tomato plants against FOW.
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Fusarium , Enfermedades de las Plantas , Solanum lycopersicum , Solanum lycopersicum/microbiología , Solanum lycopersicum/inmunología , Solanum lycopersicum/efectos de los fármacos , Fusarium/patogenicidad , Fusarium/efectos de los fármacos , Enfermedades de las Plantas/microbiología , Enfermedades de las Plantas/inmunología , Enfermedades de las Plantas/prevención & control , Algas Marinas , Inmunidad de la Planta/efectos de los fármacos , Extractos Vegetales/farmacología , Extractos Vegetales/química , Rhodophyta , Antifúngicos/farmacologíaRESUMEN
Mesenchymal-epithelial transition factor (MET) is a receptor tyrosine kinase that serves a critical function in numerous developmental, morphogenic, and proliferative signaling pathways. If dysregulated, MET has been shown to be involved in the development and survival of several cancers, including non-small cell lung cancer (NSCLC), renal cancer, and other epithelial tumors. Currently, the clinical efficacy of FDA approved MET inhibitors is limited by on-target acquired resistance, dose-limiting toxicities, and less than optimal efficacy against brain metastasis. Therefore, there is still an unmet medical need for the development of MET inhibitors to address these issues. Herein we report the application of structure-based design for the discovery and development of a novel class of brain-penetrant MET inhibitors with enhanced activity against clinically relevant mutations and improved selectivity. Compound 13 with a MET D1228N cell line IC50 value of 23 nM showed good efficacy in an intracranial tumor model and increased the median overall survival of the animals to 100% when dosed orally at 100 mg/kg daily for 21 days.
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OBJECTIVE: Preparation and characterization of nano-emulsion formulations for Asparagus densiflorus aerial and root parts extracts. SIGNIFICANCE: Genus Asparagus is known for its antimicrobial and anticancer activities, however, freeze dried powder of aqueous - alcoholic extract prepared in this study, exhibited a limited water solubility, limiting its therapeutic application. Thus, encapsulation of its phytochemicals into nano-emulsion is proposed as a solution to improve water solubility, and facilitate its clinical translation. METHODS: the composition of extracts for both aerial and root parts of Asparagus densiflorus was identified by HPLC and LC-MS analysis. Nano-emulsion was prepared via homogenization where a mixture of Castor oil: phosphate buffered saline (10 mM, pH 7.4): Tween 80: PEG 600 in a ratio of 10: 5: 2.5: 2.5, respectively. Nano-emulsion formulations were characterized for particle size, polydispersity index (PDI), zeta potential, TEM, viscosity and pH. Then, the antibacterial and anticancer activities of nano-emulsion formulations versus their pure plant counterparts was assessed. RESULTS: The analysis of extracts identified several flavonoids, phenolics, and saponins which were reported to have antimicrobial and anticancer activities. Nano-emulsion formulations were monodispersed with droplet sizes ranging from 80.27 ± 2.05 to 111.16 ± 1.97 nm, and polydispersity index ≤0.3. Nano-emulsion formulations enhanced significantly the antibacterial (multidrug resistant bacteria causing skin and dental soft tissues infections) and anticancer (HuH7, HEPG2, H460 and HCT116) activities compared to their pure plant extract counterparts. CONCLUSION: Employing a nano-delivery system as a carrier for phytochemicals might be an effective strategy to enhance their pharmacological activity, overcome their limitations, and ultimately increase their potential for clinical applications.
