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• Piroxicam has been efficiently loaded into nano-engineered vesicles. • Piroxicam nano-vesicles were homogenously incorporated into alginate/pectin composite gel. • Nano-sized piroxicam gel demonstrated enhanced significant dose-dependent wound closure percentage compared to control. Drug repurposing is a potential strategy to overcome the huge economic expenses of wound healing products. This work aims to develop a topical gel of piroxicam encapsulated into a nanospanlastics vesicular system as an effective, dermal wound dressing. Firstly, piroxicam was entrapped into nanospanlastics formulations and optimized utilizing 23 full factorial experimental designs. The scrutinized factors were Span 60: Edge activator ratio, edge activator type, and permeation enhancer type. The measured responses were vesicle size (VS), polydispersity index (PDI), and% entrapment efficiency (EE). The optimized formula was further adopted into an alginate-pectin gel matrix to maximize adherence to the skin. The rheology and in-vitro release were studied for the developed nanospanlastics gel. Cytotoxicity and wound healing potential using scratch assay were assessed on human adult dermal fibroblast cells. The optimal piroxicam nanospanlastics formula demonstrated a VS of 124.1 ± 1.3 nm, PDI of 0.21 ± 0.01, and EE% of 97.27±0.21%. About 70.0 ± 0.9% and 57.4 ± 0.1% of piroxicam were released from nanospanlastics dispersion and gel within 24 h, respectively. Nanospanlastics gel of piroxicam flowed in a non-Newtonian pseudoplastic shear thinning pattern. It was also biocompatible with the human dermal fibroblast cells and significantly promoted their migration rate which suggests an auspicious cutaneous wound healing aptitude. [Display omitted] [ABSTRACT FROM AUTHOR]

Bio-inspired zinc oxide nanoparticles are gaining immense interest due to their safety, low cost, biocompatibility, and broad biological properties. In recent years, much research has been focused on plant-based nanoparticles, mainly for their eco-friendly, facile, and non-toxic character. Hence, the current study emphasized a bottom-up synthesis of zinc oxide nanoparticles (ZnO NPs) from Psidium guajava aqueous leaf extract and evaluation of its biological properties. The structural characteristic features of biosynthesized ZnO NPs were confirmed using various analytical methods, such as UV–Vis spectroscopy, X-ray diffraction (XRD), energy-dispersive X-ray analysis (EDX), Fourier transform infrared spectroscopy (FT-IR), dynamic light scattering (DLS), Scanning electron microscopy (SEM) and high-resolution transmission electron microscopy (HR-TEM). The synthesized ZnO NPs exhibited a hydrodynamic shape with an average particle size of 11.6–80.2 nm. A significant antimicrobial efficiency with minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of 40 and 27 µg/ml for Enterococcus faecalis, followed by 30 and 40 µg/ml for Staphylococcus aureus, 20 and 30 µg/ml for Staphylococcus mutans, 30 µg/ml for Candida albicans was observed by ZnO NPs. Additionally, they showed significant breakdown of biofilms of Streptococcus mutans and Candida albicans indicating their future value in drug-resistance research. Furthermore, an excellent dose-dependent activity of antioxidant property was noticed with an IC50 of 9.89 µg/ml. The antiproliferative potential of the ZnO NPs was indicated by the viability of MDA MB 231 cells, which showed a drastic decrease in response to increased concentrations of biosynthesized ZnO NPs. Thus, the present results open up vistas to explore their pharmaceutical potential for the development of targeted anticancer drugs in the future. [ABSTRACT FROM AUTHOR]

Super-paramagnetic iron oxide nanoparticles were synthesized by a co-precipitation method, which was further functionalized with chitosan (CS). The composite was investigated for binding with Nystatin (Nyst), a polyene polyhydroxy antifungal widely used in management of mucocutaneous fungal infections. The structure of the Fe3O4/CS/Nyst composite was characterized by different physicochemical techniques. Transmission electron microscope analysis revealed the Fe3O4/CS/Nyst composite with a mean diameter of ∼10–20 nm in a monodispersed spherical form. Fourier-transform infrared spectroscopy analysis confirmed the binding of CS on Fe3O4 NPs and also the loading of Nyst on the nanostructure. The UV–Vis absorption spectroscopy demonstrated the Nyst drug loading by 22% capacity. The antifungal activity of the Fe3O4/CS/Nyst was evaluated against Candida species and Aspergillus fumigatus, which demonstrated excellent activity with a minimum inhibitory concentration ranging from 2 to 16 μg/mL. The MTT assay was used to evaluate the toxicity of compounds which did not reveal any toxic effect on the adipose derived mesenchymal stem cells. Regarding remarkable antifungal activities and low toxicity of this magnetic nano-compound, it could be a good candidate for target therapy of mucocutaneous and local fungal infections. [ABSTRACT FROM AUTHOR]

Prior studies have extensively investigated the essential oil derived from the Mediterranean cypress, Cupressus sempervirens. However, the 'Stricta' variety, known for its ornamental value, has received less attention in terms of its oil composition and potential health benefits. The objective of this research was to comprehensively analyze the chemical components and medicinal properties of the essential oil extracted from C. sempervirens 'Stricta' (CSSLEO) grown in Egypt. Utilizing gas chromatography–mass spectrometry (GC–MS), the investigation identified 22 compounds within CSSLEO, with α-pinene and δ-3-carene being predominant, accounting for 96.01% of the oil. In vitro assays evaluated CSSLEO's cytotoxic effects on cancer cell lines, revealing notable anticancer potential. Additionally, the oil displayed antidiabetic properties by impeding crucial enzymes involved in glucose metabolism. Complementary in silico network pharmacology and molecular docking studies provided insights into the possible interactions between CSSLEO's key compounds and essential proteins and pathways in cancer treatment. The results underscored CSSLEO's intricate composition and its promising applications in cancer prevention and diabetes management. The conclusions drawn from this research underscore the need for further investigation to validate CSSLEO's clinical effectiveness and to gain a deeper understanding of its therapeutic mechanisms, with a view to harnessing its potential in oncology and endocrinology. [ABSTRACT FROM AUTHOR]

Organometallic ruthenium complexes with p-cymene = 1-methyl-4-(1-methylethyl)-benzene and N^N = bidentate polypyridyl ligands constitute interesting candidates with biological and catalytic properties. Towards this aim, we have synthesized four ruthenium(II)–arene complexes of the type [Ru(η6-p-cymene)(N^N)Cl][X] (N^N = Br-Qpy = 6-bromo-4-phenyl-2-pyridin-2-yl-quinoline, X = Cl− (1a); PF6− (1b); N^N = OH-Ph-Qpy = 4-(4-phenyl-2-(pyridin-2-yl)quinolin-6-yl)phenol, X = Cl− (2a); PF6− (2b)). This is the first report of ruthenium(II) p-cymene complexes incorporating substituted pyridine–quinoline ligands, with –Br and –C6H4OH groups in the 6-position of quinoline. We also refer to the cytotoxicity of the ligands and their possible effect of modulating the activity of the ruthenium(II) complexes. These were characterized by a combination of spectroscopic methods (ATR-IR, UV–Vis, multinuclear NMR), elemental analysis, and conductivity measurements. The solid-state structure of 2b, determined by single-crystal X-ray diffraction, reveals a three-legged piano-stool geometry. The in vitro cytotoxic activities of the new complexes were evaluated in HEK293T (human embryonic kidney cells) and in HeLa cells (cervical cancer cells), via the MTT assay. Poor in vitro anticancer activities were observed for the HeLa cancer cell line, with 2a being the most potent (IC50 = 75 μΜ). The cytotoxicity of Br-Qpy in HEK293T is comparable to that of cisplatin. Both complexes 1a and 1b successfully catalyze the transfer hydrogenation of benzophenone to benzhydrol by 2-propanol at 82 °C. The catalytic performance of 1a in the ratio of S:Cat:B = 400:1:40 (S = substrate, Cat = catalyst, B = base = KOiPr) leads to a conversion of 94%, within 3 h of reaction. Presumably, catalytic transformation takes place via ruthenium(II) hydride species being the active catalyst. [ABSTRACT FROM AUTHOR]

