Human Liver Carcinoma HepG2 Cells Research Articles

Mitochondria-targeted neutral and cationic iridium(III) anticancer complexes chelating simple hybrid sp2-N/sp3-N donor ligands.

Most platinum group-based cyclometalated neutral and cationic anticancer complexes with the general formula [(C^N)2Ir(XY)]0/+ (neutral complex: XY = bidentate anionic ligand; cationic complex: XY = bidentate neutral ligand) are notable owing to their intrinsic luminescence properties, good cell permeability, interaction with some biomolecular targets and unique mechanisms of action (MoAs). We herein synthesized a series of neutral and cationic amine-imine cyclometalated iridium(III) complexes using Schiff base ligands with sp2-N/sp3-N N^NH2 chelating donors. The cyclometalated iridium(III) complexes were identified by various techniques. They were stable in aqueous media, displayed moderate fluorescence and exhibited affinity toward bovine serum albumin (BSA). The complexes demonstrated promising cytotoxicity against lung cancer A549 cells, cisplatin-resistant lung cancer A549/DDP cells, cervical carcinoma HeLa cells and human liver carcinoma HepG2 cells, with IC50 values ranging from 9.98 to 19.63 μM. Unfortunately, these complexes had a low selectivity (selectivity index: 1.62-1.98) towards A549 cells and BEAS-2B normal cells. The charge pattern of the metal center (neutral or cationic) and ligand substituents showed little influence on the cytotoxicity and selectivity of these complexes. The study revealed that these complexes could target mitochondria, cause depolarization of the mitochondrial membrane, and trigger the production of intracellular ROS. Additionally, the complexes were observed to induce late apoptosis and perturb the cell cycle in the G2/M or S phase in A549 cells. Based on these results, it appears that the anticancer efficacy of these complexes was predominantly attributed to the redox mechanism.

Molecular Mechanism of Apoptotic Cell Death in Cyanidin-3-glucoside-induced Cytotoxic Potential on Human Liver Carcinoma (HepG2) Cell Line

Molecular Mechanism of Apoptotic Cell Death in Cyanidin-3-glucoside-induced Cytotoxic Potential on Human Liver Carcinoma (HepG2) Cell Line

Potent Half-Sandwich 16-/18-Electron Iridium(III) and Ruthenium(II) Anticancer Complexes with Readily Available Amine-Imine Ligands.

The synthesis and biological evaluation of stable 16-electron half-sandwich complexes have remained scarce. We herein present the different coordination modes (16-electron or 18-electron) between half-sandwich iridium(III) complexes and ruthenium(II) complexes derived from the same amine-imine ligands chelating hybrid sp3-N/sp2-N donors. The 16-electron iridium(III) and 18-electron ruthenium(II) complexes with different counteranions were obtained and identified by various techniques. The promising cytotoxicity of these complexes against A549 lung cancer cells, cisplatin-resistant A549/DPP cells, cervical carcinoma HeLa cells, and human hepatocellular liver carcinoma HepG2 cells was observed with IC50 values ranging from 5.4 to 16.3 μM. Moreover, these complexes showed a certain selectivity (selectivity index: 2.1-3.7) toward A549 cells and BEAS-2B normal cells. The variation of metal center, counteranion, 16/18-electron coordination mode, and ligand substituents showed little influence on the cytotoxicity and selectivity of these complexes. The mechanism of action study showed that these complexes could target mitochondria, induce the depolarization of the mitochondrial membrane, and promote the generation of intracellular reactive oxygen species (ROS). Further, the induction of cell apoptosis and the perturbation of the cell cycle in the G0/G1 phase were also observed for these complexes. Overall, it seems that the redox mechanism dominated the anticancer efficacy of these complexes.

Differential genomic effects of four nano-sized and one micro-sized CeO2 particles on HepG2 cells.

