41,124 results match your criteria hepg2 cells

Deep-learning models for lipid nanoparticle-based drug delivery.

Nanomedicine (Lond) 2021 May 5. Epub 2021 May 5.

Department of Pharmaceutical Biosciences, Uppsala University, Uppsala, Sweden.

Early prediction of time-lapse microscopy experiments enables intelligent data management and decision-making. Using time-lapse data of HepG2 cells exposed to lipid nanoparticles loaded with mRNA for expression of GFP, the authors hypothesized that it is possible to predict in advance whether a cell will express GFP. The first modeling approach used a convolutional neural network extracting per-cell features at early time points. Read More

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Phenylethanoid Glycosides Induce Apoptosis of Hepatocellular Carcinoma Cells by Mitochondria-Dependent and MAPK Pathways and Enhance Antitumor Effect through Combination with Cisplatin.

Integr Cancer Ther 2021 Jan-Dec;20:15347354211013085

Xinjiang University, Urumqi, Xinjiang, China.

is a type of Chinese herbal medicine and exerts various biological functions. Previous studies have been demonstrated that phenylethanoid glycosides (CTPG) exhibit antitumor effects on a variety of tumor cells. However, the antitumor effects of CTPG on HepG2 and BEL-7404 hepatocellular carcinoma (HCC) cells are still elusive. Read More

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Pyridine-derived VEGFR-2 inhibitors: Rational design, synthesis, anticancer evaluations, in silico ADMET profile, and molecular docking.

Arch Pharm (Weinheim) 2021 May 5:e2100085. Epub 2021 May 5.

Department of Pharmaceutical Medicinal Chemistry and Drug Design, Faculty of Pharmacy (Boys), Al-Azhar University, Cairo, Egypt.

Novel pyridine-derived compounds (5-19) were designed and synthesized, and their anticancer activities were evaluated against HepG2 and MCF-7 cells, targeting the VEGFR-2 enzyme. Compounds 10, 9, 8, and 15 were found to be the most potent derivatives against the two cancer cell lines, HepG2 and MCF-7, respectively, with IC  = 4.25 and 6. Read More

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RRx-001 Increases Erythrocyte Preferential Adhesion to the Tumor Vasculature.

Int J Mol Sci 2021 Apr 29;22(9). Epub 2021 Apr 29.

Department of Bioengineering, University of California, San Diego, La Jolla, CA 92093-0412, USA.

Red blood cells (RBCs) serve a variety of functions beyond mere oxygen transport both in health and pathology. Notably, RRx-001, a minimally toxic pleiotropic anticancer agent with macrophage activating and vascular normalization properties currently in Phase III trials, induces modification to RBCs which could promote vascular adhesion similar to sickle cells. This study assessed whether RBCs exposed to RRx-001 adhere to the tumor microvasculature and whether this adhesion alters tumor viability. Read More

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Synthesis and Evaluation of the Cytotoxic Activity of Water-Soluble Cationic Organometallic Complexes of the Type [Pt(η-CHOMe)(L)(Phen)] (L = NH, DMSO; Phen = 1,10-Phenanthroline).

Pharmaceutics 2021 Apr 30;13(5). Epub 2021 Apr 30.

Dipartimento di Scienze e Tecnologie Biologiche ed Ambientali, Università del Salento, Prov.le Lecce-Monteroni, Centro Ecotekne, 73100 Lecce, Italy.

Starting from the [PtCl(η-CHOMe)(phen)] (phen = 1,10-phenanthroline, ) platinum(II) precursor, we synthesized and characterized by multinuclear NMR new [Pt(η-CHOMe)(L)(phen)] (L = NH, ; DMSO, ) complexes. These organometallic species, potentially able to interact with cell membrane organic cation transporters (OCT), violating some of the classical rules for antitumor activity of cisplatin analogues, were evaluated for their cytotoxicity. Interestingly, despite both complexes and resulting in greater cell uptake than cisplatin in selected tumor cell lines, only showed comparable or higher antitumor activity. Read More

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Validation of a Gas Chromatography-Mass Spectrometry Method for the Measurement of the Redox State Metabolic Ratios Lactate/Pyruvate and β-Hydroxybutyrate/Acetoacetate in Biological Samples.