Sulfonamides are important compounds with special applications in pharmaceuticals due to their antibacterial and antiparasitic properties, and they are known as sulfa drugs (SDs). In this study, we focused on the multifunctional therapeutic compound sulfathiazole (ST) and investigated its hybridization of imine bonds with various azo compounds. A series of novel azoimino-sulfathiazoles (AIST) was successfully synthesized using a one-pot three-component reaction (3MCR) methodology. Additionally, we reported the design and synthesis of two ST derivatives bound to an azo group in a 3MCR dish. The structure of the newly synthesized AISD after separation and purification was examined and confirmed by TLC, M.P., FT-IR, 1H NMR, and 13C NMR. Furthermore, their cytotoxicity was evaluated via MTT assay. The antibacterial, antioxidant, and anticancer activities of the AISD compounds were assessed using the MTT assay, focusing on the PC-3 human prostate cancer cell line. The results showed good resistance to E. coli and S. aureus, with inhibition zones of 27 and 31 mm, respectively, compared to standard penicillin G. More importantly, certain AIST compounds exhibited superior antibacterial activity compared to penicillin G. To understand the mode of action of the proteins and potential interactions, docking calculations were performed using the target proteins 1FDW, 3FC2, and 5GWK. 5GWK achieved the highest placement score, followed by 1FDW and 3FC2, which showed strong closeness. A detailed analysis of the ligand–protein interactions revealed the strongest interaction with human topoisomerase II alpha (5GWK) as the target protein. [ABSTRACT FROM AUTHOR]

We herein described a biogenic route for the in situ supporting silver nanoparticles on hydroxymethylated lignin (HL) coated Fe3O4 (iron oxide) magnetic nanoparticles using the Cydonia oblonga flower extract (Fe3O4@HL/Ag NPs) and its catalytic activity in the acetylation of alcohols and subsequent its biological activity are investigated. The successful fabrication of Fe3O4@HL/Ag NPs was established by using advanced analytical techniques such as Fourier Transformed Infra-Red spectroscopy, Transmission Electron Microscopy, Field Emission Scanning Electron Microscopy, Energy Dispersive X-ray spectroscopy, elemental mapping and Vibrating Sample Magnetization. The 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay was used to measure anti-thyroid cancer (on WRO, FTC133, BCPAP, TPC1, K1, and 8505C cells) properties of Fe3O4@HL/Ag NPs nanocomposite. The findings indicate that in 3 days, the cancer cell survival percentage in various dilations reduced as much as the Fe3O4@HL/Ag NPs nanocomposite concentration increased. The best anticancer effect was reported at 1000 μg/ml dilation. MTT findings reveal that IC50 = 146, 181, 250, 141, 170, and 125 µg/ml is a Fe3O4@HL/Ag NPs nanocomposite concentration in which 50% of the WRO, FTC133, BCPAP, TPC1, K1, and 8505C thyroid carcinoma cells. The results indicated that these Fe3O4@HL/Ag NPs nanocomposite could inhibit thyroid cancer cells more strongly than normal cells. Fe3O4@HL/Ag NPs nanocomposite shows high antioxidant effects against DPPH. [ABSTRACT FROM AUTHOR]

(1) Background: The aim of this study was to compare the cytotoxicity of selected resin-modified materials used in direct contact with the dental pulp (TheraCal LC, TheraCal PT, and ApaCal ART) with calcium silicate cement (Biodentine). (2) Methods: The mouse fibroblast Balb/3T3 cell line and the extracts of tested materials in four concentrations were used for the testing. An MTT assay was performed in three independent experiments with six replicates for each concentration of tested material. The cell viability (%) and cytotoxicity were expressed (cytotoxic effect is considered in cases where the cell viability is lower than 70%). The mean of the cell viability and the standard deviation were expressed for each material at all concentrations. ANOVA and Dunnet's post hoc tests were used for the statistical analysis. All of these tests were performed at the 0.05 significance level. (3) Results: At all concentrations, the cell viability was statistically significantly lower (p ≤ 0.002) for all tested materials compared to Biodentine. ApaCal ART showed a high level of cytotoxicity at all concentrations (cell viability lower than 47.71%, p < 0.0001). The same result was found for TheraCal LC at concentrations of 100%, 50% and 25% and TheraCal PT at concentrations of 100% and 50%. TheraCal LC at a 10% concentration (cell viability 68.18%) and TheraCal PT at a 25% concentration (cell viability 60.63%) indicated potential cytotoxicity. TheraCal PT at a 10% concentration was not found to be cytotoxic (cell viability 79.18%, p = 0.095). (4) Conclusion: The resin-modified calcium silicate and calcium phosphate materials showed higher cytotoxic potential, so they should be used with caution when in direct contact with the dental pulp. [ABSTRACT FROM AUTHOR]

Cancer, one of the deadliest diseases, is the second leading cause of mortality all over the world. The study aims to investigate the phytochemical profile and in vitro antioxidant activity of ethanol extracts from Ipomoea pes-tigridis and assess its cytotoxicity against three cell lines. Its qualitative and quantitative phytochemical analysis revealed that the plant possesses various secondary metabolites like tannins and flavonoids, which have potent antioxidant properties. The DPPH (2,2-Diphenyl-1-picrylhydrazyl) and nitric oxide (NO) free radical assays showed promising in vitro antioxidant potential. The ethanol extracts demonstrated significant cytotoxicity against A375, B-16-F10, and NHDF cell lines, with IC50 values ranging from 12.02 ± 3.14 μg/mL to 136.42 ± 2.92 μg/mL. These findings suggest that Ipomoea pes-tigridis may contain compounds with potential anticancer properties, which warrant further investigation for identification and characterisation. The observed activities of the plant can be credited to the polyphenolic compounds, and future research is needed to assess the detailed phytochemistry and biological activities of Ipomoea pestigridis. [ABSTRACT FROM AUTHOR]

Cerium oxide nanoparticles possess unique properties that make them promising candidates in various fields, including cancer treatment. Among the proposed synthesis methods for CNPs, biosynthesis using natural extracts, offers an eco-friendly and convenient approach for producing CNPs, particularly for biomedical applications. In this study, a novel method of biosynthesis using the aqueous extract of Eucalyptus camaldulensis leaves was used to synthesize CNPs. Scanning electron microscopy and Transmission electron microscopy (TEM) techniques revealed that the synthesized CNPs exhibit a flower-like morphology. The particle size of CNPs obtained using Powder X-ray diffraction peaks and TEM as 13.43 and 39.25 nm. Energy-dispersive X-ray spectroscopy and Fourier transform infrared spectroscopy confirmed the effect of biomolecules during the synthesis process and the formation of CNPs. The cytotoxicity of biosynthesized samples was evaluated using the MTT method demonstrating the potential of these samples to inhibit MCF-7 cancerous cells. The viability of the MCF-7 cell line conducted by live/dead imaging assay confirmed the MTT cytotoxicity method and indicated their potential to inhibit cancerous cells. Furthermore, the successful uptake of CNPs by MCF-7 cancer cells, as demonstrated by confocal microscopy, provides evidence that the intracellular pathway contributes to the anticancer activity of the CNPs. In general, results indicate that the biosynthesized CNPs exhibit significant cytotoxicity against the MCF-7 cancerous cell line, attributed to their high surface area. [ABSTRACT FROM AUTHOR]

Helicobacter pylori, a leading human pathogen associated with duodenal ulcer and gastric cancer, presents a significant threat to human health due to increasing antibiotic resistance rates. This study investigates G‐quadruplexes (G4s), which are non‐canonical secondary structures form in G‐rich regions within the H. pylori genome. Extensive research on G4s in eukaryotes has revealed their role in epigenetically regulating cellular processes like gene transcription, DNA replication, and oncogene expression. However, understanding of G4‐mediated gene regulation in other organisms, especially bacterial pathogens, remains limited. Although G4 motifs have been extensively studied in a few bacterial species such as Mycobacterium, Streptococci, and Helicobacter, research on G4 motifs in other bacterial species is still sparse. Like in other organisms such as archaea, mammals, and viruses, G4s in H. pylori display a non‐random distribution primarily situated within open reading frames of various protein‐coding genes. The occurrence of G4s in functional regions of the genome and their conservation across different species indicates that their placement is not random, suggesting an evolutionary pressure to maintain these sequences at specific genomic sites. Moreover, G‐quadruplexes show enrichment in specific gene classes, suggesting their potential involvement in regulating the expression of genes related to cell wall/membrane/envelope biogenesis, amino acid transport, and metabolism. This indicates a probable regulatory role for G4s in controlling the expression of genes essential for H. pylori survival and virulence. Biophysical techniques such as Circular Dichroism spectroscopy and Nuclear Magnetic Resonance were used to characterize G4 motifs within selected H. pylori genes. The study revealed that G‐quadruplex ligand inhibited the growth of H. pylori, with minimal inhibitory concentrations in the low micromolar range. This suggests that targeting G4 structures could offer a promising approach for developing novel anti‐H. pylori drugs. [ABSTRACT FROM AUTHOR]