The objective of this research was to perform a genomics study of five cerium oxide particles, 4 nano and one micrometer-sized particles which have been studied previously by our group with respect to cytotoxicity, biochemistry and metabolomics. Human liver carcinoma HepG2 cells were exposed to between 0.3 to 300 ug/ml of CeO2 particles for 72 hours and then total RNA was harvested. Fatty acid accumulation was observed with W4, X5, Z7 and less with Q but not Y6. The gene expression changes in the fatty acid metabolism genes correlated the fatty acid accumulation we detected in the prior metabolomics study for the CeO2 particles named W4, Y6, Z7 and Q, but not for X5. In particular, the observed genomics effects on fatty acid uptake and fatty acid oxidation offer a possible explanation of why many CeO2 particles increase cellular free fatty acid concentrations in HepG2 cells. The major genomic changes observed in this study were sirtuin, ubiquitination signaling pathways, NRF2-mediated stress response and mitochondrial dysfunction. The sirtuin pathway was affected by many CeO2 particle treatments. Sirtuin signaling itself is sensitive to oxidative stress state of the cells and may be an important contributor in CeO2 particle induced fatty acid accumulation. Ubiquitination pathway regulates many protein functions in the cells, including sirtuin signaling, NRF2 mediated stress, and mitochondrial dysfunction pathways. NRF2-mediated stress response and mitochondrial were reported to be altered in many nanoparticles treated cells. All these pathways may contribute to the fatty acid accumulation in the CeO2 particle treated cells.

Long-circulating gambogic acid-loaded nanodiamond composite nanosystem with inhibition of cell migration for tumor therapy

Herein, ultra dispersed and stably suspended nanodiamonds (NDs) were demonstrated to have a high load capacity, sustained release, and ability to serve as a biocompatible vehicle for delivery anticancer drugs. NDs with size of 50–100 nm exhibited good biocompatibility in normal human liver (L-02) cells. In particular, 50 nm ND not only promoted the noticeable proliferation of the L-02 cells but also can effectively inhibited the migration of human liver carcinoma (HepG2) cells. The gambogic acid-loaded nanodiamond (ND/GA) complex assembled by π–π stacking exhibits ultrasensitive and apparent suppression efficiency on the proliferation of HepG2 cells through high internalization and less efflux compared to free GA. More importantly, the ND/GA system can significantly increase the intracellular reactive oxygen species (ROS) levels in HepG2 cells and thus induce the cell apoptosis. The increase in intracellular ROS levels causes damage to the mitochondrial membrane potential (MMP) and activates cysteinyl aspartate specific proteinase 3 (Caspase-3) and cysteinyl aspartate specific proteinase 9 (Caspase-9), which leads to the occurrence of apoptosis. In vivo experiments also confirmed that the ND/GA complex has a much higher anti-tumor capability than free GA. Thus, the current ND/GA system is promising for cancer therapy.

Novel Steroidal[17,16-d]pyrimidines Derived from Epiandrosterone and Androsterone: Synthesis, Characterization and Configuration-Activity Relationships.

Two series of novel steroidal[17,16-d]pyrimidines derived from natural epiandrosterone and androsterone were designed and synthesized, and these compounds were screened for their potential anticancer activities. The preliminary bioassay indicated that some of these prepared compounds exhibited significantly good cytotoxic activities against human gastric cancer (SGC-7901), lung cancer (A549), and hepatocellular liver carcinoma (HepG2) cell lines compared with 5-fluorouracil (5-FU), epiandrosterone, and androsterone. Especially the respective pairs from epiandrosterone and androsterone showed significantly different inhibitory activities, and the possible configuration-activity relationships have also been summarized and discussed based on kinase assay and molecular docking, which indicated that the inhibition activities of these steroidal[17,16-d]pyrimidines might obviously be affected by the configuration of the hydroxyl group in the part of the steroidal scaffold.

Sustainable biosynthesized bimetallic ZnO@SeO nanoparticles from pomegranate peel extracts: antibacterial, antifungal and anticancer activities.