Int J Mol Sci 2021 Apr 30;22(9). Epub 2021 Apr 30.

Service of Biochemistry and Molecular Genetics, Hospital Clinic Universitari, Centro de Investigación Biomédica en Red de Enfermedades Hepáticas y Digestivas (CIBERehd), Institut d'Investigacions Biomèdiques August Pi i Sunyer (IDIBAPS), Carrer de Villarroel 170, 08036 Barcelona, Spain.

The metabolic ratios lactate/pyruvate and β-hydroxybutyrate/acetoacetate are considered valuable tools to evaluate the in vivo redox cellular state by estimating the free NAD+/NADH in cytoplasm and mitochondria, respectively. The aim of the current study was to validate a gas-chromatography mass spectrometry method for simultaneous determination of the four metabolites in plasma and liver tissue. The procedure included an o-phenylenediamine microwave-assisted derivatization, followed by liquid-liquid extraction with ethyl acetate and silylation with bis(trimethylsilyl)trifluoroacetamide:trimethylchlorosilane 99:1. Read More

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Ziyuglycoside II inhibits the growth of digestive system cancer cells through multiple mechanisms.

Chin J Nat Med 2021 May;19(5):351-363

School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100029, China. Electronic address:

Digestive system cancers, including liver, gastric, colon, esophageal and pancreatic cancers, are the leading cause of cancers with high morbidity and mortality, and the question of their clinical treatment is still open. Previous studies have indicated that Ziyuglycoside II (ZYG II), the major bioactive ingredient extract from Sanguisorba officinalis L., significantly inhibits the growth of various cancer cells. Read More

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Pinus kesiya Royle ex Gordon induces apoptotic cell death in hepatocellular carcinoma HepG2 cell via intrinsic pathway by PARP and Topoisomerase I suppression.

Biomed Pharmacother 2021 Apr 30;139:111628. Epub 2021 Apr 30.

Research Institute for Human High Performance and Health Promotion, Khon Kaen University, 40002, Thailand; Division of Pharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Khon Kaen University, Khon Kaen 40002, Thailand. Electronic address:

Pinus kesiya Royle ex Gordon (PK), widely found in Southeast Asia, has been traditionally used for the treatment of several illnesses. Our previous studies showed that PK was highly cytotoxicity against liver cancer cells. The detailed mechanism of anticancer action of 50% hydro-ethanolic extract of PK's twig was, therefore, investigated in hepatocellular carcinoma HepG2 cells. Read More

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Synthesis of alkynylated 1,2,4-oxadiazole/1,2,3-1H-triazole glycoconjugates: Discovering new compounds for use in chemotherapy against lung carcinoma and Mycobacterium tuberculosis.

Eur J Med Chem 2021 Apr 18;220:113472. Epub 2021 Apr 18.

Department of Chemistry, Federal Rural University of Pernambuco, Dois Irmãos, 52171-900, Recife, Brazil. Electronic address:

A total of forty-three compounds were synthesized, including thirty-two new ones. Among those compounds, seventeen were selected and tested on human tumor cell lines: PC-3 (prostate adenocarcinoma), HCT-116 (colorectal tumor), NCIH-460 (lung carcinoma), SKMEL-103 (melanoma) and AGP-01 (gastric tumor). Alkynylated 1,2,4-oxadiazoles 2m, 3g and 3k exhibited antiproliferative activities against NCIH-460 in culture. Read More

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Design, synthesis and biological evaluation of novel imidazole-chalcone derivatives as potential anticancer agents and tubulin polymerization inhibitors.

Bioorg Chem 2021 Apr 20;112:104904. Epub 2021 Apr 20.

Biotechnology Research Center, Mashhad University of Medical Sciences, Mashhad, Iran; Department of Medicinal Chemistry, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran.