In this work, we describe the synthesis and characterisation of the starting materials [Cp*IrCl2]2 and four new ruthenium(II) and iridium(III) complexes half sandwich, contain the fragments [(p-cymene)Ru]2+ and [Cp*Ir]2+; (Cp* = CpMe4Et) of stoichiometry: [Cp*IrCl2(2-aminopyridine)] (I), [Cp*IrCl2(4-aminopyridine)] (II), [Cp*IrCl2(adenine)] (III) and [(p-cymene)RuCl2(adenine)] (IV). The new compounds have been characterised by C, H, and N elemental analysis; infrared and 1H NMR spectroscopy with 1H–1H COSY, ESI/TOF mass spectrometry and thermogravimetry. A study of the cytotoxicity of these compounds against the Hela cell line was carried out, with results indicating a low activity. [ABSTRACT FROM AUTHOR]

In the area of drug development the solubility of an active ingredient plays a very crucial and vital part and is of the highest significance. Increasing importance is being placed on the research into active ingredient solubilization. The designing of a host guest complex with a compound that has a higher dissolubility profile can work with the solubilization of lipophilic drugs. In this research work optimized nano-carriers were effectively synthesized utilizing thin-film hydration strategies. The drug sulfonated calix[4]resorcinarene blend (1:10) containing ethanol was dispersed and sonicated with an estimated three cycles, at an amplitude 70 with a 20-s interval for an optimized time. The synthesized nanovesicles have an average diameter of 477.7 nm, a higher mono dispersity (PDI-0.282), and a greater loading capacity of the drugs is 95%. Atomic force microscopy in accordance with dynamic light-scattering spectra confirmed the spherical shape of paclitaxel-loaded sulfonated calix[4]resorcinarene nanovesicles. In vitro release of medication from nanovesicles affirmed the extended discharge pattern of drugs with r2 of 0.9902 compared with the commercial formulation available on the market. MTT assay is performed to access the toxicity of the sufonated calix[4]resorcinarene in vitro. IC50 values indicate that synthesized sufonated calix[4]resorcinarene shows better IC50 values than paclitaxel and taxol. The formulated nanovesicles from sulfonated calix[4]resorcinarene showed an ideal size with higher capacity for binding drug and provide better patient compliance, which are positive for their expected application as a modular drug delivery platform for anti-cancer drugs. [ABSTRACT FROM AUTHOR]

The agricultural byproduct, represented by durian peels during the season, needs to be converted into economic value within the local area. This study aimed to assess the pharmaceutical properties, specifically antioxidant and anti-inflammatory effects, of methanol extracts from both flowers and peels of the local durian in the district. Additionally, in vitro testing was conducted to evaluate the impact on cells and the inhibition of nitric oxide induced by LPS. Results indicated that the flowers' extract exhibited a higher concentration of antioxidants compared to the peels. The FRAP assay, using Trolox and Fe(II) as standards, showed statistically significant differences (p-value < 0.05) with values of 427.40 ± 7.64 μmole TE/g extract and 3,568.47 ± 77.55 μmole Fe(II) equivalent/g extract, along with a DPPH scavenging of 85.19 % and an IC50 of 114.50 ± 7.27 μg/mL. Concerning the inhibition of LPS-induced nitric oxide content, the peels' extract, excluding KS7, demonstrated a response. KS10 exhibited the highest statistically significant difference (p-value < 0.05) in inhibition at concentrations of 0.6, 0.8 and 10 μg/mL, while others showed inhibition at 1.0 μg/mL. The outcomes of this research suggest the potential to enhance the value of agricultural waste, contributing to both the development of durian agriculture and public health at the local level. [ABSTRACT FROM AUTHOR]

Two new binuclear tetranitrosyl iron complexes of the composition [Fe2L2(NO)4] (1, L = 4-methoxybenzenemethanethiolyl; 2, L = 4-chlorobenzenemethanethiolyl) were synthesized. Their crystals were characterized by X-ray diffraction, by IR, ESR, UV, and Mössbauer spectroscopies, and by elemental analysis. The NO-donating properties and transformations of the complexes in physiological solutions, including reactions in the presence of bovine serum albumin, were studied. The cytotoxicity of compounds 1 and 2 was studied on normal Vero cells. The effect of the complexes on enzymes was investigated taking guanylate cyclase and adenylate cyclase as examples. The results obtained allow one to recommend compound 2 for further investigations as a potential drug with vaso- and bronchodilator properties. [ABSTRACT FROM AUTHOR]

Sodium acetate (NaA) and sodium sulfite (NaS) are two food additives in the class of preservatives. In this study, 3-(4,5-dimethyl thiazolyl-2)-2,5 diphenyltetrazolium bromide (MTT) assay was established to detect the cytotoxicity, and comet assay was used to determine the genotoxicity of NaA and NaS. For the MTT assay, human hepatocellular carcinoma (HepG2) cells were treated with different concentrations of each preservative (15.63, 31.25, 62.50, 125, 250, 500, 1000 and 2000 μg/mL for NaA; 3.91, 7.81, 15.62, 31.25, 62.50, 125, 250 and 500 μg/mL for NaS, respectively) for 24-h. non-treated wells used as control (only medium) were included. Comet assay was performed on lymphocytes isolated from healthy donors with multiple concentrations of NaA (15.63, 31.25, 62.50, 125, 250 μg/mL) and NaS (3.91, 7.81, 15.62, 31.25, 62.50 μg/mL) for 1 h. A negative (distilled water) and a positive control (100 μM H2O2) were also included. Significant cytotoxic activity was detected for NaA and NaS only at the highest concentration. Besides, both substances significantly increased DNA damage compared to the control at almost all concentrations (except at low concentrations). In general, both food preservatives exhibited weak cytotoxic effects in HepG2 cells. These food preservatives showed genotoxic activity, especially at higher concentrations. [ABSTRACT FROM AUTHOR]

Abstract Cerium oxide nanoparticles possess unique properties that make them promising candidates in various fields, including cancer treatment. Among the proposed synthesis methods for CNPs, biosynthesis using natural extracts, offers an eco-friendly and convenient approach for producing CNPs, particularly for biomedical applications. In this study, a novel method of biosynthesis using the aqueous extract of Eucalyptus camaldulensis leaves was used to synthesize CNPs. Scanning electron microscopy and Transmission electron microscopy (TEM) techniques revealed that the synthesized CNPs exhibit a flower-like morphology. The particle size of CNPs obtained using Powder X-ray diffraction peaks and TEM as 13.43 and 39.25 nm. Energy-dispersive X-ray spectroscopy and Fourier transform infrared spectroscopy confirmed the effect of biomolecules during the synthesis process and the formation of CNPs. The cytotoxicity of biosynthesized samples was evaluated using the MTT method demonstrating the potential of these samples to inhibit MCF-7 cancerous cells. The viability of the MCF-7 cell line conducted by live/dead imaging assay confirmed the MTT cytotoxicity method and indicated their potential to inhibit cancerous cells. Furthermore, the successful uptake of CNPs by MCF-7 cancer cells, as demonstrated by confocal microscopy, provides evidence that the intracellular pathway contributes to the anticancer activity of the CNPs. In general, results indicate that the biosynthesized CNPs exhibit significant cytotoxicity against the MCF-7 cancerous cell line, attributed to their high surface area.

AbstractThe various therapeutic drugs that are currently utilized for the management of cancer, especially breast cancer, are greatly challenged by the augmented resistance that is either acquired or de novo by the cancer cells owing to the long treatment periods. So, this study aimed at elucidating the possible anticancer potential of four compounds 7, 4′, 7′′, 4′′′-tetra-O-methyl amentoflavone, hesperidin, ferulic acid, and chlorogenic acid that are isolated from Cycas thouarsii leaves n-butanol fraction for the first time. The MTT assay evaluated the cytotoxic action of four isolated compounds against MDA-MB-231 breast cancer cells and oral epithelial cells. Interestingly, ferulic acid revealed the lowest IC50 of 12.52 µg/mL against MDA-MB-231 cells and a high IC50 of 80.2 µg/mL against oral epithelial cells. Also, using an inverted microscope, the influence of ferulic acid was studied on the MDA-MB-231, which revealed the appearance of apoptosis characteristics like shrinkage of the cells and blebbing of the cell membrane. In addition, the flow cytometric analysis showed that the MDA-MB-231 cells stained with Annexin V/PI had a rise in the count of the cells in the early and late apoptosis stages. Moreover, gel electrophoresis detected DNA fragmentation in the ferulic acid-treated cells. Finally, the effect of the compound was tested at the molecular level by qRT-PCR. An upregulation of the pro-apoptotic genes (BAX and P53) and a downregulation of the anti-apoptotic gene (BCL-2) were observed. Consequently, our study demonstrated that these isolated compounds, especially ferulic acid, may be vital anticancer agents, particularly for breast cancer, through its induction of apoptosis through the P53-dependent pathway.

