In this study, gold nanoparticles (AuNPs) were developed using Laurus nobilis (LN) leaf extract, and their cytotoxic and antimigratory effects were evaluated in vitro to investigate their potential in cancer treatment and wound healing. AuNPs were synthesized by green reduction of HAuCl₄ using LN extract at room temperature. Characterization was carried out by UV-Vis, TEM, SEM, EDX, FTIR and DLS. Cytotoxicity was assessed by MTT assay in four cancer cell lines: A549, MDA-MB-231, SH-SY5Y, and L929. An in vitro wound healing assay using A549 cells was conducted to assess the antimigratory effects. Statistical analysis included IC₅₀ values, effect size (Cohen’s d), AUC, and non-parametric testing. LN-AuNPs showed a sharp plasmon resonance peak ( 540 nm), narrow size distribution ( 69 nm), and minimal aggregation. Spectral and elemental data confirmed phytochemical-mediated reduction. LN-AuNPs significantly decreased cell viability in all tested lines, with the lowest IC₅₀ observed in L929 cells (0.02 µg/mL). All groups exhibited large effect sizes and statistical significance. Additionally, LN-AuNPs markedly inhibited cell migration in A549 cells, confirming their antimigratory potential. This is the first study to report both cytotoxic and wound-healing-inhibitory effects of LN-AuNPs. The findings highlight LN-AuNPs as promising green-synthesized nanoplatforms for integrated cancer treatment and regenerative medicine applications.
Targeted drug therapy is very important for the treatment of triple-negative breast cancer (TNBC), and the development of carrier systems to deliver apoptosis-inducing proteins such as TRAIL to cells is important in cancer therapy. In this study, a nanosystem formulation (TRAIL-PEG-Apt-PLGA) encapsulating TNBC-targeted aptamer-bound-TRAIL protein was performed and the efficacy of this system was evaluated in a mouse tumor model. The characterization of TRAIL-PEG-Apt-PLGA was confirmed by FTIR, NTA and SEM microscopy. The efficacy of TRAIL-PEG-Apt-PLGA was evaluated by in vitro release assays and interactions with TNBC cells (MDA-MB-231) and healthy breast cells (MCF-10A). TRAIL-PEG-Apt-PLGA was administered intravenously to NOD/SCID gamma mouse breast tumors and evaluated in vivo. Pharmacokinetics, bioavailability testing, histological staining (DR4/DR5, TUNEL, HE staining) and molecular alterations with PCR array were evaluated in tumor tissues. TRAIL-PEG-Apt-PLGA induced apoptosis in both in vivo and in vitro studies. It was found that it regulated cellular responses along with apoptotic mechanisms in cells without developing resistance in suppressing tumor growth by making changes on Atf2, Casp8, Bcl2 and Irf5 genes and proteins. As a result, the biotechnological drug potential of TRAIL was discovered in an aptamer-bound nanosystem for the treatment of triple-negative breast cancer and innovative applications for clinical use.
A series of nimesulide-derived ureas were synthesized in high yields (69–91%) via a novel synthetic method under organotin catalysis. The structural characterization of the synthesized compounds was determined using a variety of spectroscopic methods, including ¹H NMR, ¹³C NMR, FTIR, and HRMS. Following initial screening, selected compounds were further evaluated using specific biological assays, including cytotoxicity analysis, apoptosis assessment by Annexin V/PI staining, analysis of Bax and Bcl-2 protein expression, and detection of DNA fragmentation using AO/EB staining. These evaluations were carried out in a variety of cell lines, including MDA-MB-231 (human triple-negative breast cancer cells), HeLa (human cervical cancer cells), PC-3 (androgen-independent human prostate cancer cells), MKN-45 (human gastric cancer cells), U87 (human glioblastoma cancer cells), and HUVEC (human umbilical vein endothelial cells). Three of the compounds demonstrated efficacy in MDA-MB-231 cells, resulting in increased AO/EB staining and annexin-V-PI binding levels, and increased Bax/Bcl-2 ratios. Numerous studies implicate MetAP2 in angiogenesis. MetAP2 stimulates cancer cell proliferation when it is upregulated and appears to play an essential role in tumor progression. In connection with the cell lines studied in this study, a crucial MetAP2 enzyme target was selected for in silico studies to support the experimental outcomes. The three promising compounds have been demonstrated to accelerate cell apoptosis and inhibit cell division by targeting MetAP2. The compounds synthesized in this study potential to overcome the challenges of targeted therapies in triple-negative breast cancer. Alongside these findings, the antioxidant potential of the synthesized compounds was evaluated using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay. One of the compounds exhibited a radical scavenging activity comparable to the reference standard. In-silico molecular modeling studies were conducted in the final phase to evaluate the newly designed inhibitors as potential anticancer and antioxidant drug candidates. The most likely conformations of the MetAP2-ligand complex were sorted according to the free energy of binding score (kcal/mol) and agree with the experimental inhibition values. The computational results suggest that the newly synthesized compounds may be potential anticancer drug candidates.