Sustainable bimetallic nanoparticles (NPs) have attracted particular attention in the past decade. However, the efficiency and environmental concerns are associated with their synthesis and properties optimization. We report herein biosynthesis of bimetallic ZnO@SeO NPs based on green and ecofriendly methods using pomegranate peel extract (PPE). Pyrochemical ultraviolet-visible (UV-vis), Fourier-transform infrared (FTIR) and X-ray diffraction (XRD) spectroscopy as well as TEM and EDX supported successful synthesis. Antibacterial, antifungal, and cytotoxic activities were indicative of biological worth of sustainable bimetallic ZnO@SeO NPs, exhibiting antibacterial activity compared to monometallic ZnO and SeO NPs. The values of Minimum Inhibitory Concentration (MIC) of bimetallic ZnO@SeO NPs toward E. coli, P. aeruginosa, B. subtilis and S. aureus were 3.9, 15.62, 3.9 and 7.81 μg ml-1, respectively. Likewise, a promising antifungal activity against Candida albicans, Aspergillus flavus, A. niger and A. fumigatus was achieved (MICs: 31.25, 1.95, 15.62 and 15.62 μg ml-1, respectively). The cytotoxicity results suggest that bimetallic ZnO@SeO NPs are non-toxic and biomedically safe, evidenced by in vitro anticancer activity against human liver carcinoma (Hep-G2) cell line (with a half-maximal inhibitory concentration (IC50) > 71 μg ml-1). The bimetallic ZnO@SeO NPs successfully biosynthesized using PPE showed a high potential for biomedical engineering.

Efficient Synthesis of Densely Functionalized Pyrido[2,3-d]Pyrimidines via Three-component One-pot Domino Knoevenagel aza-Diels Alder Reaction and Induces Apoptosis in Human Cancer Cell Lines via Inhibiting Aurora A and B Kinases

The identification of novel aurora kinase inhibitors is one of the most attractive directions in the field of anticancer research and development. In our ongoing efforts to pursue the class of inhibitors, a series of pyrido[2,3-d]pyrimidines were synthesized in DIPEAc/EtOH media. The advantages of the present methodology include a one-pot multicomponent environmentally friendly approach, cost effectiveness, broad substrate scope, operational simplicity, short reaction times, easy workup procedure and high yields. Synthesized compounds were screened against human lung carcinoma A549 cells, human hepatocellular liver carcinoma HepG2 cells and human cervical carcinoma epithelial HeLa cells. Compound 6 b i.e. diethyl 5-(4-methoxyphenyl)-2,4-dioxo-1,2,3,4-tetrahydroquinazoline-6,7-dicarboxylate was found to be equipotent than the standard drug VX-680 against selected cancer cell lines. The selected compounds (6b, 6d and 6h) exhibit potent inhibition against Aurora A and B with IC50 values (9.4–25 mg/L). Molecular docking model showed that the compounds can bind well to the target by interacting with amino acid residues. It will provide some valuable information for the commercial Aurora Kinase inhibitors.

Toxicity Assessment of Octachlorostyrene in Human Liver Carcinoma (HepG2) Cells.

Octachlorostyrene (OCS) is a ubiquitous persistent organic pollutant; however, information regarding the toxicological effects of OCS remains limited. In this study, we studied the toxicity mechanisms of OCS using human liver carcinoma (HepG2) cells. The results showed that OCS reduced cell viability in a time- and dose-dependent manner. Compared with that in the control, the level of reactive oxygen species (ROS) was significantly increased in all treated HepG2 cells. We also found that (1) OCS induced damage in the HepG2 cells via the apoptotic signaling pathway, (2) OCS increased intracellular free Ca2+ concentration (>180%), and (3) following exposure to 80 μM OCS, there was an increase in mitochondrial transmembrane potential (MMP, ~174%), as well as a decrease in ATP levels (<78%). In conclusion, OCS is cytotoxic and can induce apoptosis, in which ROS and mitochondrial dysfunction play important roles; however, the observed increase in MMP appears to indicate that HepG2 is resistant to the toxicity induced by OCS.