Leaves of Stevia rebaudiana are rich source of sweet glycosides of steviol. The major glycoside, stevioside, diterpenoid glycoside--is used in India and various countries as a food sweetener for diabetic patients. Its medical use is also reported in various ailments like heart, liver, pancrease etc. Besides this it is also being used against obesity, stomach burn and to lower uric acid levels in blood. In present study the leaf extract with various extract were tested for immunomodulatry properties. We performed MTT assay to check the cell viability and cytotoxicity in peripheral blood mononuclear cell (PBMC) and also calculated the Trolox equivalent values to assess the antioxidant properties of Stevia rebaudiana.. Percent cell viability values of cells were found to be more than 50 percentages with increase in concentration. At higher dose all these extract showed significant inhibitory effects on proliferation. The aqueous extracts shown the maximum value of Trolox equivalent with 1:16 dilution. It means with the increase in the concentration of extract there is substantial increase in antioxidant property or we can assume antioxidant is dose dependent. But in same time cell viability gets reduced with increase in concentration. [ABSTRACT FROM AUTHOR]

The aim of the study was to prepare nanostructured lipid carriers (NLCs) co-encapsulated with Quercetin and Morin and to compare the cytotoxicity of the NLCs with individual drugs as well as with their combination form. The Quercetin and Morin co-encapsulated NLCs were prepared by ultrasonication method. The size of the NLCs particles, the zeta potential value, % of drug entrapment efficiency (% EE), and % of cumulative drug release (% CDR) were estimated. The in vitro cytotoxicity study was carried out in MCF 7 cancer cell. The size of the NLCs particles ranged from 297.6 ± 14.1 to 456.4 ± 14.1 nm. The % EE of Quercetin and Morin in the optimized NLCs formulation (F6) were found to be 84.27 ± 2.1% and 87.11 ± 2.6%, respectively. However, the % CDR of Morin and Quercetin from the F6 formulation were 72.11 ± 3.4% and 81.56 ± 3.6%, respectively. The results of FTIR spectroscopy study indicated that the functional groups of Quercetin and Morin were remained intact in NLCs formulations. The TEM study result revealed that the prepared NLCs were spherical in shape. The in vitro cytotoxicity study result revealed that dual drug loaded NLCs showed higher cytotoxicity as compared to individual drug and their combinations. It was concluded that the Quercetin and Morin co-encapsulated NLCs formulation could be a promising candidate for combating the chemotherapy resistance in breast cancer. [ABSTRACT FROM AUTHOR]

This study aims to evaluate the biocompatibility of a novel filler material intended to improve the longevity of polymer systems used in prosthetics in respect of cytotoxicity and skin irritation. RTV50F silicone elastomer incorporated with various percentages of hexagonal boron nitride (H-BN) (0.1, 0.3, 0.5, 0.7, and 1 wt%) have been tested. Silicone without H-BN was utilized as the control for comparison. The in vitro cytotoxicity test includes specimens (n=18) with 10 mm in diameter and 2 mm in thickness applied directly to the normal human fibroblast cell line (NHF) and incubated for 72 hours, then 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay was used to determine the cell viability. The skin irritation test was conducted in vivo, in which specimens (n=12) with 25 mm × 25 mm dimensions were applied on the back of 5 different rabbits for 4 hours, then the skin response was evaluated after 24, 48, and 72 hours. The acquired in vitro data were statically analyzed using one-way ANOVA and post-hoc Tukey’s tests with GraphPad Prism 8, where P-value < 0.05 was considered statistically significant. The H-BN powder and silicone specimens were studied via field emission scanning electron microscopy (FE-SEM). The results revealed a negligible effect of maxillofacial silicone on cell viability after 72 hours of incubation, only one group (1wt%) showed a significant difference compared to the control group but the toxicity percentage didn’t exceed 30% of cell viability and there was no skin irritation during the in vivo test.

Abstract Recently, there is a particular interest to utilize protic ionic liquids (PILs) in drug solubility. This study is exploring the effect of three protic ionic liquids (PILs) based on 2-hydroxyethylammonium carboxylate [2-hydroxyethylammonium acetate (MEAA), 2-hydroxyethylammonium lactate (MEAL), and 2-hydroxyethylammonium propionate (MEAP)] on the solubility of the very poorly soluble drug in water, indomethacin (IMC). The shake flask method was used to measure the experimental solubility of IMC at the different temperatures range (298.15–313.15) K. The results demonstrate significantly enhancment the solubility of IMC in PILs compared to pure water, with an approximate increase of 200 times. The experimental solubility data have been correlated using the empirical models which showed the performance as the order: Modified Apelblat–Jouyban–Acree > Van’t Hoff–Jouyban–Acree > Modified Apelblat equations and also the performance for the Wilson model indicated as the order (absolute relative deviation): 2-hydroxyethylammonium acetate (3.030) > 2-hydroxyethylammonium propionate (3.239) > 2-hydroxyethylammonium lactate (7.665). Then the thermodynamic dissolution properties were obtained by usage of Gibbs and Van’t Hoff equations to investigate the thermodynamic behavior of the IMC in the aqueous solution PILs. Eventually, the cytotoxicity of the co-solvents (PILs) under study was evaluated using a standard MTT assay. The results showed that the cell viability percentage increased in the following order: MEAA

Abstract Carbon nanotubes (CNTs) have the potential to serve as delivery systems for medicinal substances and gene treatments, particularly in cancer treatment. Co-delivery of curcumin (CUR) and Methotrexate (MTX) has shown promise in cancer treatment, as it uses fewer drugs and has fewer side effects. This study used MTX-conjugated albumin (BSA)-based nanoparticles (BSA-MTX) to enhance and assess the efficiency of CUR. In-vitro cytotoxicity tests, DLS, TEM, FTIR, UV/Vis, SEM, and DSC studies assessed the formulations' physical and chemical properties. The Proteinase K enzyme was used to severe amidic linkages between MTX and BSA. The findings demonstrated the efficacy of using ƒ-MWCNT-CUR-BSA-MTX as a vehicle for efficient co-delivery of CUR and MTX in cancer treatment. The MTT colorimetric method was used to evaluate the effect of chemical and medicinal compounds. Cell division was studied using the MTT method to investigate the effect of pure MWCNT, pure CUR, MTX-BSA, and ƒ-MWCNT-CUR-MTX-BSA. Studies on cell lines have shown that the combination of curcumin and MTX with CNT can increase and improve the effectiveness of both drugs against cancer. A combination of drugs curcumin and methotrexate simultaneously had a synergistic effect on MCF-7 cells, which indicated that these drugs could potentially be used as a strategy for both prevention and treatment of breast cancer. Also, ƒ-MWCNT-CUR-MTX-BSA was found to have a significant effect on cancer treatment with minimal toxicity compared to pure curcumin, pure MTX-BSA, MTX, and ƒ-MWCNT alone. Unique properties such as a high ratio of specific surface area to volume, high chemical stability, chemical adsorption ability, high capacity of drug and biomolecules of carbon nanotubes, as well as multiple drug loading at the same time The combination of ƒ-MWCNT-CUR-BSA MTX significantly impacts cancer therapy), are desirable as an alternative option for targeted drug delivery and high therapeutic efficiency.

