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Acrylamide is broadly utilized in numerous areas with different purposes including being an additive, flocculating, sealing, dry strength improver and polymerizing agent, and so forth. Furthermore, it forms in certain food products at high temperatures. It poses serious hazard since its readily water‐soluble and very reactive nature. Besides in vivo studies, several in vitro studies with various cell lines are carried out to evaluate its toxicity. However, of these cell line studies, there are no mesothelium or mesothelioma cell lines. To fill this lacuna, we aimed at examining various dose range of acrylamide on SPC212 human mesothelioma cell line. First, we executed MTT and neutral red cytotoxicity tests and ascertained IC50 dose. Next, we performed inverted, light (haematoxylin–eosin and May Grünwald), fluorescent (DAPI) and confocal microscope (AO/EB) analyses as well as immunohistochemistry for Bax, Bcl‐2 and PCNA proteins. As a result, we found IC50 of acrylamide at 2.65 mM. Starting from 3.13 mM of acrylamide dose, a deep decrease in cell proliferation was observed. Particularly in MTT assay, a proliferative action of acrylamide was detected at 0.39 and 0.78 mM, supported with inverted microscope images. In light microscope analysis, several cellular degenerations, including condensed and kidney‐shaped nucleus were evident. In AO/EB staining, cells with apoptotic characteristics augmented dose‐dependently, being upheld by a parallel uptick in Bax and a dimunition in Bcl‐2 staining. Besides, PCNA decreased at IC50 dose of acrylamide. This is the acrylamide‐associated first study conducted on SPC212 mesothelioma cells encompassing advanced morphological analysis. We believe this study to be an incentive for future studies. [ABSTRACT FROM AUTHOR]

Thallium (Tl) is a highly toxic heavy metal whose mechanism of toxicity is still not completely understood. The aim of this study was to test Tl cytotoxicity on several cell lines of different tissue origin in order to clarify specific Tl toxicity to a particular organ. In addition, possible interference of Tl with cell potassium (K) transport was examined. Human keratinocytes (HaCaT), human hepatocellular carcinoma (HepG2), porcine kidney epithelial cells (PK15), human neuroblastoma (SH-SY5Y) and Chinese hamster lung fibroblast cells (V79) were treated with thallium (I) acetate in a wide concentration range (3.9–500 µg/mL) for 24 h, 48 and 72 h. To assess competitive interaction between Tl and K, the cells were treated with four Tl concentrations close to IC50 (15.63, 31.25, 62.50, 125 µg/mL) in combination with/or without potassium (I) acetate (500 µg/mL). The cells' morphology was monitored, and cytotoxic effect was assessed by 3-(4, 5-dimethylthiazole-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) test. The most sensitive to Tl exposure were SH-SY5Y cells, while HepG2 were the most resistant. The combined exposure to thallium (I) acetate and potassium (I) acetate for every cell line, except V79 cells, resulted in higher cell viability compared to thallium (I) acetate alone. The results of our study indicate that cell sensitivity to Tl treatment is largely affected by tissue culture origin, its function, and Na+/K+-ATPase activity. [ABSTRACT FROM AUTHOR]

Chlorella species are fast-growing microalgae with significant industrial applications. The aim of the present study was to investigate the antitumor, antioxidant, and hemolytic activities of Chlorella sorokiniana UTEX 1230 crude methanol extracts and fractions. Ch. sorokiniana crude methanol extracts and collective fractions (CFs) were obtained from lyophilized biomass by maceration and column chromatography. Antitumor assays against murine lymphoma L5178Y-R and human breast cancer MCF-7 cells were performed by the colorimetric 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) reduction technique, using human peripheral blood mononuclear cells (PBMC) as the control group. Antioxidant and hemolytic activities were evaluated using the 2,2-diphenyl-1-picrylhydrazyl radical scavenging assay (DPPH) and erythrocyte hemolysis, respectively. We showed that crude methanol extracts (IC50) increased L5178Y-R and MCF-7 cell growth inhibition, without affecting PBMC. In addition, all evaluated CFs showed significantly higher antioxidant activity than the positive control (ascorbic acid). CF3 and CF4 showed the highest cytotoxicity against L5178Y-R, whereas CF3, CF4, and CF5 caused the highest antitumor activity against MCF-7 cells. CF3, CF4, and CF5 induced significantly higher hemolytic activity compared with all other fractions. CF characterization revealed loliolide, cinnamic acid, methyl dihydrojasmonate, salsalvamide A, 1-monolinolenin, cryptophycin 29, costunolide, riboflavin lumicrome, and germicidin B, which have been related to antitumor and antioxidant activities. In conclusion, we demonstrated that Ch. sorokiniana extracts and fractions possess antitumor and antioxidant potential, without affecting human erythrocytes and PBMC. [ABSTRACT FROM AUTHOR]

α-Pinene (PEN) is a phyto compound present in terpene plants. In traditional medicine, PEN has been used for its anti-inflammatory, pain-relieving, and bronchodilator properties. The effect of PEN in combination with temozolomide (TMZ) in glioblastoma multiforme (GBM) cells has been evaluated. The action of the PEN + TMZ combination on cell migration, soft-agar, and cell death was determined in LN229 and U87MG human glioblastoma cells. In combination, PEN with TMZ showed a synergistic inhibitory effect in the GBM cells. The PEN + TMZ treatment showed a higher fluorescent intensity and reduced the percentage of wound area closure compared to the compound alone. The compounds in combination also resulted in a reduction in single-cell colony formation. To conclude, the study showed that plant-derived PEN enhanced the effectiveness of standard chemotherapeutic, TMZ, in LN229 and U87MG cells. [ABSTRACT FROM AUTHOR]

OBJECTIVES: The main purpose of this study is to predict the effect of Tyr-Lys-Thr (YKT) tripeptide, recognized for its anticancer properties, on lung cancer through theoretical and experimental analyzes. BACKGROUND: Peptides are important therapeutic compounds that have been studied for many years. Among these, YKT tripeptide emerges as a significant therapeutic peptide, exhibiting cytotoxic effects on various cancer cell lines. METHODS: The study investigated the involvement of the PI3K/Akt/mTOR pathway, commonly activated in human cancer, and the pivotal role of caspases in apoptosis. The interactions of YKT tripeptide with mTOR, Akt, PI3K, caspase-3, and caspase-8 were investigated through the molecular docking method. Additionally, MTT test was used to determine the cytotoxic activity of YKT against the A549 cell line across concentrations set at 0.1, 0.25, 0.5, 1, 2.5 and 5 mg/mL for 24 and 48 h. RESULTS AND CONCLUSION: In silico docking studies were conducted with PI3K, Akt1, and mTOR, known to be active in human cancer, as well as caspase-3 and caspase-8, key enzymes in apoptosis. It was determined that YKT exhibited a robust binding tendency with each receptor. YKT tripeptide was also found to have a cytotoxic effect on human lung carcinoma cell line A549 [ABSTRACT FROM AUTHOR]

This paper describes the synthesis of ZnO nanoparticles using air microplasma jets as the main reaction medium. Various techniques, including X-ray diffraction (XRD), field emission scanning electron microscopy (FE-SEM) and UV—Vis spectroscopy, were employed to confirm the characterization of the artificially synthesized ZnO nanoparticles. The absence of additional peaks associated with secondary phases of ZnO, as revealed by the XRD analysis, indicates the exceptional purity of these nanoparticles. Through the use of SEM, we examined the surface morphology and observed a substantial rate of agglomeration. The energy band gaps of ZnO nanoparticles were determined to be 3.3 electron volts (eV). The cytotoxic effects of zinc oxide nanoparticles were assessed using the methyl thiazolyl tetrazolium (MTT) assay on breast cancer cells exposed to various doses of the nanoparticles. The Acridine-Orange/Ethidium-bromide (AO/EB) dual stain was employed to assess apoptotic cells. The data indicate that ZnO NPs can induce apoptosis, suggesting their potential as an anticancer treatment in breast cancer cell lines. The presented findings indicate that nanoscale zinc oxide particles (ZnO NPs) possess significant potential for future utilization in many biological applications. An example of such an application could be the prospective substitution for chemotherapy in the management of various forms of cancer diseases. [ABSTRACT FROM AUTHOR]