Novel imidazole-chalcone derivatives were designed and synthesized as tubulin polymerization inhibitors and anticancer agents. The antiproliferative activity of the imidazole-chalcone was assessed on some human cancer cell lines including A549 (adenocarcinoma human alveolar basal epithelial cells), MCF-7 (human breast cancer cells), MCF-7/MX (mitoxantrone resistant human breast cancer cells), and HEPG2 (human hepatocellular carcinoma cells). Generally, the imidazole-chalcone derivatives exhibited more cytotoxicity on A549 cancer cells in comparison to the other three cell lines, among them compounds 9j' and 9g showed significant cytotoxicity with IC values ranging from 7. Read More

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Initial assessment of suitability of MCF-7 and HepG2 cancer cell lines for AQP3 research in cancer biology.

Acta Histochem 2021 Apr 29;123(4):151716. Epub 2021 Apr 29.

Department of Histology and Developmental Biology, Pomeranian Medical University, Żołnierska 48, 71-210, Szczecin, Poland.

Cancer cell lines are widely used as in vitro models to elucidate biological processes in cancer, and as a tool to evaluate anticancer agents. In fact, the use of an appropriate cancer cell line in cancer research is crucial for investigating new, potential factors involved in carcinogenesis. One of them is aquaporin-3 (AQP3), which is a small, hydrophobic, integral membrane protein with a predominant role in water and glycerol transport. Read More

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Intermittent hypoxia preconditioning protects WRL68 cells against oxidative injury: involvement of the PINK1/Parkin-mediated mitophagy regulated by nuclear respiratory factor 1.

Mitochondrion 2021 Apr 29. Epub 2021 Apr 29.

Institute of Special Environmental Medicine, Nantong University, Nantong 226019, China. Electronic address:

The protective effect of intermittent hypoxia (IH) preconditioning against oxidative injury in hepatic cells was investigated and the involvement of the PINK1/Parkin-mediated mitophagy regulated by nuclear respiratory factor 1 (NRF-1) was evaluated. The results showed that IH preconditioning protected HepG2 cells against oxygen and glucose deprivation/reperfusion (OGD/Rep)-induced injury and protected WRL68 cells against HO or AMA-induced oxidative injury. IH preconditioning up-regulated the protein level of NRF-1, PINK1, Parkin, and LC3 II, promoted the recruitment of the cytosolic Parkin, indicating the initiation of the PINK1/Parkin-mediated mitophagy in WRL68 cells. Read More

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Expression and purification of a recombinant ELRL-MAP30 with Dual-targeting anti-tumor bioactivity.

Protein Expr Purif 2021 Apr 29:105893. Epub 2021 Apr 29.

College of Life Science, Zhejiang Chinese Medical University, Hangzhou 310053, China. Electronic address:

MAP30 (Momordica antiviral protein 30kD) is a single-chain Ⅰ-type ribosome inactivating protein with a variety of biological activities, including anti-tumor ability. It was reported that MAP30 would serve as a novel and relatively safe agent for prophylaxis and treatment of liver cancer. To determine whether adding two tumor targeting peptides could improve the antitumour activities of MAP30, we genetically modified MAP30 with an RGD motif and a EGFRi motif, which is a ligand with high affinity for αvβ3 integrins and with high affinity for EGFR. Read More

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Self-assembled biodegradable core-shell nanocomposites of amphiphilic retinoic acid-LMW bPEI conjugates exhibit enhanced transgene expression in hepatocellular carcinoma cells with inherent anticancer properties.

J Pharm Sci 2021 Apr 29. Epub 2021 Apr 29.

Nucleic Acids Research Laboratory, CSIR-Institute of Genomics and Integrative Biology, Mall Road, Delhi-110007, India; Academy of Scientific and Innovation Research (AcSIR), Ghaziabad- 201002, India. Electronic address:

Low molecular weight branched polyethylenimines (LMW bPEIs) are almost non-toxic but display poor transfection efficiency due to lack of adequate complexation ability with nucleic acids followed by transportation across the cell membrane. Here, a series of amphiphilic retinoyl-bPEI conjugates (RP-1, RP-2 and RP-3) has been synthesized by allowing the reaction between bPEI (1.8 kDa) and a bioactive and hydrophobic vitamin A metabolite, all-trans-retinoic acid (ATRA), in varying amounts. Read More

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Disaccharide-polyethylenimine organic nanoparticles as non-toxic in vitro gene transporters and their anticancer potential.