Abstract Sirtuin 3 (SIRT3) belongs to the Sirtuin protein family, which consists of NAD+-dependent lysine deacylase, involved in the regulation of various cellular activities. Dysregulation of SIRT3 activity has been linked to several types of cancer, including breast cancer. Because of its ability to stimulate adaptive metabolic pathways, it can aid in the survival and proliferation of breast cancer cells. Finding new chemical compounds targeted towards SIRT3 was the primary goal of the current investigation. Virtual screening of ~ 800 compounds using molecular docking techniques yielded 8 active hits with favorable binding affinities and poses. Docking studies verified that the final eight compounds formed stable contacts with the catalytic domain of SIRT3. Those compounds have good pharmacokinetic/dynamic properties and gastrointestinal absorption. Based on excellent pharmacokinetic and pharmacodynamic properties, two compounds (MI-44 and MI-217) were subjected to MD simulation. Upon drug interaction, molecular dynamics simulations demonstrate mild alterations in the structure of proteins and stability. Binding free energy calculations revealed that compounds MI-44 (− 45.61 ± 0.064 kcal/mol) and MI-217 (− 41.65 ± 0.089 kcal/mol) showed the maximum energy, suggesting an intense preference for the SIRT3 catalytic site for attachment. The in-vitro MTT assay on breast cancer cell line (MDA-MB-231) and an apoptotic assay for these potential compounds (MI-44/MI-217) was also performed, with flow cytometry to determine the compound’s ability to cause apoptosis in breast cancer cells. The percentage of apoptotic cells (including early and late apoptotic cells) increased from 1.94% in control to 79.37% for MI-44 and 85.37% for MI-217 at 15 μM. Apoptotic cell death was effectively induced by these two compounds in a flow cytometry assay indicating them as a good inhibitor of human SIRT3. Based on our findings, MI-44 and MI-217 merit additional investigation as possible breast cancer therapeutics.

Based on data released by Globocan in 2020, the incidence of colorectal cancer is the fourth highest in Indonesia (8.6%) and the third in the world (10%). This disease is hard to treat because the available therapy is less effective. Therefore, it is necessary to develop effective alternative therapies, especially those originating from Indonesia's natural resources, easy to obtain and reproduce. This study aims to determine the potential of red eye snail extract as an anticancer through cytotoxicity tests with the MTT Assay method on colon cancer cells WiDr and DNA fragmentation tests with Hoescth staining. In this study, we used various concentrations of the red-eye snail extract to test with 3-(4,5-dimethylthiazol-2-yl)-2-5-diphenyltetrazolium bromide (MTT) and doxorubicin reagents as positive controls. Absorbance values were read using a microplate reader at a wavelength of 595 nm. The cell absorbance data was converted into cell viability and probit analyzed to obtain the IC50 value. The results showed that the higher the concentration of the extract caused a decrease in the number of WiDr cells and an increase in damage to the structure of WiDr cells. Based on the results of probit analysis, it was found that the IC50 value of the extract was 36.28 µg/mL or classified as moderate cytotoxicity. The DNA fragmentation test showed that at concentrations of 125 ppm and 62.5 ppm, it was able to provide an effect similar to doxorubicin, namely triggering apoptosis in WiDr colon cancer cells.

BackgroundCancer rates continue to climb, owing largely to the world population’s aging and growth, as well as economically developing countries, a surge in cancer-causing behavior, particularly smoking. The third or fourth most prevalent type of cancer is colon cancer. Cancer of the large intestine (colon) is one of the primary causes of death from cancer. Colorectal cancer prevention is mostly based on adenomatous disease screening approaches. The cytotoxic and pharmacological properties of Phoenix pusilla are widely documented. As a result, there is little recorded evidence of its cytotoxic activity against colon cancer cells. Therefore, we planned to study the efficacy of a methanolic leaf extract of Phoenix pusilla against in vitro colon cancer cells. AimTo evaluate the anti-cancer effects of the methanolic leaf extract of Phoenix pusilla on colon cancer cell lines. Materials and MethodsIn vitro screening and anti-cancer effects of the methanolic effect of Phoenix pusilla on colon cancer cell lines were assessed by cell viability assays and cell and nuclear morphological studies. For the in vitro cell culture study, different concentrations of Phoenix pusilla leaf extract (0, 25, 50, 75, 100, 150 μg/ml) were used, and IC50 doses were calculated. ResultsThe results of the MTT (3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide) assay revealed that the fraction of viability cells significantly decreased in treated cells when compared to untreated control groups, was expressed as 100%, and an inhibitory concentration of μg/ml was identified. A phase-contrast microscope was used to observe cell shrinkage and cytoplasmic membrane blebbing. A fluorescent microscope was used to examine the apoptotic nuclei (internally dyed nuclei, shattered nuclei, and condensed chromatin). ConclusionIn conclusion, the present study results showed that the leaf extracts of Phoenix pusilla had a strong cytotoxic effect and induced significant apoptosis in the colon cancer cell lines at a concentration of 75 μg/ml in the 24 h incubation period. More research is needed to investigate the extract’s active components as well as the molecular mechanisms underlying its anti-cancer properties.

ObjectiveThe aim of study’s goal was to look into the anticancer efficacy of a methanolic extract of Justicia gendarussa against a lung cancer cell line. Materials and MethodsCell viability assays and cell and nuclear morphology examinations were used to evaluate the anticancer efficacy against methanolic extract of Justicia gendarussa on lung cancer cell lines. The IC50 doses were calculated using different concentrations of Justicia gendarussa extract (0, 10, 20, 40, 60, and 80 μg/mL). ResultsThe results of MTT (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl-tetrazolium bromide) assay revealed that the percentage of viability in treated cells was significantly lower as compared with untreated control groups, which represented as 100%, and an inhibitory concentration of 40 μg/mL was observed. Under a phase-contrast microscope, morphological changes revealed cell shrinkage and cytoplasmic membrane blebbing. The apoptotic nuclei (intensely colored, broken nuclei, and compacted chromatin) were examined under a fluorescence microscope. ConclusionsThe outcome of the research work on Justicia gendarussa was investigated for anticancer properties. The results revealed the proapoptotic and cytotoxic effects of Justicia gendarussa extract on lung cancer cell lines. From the above results and findings, it could be concluded that the Justicia gendarussa methanolic leaf extract exhibited potent anticancer activity against a lung cancer cell line. Further study needs to be conducted to investigate the active chemicals in the extract as well as the molecular mechanisms underlying its anticancer benefits.

Purpose: Ovarian cancer is the fifth leading cause of cancer death in women, leading cause of death from gynecologic malignancies, and the second most commonly diagnosed gynecologic malignancy, however the underlying pathophysiology is not clearly understood. Calcitriol, the active form of vitamin D serves its activity by binding to the vitamin D receptor (VDR). Calcitriol regulates multiple signaling pathways such as proliferation, apoptosis, differentiation, inflammation, invasion, angiogenesis and metastasis. It has been found to have a broad effect on several cancer types such as colon, breast and prostate cancer. Therefore, the study aimed to investigate the effects of calcitriol on human ovarian cancer cells. Material and Methods: The human MDAH-2774 ovarian carcinoma cells were exposed to different dose ranges of calcitriol for 24 and 48 hours. Cultured cells were evaluated in terms of MTT assay and quantitative- Real time-PCR. Results: As evidenced by the MTT assay, calcitriol treatment resulted in the reduction of cell viability in human MDAH-2774 cells. The gene expressions of VDR and p53 were increased with the calcitriol treatment compared to control. Additionally the gene expression of proapoptotic marker Bax increased and the anti-apoptotic marker Bcl-2 decreased with the presence of the calcitriol. Conclusion: In conclusion calcitriol treatment decreased cell proliferation and induced apoptosis in ovarian cancer cells, therefore we can suggest that calcitriol, either by itself or in combination with chemotherapy drugs, may be effective in treating ovarian cancer.

Abstract Background Despite the fact that natives of Southeast Asia have been consuming Prismatomeris glabra for decades for a variety of health benefits, research on this species is not as extensive as that on other species due to its limited distribution. The purpose of this study was to determine the cytotoxicity and identify the bioactive compounds of P. glabra crude leaf extracts against the MCF-7 cell line. Results We first examined the potential cytotoxic activity of P. glabra using the MTT assay against the MCF-7 cell line to determine the IC50 of the plant extracts at various concentrations at three time points (24 h, 48 h, and 72 h). Across all time points, the MTT assay revealed that the aqueous extract exhibited the lowest IC50 values (p

In the present study, we derivatized several hydroxycinnamic and hydroxybenzoic acids to phenolic amides (PAMs) via one step BOP mediated amide coupling reactions. Fifteen PAMs were synthesized in >40% yields and were screened for their cytotoxic activities against four cancer cell lines: THP-1 (leukaemia), HeLa (cervical), HepG2 (liver), and MCF-7 (breast), in comparison to 5-flurouracil (5-FU). Four amides showed IC50 ranging from 5 to 55 µM against all four cell lines. In contrast, tetradecyl-gallic-amide (13) affected only THP-1 leukaemia cells with IC50 of 3.08 µM. The activities of these compounds support the promise of phenolic amides as anticancer agents. [ABSTRACT FROM AUTHOR]