In this study, Fe3O4 nanoparticles (NPs) were synthesized via a green approach using Alchemilla vulgaris (AV) extract and comparatively evaluated against bare Fe3O4 NPs in terms of physicochemical characteristics and biological responses. Comprehensive analyses confirmed successful nanoparticle formation and the presence of AV derived surface functionalization. Biological assessments demonstrated dose dependent cytotoxic effects in A549, MDA MB 231, SH SY5Y, and L929 cell lines for both nanoparticle formulations. While differences between formulations were observed depending on cell type and dose, AV-Fe3O4 NPs did not exhibit consistently higher cytotoxicity across all cancer cell lines. However, variations in cytotoxic response patterns suggested that surface functionalization influences nano bio interactions. Intracellular reactive oxygen species (ROS) levels increased with nanoparticle concentration in all cell lines, whereas ROS production did not consistently differ between Fe3O4 and AV-Fe3O4 NPs. Notably, differences in cell viability were observed under comparable ROS levels, indicating that cytotoxic effects are not solely governed by ROS magnitude. These findings suggest that AV derived surface functionalization modulates the cellular response to oxidative stress rather than directly enhancing ROS generation. Overall, this study highlights the role of plant mediated surface chemistry in tuning nano bio interface interactions and influencing ROS related cytotoxic mechanisms in iron oxide nanoparticle systems.
INTRODUCTION:Wound healing is a complex, multistage process regulated by inflammatory, oxidative, regenerative processes, and marine-derived compounds are increasingly recognized for their therapeutic potential. OBJECTIVE:This study evaluated the wound-healing efficacy of an aqueous Posidonia oceanica (PO) leaf extract in standardized full-thickness mice wounds, compared with alginate hydrogel (AH), fusidic acid + Centella asiatica cream (FM), and untreated controls (NC). MATERIALS AND METHODS:Ninety-six (6-8-week-old) male BALB/c mice were randomized into four groups; four 4-mm dorsal wounds were created on each animal, and treatments were applied topically once daily for 14 days. Wound healing was assessed by planimetric wound area measurements, histological evaluations, biochemical analysis of oxidative stress, inflammatory biomarkers and growth factors, hydroxyproline levels, and gene expression analysis of MMP-2 and MMP-9. RESULTS:Application of PO extract significantly reduced wound areas from day 3 onward compared with NC and FM groups, with effects comparable to AH group by day 14. PO treatment increased epithelialization, fibroblast growth factor, and hydroxyproline levels, while reducing macrophage infiltration, oxidative stress, and inflammatory cytokines. Genomic analyses further indicated that topical PO extract significantly downregulated the expression of MMP-2 and MMP-9, supporting balanced extracellular matrix remodeling. CONCLUSIONS:PO extract promoted wound healing comparable to AH and superior to FM treatment, providing the first in vivo evidence for P. oceanica as a promising marine-derived therapeutic candidate for wound care.