Over the past few years, numerous bacterial strains have become resistant to selected drugs from various therapeutic groups. A potential tool in the fight against these strains is antimicrobial photodynamic therapy (APDT). APDT acts in a non-specific manner by generating reactive oxygen species and radicals, thereby inducing multidimensional intracellular effects. Importantly, the chance that bacteria will develop defense mechanisms against APDT is considered to be low. In our research, we performed the synthesis and physicochemical characterization of curcumin derivatives enriched with morpholine motifs. The obtained compounds were assessed regarding photostability, singlet oxygen generation, aggregation, and acute toxicity toward prokaryotic Aliivibrio fischeri cells in the Microtox® test. The impact of the compounds on the survival of eukaryotic cells in the MTT assay was also tested (WM266-4, WM115—melanoma, MRC-5—lung fibroblasts, and PHDF—primary human dermal fibroblasts). Initial studies determining the photocytotoxicity, and thus the potential APDT usability, were conducted with the following microbial strains: Candida albicans, Escherichia coli, Staphylococcus aureus, Streptococcus pneumoniae, and Pseudomonas aeruginosa. It was noted that the exposure of bacteria to LED light at 470 nm (fluence: 30 J/cm2) in the presence of quaternized curcumin derivatives at the conc. of 10 µM led to a reduction in Staphylococcus aureus survival of over 5.4 log. [ABSTRACT FROM AUTHOR]

Background and Objectives: Napabucasin (NP) was discovered as a natural compound that suppresses cancer stemness by inhibiting the signal transducer and activator of the transcription 3 (STAT3) signaling pathway. In this study, the anti-proliferative and apoptotic effects of NP and the chemotherapy agent doxorubicin (DX), a natural compound, on glioblastoma cells (U87) were investigated. Materials and Methods: In this study, the effects of NP and DX on cell viability on the glioblastoma U87 cell line were determined by MTT test. Expressions of Jak2/Stat3 genes were examined by qRT-PCR. Apoptosis was evaluated by Hoescht 33258 staining. Moreover, NP, its antagonistic–synergistic effects and IC50 doses of the combined treatment of DX were determined. Results: Napabucacin and doxorubicin were found to inhibit glioblastoma U87 cell proliferation. It was determined that NP applied in the range of 0.3–1 µM and its combination with DX killed almost all of the glioblastoma cells in 48 h of application. Additionally, it was observed that Jak2/Stat3 expressions downregulated. Conclusions: These results show that NP suppresses the proliferation of glioblastoma cells. It was shown that the combination of NP and DX can prevent invasion of the U87 cell line due to its Jak2/Stat3 inhibitory effect. Since it can suppress Jak2/Stat3, an important cancer cell proliferation pathway in glioblastoma, the combination of NP and DX can be used as an alternative treatment agent. But no synergistic effect of NP and DX on the U87 cells of the glioblastoma cell line was observed. [ABSTRACT FROM AUTHOR]

The present study was aimed to synthesize the silver nanoparticles from Alangium salvifolium Wang. and evaluating its biomedical applications. The leaves of A. salvifolium collected and subjected for the standard procedure of Soxhlet extraction using distilled water as a solvent. With the help of an aqueous extract AgNPs were synthesized from silver nitrate using phyto-reduction method. Further, synthesized AgNPs were characterized using several analytical techniques such as UV, FTIR, SEM–EDX, XRD, particles size and zeta potential. Synthesized AgNPs were tested for antibacterial, antioxidant, anticancer for lung cancer cell line and flowcytometry-based pathway studies. The visual observation confirmed the formation of AgNPs from the aqueous extract by changing yellow to brown colour formation. Further, characterization techniques also confirmed the formation of AgNPs. Antibacterial activity results showed that the tested AgNPs were potent against bacterial pathogens with a higher zone of inhibition. Further, the antioxidant and anticancer activity of AgNPs revealed that the AgNPs have exhibited significant results with a good percentage of inhibition. Further, the flow cytometry studies confirmed that the AgNPs inducing apoptosis and cell cycle arrest in lung cancer. The phytochemicals of A. salvifolium plant have successfully synthesized AgNPs. In the case of performed biological activity, the synthesized silver nanoparticles exhibited potent activity. In future these AgNPs can be taken for molecular and in vivo studies to identify their efficacy using in vivo and molecular models. [ABSTRACT FROM AUTHOR]

AbstractTo elucidate the structure-activity relationship of 17 matrine alkaloids from Oxytropis ochrocephala Bunge, their effect on hepatitis B surface antigen (HBsAg) secretion was studied using the MTT assay. A 3D-QSAR analysis showed a strong correlation between chemical structures and biological activities (q2 = 0.625, r2 = 0.859). Molecular docking and molecular dynamics simulations revealed that hydrogen bonding and hydrophobic interactions with hepatitis B core protein (PDB:5T2P) are key to inhibiting HBsAg secretion, suggesting potential for developing natural anti-hepatitis B drugs. [ABSTRACT FROM AUTHOR]

Colorectal cancer (CRC) is a common and life-threatening neoplastic disease that continues to pose a formidable challenge to global health. The present work was performed to evaluate the anticancer properties of betanin and betanin (BT) loaded starch nanoparticles (S-BT). The BT and S-BT were characterized by DLS, SEM, UV spectroscopy, XPS and FTIR. The cytotoxic effect was assessed by MTT and LDH assay. The apoptotic potential of BT and S-BT was assessed by DCFDA, Rh123, AO/EB and DAPI staining methods. Cell cycle arrest was depicted using flow cytometry. The antimetastatic potential of BT and S-BT was evaluated by wound healing assay. The S-BT showed a spherical morphology with a size of 175 nm. The betanin contained SNPs were found to have strong encapsulation efficiency and favorable release profiles. Both BT and S-BT exhibited cytotoxicity in SW480 cells but S-BT displayed increased cytotoxicity when compared to BT alone. Loss of mitochondrial membrane potential, nuclear fragmentation, chromatin condensation and generation of ROS, all indicative of apoptotic mode of cell death, were revealed by fluorescence imaging. The cells were arrested in the G2M phase. Moreover, both BT and S-BT were able to inhibit the migratory potential of SW480 cells. Overall, our results indicated that both BT and S-BT were able to induce anticancer effects; and, S-BT was found to have increased therapeutic efficacy when compared to BT alone. [ABSTRACT FROM AUTHOR]

Introduction: Glioblastoma (GBM), which is a heterogeneous and aggressive type of brain tumor, is known for its poor survival outcomes. The treatment of GBM remains challenging primarily due to the drug resistance to the current standard therapeutic option, temozolomide (TMZ). Researchers are currently focusing on developing an appropriate alternative combinatorial therapeutic to enhance treatment outcomes. D-limonene (DL) is a monoterpene derived from citrus fruit. This study aims to assess the impact of combining DL with TMZ and explore its potential mechanism of action in U87MG and LN229 GBM cells. Methods: The effects of the combined treatment of DL and TMZ were assessed on various cellular aspects, including cell viability, anchorage-independent cell growth, and DNA damage. Furthermore, the influence of this combination on cell cycle progression, cell migration, and cell death was also investigated. Results: The combination of DL+TMZ demonstrated a synergistic effect, resulting in reduced cell proliferation and suppressing the colony formation ability of a single cell. Treatment with DL and TMZ arrested the cells in G0/G1 phase. Furthermore, the DL+TMZ combination induced apoptosis by upregulating the expression of Bax, and Caspase (CASP)-3, while reducing the expression of the Bcl-2 gene in GBM cells. In addition, the combined treatment of DL+TMZ significantly decreased the expression of matrix metalloproteinase (MMP)-2 and MMP-9, expression, indicating inhibition of cell migration in GBM cells. Conclusion: In conclusion, the combination of DL and TMZ demonstrated a synergistic effect in reducing cell proliferation, suppressing colony formation, inducing apoptosis, and inhibiting cell migration in GBM cells. These findings suggest the potential of DL+TMZ combination therapy as an effective treatment for GBM. [ABSTRACT FROM AUTHOR]

The prevalence of cancer is so high globally that it is imperative to identify effective treatments. The use of bee products in the field of cancer therapeutics has gained significant attention as a promising alternative. Female worker bees (Apis mellifera) produce bee venom, which contains a complex array of biologically active compounds, including enzymes and peptides. Bee venom exhibits a range of biological activities with potential human health benefits, which vary across bee species and geographic locations. The objective of this study was to investigate the cytotoxicity of Turkish bee venom for the first time on some of the selected cancer cell lines. Bee venom was collected and resuspended in water and ethanol. The study analyzed both forms of Turkish bee venom for major peptides and proteins using HPLC-VWD and SDS-PAGE. The major components identified were apamin, melittin, phospholipase A2, and hyaluronidase. Cytotoxic activities were evaluated on eight distinct cell lines (seven cancerous cells and one control) using MTT assays. The Turkish bee venom demonstrated cytotoxicity with 48-hour IC50 values of 14.8 ± 0.6, 5.7 ± 0.2, 8.1 ± 0.1, 7.1 ± 0.1, 8.5 ± 0.2, 7.2 ± 0.1, 7.9 ± 0.1, and 8.0 ± 0.1 µg/mL for Phoenix-AMPHO (CRL-3213), PC-3, Huh-7, Caco-2, HT-29, SW-48, CARM-L12 TG3, and A-673, respectively. The 72-hour IC50 values were 8.2 ± 0.2, 4.5 ± 0.3, 7.1 ± 0.1, 6.4 ± 0.1, 6.0 ± 0.3, 7.2 ± 0.1, 2.1 ± 0.1, and 6.0 ± 0.2 µg/mL, respectively. In conclusion, the study demonstrated that both forms of Turkish bee venom exhibited significant cytotoxic effects on the analyzed cancer cells. The cell lines CARM-L12 TG3, PC-3, and A-673 exhibited the most pronounced responses to the bee venom. [ABSTRACT FROM AUTHOR]