With the increasing demand for environmentally friendly and effective biomedical solutions, the synthesis of nanoparticles with enhanced properties has become imperative. This study addresses this demand by employing a green method that utilizes Ficus Drupacea fruit extract to produce ZnO/CuO nanostructures, offering versatile biomedical applications. While several reports exist on the synthesis of nanostructures using plant extracts, this is the primary report on the utilization of Ficus Drupacea fruit extract for creating ZnO/CuO nanostructures. A series of five ZnO/CuO nanostructures (ZC0, ZC25, ZC50, ZC75, and ZC100) were synthesized by varying the proportion of CuO and ZnO. Through comprehensive characterization techniques including XRD (X‐Ray Diffraction), HR‐TEM (High‐Resolution Transmission Electron Microscopy), and UV‐Vis spectroscopy, the successful synthesis and tunable properties of the nanostructures were confirmed, with average crystal sizes ranging from 14.32 nm to 38.61 nm. The study unveils the significant cytotoxicity of the synthesized nanostructures against MCF‐7 breast cancer cells, with ZC25 demonstrating the highest activity and an LC50 (Lethal Concentration 50) value below 50 μg/mL. Antimicrobial assays underscore the potent activity of ZC100 against Streptococcus mutans and Acinetobacter baumannii, with MIC (Minimum Inhibitory Concentration) values below 1.5 mg/mL. These findings emphasize the potential of these nanostructures for advanced biomedical applications. [ABSTRACT FROM AUTHOR]

The reaction of substituted acylthiourea derivatives (L1–L4) with [(PPh3)2Cu(μ‐Cl)2Cu(PPh3)] in a proper stoichiometric proportion gave the complexes (1–4) in good yields. The structures of the compounds (ligands and complexes) were advocated through spectroscopic analyses and x‐ray diffraction (XRD) studies; the latter confirmed their molecular structures. The complexes (1–4) were assessed for their cytotoxic potential through MTT assay against A549, T24, and HepG2 cancer cells, and their toxicity was evaluated using Vero and MCF‐10a normal cells. The complexes (1–4) displayed better cytotoxic action toward HepG2 cancer cells than cisplatin. Complexes 3 and 4 significantly destroyed A549 cancer cells with the IC50 values of 16.25 and 4.90 μM, respectively, which were lower than that of cisplatin (IC50 = 17.73 μM). Furthermore, the higher IC50 values in normal cells showed that the complexes were less hazardous to the normal cells except complex 3. The biocompatibility study showed that the complexes had minimal impact on normal human dermal fibroblast (NHDF) cells. The mode of cell death of complexes 3 and 4 against cancer cells was evaluated using staining assays. Both compounds demonstrated a significant reduction in live cells, an increase in early apoptotic cells, and pronounced proapoptotic effects, as evidenced by fragmented nuclei. Flow cytometry revealed a distinctive subpopulation in the subG0 phase, highlighting the compounds' ability to induce apoptosis and inhibit cell cycle progression. [ABSTRACT FROM AUTHOR]

This study was planned to prepare new mixed ligand chelates derived from N‐(4,6‐dimethylpyrimidin‐2‐yl)‐3a,4,5,6,7,7a‐hexahydro‐1H‐benzimidazol‐2‐amine (BIP), and imidazole (I). They identified through CHN study, spectroscopic (NMR, FT‐IR, and UV–Vis), conductivity, magnetic susceptibility, mass analysis, and thermal analysis. Correlation between all results exposed that the BIP ligand performed as a bi‐dentate ligand through NN donation locations, where the co‐ligand shows as N–H monodentate. The optimization for the studied chelates led to the formation of distorted octahedral geometry for BIPICu and BIPIVO chelates, distorted (tetrahedral and square planar) geometry for BIPIAg and BIPIPd chelates, respectively, around the metal salt. The B3LYP level, B3LYP/6‐311G** level for the free ligand, and B3LYP/6–311G**‐LANL2DZ functional level for the solid chelates were used in density functional theory (DFT) calculations. The findings showed that DFT calculations produce conclusions that are consistent with those of the experiments. The resulting compounds' nonlinear optical properties were examined by calculating the hyperpolarizability (β) and molecular polarizability (α) parameters, which gave rise to several unexpected optical properties for the synthesized compounds. Using the agar well diffusion method, the antimicrobial activity of the produced compounds was experimentally confirmed against a subset of G+ and G− bacteria. To ascertain how these substances attach to the targeted protein binding sites, a molecular docking mechanism between the microbially resistant chelates and their suppressed microbial protein pocket receptors was investigated. Also, DNA binding estimated for studied structures was tested by electronic absorption spectrum, viscosity estimation, and gel electrophoresis. Data proposed that all tested compounds link with DNA using an intercalation, electrostatic, and covalent binding mechanism. Moreover, antioxidant performance for studied compounds was governed by radical scavenging techniques in vitro. In addition, an MTT assay has been worked out to explore in vitro cytotoxic impending. All the tested chelates assumed antimicrobial, antitumor, and antioxidant performances that cause them to suggest drugs. [ABSTRACT FROM AUTHOR]

The search for promising substances aimed at creating new chemotherapeutic drugs based on them is relevant in modern oncology. In this regard, new azoloazine derivatives, which are analogs of the well-known anticancer drug temozolomide, may be promising. The goal was to study the antitumor activity of 11 new azoloazine derivatives in vitro and in vivo. The MTT assay was used to assess the cytotoxic effect of the azoloazines on MCF-7 and CHO cells. BALB/c mice were orthotopically injected with 106 MCF-7 cells to simulate a xenogenic model of breast cancer. The test substances were administered at doses 1/2 IC50 once intraperitoneally 72 hours after tumor transplantation. The degree of differentiation and tumor extent in the tissue and the nature of metastasis were studied by analyzing histological sections of animals removed from the experiment. The volume of the primary tumor was measured. An evaluation of the cytotoxic activity of the new azoloazine derivatives showed that compounds 4, 6, and 9 were the most toxic to MCF-7 cells. Therefore, they were selected for cytotoxicity studies on normal cells (cultured CHO cells). Selected compounds 6 and 9 had low cytotoxicity against CHO cells, which was regarded as a positive aspect for their use as anticancer drugs. An in vivo experiment showed that administration of selected compounds 4, 6, and 9 led to more pronounced inhibition of tumor growth than the use of epirubicin alone. Histological analysis also revealed that compounds 4, 6, and 9 exhibited antitumor activity. The antitumor effects of the new azoloazine derivatives obtained in in vitro and in vivo experiments proved their high activity as potential chemotherapeutic agents and their prospects for further studies aimed at creating new antitumor drugs based on them. [ABSTRACT FROM AUTHOR]

Pink pepper is classified into the Californian/Peruvian type (Schinus molle) and the Brazilian type (S. terebinthifolia). According to studies, pink pepper extracts and essential oils have shown anti-inflammatory, antioxidant, genotoxic and antidiabetic properties in in vitro and in vivo studies. The results of bioactivity tests vary depending on the geographical origin of the pepper. In this paper, the cytotoxic, antioxidant and antibacterial effects of the essential oil of the commercial pink pepper fruit from the Tuzla market were investigated. To assess the cytotoxic potential, a tetrazolium salt reduction (MTT) viability assay was performed. The antioxidant potential was examined spectrophotometrically, using DPPH and FRAP methods. Diffusion techniques were used to evaluate the antibacterial activity of the essential oil. Using GC/MS, 24 components of red pepper essential oil were identified, of which α-pinene, α-phellandrene, δ-3-carene and D-limonene dominate. The studied pink pepper essential oil inhibited the cell proliferation in the HeLa cell line, causing a dose-dependent cytotoxic effect (IC50=389.46 µg/mL). The essential oil inhibits DPPH radicals. The reducing ability is relatively weak. For the essential oil, an extremely good ability to inhibit the growth of the bacteria used in this study was confirmed. These results indicate a very high potential of essential oil of pink pepper fruit as an inhibitor of pathogenic organisms. [ABSTRACT FROM AUTHOR]