Despite the efforts to treat cancer with chemotherapeutic agents targeting different mechanisms, cancer is still one of the most important health problems today. The increase in cancer incidence has led researchers to discover new, effective, and selective molecules. For this purpose, novel thiosemicarbazide (3a-3i) and 1,3,4-thiadiazole derivatives (4a-4i) were synthesized from clopidogrel bisulfate and their cytotoxic activities were investigated against glioblastoma (U87) cell line and healthy fibroblast (L929) cell line by MTT assay. Among the synthesized compounds; 3b, 3g, 4b, 4d, and 4i exhibited higher cytotoxic activities than the standard drug paclitaxel against U87 cancer cells. Cell apoptosis was detected by Bax, Bcl-2, caspase-3 activity, and Annexin V assay. The results displayed that compounds 3b, 3g, 4b, 4d, and 4i induced apoptosis in U87 cells. Moreover, all compounds were investigated for DNA methyltransferase (DNMT) activity in U87 cells. DNMT enzyme activity was decreased in these compounds' treated cells. Cyclohexyl ring-bearing compound 4d, which showed the highest activity against U87 cells, was the most potent inhibitor of DNMT with an IC50 value of 5.78 +/- 1.07 mu M compared to paclitaxel (82.05 +/- 4.67 mu M). Molecular docking studies were also performed to identify the interactions between the compounds and the active sites of DNMT.
Breast cancer is the second leading cause of mortality among women globally. In this study, novel promising urea derivatives containing a 4-phenyl-5-sulphanylidene-4,5-dihydro-1H-1,2,4-triazole group were synthesized and evaluated for their biological activities against breast cancer. The cytotoxicity and apoptotic profiles of these compounds were assessed on the MCF7 breast cancer cell line and the L929 fibroblast cell line. Compound 5c exhibited the strongest anticancer activity against MCF7 cells with an IC50 value of 56.97+4.22 mu M, while it showed significantly lower cytotoxicity against L929 cells (IC50 = 1651+18.39 mu M). Compound 5c also induced early apoptosis in MCF7 cells, with an apoptosis rate of 18.40% and 5.28%, respectively. Additionally, the EGFR inhibitory activities of the synthesized compounds were evaluated, with compound 5i demonstrating the most potent EGFR inhibition, showing an IC50 value of 35.1 nM. These results suggest that compound 5c likely exerts its anticancer effects through mechanisms other than EGFR inhibition, while compound 5i has significant potential as an effective EGFR inhibitor. Molecular modeling studies were conducted to suggest putative binding interactions of compounds 5d, 5e and 5i with wildtype hEGFR. Further studies are warranted to explore their activity against other cancer types.
Hydrazone derivatives are one of the scaffolds frequently used in new drug development studies. Due to the promising pharmacological effects of the hydrazone structure, fifteen new hydrazide-hydrazone compounds containing flurbiprofen 1,2,4-triazole were synthesized in this study and their in vitro anticancer effects were tested. All compounds were tested for cytotoxic effects against breast cancer cell lines (MCF-7 and MDA-MB231), and glioblastoma cell line (U87) by using MTT assay. Among the synthesized compounds, compounds 7a and 7c exhibited the most potent cytotoxic activity with IC50 values of 7.80 ± 1.20 µM and 2.40 ± 0.93 µM against MCF-7 cell line, while compound 7a showed the highest activity with IC50 value of 7.63 ± 1.05 µM against MDA-MB231 cell line. In addition, compounds 7c and 7n presented cytotoxic activity with IC50 values of 10.31 ± 4.63 µM and 10.81 ± 6.11 µM against U87 cell line. The possible cytotoxic effects of compounds on mouse fibroblast cell line (L929) were assessed for their safety and compounds 7a, 7c, and 7n were found less toxic than 5-fluorourasil. Additionally, compound 7c was further studied to investigate its effects on apoptosis and PI3K activity, which play a role in cancer development. The results showed that compound 7c increased apoptosis in MCF-7 cells and it displayed PI3K enzyme inhibitory activity. Our study revealed that the synthesized hydrazone compounds have the potential to be lead compounds for further studies on cancer.