RETRACTED ARTICLE: In vitro antioxidant, anticancer, anti-inflammatory, anti-diabetic and anti-Alzheimer potentials of innovative macroalgae bio-capped silver nanoparticles

The antagonistic side effects of chemical medications led to the search for safe strategies such as biogenic agents. Correspondingly, this study aims to create biogenic, appropriate, auspicious and innovative therapeutic agents like Galaxaura elongata {GE}, Turbinaria ornata {TO} and Enteromorpha flexuosa {EF} macroalgae-based silver nanoparticles (Ag-NPs). The Ag+ reduction and the creation of Ag[GE]-NPs, Ag[TO]-NPs and Ag[EF]-NPs have been validated using UV–visible spectroscopy, Fourier transform infrared spectroscopy (FTIR), scanning electron microscope (SEM) and zeta potential analysis, and the chemical composition of macroalgae crude extracts was estimated through gas chromatography–mass spectrometry (GC–MS). Further, macroalgae-based Ag-NPs were tested for their free radical scavenging activity DPPH, ABTS, anticancer activity in human liver carcinoma (HepG2) cell line, distinctive inflammation forms and elevated α-amylase. Results showed that the biosynthesized Ag-NPs have unique mechanical and physicochemical characters attributed to their high relative surface area, nanosized dimensions and spherical shape. At dose of 200 µg/mL, the DPPH radical scavenging capacity was maximized with Ag[TO]-NPs (67.26%); however, Ag[EF]-NPs was the most potent as ABTs scavenger (97.74%). Additionally, Ag[GE]-NPs had the maximum proteinase inhibitory action with 59.78%. The 1000 µg/mL of Ag[GE]-NPs, Ag[TO]-NPs and Ag[EF]-NPs revealed significant inhibitions of cell growth of HepG2 resulting in cell viabilities 5.92%, 4.44% and 11.33%, respectively. These findings suggest that macroalgae bio-capped Ag-NPs have magnificent biological potentials for safe biomedical applications.

In vitro anticancer activity of silver nanoparticles phyto-fabricated by Hylocereus undatus peel extracts on human liver carcinoma (HepG2) cell lines

Every year, millions of people die from cancer, and most anticancer medications have a low specificity of action and significant toxicity, resulting in severe side effects. As a result, the discovery of effective anticancer drugs is a top priority. Hence, the focal point of this research is to synthesize the dragon fruit peel aqueous extract fabricated silver nanoparticles (DFPAE-AgNPs) in a facile and green chemistry approach as a new-fangled anticancer agent. The selected primary phytochemicals are qualitatively screened for their presence in dragon fruit peel aqueous extract utilized for the fabrication of AgNPs. The analytical results revealed that DFPAE-AgNPs were crystalline, spherical in shape in the size range of 10–50 nm, and composed of 73.90% weight of a silver element. The IC50 value of the DFPAE-AgNPs is evaluated as 37.98 ± 0.21 µg mL−1 with a HepG2 cell line. Acridine orange- ethidium bromide (AO-EtBr) staining and nuclear acid staining assays demonstrated the dose-dependent (10–50 µg mL−1) apoptotic increase phenomenon of the DFPAE-AgNPs in the HepG2 cell line at 24 h. The current study suggested DFPAE as a vital, reliable, and active phytoconstituents for the fabrication of AgNPs with anticancer potentials in a rapid and eco-friendly way. Further meticulous investigation on the DFPAE-AgNPs behavioral nature is recommended to make use of these as alternatives to synthetic drugs in wider anticancer applications.

Degradation of dye wastewater by using cobalt, copper and nickel Schiff base complexes as catalysts: spectral, molecular modelling, catalytic activity and metal removal from aqueous solution

ABSTRACT Metal complexes of Co(II), Cu(II) and Ni(II) with the Schiff base ligand, 6,6ʹ-(([1,1ʹ-biphenyl]-4,4ʹ diylbis(azaneylylidene))bis(methaneylylidene))bis(2,4-dichlorophenol) (H2L) were synthesised. All synthesised compounds were identified and characterised. The conductivity measurements showed the non-electrolytic nature of all the complexes. The decomposition of all complexes ended with metal oxide. Octahedral geometries were proposed for all complexes. Photocatalytic degradation of methylene blue dye (MB) in the presence and absence of hydrogen peroxide was studied by using Co(II), Cu(II) and Ni(II) complexes as catalysts. Fluorescence studies have shown that the reported compounds can act as photoactive materials. Density functional theory was used to investigate the geometries of the ligand and its complexes. The adsorption of Co2+, Ni2+ and Cu2+ in an aqueous solution on H2L ligand under various conditions was studied. The optical properties of all complexes were studied. Antimicrobial activities of the ligand and its transition metal complexes were studied. The in-vitro cytotoxicity of ligand and its cobalt(II), nickel(II) and copper(II) complexes were evaluated towards the human Liver Carcinoma (HepG2) cell line and compared with standard cisplatin.