Microbial infections are a global health challenge often treated with antibiotics, but their overuse can lead to antibiotic resistance. To address this, there is a need for more efficient personal protective equipment (PPE) with novel antimicrobial techniques. One such technique involves using carbon dots (CDs) to create self-disinfecting fabrics. This study focused on synthesizing phenylboronic-acid-functionalized piperine-based carbon dots (PBA-PPCDs) and boronic acid carbon dots (BACDs) as potential antimicrobial agents. The materials were successfully synthesized using a hydrothermal method and characterized using various techniques to confirm the size, charge, fluorescence properties, and inner morphology of the CDs. The CDs showed bactericidal activity against gram-positive and gram-negative bacteria, with potent inhibition in growth especially in the presence of simulated sunlight. The antibacterial properties of the CDs were tested on cellulose discs, demonstrating strong adherence and significant inhibition of bacterial cells. The cytotoxicity studies showed that these CDs, at concentrations up to 0.1 mg/mL, and the CD-modified fibers are benign to mammalian cells, emphasizing their safety for human use. Overall, the study concluded that PBA-PPCDs and BACDs are promising candidates for modifying fibers and inducing antimicrobial activity in fabrics made of cellulose fibers.Article highlights: New self-disinfecting fabrics kill bacteria with light-activated carbon dots, no harsh chemicals needed. Self-disinfecting fabrics fight bacteria, reduce antibiotic use, and slow superbug growth. Safe and effective: Carbon dot fabrics harmless to humans, promising for PPE. [ABSTRACT FROM AUTHOR]

Background: The growing concern of antibiotic-resistant microbial strains worldwide has prompted the need for alternative methods to combat microbial resistance. Biofilm formation poses a significant challenge to antibiotic efficiency due to the difficulty of penetrating antibiotics through the sticky microbial aggregates. Drug repurposing is an innovative technique that aims to expand the use of non-antibiotic medications to address this issue. The primary objective of this study was to evaluate the antimicrobial properties of Diltiazem HCl, a 1,5-benzothiazepine Ca2+ channel blocker commonly used as an antihypertensive agent, against four pathogenic bacteria and three pathogenic yeasts, as well as its antiviral activity against the Coxsackie B4 virus (CoxB4). Methods: To assess the antifungal and antibacterial activities of Diltiazem HCl, the well diffusion method was employed, while crystal violet staining was used to determine the anti-biofilm activity. The MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) colorimetric assay was utilized to evaluate the antiviral activity of Diltiazem HCl against the CoxB4 virus. Results: This study revealed that Diltiazem HCl exhibited noticeable antimicrobial properties against Gram-positive bacteria, demonstrating the highest inhibition of Staphylococcus epidermidis, followed by Staphylococcus aureus. It effectively reduced the formation of biofilms by 95.1% and 90.7% for S. epidermidis, and S. aureus, respectively. Additionally, the antiviral activity of Diltiazem HCl was found to be potent against the CoxB4 virus, with an IC50 of 35.8 ± 0.54 μg mL−1 compared to the reference antiviral Acyclovir (IC50 42.71 ± 0.43 μg mL−1). Conclusion: This study suggests that Diltiazem HCl, in addition to its antihypertensive effect, may also be a potential treatment option for infections caused by Gram-positive bacteria and the CoxB4 viruses, providing an additional off-target effect for Diltiazem HCl. [ABSTRACT FROM AUTHOR]

Material scientists are becoming less and less optimistic about the use of renewable resources in novel applications. In turn, there is significant promise for carbon dots (CDs), carbon dot-silver nanocomposite (CD-AgNC), and other zero-dimensional carbon-based nanomaterials to be used as anti-bacterial, anti-cancer, and mosquitocidal agents in the fight against new infectious illnesses. Further, it possesses acceptable properties such as a high level of stability, straightforward synthesis protocol (green technology), and non-toxicity to the environment. In our present study, we aimed to investigate the potential of CD-AgNC on mosquitocidal, anti-bacterial, and anti-cancer using the marine algae–mediated synthesis of CD-AgNC as a novel approach. The c-dot precursor in this experiment was the marine red algae Chondrococcus hornemanni. The CD-AgNC was produced without the use of a reducing agent using a straightforward thermal processing approach. UV, FTIR, XRD, TEM, EDX, and Zeta potential were used to characterize the synthesized CD-AgNC. For mosquitocidal activity, we adopted the WHO method to determine the anti-larvicidal. The antibacterial study was performed using the disk diffusion method and anticancer studies were demonstrated with breast cancer cell line (MDA-MB-231) and the fluorescence staining analysis (AO/EtBr, DCFH-DA, Rho-123 (ΔΨm), and Hoechst-33342) was used to prove the cell apoptosis. The CD-Ag showed high larvicidal activity against Ae. aegypti, in particular, the LC50 of CD-AgNC against 3rd instar larvae at 27.59 µg/mL and 4th instar larvae at 39.18 µg/mL. The CD-AgNC decreased the longevity and fecundity of Ae. aegypti. Moreover, CD-AgNC showed significant anti-bacterial effects against several pathogenic. Mainly, CD-AgNC induces the IC50 value at 12 µg/mL with produced dead cells in MDA-MB-231. More on, it creates hyper ROS with altered MMP (ΔΨm) in the cell cytoplasm. The overall findings illustrated that the C. hornemanni–mediated synthesized CD-AgNC actively works against the dengue vector and shows a good anti-bacterial effect along with anti-cancer properties characterized by cytotoxicity effect. [ABSTRACT FROM AUTHOR]

The effects of Nano propolis (NP-Pro) alone or combined with radiation in human liver cancer cell line (HepG2) in vitro were evaluated. NP-Pro is made up of natural propolis particles that are between 1 and 100 nm in diameter that have been linked together to increase its effectiveness without altering its original characteristics. Numerous benefits of propolis include its anti-inflammatory, antioxidant, anti-cancer, and antifungal properties. Propolis nanoparticles were characterized using dynamic light scattering (DLS), transmission electron microscopy (TEM), and X-ray diffraction (XRD). Cell viability was examined using MTT (3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide) assay, and apoptosis was assessed using flow cytometry. HepG2 was treated with both different concentrations of NP-Pro and irradiated 10 Gy using a 137Cs gamma source. The cytotoxic effect of the studied NP-Pro increased with an increase in concentrations. The IC50 of NP-Pro in the cytotoxicity test with the HepG2 cells in combination with a radiation dose of 10 Gy was 7.58 ± 0.39 µg/mL, while for free NP-Pro, it was 29.58 ± 1.27 µg/mL. The effects of the combined use of NP-Pro and irradiated 10 Gy on cytotoxicity, generation of reactive oxygen species, and activity of apoptosis-mediated signaling pathways were studied on the HepG2 cell line. Cell apoptosis tests have shown that HepG2 cells that are exposed to nano propolis + 10 Gy undergo apoptosis, and their population is dramatically decreased (p < 0.005). All these studies concluded that propolis nanoparticles could be a good alternative to existing anticancer materials in combination with gamma radiation. [ABSTRACT FROM AUTHOR]

Background. Esophageal cancer is the eighth most common cancer in the world. The antitumor effects of medicinal plants have been shown as a therapeutic strategy to treat esophageal cancer. This study aimed to evaluate in vitro effects of Cuscuta epithymum extract on the survival and apoptosis of esophageal cancer cell line. Material and Methods. Here, the hydroalcoholic Soxhlet extract of C. epithymum plant was prepared. The cell viability of esophageal cancer cell line KYSE-30 was evaluated by MTT assay after 24 h treatment with concentrations of 50, 100, 200, 400, 600, 800 and 1000 μg/ml of the extract. Then, the apoptotic effect of extract was evaluated by flow cytometry using Propidium Iodide (PI) staining and sub-G1 peak analysis, and Annexin V-FITC/PI staining in cells treated with concentrations of 125, 250, 500 and 750 μg/ml as well as morphological change of healthy cells to apoptotic and necrotic form. Results. The hydroalcoholic extract of C. epithymum decreases the viability of KYSE-30 cells in a dose-dependent manner with an IC50 of 646 µg/ ml at 24 h. A significant increase was observed in the percentage of sub-G1 phase in cells treated with 500, 750, and 1000 μg/ml of C. epithymum extract for 24 h compared to the control group (p