Acanthamoeba spp. potansiyel patojenik serbest yaşayan amipler arasında yer almakta olup insanlarda keratit ve granulomatöz ensefalite neden olabilmektedir. Bu çalışmada, Rosa gallica ve Picea orientalis'in yaprak özütlerinin Acanthamoeba spp.’ye karşı anti-amebik ve iki faklı hücre hattında sitotoksik aktivitelerinin araştırılması amaçlanmıştır. Çevresel örnekten izole edilen Acanthamoeba spp. izolatı, Escherichia coli ile kaplanmış besleyici değeri olmayan agar kültüründe çoğaltılmıştır. Farklı konsantrasyonlardaki özütler ile inkübe edilen parazitin canlılığı, trypan mavisi yöntemiyle ve morfolojik değişiklikler gözlemlenerek takip edilmiştir. Ayrıca, özütlerin sitotoksik aktiviteleri, SH-SY5Y (insan nöroblastoma) ve HaCaT (insan keratinosit) hücre hatlarında MTT yöntemiyle test edilmiştir. Altı saatlik 30 mg mL-1 P. orientalis özütü inkübasyonu sonrasında canlı trofozoite rastlanmazken, aynı konsantrasyonda R. gallica özütü ile 24 saatlik inkübasyon sonrası trofozoitlerin ortalama %20.7’sinin canlı kaldığı gözlemlenmiştir. Trofozoit formunun aksine her iki özüt de, Acanthamoeba spp.'nin kist formuna karşı sınırlı etki göstermiştir; kistler 24 saatlik inkübasyon sonrasında %70’in üzerinde canlı kalmıştır. Ayrıca, her iki özüt de SH-SY5Y ve HaCaT hücrelerinde doz bağımlı sitotoksik etki göstermiştir. Bu in vitro çalışma sonucunda R. gallica ve P. orientalis yaprağı su özütlerinin anti-amebik aktivitesine dair ilk veriler elde edilmiştir. Özütlerin terapötik uygulama potansiyellerinin değerlendirilmesi için in-vivo çalışmalara ihtiyaç bulunmaktadır.
Synthesis of nanoparticles with a green approach using plants has attracted great attention from scientific communities because of its characteristics, such as environmentally friendly and time-efficient. In this study, green synthesis of zinc oxide nanoparticles was performed by Citrus aurantium aqueous peel extract. UV-VIS, FTIR, zeta potential, SEM, and EDX were used in characterization studies. In the UV-Vis spectrum, a heightening of the absorbance was monitored in the range of 260-390nm specific to ZnO. The mean particle size of zinc oxide NPs (ZnONPs) was characterized as 632 +/- 41nm with low polydispersity (0.174 +/- 0.055). As a result of EDX analysis, the presence of Zn in the scanned area was determined as 2.32%. The cytotoxic behaviors of ZnONPs on human breast cancer cells (MDA-MB-231) were carried out by MTT method. It was discovered that after ZnONPs application, cell migration decreased and apoptotic cell rate increased with Hoescht/PI staining in MDA-MB-231 cells.