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A series of 20 new structure-modified quinolin-2-one derivatives were prepared for biological evaluation. This was successfully achieved based on chemoselective reactions of heterocyclic amides with acrylic acid derivatives, which gave 3-[2-oxoquinolin-1-(2H)-yl] propanoic acid derivatives (N-substitution via a unique behavior). The ester was reacted with hydrazine to afford the corresponding hydrazide. Both the corresponding ester and hydrazide were used as building blocks to modify the quinolone structure and give N-hydroxyl propanamides, oxadiazoles, and thiosemicarbazides. The corresponding carboxylic acid and hydrazide were used to prepare several amides: N-alkyl-3-[2-oxoquinolin-1(2H)-yl]propanamides via azide and dicyclohexyl carbodiimide coupling methods. Among derivatives, compound 9e exhibited potent cytotoxicity against MCF-7 cells with an IC50 value of 1.32 µM compared to doxorubicin with an IC50 value of 1.21 µM. Additionally, it caused potent EGFR inhibition by 97% with an IC50 value of 16.89 nM compared to Erlotinib with an IC50 value of 29.8 nM. Finally, the binding mode of compound interactions toward EGFR was highlighted using a molecular docking study; compound 9e exhibited good binding affinity with a binding energy of -17.89 kcal/mol, and it formed H-bond interactions with Met 769 as the key amino acid of interaction. Accordingly, compound 9e may be developed as an EGFR-oriented chemotherapeutic antibreast cancer agent.
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The meta-analysis sought to evaluate and compare the effect of obesity on surgical site wound problems in subjects after primary ovarian cancer surgery. The results found by this meta-analysis were analyzed, and then odds ratio (OR) and mean difference (MD), at 95% confidence intervals (CIs), were calculated. These models might be dichotomous or contentious, random, or fixed effect models. The current meta-analysis included nine exams from 2009 to 2023, including 4362 females with primary ovarian cancer surgeries. Obesity had a significantly higher risk of surgical site wound infections (OR, 2.90; 95% CI, 2.27-3.69, p < 0.001), and wound problems (OR, 4.14; 95% CI, 1.83-9.34, p < 0.001) compared to non-obesity in females with primary ovarian cancer surgeries. It was revealed, by examining the data, that obesity was associated with significantly higher incidence of surgical site wound infections, and wound problems compared to non-obesity in females with primary ovarian cancer surgeries. However, attention should be given to the values because some of the comparisons included a small number of chosen studies,.
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Obesidad , Neoplasias Ováricas , Infección de la Herida Quirúrgica , Humanos , Femenino , Infección de la Herida Quirúrgica/epidemiología , Infección de la Herida Quirúrgica/etiología , Neoplasias Ováricas/cirugía , Obesidad/complicaciones , Obesidad/cirugía , Obesidad/epidemiología , Factores de Riesgo , Incidencia , Oportunidad RelativaRESUMEN
Irreversible cardiotoxicity limits the clinical application of doxorubicin (DOX). DOX-induced cardiotoxicity has been associated with induction of senescence and activation of the p38 MAPK pathway. Losmapimod (LOSM), an orally active p38 MAPK inhibitor, is an anti-inflammatory agent with cardioprotective effects. Nevertheless, the effect of LOSM against DOX-induced cardiotoxicity has not been reported. In this study, we determined the effects of LOSM on DOX-induced chronic cardiotoxicity in C57BL/6â¯N mice. Five-week-old C57BL/6â¯N mice were fed diet containing LOSM (estimated daily intake 12â¯mg/kg/day) or a control diet for four days. Thereafter, mice were randomized to receive six weekly intraperitoneal injections of either DOX (4â¯mg/kg) or saline. Three days after the last injection, cardiac function was assessed by trans-thoracic echocardiography. Activation of p38, JNK, and ERK1/2 MAPKs were assessed by immunoblotting in the heart and liver. Gene expressions of senescence, inflammatory, oxidative stress, and mitochondrial function markers were quantified using real-time PCR and serum inflammatory markers were assessed by Luminex. Our results demonstrated that LOSM attenuated p38 MAPK activation, ameliorated DOX-induced cardiac dysfunction, and abrogated DOX-induced expression of the senescence marker p21Cip1. Additionally, LOSM demonstrated anti-inflammatory effects, with reduced cardiac Il-1α and Il-6 gene expression in DOX-treated mice. Systemic inflammation, assessed by serum cytokine levels, showed decreased IL-6 and CXCL1 in both DOX-treated mice and mice on LOSM diet. LOSM significantly increased mitofusin2 gene expression, which may enhance mitochondrial fusion. These findings underscore the potential therapeutic efficacy of p38 MAPK inhibition, exemplified by LOSM, in ameliorating DOX-induced cardiotoxicity, senescence, and inflammation.