The aim of the study was to improve the mechanical, biodegradation and in vitro biocompatible characteristics of as received rolled AZ31 (Mg-1%Zn-3%Al) alloy by develop the surface composite of Mg-Titania. The surface composite was developed by friction stir processing (FSP) and it's used for prosthetic applications. The influence of tool rotation speed and number of FSP passes on grain structure, grain refinement, tensile strength, hardness, in vitro degradation rate and in vitro biocompatibility were explored. The obtained results support the capability of FSP in terms of mechanical strengthening, refinement of grain structure, dispersion of reinforcement (i.e. TiO2) and controlled degradation rate. Grain structure at stir zone, advancing side and retreating side were investigated. The large grains in the alloy were reduced to a fine equiaxial grains of average dimension of ≈ 3 μm by 3rd pass of FSP. The process was performed under two different tool rotation speed, i.e. 1550 and 2260 RPM. The addition of second phase in the matrix significantly improve the grain refinement. The results obtained from tensile test revealed the improvement in the percentage elongation without compromising the strength. The micro hardness of specimens of different parametric combination were evaluated and found ≈ 30–50% improvement in the micro hardness. The degradation rate by immersion test in simulated body fluid (SBF) for 3, 6 and 10 days were performed and found a significant reduction in degradation rate. The MTT assay for the biocompatibility performed by indirect method, the results validate the non-toxic behavior of processed specimen. [ABSTRACT FROM AUTHOR]

Seseli is an important genus of the Apiaceae family with many aromatic species. These plants are widely used in traditional medicine, but there is little information about their phytochemical compositions and biological activities. An ecotype of Seseli transcaucasicum (Schischk.) Pimenov & Sdobnina, about which there is little phytochemical information, grows in the Hezar-Masjed Mountains of northeastern Iran. The aim of this study was to investigate the anticancer activity and antioxidant properties of ethanolic and methanolic extracts from the leaves and seeds of this plant. Cytotoxic activity against MCF7 and HSkMC was determined by the MTT method, and the antioxidant properties of the extracts were evaluated by the DPPH and PFRAP methods. The results showed that the methanolic extract of seeds had the greatest effect on inhibiting the growth of cancer cells at 48 and 72 hours, with IC50 values of 54.35 and 50.52 μg/ml, respectively. Moreover, the methanolic extract of the seeds had the greatest effect on the degradation of DPPH free radicals with an IC50 value of 44.64 μg/ml, and this inhibitory effect was comparable to the effect of ascorbic acid. The antioxidant effect of iron reduction of the different extracts was significantly lower than that of ascorbic acid. However, among the extracts, the reducing power of the methanolic seed extract was better than the others. Considering that the methanolic seed extract had the most lethal effect on cancer cells, it seems that the extract that has stronger antioxidant power also has stronger anticancer properties. [ABSTRACT FROM AUTHOR]

Uncaria nervosa Elmer is a medicinal plant distributed in Indonesia, New Guinea and the Western Pacific. Traditionally, this plant is used for cancer treatment. This study aims to determine the cytotoxic activity, cell migration and apoptosis of n-hexane, ethyl acetate and butanol fractions in MCF-7 HER 2 breast cancer cells. The ethanol extract of U. nervosa Elmer leaves was fractionated using a separating funnel. Fractionation used solvents with varying polarities, n-hexane, ethyl acetate and butanol. The three fractions were tested for their cytotoxic activity by the MTT assay method. The concentrations of the fractions were 100, 10 and 1 µg/ml. The effect of inhibiting cell migration on the fractions using the scratch wound healing assay was observed at 0, 24 and 48 hours and the apoptosis effect was observed using the double staining assay at 48 hours. The results showed that n-hexane and ethyl acetate fractions had IC50 values31,44 and 16,422 µg/ml, respectively and the butanol fraction had no activity on MCF-7 HER 2cells at a concentration of 100 µg/ml. Wound healing assays explained the potency of fraction to decrease the cell migration after 24 hours. Apoptosis effect of the fraction of the double staining test results showed MCF-7 HER 2 cells experiencing yellow and orange fluorescence. The n-hexane and ethyl acetate fractions having moderate and strong cytotoxic activity and were able to inhibit cell migration as well as caused death of MCF-7 HER 2 breast cancer cells by apoptosis. [ABSTRACT FROM AUTHOR]

Sirtuin 3 (SIRT3) belongs to the Sirtuin protein family, which consists of NAD+-dependent lysine deacylase, involved in the regulation of various cellular activities. Dysregulation of SIRT3 activity has been linked to several types of cancer, including breast cancer. Because of its ability to stimulate adaptive metabolic pathways, it can aid in the survival and proliferation of breast cancer cells. Finding new chemical compounds targeted towards SIRT3 was the primary goal of the current investigation. Virtual screening of ~ 800 compounds using molecular docking techniques yielded 8 active hits with favorable binding affinities and poses. Docking studies verified that the final eight compounds formed stable contacts with the catalytic domain of SIRT3. Those compounds have good pharmacokinetic/dynamic properties and gastrointestinal absorption. Based on excellent pharmacokinetic and pharmacodynamic properties, two compounds (MI-44 and MI-217) were subjected to MD simulation. Upon drug interaction, molecular dynamics simulations demonstrate mild alterations in the structure of proteins and stability. Binding free energy calculations revealed that compounds MI-44 (− 45.61 ± 0.064 kcal/mol) and MI-217 (− 41.65 ± 0.089 kcal/mol) showed the maximum energy, suggesting an intense preference for the SIRT3 catalytic site for attachment. The in-vitro MTT assay on breast cancer cell line (MDA-MB-231) and an apoptotic assay for these potential compounds (MI-44/MI-217) was also performed, with flow cytometry to determine the compound's ability to cause apoptosis in breast cancer cells. The percentage of apoptotic cells (including early and late apoptotic cells) increased from 1.94% in control to 79.37% for MI-44 and 85.37% for MI-217 at 15 μM. Apoptotic cell death was effectively induced by these two compounds in a flow cytometry assay indicating them as a good inhibitor of human SIRT3. Based on our findings, MI-44 and MI-217 merit additional investigation as possible breast cancer therapeutics. [ABSTRACT FROM AUTHOR]

Carbon nanotubes (CNTs) have the potential to serve as delivery systems for medicinal substances and gene treatments, particularly in cancer treatment. Co-delivery of curcumin (CUR) and Methotrexate (MTX) has shown promise in cancer treatment, as it uses fewer drugs and has fewer side effects. This study used MTX-conjugated albumin (BSA)-based nanoparticles (BSA-MTX) to enhance and assess the efficiency of CUR. In-vitro cytotoxicity tests, DLS, TEM, FTIR, UV/Vis, SEM, and DSC studies assessed the formulations' physical and chemical properties. The Proteinase K enzyme was used to severe amidic linkages between MTX and BSA. The findings demonstrated the efficacy of using ƒ-MWCNT-CUR-BSA-MTX as a vehicle for efficient co-delivery of CUR and MTX in cancer treatment. The MTT colorimetric method was used to evaluate the effect of chemical and medicinal compounds. Cell division was studied using the MTT method to investigate the effect of pure MWCNT, pure CUR, MTX-BSA, and ƒ-MWCNT-CUR-MTX-BSA. Studies on cell lines have shown that the combination of curcumin and MTX with CNT can increase and improve the effectiveness of both drugs against cancer. A combination of drugs curcumin and methotrexate simultaneously had a synergistic effect on MCF-7 cells, which indicated that these drugs could potentially be used as a strategy for both prevention and treatment of breast cancer. Also, ƒ-MWCNT-CUR-MTX-BSA was found to have a significant effect on cancer treatment with minimal toxicity compared to pure curcumin, pure MTX-BSA, MTX, and ƒ-MWCNT alone. Unique properties such as a high ratio of specific surface area to volume, high chemical stability, chemical adsorption ability, high capacity of drug and biomolecules of carbon nanotubes, as well as multiple drug loading at the same time The combination of ƒ-MWCNT-CUR-BSA MTX significantly impacts cancer therapy), are desirable as an alternative option for targeted drug delivery and high therapeutic efficiency. [ABSTRACT FROM AUTHOR]

In this study, we assess the impact of photodynamic therapy (PDT) using aluminum phthalocyanine tetrasulfonate (AlPcS4) on the viability and cellular stress responses of MCF-7 breast cancer cells. Specifically, we investigate changes in cell viability, cytokine production, and the expression of stress-related genes. Experimental groups included control cells, those treated with AlPcS4 only, light-emitting diode (LED) only, and combined PDT. To evaluate these effects on cell viability, cytokine production, and the expression of stress-related genes, techniques such as 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide (MTT) assay, enzyme-linked immunosorbent assays (ELISA), and real-time quantitative PCR (RT‒qPCR) were employed. Our findings reveal how PDT with AlPcS4 modulates mitochondrial activity and cytokine responses, shedding light on the cellular pathways essential for cell survival and stress adaptation. This work enhances our understanding of PDT's therapeutic potential and mechanisms in treating breast cancer. [ABSTRACT FROM AUTHOR]