Colorectal cancer is the second deadliest cancer worldwide. The side effects and resistance of existing chemotherapy drugs are the background for various studies looking for potential plant extracts as new anticancer agents. This study aims to determine the cytotoxic activity of simpor leaf extract from Belitung and its effect on apoptosis of WiDr colorectal cancer cells. The compound content in simpor leaf extract was analyzed using Gas Chromatography-Mass Spectrometry (GC-MS). The cytotoxic activity of simpor leaf extract at different concentrations (25, 50 and 100 ppm) was determined by the MTT test and apoptosis induction by Annexin V/PI flow cytometry analysis. Based on the GC-MS chromatogram results, 13 different compounds were detected. Analysis of the relationship between extract concentration and the percentage of WiDr cell inhibition showed that an extract concentration of 100 ppm was the concentration with the highest percentage of inhibition (20.12 % ± 4.99) compared to concentrations of 50 ppm (13.95 % ± 2.32) and 25 ppm (15.90 % ± 1.38) with an inhibitory concentration value (IC50) of simpor leaf extract of 10.45 ppm. Induction of WiDr cell apoptosis by the extract was influenced by the concentration of simpor leaf extract, which was increase in the percentage of apoptotic cells from 16 % at a concentration of 25 ppm to 70.5 % at a concentration of 100 ppm. The results of this study show that simpor leaf extract from Belitung is able to induce apoptosis in WiDr colorectal cancer cells. [ABSTRACT FROM AUTHOR]

Lemna aequinoctialis (duckweed) is the smallest and fast-growing aquatic plant species producing protein-rich biomass with high protein nutritional value, phytoremediation capacity, and nutrient removal from wastewater. Duckweed may also be used as a new potential bioreactor for biological products, such as vaccines, antibodies, and pharmaceutical proteins. Based upon the potential importanc of L. aequinoctialis in phytoremediation and as a bioreactor the aim of this study was to (1) characterize the chemical and nutritional profiles of L. aequinoctialis biomass utilizing an integrated multi-trophic aquaculture system (IMTA) and a pond, and (2) investigate the cytotoxic potential of different concentrations of organic extracts and fractions using the MTT bioassay. EDXRF and ICP-MS analyses indicated the presence of trace elements in lower amounts in relation to the biomass of L. aequinoctialis in the lagoon, emphasizing the importance of plant inclusion management to reduce bioaccumulation of these elements. Analysis of mineral profiles, fatty acids, and amino acids indicated a satisfactory nutritional composition for the use of biomass as a bioproduct. Pigment analysis showed a high concentration of carotenoids, especially astaxanthin. After standardizing the controls, the MTT cell viability test was carried out utilizing rat hepatoma cell line (HTC), which are metabolizing cells that were treated with aqueous or ethanolic extracts and the dichloromethane, ethyl acetate, and methanol fractions at different concentrations. No apparent cytotoxic potential was observed following treatments, since there was no significant reduction in cell viability. Therefore, this study provides information regarding the biomass of L. aequinoctialis derived from the IMTA system, which might support further research into the application of this species as a bioproduct. [ABSTRACT FROM AUTHOR]

Objective: Amygdalin (Vitamin B-17) is a type of vitamin, naturally found in many fruits and plants. The aim of the study was the evaluation of Amygdalin effect on the oxidant capacity and oxidant status of the T98G cancer cells. A T98G cell line was used in the study. Cell viability and oxidative stress evaluation were done. Methods: Amygdalin was used at 1, 4, and 8 µg/mL doses. TAC and TOS values were measured. Results: According to the result, amygdalin 8 µg/mL shows the highest anticancer effects. TAC level was 3.2 Trolox Equiv/L and TOS was 3.6 H2O2 Equiv/L. Conclusion: Vit B17 can increase oxidative stress in T98G cells and decrease cell viability

In this study, gold nanoparticles were rapidly synthesized with a low-cost and environmentally friendly approach through the extract prepared using agricultural waste parts of the Nigella sativa L. plant. Properties of gold nanoparticles from N. sativa leaf extract UV-visible Spectrophotometer, X-ray diffraction, Electron Disperse X-ray, Zeta potential and Zetasizer, Field Emission Scan Electron Microscopy (FESEM), Atomic Power Microscopy, Transmission Electron Microscopy (TEM), thermogravimetric and differential thermal analysis characterized by its data. It was observed that the morphologies of the synthesized gold nanoparticles (AuNPs) exhibited a spherical appearance with an average size distribution of 107 nm and a monodisperse. In addition, they were found to be stable structures at -17.7 mV surface charge, and maximum absorbance at 538.41 nm. For the usability of AuNPs as biomedical agents, antimicrobial and anticancer effects were evaluated using Microdilution and MTT methods, respectively. It was determined that AuNPs were effective in suppressing the proliferation of 0.02-1.00 μg/mL concentration range on Staphylococcus aureus ATCC 29213, Bacillus subtilis ATCC 11774, Escherichia coli ATCC25922, Pseudomonas aeruginosa (ATCC27833) and Candida albicans pathogenic strains. The viability of CaCo-2, Skov-3, and U118 cancer cells was effectively inhibited by the produced AuNPs by, respectively, 66.73%, 30.93%, and 23.23%. It has been determined that AuNPs have significant antimicrobial and anticancer effects on hospital pathogens and cancer cell lines.

Abstract Background The ineffectiveness of treatments for infections caused by biofilm-producing pathogens and human carcinoma presents considerable challenges for global public health organizations. To tackle this issue, our study focused on exploring the potential of synthesizing new complexes of Co(II), Cu(II), Ni(II), and Zn(II) with sorbic acid to enhance its antibacterial, antibiofilm, and anticancer properties. Methods Four novel complexes were synthesized as solid phases by reacting sorbic acid with Co(II), Cu(II), Ni(II), and Zn(II). These complexes were characterized by various technique, including infrared spectra, UV–Visible spectroscopy, proton nuclear magnetic resonance (1H NMR), and thermal analysis techniques, including thermogravimetry (TG). Results The data acquired from all investigated chemical characterization methods confirmed the chemical structure of the sorbate metal complexes. These complexes exhibited antibacterial and antibiofilm properties against both Gram-positive and Gram-negative bacteria. Furthermore, these complexes enhanced the antibacterial effects of commonly used antibiotics, such as gentamicin and imipenem, with fractional inhibitory concentration (FIC) indices ≤ 0.5. Notably, the Cu(II) complex displayed the most potent antibacterial and antibiofilm activities, with minimum inhibitory concentration (MIC) values of 312.5 µg/mL and 625.0 µg/mL for Bacillus cereus and Escherichia coli, respectively. Additionally, in vitro assays using the methyl thiazolyl tetrazolium (MTT) method showed inhibitory effects on the growth of the human colon carcinoma cell line (HCT-116 cells) following treatment with the investigated metal complexes. The IC50 values for Co(II), Cu(II), Zn(II), and Ni(II) were 3230 µg/mL, 2110 µg/mL, 3730 µg/mL, and 2240 µg/mL, respectively. Conclusion Our findings offer potential for pharmaceutical companies to explore the development of novel combinations involving traditional antibiotics or anticancer drugs with sorbate copper complex.

Abstract Based on unselectively, several side effects and drug resistance of available anticancer agents, the development and research for novel anticancer agents is necessary. In this study, a new series of quinazoline-4(3H)-one derivatives having a thiol group at position 2 of the quinazoline ring (8a-8 h) were designed and synthesized as potential anticancer agents. The Chemical structures of all compounds were characterized by 1H-NMR, 13C-NMR, and Mass spectroscopy. The antiproliferative activity of all derivatives were determined against two cancer cell lines (MCF-7 and SW480) and one normal cell lines (MRC-5) by the MTT method. Cisplatin, Erlotinib and Doxorubicin were used as positive controls. The results of in vitro screening showed that 8a with an aliphatic linker to SH group was the most potent compound with IC50 values of 15.85 ± 3.32 and 17.85 ± 0.92 µM against MCF-7 and SW480 cell lines, respectively. 8a indicated significantly better potency compared to Erlotinib in the MCF-7 cell line. The cytotoxic results obtained from testing compound 8a on the normal cell line, revealing an IC50 value of 84.20 ± 1.72 µM, provide compelling evidence of its selectivity in distinguishing between tumorigenic and non-tumorigenic cell lines. Structure–activity relationship indicated that the variation in the anticancer activities of quinazoline-4(3H)-one derivatives was affected by different substitutions on the SH position. Molecular docking and MD simulation were carried out for consideration of the binding affinity of compounds against EGFR and EGFR-mutated. The binding energy of compounds 8a and 8c were calculated at -6.7 and − 5.3 kcal.mol− 1, respectively. Compounds 8a and 8c were found to establish hydrogen bonds and some other important interactions with key residue. The DFT analysis was also performed at the B3LYP/6–31 + G(d, p) level for compounds 8a, 8c and Erlotinib. Compound 8a was thermodynamically more stable than 8c. Also, the calculated theoretical and experimental data for the IR spectrum were in agreement. The obtained results delineated that the 8a can be considered an appropriate pharmacophore to develop as an anti-proliferative agent.