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Obesity is a well-known risk factor for testicular function; however, dulaglutide's effect on the testis in obesity has received little attention. Currently, clinicians prescribe the antidiabetic drug dulaglutide only off-label for weight management in non-diabetics. Investigating the impact of this novel compound on obesity is critical for determining whether it has any disruptive effects on testicular cells. We used a well-known animal model of high-fat diet-induced obesity in this investigation, and testicular dysfunction was determined by sperm DNA damage, spermatocyte chromosomal abnormalities, and spermiogram analysis. Following a 12-week high-fat diet challenge, mice were randomly assigned to dulaglutide (0.6â¯mg/kg/day) or saline treatments for five weeks. Testes and sperm cells were collected 24â¯h after the last dulaglutide injection. Untreated obese mice had a lower testes/body weight ratio, more sperm DNA damage, diakinesis-metaphase I chromosomal abnormalities, a lower sperm count/motility, more cell morphological defects, and an altered testicular redox balance. In obese mice, dulaglutide injection efficiently restored all disturbed parameters to their control levels. Dulaglutide injection into healthy mice exhibited no significant harmful effects at the applied regimen. As a result, we infer that dulaglutide therapy might bring obese men additional benefits by recovering testicular dysfunction induced by obesity.
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Dieta Alta en Grasa , Modelos Animales de Enfermedad , Péptidos Similares al Glucagón , Fragmentos Fc de Inmunoglobulinas , Obesidad , Proteínas Recombinantes de Fusión , Testículo , Animales , Masculino , Fragmentos Fc de Inmunoglobulinas/farmacología , Obesidad/tratamiento farmacológico , Péptidos Similares al Glucagón/análogos & derivados , Péptidos Similares al Glucagón/farmacología , Péptidos Similares al Glucagón/uso terapéutico , Dieta Alta en Grasa/efectos adversos , Ratones , Proteínas Recombinantes de Fusión/farmacología , Testículo/efectos de los fármacos , Testículo/patología , Testículo/metabolismo , Daño del ADN/efectos de los fármacos , Espermatozoides/efectos de los fármacos , Hipoglucemiantes/farmacología , Motilidad Espermática/efectos de los fármacos , Ratones Endogámicos C57BL , Aberraciones Cromosómicas/efectos de los fármacos , Enfermedades Testiculares/tratamiento farmacológicoRESUMEN
The unique structure of spirooxindoles and their ability to feature various pharmacophoric motifs render them privileged scaffolds for tailoring new multitarget anticancer agents. Herein, a stereoselective multicomponent reaction was utilized to generate a small combinatorial library of pyrazole-tethered spirooxindoles targeting DNA and CDK2 with free radical scavenging potential as an extra bonus. The designed spirooxindoles were directed to combat NSCLC via inducing apoptosis and alleviating oxidative stress. The series' absolute configuration was assigned by X-ray diffraction analysis. Cytotoxicity screening of the developed spirooxindoles against NSCLC A549 and H460 cells compared to normal lung fibroblasts Wi-38 revealed the sensitivity of A549 cells to the compounds and raised 6e and 6h as the study hits (IC50 â¼ 0.09 µM and SI > 3). They damaged DNA at 24.6 and 35.3 nM, and surpassed roscovitine as CDK2 inhibitors (IC50 = 75.6 and 80.2 nM). Docking and MDs simulations postulated their receptors binding modes. The most potent derivative, 6e, induced A549 apoptosis by 40.85% arresting cell cycle at G2/M phase, and exhibited antioxidant activity in a dose-dependent manner compared to Trolox as indicated by DPPH scavenging assay. Finally, in silico ADMET analysis predicted the drug-likeness properties of 6e.