Characterization and Antitumoral Activity of Biohybrids Based on Turmeric and Silver/Silver Chloride Nanoparticles.

The phyto-development of nanomaterials is one of the main challenges for scientists today, as it offers unusual properties and multifunctionality. The originality of our paper lies in the study of new materials based on biomimicking lipid bilayers loaded with chlorophyll, chitosan, and turmeric-generated nano-silver/silver chloride particles. These materials showed a good free radical scavenging capacity between 76.25 and 93.26% (in vitro tested through chemiluminescence method) and a good antimicrobial activity against Enterococcus faecalis bacterium (IZ > 10 mm). The anticancer activity of our developed bio-based materials was investigated against two cancer cell lines (human colorectal adenocarcinoma cells HT-29, and human liver carcinoma cells HepG2) and compared to one healthy cell line (human fibroblast BJ cell line). Cell viability was evaluated for all prepared materials after a 24 h treatment and was used to select the biohybrid with the highest therapeutic index (TI); additionally, the hemolytic activity of the samples was also evaluated. Finally, we investigated the morphological changes induced by the developed materials against the cell lines studied. Biophysical studies on these materials were done by correlating UV–Vis and FTIR absorption spectroscopy, with XRD, SANS, and SAXS methods, and with information provided by microscopic techniques (AFM, SEM/EDS). In conclusion, these “green” developed hybrid systems are an important alternative in cancer treatment, and against health problems associated with drug-resistant infections.

A novel bis(pyrazolyl)methane compound as a potential agent against Gram-positive bacteria

This study was designed to propose alternative therapeutic compounds to fight against bacterial pathogens. Thus, a library of nitrogen-based compounds bis(triazolyl)methane (1T–7T) and bis(pyrazolyl)methane (1P–11P) was synthesised following previously reported methodologies and their antibacterial activity was tested using the collection strains of Staphylococcus aureus, Enterococcus faecalis, Escherichia coli, and Pseudomonas aeruginosa. Moreover, the novel compound 2P was fully characterized by IR, UV–Vis and NMR spectroscopy. To evaluate antibacterial activity, minimal inhibitory concentrations (MICs), minimal bactericidal concentrations (MBCs), minimum biofilm inhibitory concentrations (MBICs), and minimum biofilm eradication concentrations (MBECs) assays were carried out at different concentrations (2–2000 µg/mL). The MTT assay and Resazurin viability assays were performed in both human liver carcinoma HepG2 and human colorectal adenocarcinoma Caco-2 cell lines at 48 h. Of all the synthesised compounds, 2P had an inhibitory effect on Gram-positive strains, especially against S. aureus. The MIC and MBC of 2P were 62.5 and 2000 µg/mL against S. aureus, and 250 and 2000 µg/mL against E. faecalis, respectively. However, these values were > 2000 µg/mL against E. coli and P. aeruginosa. In addition, the MBICs and MBECs of 2P against S. aureus were 125 and > 2000 µg/mL, respectively, whereas these values were > 2000 µg/mL against E. faecalis, E. coli, and P. aeruginosa. On the other hand, concentrations up to 250 µg/mL of 2P were non-toxic doses for eukaryotic cell cultures. Thus, according to the obtained results, the 2P nitrogen-based compound showed a promising anti-Gram-positive effect (especially against S. aureus) both on planktonic state and biofilm, at non-toxic concentrations.