Introduction: Bone tissue engineering seeks innovative materials that support cell growth and regeneration. Electrospun nanofibers, with their high surface area and tunable properties, serve as promising scaffolds. This study explores the incorporation of flaxseed extract, rich in polyphenolic compounds, into polyvinyl alcohol (PVA) nanofibers to improve their application in bone tissue engineering. Methods: High-performance liquid chromatography (HPLC) identified ten key compounds in flaxseed extract, including polyphenolic acids and flavonoids. PVA nanofiberswere fabricated with 30 wt.% flaxseed extract (P70/E30) via electrospinning. We optimized characteristics like diameter, hydrophilicity, swelling behavior, and hydrolytic degradation. MG-63 osteoblast cultures were used to assess scaffold efficacy through cell adhesion, proliferation, viability (MTT assay), and differentiation. RT-qPCR measured expression of osteogenic genes RUNX2, COL1A1, and OCN. Results: Flaxseed extract increased nanofiber diameter from 252 nm (pure PVA) to 435 nm (P70/E30). P70/E30 nanofibers showed higher cell viability (102.6% vs. 74.5% for pure PVA), although adhesion decreased (151 vs. 206 cells/section). Notably, P70/E30 enhanced osteoblast differentiation, significantly upregulating RUNX2, COL1A1, and OCN genes. Discussion: Flaxseed extract incorporation into PVA nanofibers enhances bone tissue engineering by boosting osteoblast proliferation and differentiation, despite reduced adhesion. These properties suggest P70/E30's potential for regenerative medicine, emphasizing scaffold optimization for biomedical applications. [ABSTRACT FROM AUTHOR]

The methanolic leaf extract of the plant Evolvulus nummularius Linn, belonging to the Convolvulaceae family was evaluated for its in vitro in HepG2 cells against Non-Alcoholic Fatty Liver Disease (NAFLD) and in vivo toxicity potential. The present study aimed to explore in vitro cell line screening using HepG2 cells induced with 0.5 mM FFA (0.17 mM palmitic acid + 0.33 mM oleic acid) for fatty liver. The fatty liver in this study was tested by MTT assay, Oil Red O staining, and Nile Red Staining techniques. The in vivo toxicological study was carried out using acute and subacute toxicity experiments following OECD principles 425 and 407, respectively, on rats. Cell line screening performed on HepG2 cells, and cytotoxicity examination revealed no toxicity up to 1000 µg/mL, with no evidence of cell death found. A concentration up to 300 µg/mL and 100 µg/mL of MEEN using ORO Staining and Nile Red Staining, respectively, on HepG2 cells does not pose any threat to the liver cells. Compared to the control group, there were no differences in behaviour, body weight, hematological, biochemical parameters, or histological changes up to 2000 mg/kg. The methanolic leaf extract of Evolvulus nummularius showed no obvious cytotoxicity or toxicity, proving its safety for hepatoprotection and can be beneficial in the treatment of NAFLD. [ABSTRACT FROM AUTHOR]

Background: The ineffectiveness of treatments for infections caused by biofilm-producing pathogens and human carcinoma presents considerable challenges for global public health organizations. To tackle this issue, our study focused on exploring the potential of synthesizing new complexes of Co(II), Cu(II), Ni(II), and Zn(II) with sorbic acid to enhance its antibacterial, antibiofilm, and anticancer properties. Methods: Four novel complexes were synthesized as solid phases by reacting sorbic acid with Co(II), Cu(II), Ni(II), and Zn(II). These complexes were characterized by various technique, including infrared spectra, UV–Visible spectroscopy, proton nuclear magnetic resonance (1H NMR), and thermal analysis techniques, including thermogravimetry (TG). Results: The data acquired from all investigated chemical characterization methods confirmed the chemical structure of the sorbate metal complexes. These complexes exhibited antibacterial and antibiofilm properties against both Gram-positive and Gram-negative bacteria. Furthermore, these complexes enhanced the antibacterial effects of commonly used antibiotics, such as gentamicin and imipenem, with fractional inhibitory concentration (FIC) indices ≤ 0.5. Notably, the Cu(II) complex displayed the most potent antibacterial and antibiofilm activities, with minimum inhibitory concentration (MIC) values of 312.5 µg/mL and 625.0 µg/mL for Bacillus cereus and Escherichia coli, respectively. Additionally, in vitro assays using the methyl thiazolyl tetrazolium (MTT) method showed inhibitory effects on the growth of the human colon carcinoma cell line (HCT-116 cells) following treatment with the investigated metal complexes. The IC50 values for Co(II), Cu(II), Zn(II), and Ni(II) were 3230 µg/mL, 2110 µg/mL, 3730 µg/mL, and 2240 µg/mL, respectively. Conclusion: Our findings offer potential for pharmaceutical companies to explore the development of novel combinations involving traditional antibiotics or anticancer drugs with sorbate copper complex. [ABSTRACT FROM AUTHOR]

Background Aim Material and Methods Results Conclusions Tooth avulsion necessitates swift replantation, for which the preservation of periodontal ligament (PDL) cell viability is paramount. Various storage media have been explored, yet a comparison between amniotic fluid (AF) obtained at different gestational stages (amniocentesis and full‐term) and HBSS is lacking.This study aims to evaluate AF (amniocentesis and full‐term) against HBSS in sustaining PDL cell viability and regulating apoptosis at different time points.Periodontal fibroblasts cultured in α‐MEM were treated with 100% AF (amniocentesis), 100% AF (full‐term), and HBSS, incubated for 1, 3, 24, and 48 h at 37°C, and assessed using the MTT assay for viability and AO/EB staining for apoptosis, which was analyzed via fluorescent microscopy after 24 h. Statistical analysis was conducted using one‐way ANOVA, multivariate ANOVA, and post hoc Tukey's multiple comparison tests (p < .05).Amniotic fluid (amniocentesis) exhibited the highest optical density (OD), which implies the highest cell viability across time intervals, followed by AF (full‐term) and HBSS. While HBSS maintained PDL morphology, both AF groups showed altered morphology. No cell death was observed after 24 h.Within the limitations of this study, both AF groups showed the potential to sustain PDL cell viability after 1, 3, 24, and 48 h of storage. However, further investigation is warranted regarding their suitability as storage media. [ABSTRACT FROM AUTHOR]

The shoots of Asparagus L. are consumed worldwide, although most species belonging to this genus have a restricted range, and several taxa remain unstudied. In this work, a total of four taxa from different locations were scrutinized and compared with cultivated A. officinalis. All shoots were screened for saponins via LC-MS, and in vitro antiproliferative activities against the HT-29 colorectal cancer cell line were assessed via the MTT assay. The total saponins (TS) contained in the crude extracts ranged from 710.0 (A. officinalis) to 1258.6 mg/100 g dw (A. acutifolius). The richness of the compounds detected in this work stands out; a total of 47 saponins have been detected and quantified in the edible parts (shoots) of five taxa of Asparagus. The structure of all the saponins found present skeletons of the furostane and spirostane type. In turn, the structures with a furostane skeleton are divided into unsaturated and dioxygenated types, both in the 20–22 position. The sum of dioscin and derivatives varied largely among the studied taxa, reaching the following percentages of TS: 27.11 (A. officinalis), 18.96 (A. aphyllus), 5.37 (A. acutifolius), and 0.59 (A. albus); while in A. horridus, this compound remains undetected. Aspachiosde A, D, and M varied largely among samples, while a total of seven aspaspirostanosides were characterized in the analyzed species. The hierarchical cluster analysis of the saponin profiles clearly separated the various taxa and demonstrated that the taxonomic position is more important than the place from which the samples were acquired. Thus, saponin profiles have chemotaxonomic significance in Asparagus taxa. The MTT assay showed dose- and time-dependent inhibitory effects of all saponins extracts on HT-29 cancer cells, and the strongest cell growth inhibition was exercised by A. albus and A. acutifolius (GI50 of 125 and 175 µg/mL). This work constitutes a whole approach to evaluating the saponins from the shoots of different Asparagus taxa and provides arguments for using them as functional foods. [ABSTRACT FROM AUTHOR]