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Heavy metals are crucial carcinogenic agents threatening the environment and living habituates. Among them, arsenic (As) is an important metalloid that is categorized as a group I toxic carcinogen. Roxarsone (RX) is an organoarsenic antibiotic compound primarily used as a veterinarian drug and growth promoter for poultry animals. The extensive usage of RX increased the accumulation of As in living beings and the ecosystem. Therefore, we have prepared an electrochemical sensor based on 3D bismuth oxybromide with 2D selenium-doped graphitic carbon nitride (BOB/SCN) electrocatalyst for the rapid detection of RX. The elemental and structural details were thoroughly investigated with several spectroscopic techniques. The electrochemical properties were measured by impedance and voltammetric measurements. The electrocatalytic behavior toward the RX was estimated with different voltammetric methods. Therefore, our BOB/SCN-based electrochemical sensor demonstrated a low detection limit (2.3 nM), low quantification value (7.7 nM), optimal sensitivity (0.675 µA µM-1 cm-2), and good linear ranges (0.01-77 and 77-857 µM). Additionally, this sensor showed good electrochemical performance and was applied to monitor the RX in various real samples with remarkable recoveries. Based on these results, our BOB/SCN sensor is a promising electrochemical platform for determining RX.
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OBJECTIVE: Despite the widespread use of cyanoacrylate glue (CA) as an alternative for wound closure, its potential as a sole skin substitute material in periocular skin surgery remains unexplored. The primary objective was to determine the viability of CA as a sole skin substitute in periocular skin surgery after excision. DESIGN: Single-centre retrospective observational case series. METHODS: All patients were treated at the McGill University Health Centre from August 2023 to November 2023, where CA served as the sole skin substitute material after periocular skin excision. RESULTS: Three female and one male patient, with a mean age of 75 years, received treatment with CA after skin excision for both cancerous and benign skin lesions. Specifically, histopathology revealed 2 cases of basal cell carcinoma, 1 case of squamous cell carcinoma in situ, and 2 benign lesions. The skin defects after excision ranged from 4â¯×â¯3 mm to 15â¯×â¯30 mm. No complications were observed between CA graft insertion and final skin re-epithelization. Complete re-epithelization was achieved in all patients at final follow-up without evidence of excessive skin contraction. CONCLUSIONS: This study presents a novel approach by using CA as a skin substitute material in periocular skin excisions. Its liquid form allows for easy application and conforms well to irregular wound surfaces. CA may offer economic advantages, including lower material cost and shorter surgical operating times, compared with traditional skin substitutes. Further research is needed to comprehensively evaluate CA's role as a skin substitute in periocular skin reconstruction.
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Ultrasound (US) is a promising tool for skeletal muscle assessment; however, US studies have scarcely focused on Arabic populations. This study examined the association of handheld US indicators and bioelectrical impedance analysis (BIA) parameters in healthy Arabic females. A cross-sectional study was conducted on 60 healthy Arabic females whose muscle thickness (MT) and cross-sectional area (CSA) of the rectus femoris (RF) were measured alongside their MT and pennation angle (PA) of the medial gastrocnemius (MG) muscle (both muscles on the dominant side). Anthropometric and body composition analyses quantified fat-free mass (FFM) and appendicular skeletal muscle mass (ASMM). Muscle strength was assessed using a handgrip dynamometer, and physical activity levels were recorded with the Global Physical Activity Questionnaire (GPAQ). The CSA of the RF and the MT of both the RF and MG correlated significantly with FFM and ASMM. The PA of MG showed no significant correlations with ASMM, FFM, or handgrip strength. The CSA of RF was significantly correlated with handgrip strength (r = 0.313, p = 0.015), while the PA of MG correlated positively with GPAQ score (r = 0.346, p = 0.007). The CSA of RF significantly predicted both ASMM (ß = 0.883, p = 0.0002) and FFM (ß = 1.935, p = 0.0001). In conclusion, handheld US parameters, especially the RF's CSA, correlate with and can predict BIA-based FFM and ASMM in healthy females.