Bioorg Chem 2021 Apr 16;112:104918. Epub 2021 Apr 16.

Nucleic Acids Research Laboratory, CSIR-Institute of Genomics and Integrative Biology, Mall Road, Delhi 110007, India; Academy of Scientific and Innovative Research (AcSIR), Ghaziabad 201002, India. Electronic address:

Polyethylenimines (PEIs) have been shown as efficient gene delivery vectors due to their unique properties, however, toxicity as well as non-specific interactions with the tissues/cells because of high charge density have hampered their use in clinical applications. To counter these concerns, here, we have prepared disachharide-PEI organic nanoparticles by mixing PEIs with non-reducing disaccharides, i.e. Read More

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In VITRO biochemical characterization and genotoxicity assessment of Sapindus saponaria seed extract.

J Ethnopharmacol 2021 Apr 28:114170. Epub 2021 Apr 28.

Laboratory of Biochemistry and Function of Plant Proteins, Research center on agricultural systems, Department of Botany, Federal University of the State of Rio de Janeiro, Av. Pasteur, 458, Urca, Brazil. Electronic address:

Ethnopharmacological Relevance: Sapindus saponaria, also popularly known as soapberry, has been used in folk medicinal values because of its therapeutic properties and several compounds in its composition, which represent a target in potential for drug discovery. However, few data about its potential toxicity has been reported.

Aim Of The Study: Plant proteins can perform essential roles in survival, acting as defense mechanism, as well functioning as important molecular reserves for its natural metabolism. Read More

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Identification of the molecular targets and mechanisms of compound mylabris capsules for hepatocellular carcinoma treatment through network pharmacology and bioinformatics analysis.

J Ethnopharmacol 2021 Apr 28:114174. Epub 2021 Apr 28.

Department of Infectious Diseases, Third Affiliated Hospital of Hebei Medical University, Shijiazhuang, Hebei, 050000, China. Electronic address:

Ethnopharmacological Relevance: Traditional Chinese herbal formulas have been proven to exert an inhibitory effect on tumor. Compound mylabris capsules (CMC) has been used for treating cancer, especially hepatocellular carcinoma (HCC), for years in China. However, its therapeutic mechanisms on HCC remain unclear. Read More

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Evaluation of cyanobacterial toxicity using different biotests and protein phosphatase inhibition assay.

Environ Sci Pollut Res Int 2021 May 1. Epub 2021 May 1.

University of Novi Sad, Faculty of Sciences, Department of Biology and Ecology, Trg Dositeja Obradovića 3, Novi Sad, 21000, Serbia.

Cyanobacteria are prolific producers of numerous toxic compounds, among which microcystins (hepatotoxins) are the most frequently found. Cyanobacterial bloom in freshwaters is an increasing problem, and there is still a need for rapid and reliable methods for the detection of toxic cyanobacterial samples. In the present study, the toxicity of crude extracts of 11 cyanobacterial strains from different genera has been assessed on two cell lines (human hepatocellular carcinoma HepG2 and rainbow trout (Oncorhynchus mykiss) liver-derived RTL-W1 cells), crustaceans (Daphnia magna and Artemia salina), and zebrafish (Danio rerio) embryos, as well as by protein phosphatase 1 (PP1) inhibition assay and ELISA test to determine whether the toxicity could be due to the presence of hepatotoxins/microcystins. Read More

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Ultraviolet B-irradiated mushroom supplementation increased the Ca uptake and ameliorated the LPS-induced inflammatory responses in zebrafish larvae.

J Food Biochem 2021 Apr 30:e13742. Epub 2021 Apr 30.

Department of Biotechnology, Daegu University, Gyeongsan, Republic of Korea.