Indomethacin (INDO) has a mechanism of action based on inhibiting fatty acids cyclooxygenase activity within the inflammation process. The action mechanism could be correlated with possible anticancer activity, but its high toxicity in normal tissues has made therapy difficult. By the coprecipitation method, the drug carried in a layered double hydroxides (LDH) hybrid matrix would reduce its undesired effects by promoting chemotherapeutic redirection. Therefore, different samples containing INDO intercalated in LDH were synthesized at temperatures of 50, 70, and 90 °C and synthesis times of 8, 16, 24, and 48 h, seeking the best structural organization. X-ray diffraction (XRD), vibrational Fourier transform infrared spectroscopy (FT-IR), scanning electron microscopy (SEM), spectrophotometric analysis in UV-VIS, and differential thermogravimetric analysis (TGA/DTA) were used for characterization. Our results indicate that higher temperatures and longer synthesis time through coprecipitation reduce the possibility of INDO intercalation. However, it was possible to establish a time of 16 h and a temperature of 50 °C as the best conditions for intercalation. In vitro results confirmed the cell viability potential and anticancer activity in the LDH-INDO sample (16 h and 50 °C) for gastric cancer (AGP01, ACP02, and ACP03), breast cancer (MDA-MB-231 and MCF-7), melanoma (SK-MEL-19), lung fibroblast (MRC-5), and non-neoplastic gastric tissue (MN01) by MTT assay. Cell proliferation was inhibited, demonstrating higher and lower toxicity against MDA-MB-231 and SK-MEL-19. Thus, a clinical redirection of INDO is suggested as an integral and adjunctive anticancer medication in chemotherapy treatment. [ABSTRACT FROM AUTHOR]

Based on unselectively, several side effects and drug resistance of available anticancer agents, the development and research for novel anticancer agents is necessary. In this study, a new series of quinazoline-4(3H)-one derivatives having a thiol group at position 2 of the quinazoline ring (8a-8 h) were designed and synthesized as potential anticancer agents. The Chemical structures of all compounds were characterized by 1H-NMR, 13C-NMR, and Mass spectroscopy. The antiproliferative activity of all derivatives were determined against two cancer cell lines (MCF-7 and SW480) and one normal cell lines (MRC-5) by the MTT method. Cisplatin, Erlotinib and Doxorubicin were used as positive controls. The results of in vitro screening showed that 8a with an aliphatic linker to SH group was the most potent compound with IC50 values of 15.85 ± 3.32 and 17.85 ± 0.92 µM against MCF-7 and SW480 cell lines, respectively. 8a indicated significantly better potency compared to Erlotinib in the MCF-7 cell line. The cytotoxic results obtained from testing compound 8a on the normal cell line, revealing an IC50 value of 84.20 ± 1.72 µM, provide compelling evidence of its selectivity in distinguishing between tumorigenic and non-tumorigenic cell lines. Structure–activity relationship indicated that the variation in the anticancer activities of quinazoline-4(3H)-one derivatives was affected by different substitutions on the SH position. Molecular docking and MD simulation were carried out for consideration of the binding affinity of compounds against EGFR and EGFR-mutated. The binding energy of compounds 8a and 8c were calculated at -6.7 and − 5.3 kcal.mol− 1, respectively. Compounds 8a and 8c were found to establish hydrogen bonds and some other important interactions with key residue. The DFT analysis was also performed at the B3LYP/6–31 + G(d, p) level for compounds 8a, 8c and Erlotinib. Compound 8a was thermodynamically more stable than 8c. Also, the calculated theoretical and experimental data for the IR spectrum were in agreement. The obtained results delineated that the 8a can be considered an appropriate pharmacophore to develop as an anti-proliferative agent. [ABSTRACT FROM AUTHOR]

Organometallic complexes of the formula [Ru(N^N)(p-cymene)Cl][X] (N^N = bidentate polypyridyl ligands, p-cymene = 1-methyl-4-(1-methylethyl)-benzene, X = counter anion), are currently studied as possible candidates for the potential treatment of cancer. Searching for new organometallic compounds with good to moderate cytotoxic activities, a series of mononuclear water-soluble ruthenium(II)–arene complexes incorporating substituted pyridine–quinoline ligands, with pending -CH2OH, -CO2H and -CO2Me groups in the 4-position of quinoline ring, were synthesized, for the first time, to study their possible effect to modulate the activity of the ruthenium p-cymene complexes. These include the [Ru(η6-p-cymene)(pqhyme)Cl][X] (X = Cl− (1-Cl), PF6− (1-PF6), pqhyme = 4-hydroxymethyl-2-(pyridin-2-yl)quinoline), [Ru(η6-p-cymene)(pqca)Cl][Cl] ((2-Cl), pqca = 4-carboxy-2-(pyridin-2-yl)quinoline), and [Ru(η6-p-cymene)(pqcame)Cl][X] (X = Cl− (3-Cl), PF6− (3-PF6), pqcame = 4-carboxymethyl-2-(pyridin-2-yl)quinoline) complexes, respectively. Identification of the complexes was based on multinuclear NMR and ATR-IR spectroscopic methods, elemental analysis, conductivity measurements, UV–Vis spectroscopic, and ESI-HRMS techniques. The solid-state structures of 1-PF6 and 3-PF6 have been elucidated by single-crystal X-ray diffraction revealing a three-legged piano stool geometry. This is the first time that the in vitro cytotoxic activities of these complexes are studied. These were conducted in HEK293T (human embryonic kidney cells) and HeLa cells (cervical cancer cells) via the MTT assay. The results show poor in vitro anticancer activities for the HeLa cancer cell lines and 3-Cl proved to be the most potent (IC50 > 80 μΜ). In both cell lines, the cytotoxicity of the ligand precursor pqhyme is significantly higher than that of cisplatin. [ABSTRACT FROM AUTHOR]

In this study, gold nanoparticles were rapidly synthesized with a low-cost and environmentally friendly approach through the extract prepared using agricultural waste parts of the Nigella sativa L. plant. Properties of gold nanoparticles from N. sativa leaf extract UV-visible Spectrophotometer, X-ray diffraction, Electron Disperse X-ray, Zeta potential and Zetasizer, Field Emission Scan Electron Microscopy (FESEM), Atomic Power Microscopy, Transmission Electron Microscopy (TEM), thermogravimetric and differential thermal analysis characterized by its data. It was observed that the morphologies of the synthesized gold nanoparticles (AuNPs) exhibited a spherical appearance with an average size distribution of 107 nm and a monodisperse. In addition, they were found to be stable structures at -17.7 mV surface charge, and maximum absorbance at 538.41 nm. For the usability of AuNPs as biomedical agents, antimicrobial and anticancer effects were evaluated using Microdilution and MTT methods, respectively. It was determined that AuNPs were effective in suppressing the proliferation of 0.02-1.00 µg/mL concentration range on Staphylococcus aureus ATCC 29213, Bacillus subtilis ATCC 11774, Escherichia coli ATCC25922, Pseudomonas aeruginosa (ATCC27833) and Candida albicans pathogenic strains. The viability of CaCo-2, Skov-3, and U118 cancer cells was effectively inhibited by the produced AuNPs by, respectively, 66.73%, 30.93%, and 23.23%. It has been determined that AuNPs have significant antimicrobial and anticancer effects on hospital pathogens and cancer cell lines. [ABSTRACT FROM AUTHOR]

Bacterial contamination is a hazard in many industries, including food, pharmaceuticals, and healthcare. The availability of a rapid and simple method for detecting this type of contamination in sterile areas enables immediate intervention to avoid or reduce detrimental effects. Among these methods, colorimetric indicators are becoming increasingly popular due to their affordability, ease of use, and quick visual interpretation of the signal. In this article, a bacterial contamination indicator system was designed by incorporating MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) into an electrospun PADAS matrix, which is a biodegradable poly(ester amide) synthesized from L-alanine, 1,12-dodecanediol, and sebacic acid. Uniaxial stress testing, thermogravimetric analysis and scanning electron microscopy were used to examine the mechanical properties, thermal stability, and morphology of the mats, respectively. The capacity for bacterial detection was not only analyzed with agar and broth assays but also by replicating important environmental conditions. Among the MTT concentrations tested in this study (0.2%, 2%, and 5%), it was found that only with a 2% MTT content the designed system produced a color response visible to the naked eye with optimal intensity, a sensitivity limit of 104 CFU/mL, and 86% cell viability, which showed the great potential for its use to detect bacterial contamination. In summary, by means of the process described in this work, it was possible to obtain a simple, low-cost and fast-response bacterial contamination indicator that can be used in mask filters, air filters, or protective clothing. [ABSTRACT FROM AUTHOR]

Photosensitizers cause oxidative damages in various biological systems under light. In this study, the method for analyzing photosensitizing activity of various dietary and medicinal sources was developed using 1-(4,5-dimethylthiazol-2-yl)-3,5-diphenylformazan (thiazolyl blue formazan; MTT-F) as a probe. Significant and quantitative decolorization of MTT-F was observed in the presence of photosensitizers used in this study under light but not under dark conditions. The decolorization of MTT-F occurred irradiation time-, light intensity-, and photosensitizer concentration-dependently. The decolorized MTT-F was reversibly reduced by living cells; the LC-MS/MS results indicated the formation of oxidized products with −1 m/z of base peak from MTT-F, suggesting that MTT-F decolorized by photosensitizers was its corresponding tetrazolium. The present results indicate that MTT-F is a reliable probe for the quantitative analysis of photosensitizing activities, and the MTT-F-based method can be an useful tool for screening and evaluating photosensitizing properties of various compounds used in many industrial purposes. [ABSTRACT FROM AUTHOR]