This study presents the synthesis and comprehensive characterization of a chitosan-coated copper cobalt oxide nanocomposite (Ch/CuCo 2 O 4 NC) derived from copper cobalt oxide nanocomposites (CuCo 2 O 4 NPs) via a hydrothermal method. Structural and functional attributes of Ch/CuCo 2 O 4 NC was validated through FESEM, XRD, FTIR, TEM, and EDX analyses. X-ray diffraction confirmed a distinct cubic crystal phase, affirming structural integrity FTIR demonstrated a robust chitosan-CuCo 2 O 4 interaction, fortifying performance. The versatility of Ch/CuCo 2 O 4 nanocomposite is demonstrated by its dual functions as an effective antibacterial, anticancer agent targeting HeLa cells, and a powerful photocatalyst for dye removal. The low toxicity towards normal fibroblasts (L-929) emphasizes its potential for biomedical applications. This work originally lies in the synthesis methodology and the unique multifunctional properties exhibited by the Ch/CuCo 2 O 4 nanocomposite, paving the way for its diverse applications in environmental and biomedical domains. • CuCo 2 O 4 nanoparticles were prepared, and their surface were coated with the biopolymer chitosan. • Explored the antibacterial capabilities of the Ch/CuCo 2 O 4 nanocomposite. • Used as an anticancer agent in an in vitro study against the HeLa cell line. • Biocompatibility assessment was performed with the normal L-929 cell line. • Employed as a photocatalyst for the degradation of Methyl blue and Congo red dyes. [ABSTRACT FROM AUTHOR]

Here we report the synthesis and anticancer activities of fourteen novel imidazo[1,2-a]pyridine derivatives (6a-6n) containing S-alkyl/aryl moiety. The target compounds were obtained via a six-step synthetic route. 1-(4-Aminophenyl)ethan-1-one was the starting material. In the last step, 2-chloro-N-[4-(imidazo[1,2-a]pyridin-2-yl)phenyl]acetamide (5) was allowed to react with various aliphatic/aromatic thiol derivatives, affording the final compounds 6a-6n. The cytotoxicity of the compounds was evaluated against A549 (human non-small cell lung cancer), C6 (rat glioma), MCF-7 (human breast carcinoma) and HepG2 (human liver carcinoma) tumor cells and NIH/3T3 (mouse embryonic fibroblast cells) healthy cells. First step MTT assay reported that compounds 6a, 6d, 6e and 6i exhibited antiproliferative activity against all tested tumor lines. Second step BrdU cell proliferation assay and flow cytometric analysis revealed that compounds 6d and 6i inhibited DNA synthesis on HepG2 cell line time-dependently by apoptotic pathway. Molecular docking study of compounds 6d and 6i with caspase-3 and caspase-9 revealed their binding interactions with the enzyme's active site, confirming the experimental findings. [ABSTRACT FROM AUTHOR]

Objective: Lung cancer (LC) has the highest mortality rate globally. Most chemotherapeutic medicines now in use are cytotoxic, prompting the search for novel compounds with anticancer properties and improved safety profiles for normal cells. Dipeptidyl peptidase-4 inhibitors have demonstrated anticancer effects and apoptotic properties by specifically inhibiting dipeptidyl peptidase-4, a glycoprotein found in various organs that support the spread of cancer and tumor formation. Based on that, this study aimed to evaluate the cytotoxicity and apoptotic activity of sitagliptin (SITA) and linagliptin (LINA) against the lung cancer cell line (A549) alone and in combination with cisplatin (CP). Methods: A549 cells were categorized into six groups: control (untreated cells), CP-treated cells, SITA-treated cells, LINA-treated cells, CP plus SITA treated cells (1:1 ratio), and CP plus LINA treated cells (1:1 ratio). After 72 hours of incubation, cell viability (or cytotoxicity) and concentration required to inhibit 50% of cell viability (IC50) for each group were determined using an MTT assay. This method is safe and easy to use, has more reproducibility, and is commonly used for cell viability and cytotoxicity tests. Later, A549 cells were cultured in six flasks and exposed to the IC50 for 36 hours. Afterward, the cells were harvested and centrifuged, and the supernatant was removed. The remaining cell pellets were collected and lysed using a lysis buffer to measure B-cell lymphoma type 2 (BCL-2) levels with ELISA test kits. The data was collected and subjected to statistical analysis techniques. Results: MTT assay results determined that SITA and LINA significantly increased A549 cell cytotoxicity compared to the control group (P<0.0001). Moreover, combining SITA or LINA with CP showed markedly increased antitumor efficacy and more significant cytotoxicity directed toward A549 cells. Additionally, these combinations highly reduced IC50 in comparison to monotherapy. Considerably, both drugs showed remarkable apoptotic activity on A549 cells when used alone or combined with CP by decreasing BCL2 levels. Consequently, it potentiates apoptotic effects and cytotoxicity of CP against cancer cells. Interestingly, Lina was more potent than Sita regarding cytotoxicity and apoptotic activity on A549 cells. Conclusion: SITA and Lina exhibited significant cytotoxic and apoptotic effects against A549 cells through the induction of apoptosis. Notably, the results suggest a potential synergistic anticancer impact on CP. [ABSTRACT FROM AUTHOR]

Currently, zinc oxide (ZnO) particles are used in nanotechnology to destroy a wide range of microorganisms. Although pentavalent antimony compounds are used as antileishmanial drugs, they are associated with several limitations and side effects. Therefore, it is always desirable to try to find new and effective treatments. The aim of this research is to determine the antileishmanial effect of ZnO particles in comparison to the Antimoan Meglumine compound on promastigotes and amastigotes of Leishmania major (MRHO/IR/75/ER). After the extraction and purification of macrophages from the peritoneal cavity of C57BL/6 mice, L. major parasites were cultured in Roswell Park Memorial Institute‐1640 culture medium containing fetal bovine serum (FBS) 10% and antibiotic. In this experimental study, the effect of different concentrations of nanoparticles was investigated using the 3‐[4,5‐dimethylthiazol‐2‐yl]‐2,5‐diphenyl‐tetrazolium bromide (MTT) colorimetric method, in comparison to the glucantime on promastigotes, amastigotes and healthy macrophages in the culture medium. The amount of light absorption of the obtained color from the regeneration of tetrazolium salt to the product color of formazan by the parasite was measured by an enzyme‐linked immunosorbent assay (ELISA) reader, and the IC50 value was calculated. IC50 after 24 h of incubation was calculated as IC50 = 358.6 µg/mL. The results showed, that the efficacy of ZnO nanoparticles was favorable and dose‐dependent. The concentration of 500 µg/mL of ZnO nanoparticles induced 84.67% apoptosis after 72. Also, the toxicity of nanoparticles was less than the drug. Nanoparticles exert their cytotoxic effects by inducing apoptosis. They can be suitable candidates in the pharmaceutical industry in the future. [ABSTRACT FROM AUTHOR]

In the first phytochemical investigation of specialized metabolites from the stem bark of Alyxia fascicularis, which is used in different traditional medicines, including those of Myanmar and China, five lignans (1-5) and three coumarins (6-8) were isolated by semipreparative HPLC separations and identified mainly by 1D and 2D NMR spectral analysis. The radical scavenging activity of isolated compounds was tested using the DPPH method. Noteworthy, most lignans exhibited antiradical effects comparable to vitamin C and gallic acid. Instead, compounds 1-8 showed no cytotoxic effect on Hela cell line. A possible biosynthetic pathway to enantiomeric 3 and 4 is suggested. [ABSTRACT FROM AUTHOR]

Background: The Advent of the COVID-19 pandemic has necessitated the quick exploration of new drugs. Synthetic approach is time consuming and expensive with uncertainty. The natural products can be explored as this approach is cost effective and takes less time to investigate. The ethnic significance of Grewia hirsuta has given clues of Immunomodulator potential. Hydro ethanolic extract of Grewia hirsuta was explored and compared with established levamisole. Materials and Methods: In vitro, immunomodulator models on human lymphocytes and In vivo carbon clearance model in Swiss albino mice were studied by lymphotoxicity and lymphocyte proliferation. Results: Hydro ethanolic extract of Grewia hirsuta has shown similar results of immunomodulation comparable with levamisole in statistically significant studies assessed by Dunnett's test. Conclusion: Hydro ethanolic extract has shown decreased lymphocyte toxicity and increased lymphocyte proliferation. [ABSTRACT FROM AUTHOR]