Today, due to improved lifestyles and increased survival, the number of new cancer cases and cancer-related deaths continues to increase. In this study, novel hydroxylated and fluorinated-substituted hydrazone derivatives bearing an aromatic nitro moiety (2a-d and 3a-d) were designed as potential anticancer drug candidates, synthesized for the first time, and evaluated for their anticancer activity against chondrosarcoma (SW1353), a common primary malignant cartilage-forming tumor, neuroblastoma (SH-SY5Y), a type of brain cancer, and healthy (L929) cell lines using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) method for 24 h. The chemical structures of the target molecules were confirmed by FT-IR, 1D NMR (1H- and 13C- NMR, and APT), 2D NMR (COSY, HETCOR, and HMBC), and elemental analysis. Some of the compounds targeted against these cancer cell lines showed activity greater than 200 μM, whereas others (2d and 3a) demonstrated significant cytotoxic activity. Among them, compound 3a (IC50 = 9.45 ± 2.14 μM), a fluorinated-substituted hydrazone derivative, showed significant cytotoxic activity against the human SW1353 cell line compared to cisplatin (IC50 = 11.9 ± 0.95 μM). The anti-migratory properties of compounds 2d and 3a in SW1353 cells, were investigated. In particular, compound 3a exhibited anti-migration behavior in SW1353 cells, with a wound closure rate of 22.25 % compared with control cells. Further, scaffolds 2d and 3a exhibited the best docking with target receptor proteins 2OH4 (−8.3 and −8.4 kcal/mol) and 3QX3 (−12.2 and 11.0 kcal/mol), thereby supporting our bioactivity studies. Compounds 2a, 3a, 3b, and 3c showed high gastrointestinal (GI) absorption, with all except 3a being non-permeable to the blood-brain barrier (BBB). Most compounds, except 3d, are non-substrates of P-glycoprotein (P-gp). In conclusion, the in vitro and in silico results of some of the tested compounds indicate that they could be promising molecular frameworks for further studies.
This study involved the design, synthesis and evaluation of a series of novel thiosemicarbazide and thiazolylhydrazone derivatives. The synthesized compounds were tested for cytotoxic effects SH-SY5Y neuroblastoma cells, as well as NIH-3T3 normal cell line using the MTT assay. Among the tested compounds, 3b, 3d, 3i, 4b, 4d and 4i exhibited IC50 values ranging from 1.97 mu M to 3.22 mu M in the SH-SY5Y cancer cell line with lower cytotoxicity toward NIH-3T3 cells. Moreover, all compounds were also screened for their topoisomerase I and II inhibitory activity and compound 3b completely inhibited the topoisomerase I enzyme, whereas all compounds showed potent topoisomerase II inhibitory activity. Docking studies were performed to identify the mode of binding of the tested compounds to the active site of topoisomerase I and II. In conclusion, N-(4-(2-((2-chlor- ophenyl)carbamothioyl)hydrazine-1-carbonyl)phenyl)benzamide (3b) emerges as a promising inhibitor of topoisomerase I and II and holds potential as a lead compound in the quest for novel anticancer agents.
Aim: To evaluate i) the relationship between epilepsy and inflammation by analyzing the levels of thymus activation-regulated chemokine (TARC), and interferon regulatory factor 5 (IRF5) in healthy controls, patients with epilepsy on monotherapy and polytherapy, ii) the levels of sICAM5, chemokine (c-x3-c motif) ligand 1 (CX3CL1), and septin 7 (SEPT7) which are important in both inflammation and synaptic formation. Methods: Patients who were seizure-free with monotherapy (epilepsy group-1), patients with drug-resistant epilepsy (epilepsy group-2), and healthy controls were included. Demographical data, disease durations, and medications were noted. Measurements were made by commercial ELISA kits. Results: The numbers of epilepsy group-1, epilepsy group-2, and healthy controls were 23, 20, and 21, respectively. TARC levels were significantly lower in healthy controls than in both epilepsy groups. Higher TARC levels than 0.58 pg/ml indicated epilepsy with a sensitivity of 81.8% and specificity of 84.0%. SEPT7 levels were significantly higher in epilepsy group-1 than in those epilepsy group-2. A negative correlation was found between SEPT7 levels and disease duration as is the case for the correlation between SEPT7 and average seizure duration. A positive correlation was found between IRF5 and CX3CL1 levels, SEPT7 and IRF5 levels, and IRF5 and sICAM5 levels. Conclusions: We suggest that TARC is a promising biomarker, even in a heterogeneous epilepsy group not only for drug-resistance epilepsy but also for seizure-free epilepsy with monotherapy. Additionally, drug resistance, longer disease, and longer seizure durations are related to lower levels of SEPT7, which has an essential role in immunological functions and dendritic morphology.