We report herein, the design and synthesis of benzimidazole‐oxadiazole derivatives as new inhibitors for vascular endothelial growth factor receptor‐2 (VEGFR‐2). The designed members were assessed for their in vitro anticancer activity against three cancer cell lines and two normal cell lines; A549, MCF‐7, PANC‐1, hTERT‐HPNE and CCD‐19Lu. Compounds 4c and 4d were found to be the most effective compounds against three cancer cell lines. Compounds 4c and 4d were then tested for their in vitro VEGFR‐2 inhibitory activity, safety profiles, and selectivity indices using the normal hTERT‐HPNE and CCD‐19Lu cell lines. It was determined that compound 4c was the most effective and safe member of the produced chemical family. Vascular endothelial growth factor A (VEGFA) immunolocalizations of compounds 4c and 4d were evaluated relative to control by VEGFA immunofluorescence staining. Compounds 4c and 4d inhibited VEGFR‐2 enzyme with half‐maximal inhibitory concentration values of 0.475 ± 0.021 and 0.618 ± 0.028 µM, respectively. Molecular docking of the target compounds was carried out in the active site of VEGFR‐2 (Protein Data Bank: 4ASD). [ABSTRACT FROM AUTHOR]

The ternary complexes of the zinc(II), [Zn(met)(gly)(Cl)2] (1), and [Zn(met)(hist)(Cl)2] (2) are synthesized and illustrated utilizing spectroscopic and analytical measurements, and the geometry of the complexes has been identified to be octahedral. The Coats Red fern approach was employed to enumerate the thermodynamic and kinetic variables for both the Zn(II) complexes' decomposition. The quantum chemical variables were estimated utilizing the molecular orbital conformations' energy distribution, which was derived from optimal geometric shapes to test the stabilization of both complexes. DNA‐binding investigations by UV–Vis absorption, fluorescence, and viscosity were all exploited to examine the bonding properties between Zn(II) complexes and ct‐DNA, and a groove mode of bonding was established. The interactions between complexes and BSA/HSA were investigated by employing absorption and emission spectroscopic methods. The results demonstrate that complexes have a powerful ability to diminish BSA and HSA luminescence intensity, and overall associating mode is predominantly a static quenching process. The cytotoxic effect of the two Zn(II) complexes was additionally examined in human breast adenocarcinoma (MCF‐7 and MDA‐MB‐231) cell lines by employing the MTT technique. The IC50 values for every cell line were derived. Each of the two complexes was functional in both cell lines. [ABSTRACT FROM AUTHOR]

This study assessed the phenolic and flavonoid contents, and antioxidant, antibacterial, as well as cytotoxic properties of the protocorm extract of Dendrobium transparens and compared it to its wild equivalents. Methanol was used to extract compounds from the stems (DTSE) and protocorms (DTPE). DTSE contained 61.889 mg flavonoid and 82.00 mg phenolic content per gram extract equivalent to quercetin and gallic acid, respectively. At a concentration of 191.23 µg/mL, DTSE exhibited a 50% DPPH radical scavenging efficiency. Compared to the 3T3 cell line (2108.87 µg/mL), the DTPE's cytotoxic ability against the HeLa (229.30 µg/mL) and U251 (213.90 µg/mL) cell lines was found to be significantly stronger. However, the U251 cell line was strongly cytotoxic to DTSE (75.84 µg/mL). At a dose of 2000 mg/kg, neither DTSE nor DTPE caused any discernible harm in mice. They could inhibit the growth of Acinetobacter baumannii, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, and Staphylococcus aureus. Based upon the experimental results, the wild stems and protocorms were found to be alternatives suitable for creating pharmacologically bioactive substances. [ABSTRACT FROM AUTHOR]

Objective: Wound healing is characterized by the removal of dead/damaged tissue, the formation of new tissue, and finally, the restoration of the damaged tissue to its original function, starting from the moment of tissue injury. Vanillic acid (VA) is an important component of wheat bran and can heal wounds thanks to its antioxidant potential. This work aimed to investigate the dose-dependent effects of VA (1-2-4-8-16 and 32 µg/ml) in an in vitro way using a wound healing pattern in fibroblast cells. Methods: The MTT test was performed to determine cell viability 48 hours after VA application to the cells in which the wound model was created (except for the control and wound groups). The cells were examined morphologically with an inverted microscope. ELISA and Real-Time PCR analyses were performed to determine changes in oxidative stress parameters and FN1 and COL1α1 gene expressions. Results: The highest percentage closure rate of fibroblast cells in the in vitro wound pattern analysis and the highest percentage of cell viability by MTT analysis were determined in the VA-32 treated group. Morphological images showed that the evaluated gene expressions increased in fibroblast cells in a VA dose-dependent manner. Conclusion: Our findings demonstrated for the first time that VA promotes cell migration and proliferation by regulating oxidative stress and FN1A and COL1α1 genes. The results of this work are thought to pioneer the use of VA in in vivo wound healing studies. [ABSTRACT FROM AUTHOR]

The high-throughput metabolic viability-based colorimetric MTT test is commonly employed to screen the cytotoxicity of different chemotherapeutic drugs. The assay assumes a cell density-dependent linear correlation with the MTT spectral absorbance. Therefore, the present study aimed to compare the cytotoxicity assessment between the MTT assay and gold standard cell number enumeration. The cytotoxicity was induced by Cisplatin, Etoposide, and Doxorubicin in human lung epithelial adenocarcinoma cells (A549) and cervix carcinoma (HeLa) cell lines. The mitochondrial mass was estimated, and immunoblotting of succinate dehydrogenase (SDH-A) was performed following drug treatment in both cell lines. Student's t-test paired analysis was employed to calculate the significance of the results, where the value p < 0.05 was considered statistically significant. The drug-induced cytotoxic response estimated by MTT absorbance did not show any significant difference with respect to control, and no correlation was observed with the enumerated cell number in both A549 and HeLa cells. Interestingly, per-cell metabolic viability was found to be increased by 1.18 to 3.26-fold (p < 0.05) following drug treatment. Further, mechanistic investigation revealed a drug concentration-dependent significant increase in mitochondrial mass (1.21 to 4.2-fold) and upregulation of SDH protein (50–70%) as well as enzymatic activity with respect to control in both A549 and Hela cells. The limitation of the MTT assay for drug-induced cytotoxicity assessment is due to increased mitochondrial mass and SDH upregulation in surviving cells, leading to enhanced formazan formation. This leads to a lack of correlation between cell number and MTT spectral absorbance, suggesting that the MTT assay may provide an erroneous conclusion for cytotoxicity assessment. [ABSTRACT FROM AUTHOR]

Objective: Research has demonstrated that Leptospermum scoparium possesses various therapeutic benefits. This study set out to determine whether or not L. scoparium extracts had any effect on the ability of HepG2 and MCF-7 breast cancer cells to survive. Materials and Methods: The antiproliferative activity of L. scoparium extracts was explored using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide and lactate dehydrogenase assays. The most active fraction was selected to investigate its effects on apoptosis induction using flow cytometry and quantitative real-time polymerase chain reaction. The constituents of this fraction were characterized using GC-MS analysis. Results: Research demonstrated that the chloroform fraction of L. scoparium (LSCF) significantly impacted the HepG2 and MCF-7 cancer cell lines. Treatment with LSCF led to a notable rise in both early and late apoptotic cells. Furthermore, there was an upregulation in the mRNA levels of P53, Bax, and caspases, while the expression of Bcl-2 mRNA saw a decrease. The analysis of LSCF revealed the primary components to be cis-calamenene, beta-eudesmol, cyclododecane, and alpha-muurolene. Conclusion: The study showed the promising antiproliferative activity of L. scoparium, suggesting its potential application for cancer treatment. [ABSTRACT FROM AUTHOR]

Among aquatic creatures, fish are the most diversified organisms that have emerged among other vertebrates. The objective of this research was to evaluate the anticancer properties of toxin extracts from the marine puffer fish Chelonodon patoca. The toxins were extracted from the samples by homogenizing with acetic acid, and the clear supernatant was subjected to anticancer activities by MTT for cytotoxicity and cell viability on both Vero and cancer cell lines (A-549, AGS, HT-29, and MDA-MB-231). More than 70% of the normal cells were viable up to 200 µg/ml of toxin extracts so that hence the concentration was fixed below 200 µg/ml for the cell viability study on human cancer cells. Among the various organs, the toxin extracted from the liver showed potential antiproliferative activity at an inhibitory concentration of 50 µg/ml on HT-29 and MDA-MB231cell lines, 75 µg/ml on A549 and 100 µg/ml on AGS. The cellular and nuclear morphological changes, induction of apoptosis, and its stages were observed microscopically through different staining methods. Further, the DNA damage was confirmed by DNA fragmentation analysis to confirm apoptosis. The results suggest that the extract of toxin (liver) shows a significant antiproliferative effect on the human cancer cell lines. [ABSTRACT FROM AUTHOR]