Brefeldin A delivery nanomicelles in hepatocellular carcinoma therapy: Characterization, cytotoxic evaluation in vitro, and antitumor efficiency in vivo

Hepatocellular carcinoma (HCC) is one of the major cancers with high mortality rate. Traditional drugs used in clinic are usually limited by the drug resistance and side effect and novel agents are still needed. Macrolide brefeldin A (BFA) is a well-known lead compound in cancer chemotherapy, however, with poor solubility and instability. In this study, to overcome these disadvantages, BFA was encapsulated in mixed nanomicelles based on TPGS and F127 copolymers (M-BFA). M-BFA was conferred high solubility, colloidal stability, and capability of sustained release of intact BFA. In vitro, M-BFA markedly inhibited the proliferation, induced G0/G1 phase arrest, and caspase-dependent apoptosis in human liver carcinoma HepG2 cells. Moreover, M-BFA also induced autophagic cell death via Akt/mTOR and ERK pathways. In HepG2 tumor-bearing xenograft mice, indocyanine green (ICG) as a fluorescent probe loaded in M-BFA distributed to the tumor tissue rapidly, prolonged the blood circulation, and improved the tumor accumulation capacity. More importantly, M-BFA (10 mg/kg) dramatically delayed the tumor progression and induced extensive necrosis of the tumor tissues. Taken together, the present work suggests that M-BFA has promising potential in HCC therapy.

Pt-Coated Au Nanoparticle Toxicity Is Preferentially Triggered Via Mitochondrial Nitric Oxide/Reactive Oxygen Species in Human Liver Cancer (HepG2) Cells.

Reactive nitrogen species (RNS) that are formed from the reaction of versatile nitric oxide (NO) with reactive oxygen species (ROS) have been less explored in potential cancer therapy. This may be partly due to the fewer available agents that could induce NO in cells. Here, we report platinum-coated gold nanoparticles (Pt-coated Au NPs; 27 ± 20 nm) as a strong inducer of NO (assessed by live-cell imaging under NO-specific DAR-1 probe labeling and indirectly using a Griess reagent) in human liver carcinoma (HepG2) cells. In addition to NO, this study found a critical role of ROS from mitochondrial sources in the mechanism of toxicity caused by Pt-coated Au NPs. Cotreatment with a thiol-replenishing general antioxidant NAC (N-acetyl cysteine) led to significant amelioration of oxidative stress against NP-induced toxicity. However, NAC did not exhibit as much ameliorative potential against NP-induced oxidative stress as the superoxide radical (O2•–)-scavenging mitochondrial specific antioxidant mito-TEMPO did. The higher protective potential of mito-TEMPO in comparison to NAC reveals mitochondrial ROS as an active mediator of NP-induced toxicity in HepG2 cells. Moreover, the relatively unaltered NP-induced NO concentration under cotreatment of GSH modulators NAC and buthionine sulfoximine (BSO) suggested that NO production due to NP treatment is rather independent of the cellular thiols at least in HepG2 cells. Moreover, toxicity potentiation by exogenous H2O2 again suggested a more direct involvement of ROS/RNS in comparison to the less potentiation of toxicity due to GSH-exhausting BSO. A steeper amelioration in NP-induced NO and ROS and, consequently, cytotoxicity by mito-TEMPO in comparison to NAC reveal a pronounced role of NO and ROS via the mitochondrial pathway in the toxicity of Pt-coated Au NPs in HepG2 cells.

Synthesis, Cytotoxicity, Antioxidant and Antimicrobial Activity of Indole Based Novel Small Molecules

Aim: In this study experiments were carried out to explore antioxidant, antimicrobial, cytotoxic properties of novel indole derivative 1-ethyl-2-phenyl-3-phenylethyl-3-thiophen-2-yl-1Hindole (EPI) together with its effect on glutathione S-transferases (GST) activities in human liver carcinoma (HepG2) cells. Background:: Indoles probably represent one of the most important heterocyclic structures that have been attracting the interest of many scientists in drug discovery. Objective: The present study was carried out to explore antioxidant, antimicrobial, cytotoxic properties of novel indole derivative 1-ethyl-2-phenyl-3-phenylethyl-3-thiophen-2-yl-1H-indole (EPI) and its effect on glutathione S-transferases (GST) activities in human liver carcinoma (HepG2) cells. Materials and Methods: Pd-catalyst Sonogashira coupling reactions, MTT Assay, Antioxidant capacity test, Antimicrobial test, GST enzyme activity test. Results: 1-ethyl-2-phenyl-3-(phenylethynyl)-1H-indole had antioxidant and antimicrobial properties. It displayed significant induction in glutathione S-transferases (GST) enzyme activity in human liver cancer cell lines (HepG2), but cytotoxic effect on all tested cancer cell lines could not be observed. Conclusion:: All of these results showed that 1-ethyl-2-phenyl-3-(phenylethynyl)-1H-indole had antioxidant and antimicrobial properties without cytotoxic effect, which could make it a promising active component with further studies.