INTRODUCTION:High mortality and morbidity of neonates with necrotizing enterocolitis (NEC) necessitates the investigation of novel therapies to improve outcomes. It was aimed to elucidate the potential therapeutic effect of estrogen receptor agonists on NEC-induced intestinal and brain injury in rats. METHODS:Sprague-Dawley pups of both sexes were separated from their mothers at postnatal 5th d. Feeding with formula along with a single session of hypoxia was applied to induce NEC, while control pups were kept with their mothers. The NEC rats received either vehicle, estrogen receptor α (ERα) agonist propyl pyrazole triol (1 mg/kg/day), ERβ agonist diarylpropionitrile (1 mg/kg/day), or 17β-estradiol (1 mg/kg/day) during maternal separation. All pups were decapitated on postnatal 9th d to collect intestinal and brain tissue samples. RESULTS:Elevation in proinflammatory cytokines, apoptosis, and microscopically and biochemically evident oxidative injury in both the intestinal and brain tissues were observed in NEC-induced pups. In both the intestinal and brain tissues, nerve growth factor and brain-derived neurotrophic factor protein levels were depleted, expressions of both the ESR1 and ESR2 genes were downregulated, while treatment with 17β-estradiol or ER agonists alleviated extent of oxidative injury of the intestines and brain tissue, upregulated nerve growth factor, brain-derived neurotrophic factor, and ER gene expressions, abolished NEC-induced decrease in claudin-3 expression, increased the survival rates, improved the clinical states of the survived pups at varying degrees. CONCLUSIONS:Activation of estrogen signaling by receptor agonists alleviated NEC-induced intestinal and cerebral injury, implicating that estrogen agonists could be regarded as promising preventive/therapeutic agents for NEC.
The aim of this study is to investigate the effectiveness of fjorbid-a-mediated sono-dynamic therapy in a 3D prostate cancer cell model. The effect of fjorbid-a-mediated sonodynamic therapy was examined by crystal violet staining in a 3D cell culture model created using human PC3 cells. Furthermore, apoptosis mechanisms were an-alyzed using Hoechst and propidium iodide staining (HOPI), and the levels of total oxidant (TOS) and total antioxidant (TAS) were assessed biochemically using cor-responding kits. Crystal violet staining was employed to assess the effectiveness of sonodynamic therapy facilitated by pheophorbide-a, revealing a substantial 75% re-duction in the viability of cancer cells. HOPI staining results indicated that there was no noteworthy increment in the count of apoptotic cells in the control, drug-only, or ultrasound-only groups. However, a remarkable 80% increase in apoptotic cell count was observed following pheophorbide-a-mediated sonodynamic treatment. Addi-tionally, biochemical measurements demonstrated elevated levels of Total Oxidant Status (TOS) and decreased levels of Total Antioxidant Status (TAS) in the treatment groups in comparison to the control groups. Based on the acquired data, it was estab-lished that pheophorbide-a-induced sonodynamic therapy for prostate cancer treat-ment diminishes cell viability by inducing apoptosis through oxidative stress in a 3D cell culture system.
Objective:In animal models of obesity, adipocyte-derived versican, and macrophage-derived biglycan play a crucial role in mediating adipose tissue inflammation. The aim was to investigate levels of versican and biglycan in obese children and any potential association with body adipose tissue and hepatosteatosis. Methods:Serum levels of versican, biglycan, interleukin-6 (IL-6), and high sensitivity C-reactive protein (hsCRP) were measured by ELISA. Fat deposition in the liver, spleen, and subcutaneous adipose tissue was calculated using the IDEAL-IQ sequences in magnetic resonance images. Bioimpedance analysis was performed using the Tanita BC 418 MA device. Results:The study included 36 obese and 30 healthy children. The age of obese children was 13.6 (7.5-17.9) years, while the age of normal weight children was 13.0 (7.2-17.9) years (p=0.693). Serum levels of versican, hsCRP, and IL-6 were higher in the obese group (p=0.044, p=0.039, p=0.024, respectively), while no significant difference was found in biglycan levels between the groups. There was a positive correlation between versican, biglycan, hsCRP, and IL-6 (r=0.381 p=0.002, r=0.281 p=0.036, rho=0.426 p=0.001, r=0.424 p=0.001, rho=0.305 p=0.017, rho=0.748 p<0.001, respectively). Magnetic resonance imaging revealed higher segmental and global hepatic steatosis in obese children. There was no relationship between hepatic fat content and versican, biglycan, IL-6, and hsCRP. Versican, biglycan, hsCRP, and IL-6 were not predictive of hepatosteatosis. Body fat percentage >32% provided a predictive sensitivity of 81.8% and a specificity of 70.5% for hepatosteatosis [area under the curve (AUC): 0.819, p<0.001]. Similarly, a body mass index standard deviation score >1.75 yielded a predictive sensitivity of 81.8% and a specificity of 69.8% for predicting hepatosteatosis (AUC: 0.789, p<0.001). Conclusion:Obese children have higher levels of versican, hsCRP, and IL-6, and more fatty liver than their healthy peers.