Cancers present a significant medical problem despite the development of medical and pharmaceutical sciences leading to a search for further therapeutic approaches. One such approach could involve the use of curcumin or its derivatives. Curcumin reveals interesting antineoplastic effects that could help in the treatment of cancer diseases. However, this natural product possesses some limitations which prevent its application in medicine. Among its limitations, it is characterized by poor water solubility, low stability, and unsatisfactory bioavailability. Aiming to improve the pharmacokinetic properties and enhance the biological effects of curcumin, a series of 30 chemical compounds inspired by its structure was synthesized and characterized. New compounds were subjected to a preliminary MTT viability assessment of 5637 and SCaBER bladder cancer cell lines. Some derivatives revealed the cytotoxic activities already at the concentration of 1 µM. The most active compounds showed no significant acute toxicity in the Microtox test. Intracellular uptake on the basis of the fluorescent properties of the new compounds was analyzed. It was also found that the presence of the morpholine group in the structure improved the biological activity of studied curcumin derivatives. As selected compounds could be considered potential drug candidates, further studies are necessary towards recognition of the exact mechanism of cellular action, the in vivo stability, and toxicity. [ABSTRACT FROM AUTHOR]

Background The growing concern of antibiotic-resistant microbial strains worldwide has prompted the need for alternative methods to combat microbial resistance. Biofilm formation poses a significant challenge to antibiotic efficiency due to the difficulty of penetrating antibiotics through the sticky microbial aggregates. Drug repurposing is an innovative technique that aims to expand the use of non-antibiotic medications to address this issue. The primary objective of this study was to evaluate the antimicrobial properties of Diltiazem HCl, a 1,5-benzothiazepine Ca2+ channel blocker commonly used as an antihypertensive agent, against four pathogenic bacteria and three pathogenic yeasts, as well as its antiviral activity against the Coxsackie B4 virus (CoxB4). Methods To assess the antifungal and antibacterial activities of Diltiazem HCl, the well diffusion method was employed, while crystal violet staining was used to determine the anti-biofilm activity. The MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) colorimetric assay was utilized to evaluate the antiviral activity of Diltiazem HCl against the CoxB4 virus. Results This study revealed that Diltiazem HCl exhibited noticeable antimicrobial properties against Gram-positive bacteria, demonstrating the highest inhibition of Staphylococcus epidermidis, followed by Staphylococcus aureus. It effectively reduced the formation of biofilms by 95.1% and 90.7% for S. epidermidis, and S. aureus, respectively. Additionally, the antiviral activity of Diltiazem HCl was found to be potent against the CoxB4 virus, with an IC50 of 35.8 ± 0.54 μg mL−1 compared to the reference antiviral Acyclovir (IC50 42.71 ± 0.43 μg mL−1). Conclusion This study suggests that Diltiazem HCl, in addition to its antihypertensive effect, may also be a potential treatment option for infections caused by Gram-positive bacteria and the CoxB4 viruses, providing an additional off-target effect for Diltiazem HCl.

Objective: Research has demonstrated that Leptospermum scoparium possesses various thera¬peutic benefits. This study set out to determine whether or not L. scoparium extracts had any effect on the ability of HepG2 and MCF-7 breast cancer cells to survive. Materials and Methods: The antiproliferative activity of L. scoparium extracts was explored using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide and lactate dehydrogenase assays. The most active fraction was selected to investigate its effects on apoptosis induction using flow cytometry and quantitative real-time polymerase chain reaction. The constituents of this fraction were characterized using GC-MS analysis. Results: Research demonstrated that the chloroform fraction of L. scoparium (LSCF) significantly impacted the HepG2 and MCF-7 cancer cell lines. Treatment with LSCF led to a notable rise in both early and late apoptotic cells. Furthermore, there was an upregulation in the mRNA levels of P53, Bax, and caspases, while the expression of Bcl-2 mRNA saw a decrease. The analysis of LSCF revealed the primary components to be cis-calamenene, beta-eudesmol, cyclododecane, and alpha-muurolene. Conclusion: The study showed the promising antiproliferative activity of L. scoparium, suggesting its potential application for cancer treatment. [J Adv Vet Anim Res 2024; 11(2.000): 237-246]

ABSTRACTThe mechanisms of Pythium insidiosum-antigen (PIA) immunotherapy activating a patient’s immune system are unknown. We evaluated the interleukin-8 (IL-8) serum levels during P. insidiosum infection and after vaccination with PIA in vascular pythiosis cases. Furthermore, we studied the anti-P. insidiosum activity of neutrophils stimulated with various concentrations of PIA ex vivo in 3 strains of P. insidiosum isolated from vascular pythiosis patients. IL-8 serum levels were evaluated using the ELISA technique. We assessed the effect of PIA-stimulated neutrophils on the viability of zoospores using MTT assay, visualized neutrophil extracellular trap (NET) formation via microscopy, and measured the levels of double-stranded DNA (dsDNA) using PicoGreen dsDNA quantitation assay in 3 strains of P. insidiosum isolated from vascular pythiosis patients. Serum levels of IL-8 gradually lowered from the early to the end phases of vaccination with PIA among the surviving group of vascular pythiosis cases. Neutrophils stimulated with 0.01 µg/ml PIA reduced zoospore viability significantly compared to PIA-unstimulated neutrophils for strain 1 and strain 3 (p

Introduction: Human topoisomerase 1 (TOP1) is an important target of various anticancer compounds. The design and discovery of inhibitors targeting TOP1 are of great significance for the development of anticancer drugs. Evodiamine and thieno [2,3-d] pyridine hybrids show potential antitumor activity. Herein, the antigastric cancer activities of these hybrids were investigated. Methods: The inhibitory effects of different concentrations of ten evodiamine derivatives on the gastric cancer cell line SGC-7901 were assessed using a methyl thiazolyl tetrazolium assay. Compounds EVO-1 and EVO-6 strongly inhibited gastric cancer cell proliferation, with inhibition rates of 81.17% ± 5.08% and 80.92% ± 2.75%, respectively. To discover the relationship between the structure and activity of these two derivatives, density functional theory was used to investigate their optimized geometries, natural population charges, frontier molecular orbitals, and molecular electrostatic potentials. To clarify their antigastric cancer mechanisms, molecular docking, molecular dynamics simulations, and binding free energy calculations were performed against TOP1. Results: The results demonstrated that these compounds could intercalate into the cleaved DNA-binding site to form a TOP1-DNA-ligand ternary complex, and the ligand remained secure at the cleaved DNA-binding site to form a stable ternary complex. As the binding free energy of compound EVO-1 with TOP1 (-38.33 kcal·mol-1) was lower than that of compound EVO-6 (-33.25 kcal·mol-1), compound EVO-1 could be a more potent anti-gastric cancer agent than compound EVO-6. Discussion: Thus, compound EVO-1 could be a promising anti-gastric cancer drug candidate. This study may facilitate the design and development of novel TOP1 inhibitors. [ABSTRACT FROM AUTHOR]

• The methanol extract of Hypericum linarioides (MHL) has positive effect on human dermal fibroblast cell proliferation. • MHL-containing nanoemulsion formulation (MHL-NEF) with droplet size less than 160 nm was prepared successfully. • For MHL and MHL-NEF, the maximum cell viability% was obtained at 0.4 µg/mL. • It was observed as a result of scratch assay that NEF improved the wound-healing potential of MHL. • TGF-β1 and FGFR-2 expressions in MHL-NEF-treated fibroblast cells increased significantly at 24 h. It was aimed to develop and in vitro characterize the methanol extract of Hypericum linarioides (MHL)-containing nanoemulsion formulation (MHL-NEF) to heal the wound effectively. MHL-NEF was prepared and its droplet size, polydispersity index (PDI), viscosity, pH and zeta potential (ZP) values were determined. The effect of MHL and MHL-NEF on human dermal fibroblast cell viability was examined by MTT assay. Also, their wound healing potential was evaluated using the scratch assay. The droplet size, PDI, ZP, pH and viscosity values for the MHL-NEF were found to be 157.67±7.61 nm, 0.268±0.036, (-)40.20±6.79 mV, 4.27±0.01, and 1.82±0.01 cP, respectively. In the cell viability assay, the highest percentage of living cells was obtained at concentration of 0.4 µg/mL for the MHL and MHL-NEF. In the scratch assay, MHL-NEF showed significantly ameliorated wound closure (%) rates at 24 and 30 h than the groups of control, MHL and blank-NEF (NEF without MHL) (p < 0.001). Immunofluorescence staining was carried out. TGF-β1 and FGFR-2 expressions in MHL-NEF-treated fibroblast cells increased significantly at 24 h compared to the groups of control, MHL, and B-NEF (p < 0.001). Our findings show that MHL-NEF may be promising for better wound healing. [ABSTRACT FROM AUTHOR]