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INTRODUCTION: Femoral fractures account for â¼1% to 2% of all pediatric bone injuries and are a common occurrence in children. The conservative approach, employing either a single or one-and-a-half spica casts, has been traditionally favored, yielding satisfactory outcomes in select cases. This study aims to compare both procedures regarding functional and radiologic outcomes, complications, and parents' satisfaction. METHODS: In this randomized controlled trial, we enrolled 84 pediatric patients, aged between 2 and 6 years, presenting with femoral fractures. Participants were randomly allocated into 2 groups; one receiving single-limb spica cast fixation (n=42) and the other receiving one-and-a-half spica cast fixation (n=42). We assessed postprocedural functional and radiologic outcomes. Other evaluations focused on parental ease in maintaining hygiene for the casted child, the child's mobility capabilities including standing and crawling, and the incidence of skin complications. RESULTS: No significant variance was observed between the 2 groups concerning the time to bone union, and the overall complication rates. Parental satisfaction was notably higher in the single-limb spica group, particularly regarding the ease of maintaining hygiene for the casted child and the child's mobility while encased in the cast (P<0.001). Furthermore, a significant correlation was identified between the one-and-a-half spica application and the increased occurrence of skin pressure ulcers (P<0.001). CONCLUSION: Both single-limb and one-and-a-half spica cast applications demonstrated comparable results in functional and radiologic outcomes, as well as in complication rates. However, parents favored the single-limb method due to its facilitation of a more manageable lifestyle for both the child and their parents. These considerations suggest that the single-limb hip spica cast fixation may be preferable in managing pediatric femoral fractures. LEVEL OF EVIDENCE: Level II.
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c-MET and STAT-3 are significant targets for cancer treatments. Here, we describe a class of very effective dual STAT-3 and c-MET inhibitors with coumarin-based thiazoles (3a-o) as its scaffold. Spectroscopic evidence (NMR, HRMS, and HPLC) validated the structural discoveries of the new compounds. The cytotoxic activity of these compounds was also tested against a panel of cancer cells in accordance with US-NCI guidelines. Compound 3g proved to be active at 10 µM, thus it was automatically scheduled to be tested at five doses. Towards SNB-75 (CNS cancer cell line), compound 3g showed notable in vitro anti-cancer activity with GI50 = 1.43 µM. For the molecular targets, compound 3g displayed potent activity towards STAT-3 and c-MET having IC50 of 4.7 µM and 12.67, respectively, compared to Cabozantinib (IC50 = 15 nM of c-MET) and STAT-3-IN-3 (IC50 = 2.1 µM of STAT-3). Moreover, compound 3g significantly induced apoptosis in SNB-75 cells, causing a 3.04-fold increase in apoptotic cell death (treated cells exhibited 11.53 % overall apoptosis, against 3.04 % in reference cells) and a 3.58-fold increase in necrosis. Moreover, it arrests cells at the G2 phase. Dual inhibition of c-MET and STAT-3 protein kinase was further validated using RT-PCR. The target compound's binding mechanism was determined by the application of molecular docking.
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Chronic wounds (CWs) treatment still represents a demanding medical challenge. Several intrinsic physiological signals (i.e., pH) help to stimulate and support wound healing. CWs, in fact, are characterized by a predominantly alkaline pH of the exudate, which acidifies as the wound heals. Therefore, pH-responsive wound dressings hold great potential owing to their capability of tuning their functions according to the wound conditions. Herein, porous chitosan (CS)-based scaffolds loaded with cellulose nanocrystals (CNCs) and graphene oxide (GO) were successfully fabricated using a freeze-drying method. CNCs were extracted from bagasse pulps fibers through acid hydrolysis. GO was synthesised by Hummer's method. The scaffolds were then ionically cross-linked using the amino acid L-Arginine (Arg), as a bioactive agent, and tested as potential pH-responsive wound dressing. Notably, the effect of CNCs and GO singly and simultaneously loaded within the CS-Arg scaffolds was investigated. The modulation of CNCs and GO content within CS-Arg scaffolds facilitated the development of scaffolds with an optimal pH-dependent swelling ratio capability and extended degradation time. Furthermore, CS/CNC/GO-Arg scaffolds exhibited tuned biological features, in terms of antimicrobial activity, cellular proliferation/migration ability, and the expression of extracellular matrix specific markers (i.e., elastin and collagen I) related to wound healing in human dermal fibroblasts.