Over the past 10 years, nanotechnology has emerged as a very promising technique for a wide range of biomedical applications. Green synthesized metal and metal oxide nanoparticles (NPs) are cheap, easy to produce in large quantities, and safe for the environment. Currently, efforts are being made to dope ZnO in order to improve its optical, electrical, and ferromagnetic qualities as well as its crystallographic quality. Actually, doping is one of the simplest methods for enhancing an NP's physicochemical characteristics because it involves introducing impure ions into the crystal lattice of the particle. In this study, the biosynthesis of zinc oxide NPs (ZnONPs) and metal-doped (Mg2+ and Ag+) ZnONPs was carried out by using aqueous and water-alcoholic extracts of Cynara scolymus L. leaves, Carthamus tinctorius L. flowers, and Rheum ribes L. (RrL) plant, which are rich in phytochemical content. Plant extracts act as a natural reducing, capping, and stabilizing agent in the production. The produced NPs were characterized using a variety of methods, such as ultraviolet-visible spectroscopy, Fourier transform infrared (FTIR) spectroscopy, dynamic light scattering (DLS), and scanning electron microscopy (SEM). The produced metal-doped and undoped ZnONPs exhibited characteristic absorption peaks between 365 and 383 nm due to their surface plasmon resonance bands. SEM analysis revealed that the NPs were oval, nearly spherical, and spherical. In the FTIR spectra, the Zn-O bonding peak ranges from 400 to 700 cm-1. The peaks obtained in the range of 407-562 cm-1 clearly represent the Zn-O bond. In addition, the FTIR results showed that there were notable amounts of phenol and flavonoid compounds in both the prepared extract and ZnONPs. According to DLS analysis results, the size distribution of produced NPs is between 120 and 786 nm. The antibacterial properties of green produced NPs on Gram-positive (Staphylococcus aureus RN4220) and Gram-negative (Escherichia coli DH10B) bacterial strains were investigated by agar well diffusion method. In studies investigating the anticancer activities of biosynthesized NPs, mouse fibroblast cells (L929) were used as healthy cells and human cervical cancer cells (HeLa) were used as cancer cells. Only the produced Ag-ZnONPs showed potent dose-dependent antibacterial activity (at concentrations higher than 100 µg/mL) against Gram-positive and Gram-negative bacteria. RrL-ZnONP-600 and RrL-ZnONP-800 NPs produced with water-ethanol extract of RrL plant and calcined at 600 and 800°C were effective at high concentrations in healthy cells and at low concentrations in HeLa cancer cells, showing that they have the potential to be anticancer agents. The study's findings highlight the potential of green synthesis techniques in the production of medicinal nanomaterials for the treatment of cancer and other biological uses.