Individual and combined hepatocytotoxicity of DDT and cadmium in vitro.

The organochlorine insecticide dichlorodiphenyltrichloroethane (DDT) and heavy metal cadmium (Cd) are widespread environmental pollutants. They are persistent in the environment and can accumulate in organisms. Although the individual toxicity of DDT and Cd has been well documented, their combined toxicity is still not clear. Since liver is their common target, in this study, the individual and combined toxicity of DDT and Cd in human liver carcinoma HepG2 and human normal liver THLE-3 cell lines were investigated. The results showed that DDT and Cd inhibited the viability of HepG2 and THLE-3 cells dose-dependently and altered lysosomal morphology and function. Intracellular reactive oxygen species and lipid peroxidation levels were induced by DDT and Cd treatment. The combined cytotoxicity of DDT and Cd was greater than their individual cytotoxicity, and the interaction between Cd and DDT was additive on the inhibition of cell viability and lysosomal function of HepG2 cells. The interaction was antagonistic on the inhibition of cell viability of THLE-3 cells. These results may facilitate the evaluation of the cumulative risk of pesticides and heavy metal residues in the environment.

One-Step Synthesis of Magnetic Nanocomposite with Embedded Biologically Active Substance.

Magnetic nanocomposites based on hydroxyapatite were prepared by a one-step process using the hydrothermal coprecipitation method to sinter iron oxides (Fe3O4 and γ-Fe2O3). The possibility of expanding the proposed technique for the synthesis of magnetic composite with embedded biologically active substance (BAS) of the 2-arylaminopyrimidine group was shown. The composition, morphology, structural features, and magnetic characteristics of the nanocomposites synthesized with and without BAS were studied. The introduction of BAS into the composite synthesis resulted in minor changes in the structural and physical properties. The specificity of the chemical bonds between BAS and the hydroxyapatite-magnetite core was revealed. The kinetics of the BAS release in a solution simulating the stomach environment was studied. The cytotoxicity of (HAP)FexOy and (HAP)FexOy + BAS composites was studied in vitro using the primary culture of human liver carcinoma cells HepG2. The synthesized magnetic composites with BAS have a high potential for use in the biomedical field, for example, as carriers for magnetically controlled drug delivery and materials for bone tissue engineering.

Green and chemically synthesized zinc oxide nanoparticles: effects on in-vitro seedlings and callus cultures of Silybum marianum and evaluation of their antimicrobial and anticancer potential

Zinc oxide nanoparticles (ZnO-NPs) have been produced by physical and chemical methods. Here, the comparative evaluation of both chemically-synthesised ZnO-NPs (C-ZNPs) and in-vitro cultured S. marianum mediated green-synthesised ZnO-NPs (G-ZNPs) were investigated on seed germination frequency, root and shoot growth, callus induction and biochemical profile of medicinally important plant Silybum marianum. Of all the treatments, callus-mediated ZnO-NPs gave optimum results for seed germination (65%), plantlet’s root length (4.3 cm), shoot length (5.3 cm) and fresh and dry weights (220.4 g L−1 and 21.23 g L−1, respectively). Similarly, the accumulation of phenolic (12.3 µg/mg DW) and flavonoid (2.8 µg/mg DW) contents were also enhanced in callus cultures treated with G-ZNPs. We also observed maximum antioxidant activity (99%) in callus cultures treated with G-ZNPs, however, in case of plantlets, these activities were found highest for in-vitro whole plant-mediated ZnO-NPs. Moreover, G-ZNPs also enhanced total protein content (265.32 BSAE/20g FW) in callus cultures. G-ZNPs were further assessed for their effects on several multidrug resistant bacterial strains and human liver carcinoma (HepG2) cells and our findings revealed that callus extracts treated with G-ZNPs show ameliorated antibacterial (highest zone of inhibition (19 mm) against Klebsiella pneumonia) and anticancer (highest cytotoxicity of 64%) activities.