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This article presents a compact, wide-angle, polarization-insensitive metamaterial harvester that can efficiently harvest electromagnetic (EM) energy in the S, C, X, and Ku bands. The harvester's unit cell consists of a split ring resonator, two strip lines, and two split strip lines, giving it a total size of (10 × 10) mm2. Each split gap is filled with a 50 Ω resistive load. The input impedance of the harvester is precisely designed to match that of free space, allowing for efficient absorption of EM power and appropriate redirection towards the resistive loads. The harvester's performance is also evaluated for various polarization and incident angles, considering the Transverse Electric and Transverse Magnetic modes. The simulation results reveal that the proposed harvester exhibits a notably greater conversion efficiency of around > 95%. The simulation outcomes were carefully validated through experimental tests conducted in an anechoic chamber using a 3 × 3 cell array of the proposed design. This ensured the accuracy and reliability of the results. The strong correlation between the experimental data and the full-wave simulations strongly supports the effectiveness of the proposed harvester. Therefore, the demonstrated efficiency and compact size make it a perfect fit for energy harvesting systems in wireless sensor networks.
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A series of novel piperazine-based bis(thiazoles) 13a-d were synthesized in moderate to good yields via reaction of the bis(thiosemicarbazones) 7a, b with an assortment of C-acetyl-N-aryl-hydrazonoyl chlorides 8a-f. Similar treatment of the bis(thiosemicarbazone) 7a, b with C-aryl-N-phenylhydrazonoyl chlorides 10a, b afforded the expected bis(thiadiazole) based piperazine products 13b-d in reasonable yields. Cyclization of 7a, b with two equivalents of α-haloketones 14a-d led to the production of the corresponding bis(4-arylthiazol)piperazine derivatives 15a-h in good yields. The structures of the synthesized compounds were confirmed from elemental and spectral data (FTIR, MALDI-TOF, 1H, and 13C NMR). The cytotoxicity of the new compounds was screened against hepatoblastoma (HepG2), human colorectal carcinoma (HCT 116), breast cancer (MCF-7), and Human Dermal Fibroblasts (HDF). Interestingly, all compounds showed promising cytotoxicity against most of the cell lines. Interestingly, compounds 7b, 9a, and 9i exhibited IC50 values of 3.5, 12.1, and 1.2 nM, respectively, causing inhibition of 89.7%, 83.7%, and 97.5%, compared to Erlotinib (IC50 = 1.3 nM, 97.8% inhibition). Compound 9i dramatically induced apoptotic cell death by 4.16-fold and necrosis cell death by 4.79-fold. Compound 9i upregulated the apoptosis-related genes and downregulated the Bcl-2 as an anti-apoptotic gene. Accordingly, the most promising EGFR-targeted chemotherapeutic agent to treat colon cancer was found to be compound 9i.
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Real-time monitoring and tracking of extreme toxins that penetrate into living cells by using biocompatible, low-cost visual detection via fluorescent monitors are vitally essential to reduce health hazards. Herein, we report a simple engineering design of biocompatible and fluorescent sensors/trackers for real-time monitoring and ultra-trace tracking (up to ppb) of extremely toxic substances (such as arsenic species) in living cells. The biocompatible As(V) sensor (BAS) design is fabricated via successful dressing/decoration process of 2-hydroxy 5-methyl isophthalaldehyde fluorescent receptor into hierarchical organic-inorganic carriers that have micro-hollow geodes, swirled caves and nest-shaped cages, and uniform cubic structures. The BAS monitors show evidence for the selective trapping/detecting/tracking of As(V) species in biological cells (i.e., HeLa cells) despite the coexistence of highly competitive and interfered species. Our simple batch-contact sensing assays shows real-space evidence of the continuous monitoring of As(V) species in HeLa cells with ultra-sensitive detection (i.e., with a low detection limit of 0.149 ppb) and rapid recognition (i.e., in the order of seconds). Significantly, the BAS monitors did not affect the cell population and achieved low cytotoxicity and high cell viability during the monitoring/tracking process inside HeLa cells. The high biocompatibility of BAS remarkably allows precise quantification and real-time monitoring/tracking of toxicant targets in living cells.