Hydrazide-hydrazone derivatives have garnered significant interest from researchers globally due to their wide range of biological activities, including antiviral, anticancer, and anti-inflammatory properties. In this study, a novel series of etofenamate hydrazide-hydrazone compounds (2a-2s) and their Cu(II) complexes (3a-3s) were designed and synthesized. The compounds were characterized using various analytical techniques such as FT-IR, 1H NMR, 13C NMR, MS, and elemental analysis. Additionally, the compound 2c and Cu(II) hydrazone complex 3a were further characterized using single X-ray crystallography. The anti-proliferative activity of the compounds was evaluated against Ishikawa human endometrial cancer cell line and non-tumour L929 cells using MTT assay. Additionally, the apoptotic potential of the compounds was investigated through caspase-3 activity, Bax and Bcl-2 gene expression analysis, and annexin-V binding. Furthermore, carbonic anhydrase IX activity and in silico studies were conducted to elucidate the mechanism of action. Overall, compound 3s demonstrated significant antiproliferative effects with an IC50 value of 0.27±0.01 µM against Ishikawa cells.
Aims Putative beneficial effects of neuropeptide W (NPW) in the early phase of gastric ulcer healing process and the involvement of cyclooxygenase (COX) enzymes were investigated in an acetic acid-induced gastric ulcer model. Main methods In anesthetized male Sprague–Dawley rats, acetic acid was applied surgically on the serosa and then a COX-inhibitor (COX-2-selective NS-398, COX-1-selective ketorolac, or non-selective indomethacin; 2 mg/kg/day, 3 mg/kg/day or 5 mg/kg/day; respectively) or saline was injected intraperitoneally. One h after ulcer induction, omeprazole (20 mg/kg/day), NPW (0.1 μg/kg/day) or saline was intraperitoneally administered. Injections of NPW, COX-inhibitors, omeprazole or saline were continued for the following 2 days until rats were decapitated at the end of the third day. Key findings NPW treatment depressed gastric prostaglandin (PG) I2 level, but not PGE2 level. Similar to omeprazole, NPW treatment significantly reduced gastric and serum tumor necrosis factor-alpha and interleukin-1 beta levels and depressed the upregulation of nuclear factor kappa B (NF-κB) and COX-2 expressions due to ulcer. In parallel with the histopathological findings, treatment with NPW suppressed ulcer-induced increases in myeloperoxidase activity and malondialdehyde level and replenished glutathione level. However, the inhibitory effect of NPW on myeloperoxidase activity and NPW-induced increase in glutathione were not observed in the presence of COX-1 inhibitor ketorolac or the non-selective COX-inhibitor indomethacin. Significance In conclusion, NPW facilitated the healing of gastric injury in rats via the inhibition of pro-inflammatory cytokine production, oxidative stress and neutrophil infiltration as well as the downregulation of COX-2 protein and NF-κB gene expressions.
Objectives: We aimed to obtain local normative data on thyroid volume evaluated by ultrasonography and iodine status by measuring urine iodine levels in school-age children living in Aydin province. Methods: In this cross-sectional study, a sample comprising 1,553 cases was meticulously selected from a total cohort of 170,461 children aged 6-17, drawn from 21 distinct educational institutions located within the Aydin region, as participants in the investigation. Those with a known chronic disease or thyroid disease were excluded from the study. The children underwent physical examinations and ultrasonography imaging of the thyroid gland, and urine samples were collected to measure urinary iodine concentration (UIC). Results: The median UIC was 189.5 (IQR=134.4) mu g/L, which was optimal according to WHO criteria. Thyroid volume was found to be 4.6 (IQR=3.5) mL in girls and 4.2 (IQR=4.0) mL in boys (p=0.883). The thyroid volumes in our study were found to be smaller when compared to the WHO. According to WHO age and body surface area criteria, thyroid volume was over 97 % in 0.9 % (n=15) of cases. Thyroid volume was found to have a positive correlation with age, height, weight, body mass index (BMI), and body surface area (BSA) in both genders (p<0.001). However, there was no significant correlation between thyroid volume and UIC. Conclusions: This cross-sectional study provides normative data on thyroid volume and iodine status in school-age children in iodine-sufficient population, revealing a low prevalence of goiter and correlations between thyroid volume and anthropometric measures.