The harmful effects of excessive ultraviolet (UV) exposure are well known. However, moderate exposure to UV radiation is beneficial and required for active vitamin D synthesis in our body. People living in the coldest regions on the earth are unable to expose their skin to the solar UV radiation and, therefore, additional supplementation of Vitamin D2 is recommended. Read More

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Tumor suppressive role of mitochondrial sirtuin 4 in induction of G2/M cell cycle arrest and apoptosis in hepatitis B virus-related hepatocellular carcinoma.

Cell Death Discov 2021 Apr 30;7(1):88. Epub 2021 Apr 30.

Department of Medicine, The University of Hong Kong, Queen Mary Hospital, Hong Kong SAR, China.

Hepatocellular carcinoma (HCC) is developed from uncontrolled cell growth after the malignant transformation of hepatocytes. The hepatitis B virus (HBV) X protein (HBx) has shown to induce cell cycle progression and hepatocarcinogenesis. A sub-fraction of HBx is localized in the mitochondria. Read More

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Protective Effect of n-Butanol Extract from Viola yedoensis on Immunological Liver Injury.

Chem Biodivers 2021 Apr 30. Epub 2021 Apr 30.

Ningxia Medical University, pharmacy, 1160 Shengli Street, 750004, Yinchuan, CHINA.

Viola yedoensis Makino was used to treat inflammation, viral hepatitis, acute pyogenic infection, and ulcerative carbuncles. However, the protective effect on immunological liver injury (ILI) of V. yedoensis had been rarely reported. Read More

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Pharmacological inhibition of HDAC1/3-interacting proteins induced morphological changes, and hindered the cell proliferation and migration of hepatocellular carcinoma cells.

Environ Sci Pollut Res Int 2021 Apr 30. Epub 2021 Apr 30.

Bio-products Research Chair, Department of Zoology, College of Science, King Saud University, P.O. Box 2455, Riyadh, 11451, Saudi Arabia.

Liver diseases are particularly severe health problems, but the options available for preventing and treating them remain limited. Accumulating evidence has shown that there is altered expression of individual histone deacetylase (HDAC) family members in hepatocellular carcinoma cells. In a previous study, we have identified a set of proteins which interact with histone deacetylase 1 and 3 (HDAC1/3) in hepatocellular carcinoma cell lines HepG2 by proteomic approach. Read More

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Analysis and Optimization of Conditions for the Use of 2',7'-Dichlorofluorescein Diacetate in Cultured Hepatocytes.

Antioxidants (Basel) 2021 Apr 26;10(5). Epub 2021 Apr 26.

Jiaxing Key Laboratory for Photonanomedicine and Experimental Therapeutics, Department of Pharmaceutics, College of Medicine, Jiaxing University, Jiaxing 314001, China.

Numerous liver pathologies encompass oxidative stress as molecular basis of disease. The use of 2',7'-dichlorodihydrofluorescein-diacetate (DCFH-DA) as fluorogenic redox probe is problematic in liver cell lines because of membrane transport proteins that interfere with probe kinetics, among other reasons. The properties of DCFH-DA were analyzed in hepatocytes (HepG2, HepaRG) to characterize methodological issues that could hamper data interpretation and falsely skew conclusions. Read More

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Effect of on the Liver Protection of Non-Alcoholic Fatty Liver Disease Based on In Vitro and In Vivo Models.

Curr Issues Mol Biol 2021 Apr 28;43(1). Epub 2021 Apr 28.

Department of Food and Nutrition, College of BioNano Technology, Gachon University, Gyeonggi-do 13120, Korea.

Edible insects, (silkworm; SW), which feed on mulberry leaves, have been consumed by humans for a long time as supplements or traditional medication. Non-alcoholic fatty liver disease (NAFLD) is a liver metabolic disorder that affects many people worldwide. We examined the hepatoprotective effects of SW using in vitro and high-fat and high-fructose (HFHF) diet-induced obese in vivo model mice by real-time PCR, immunoblot analysis, and fecal microbiota analysis. Read More

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Synergistic Photothermal-Chemotherapy Based on the Use of Biomimetic Magnetic Nanoparticles.

Pharmaceutics 2021 Apr 28;13(5). Epub 2021 Apr 28.

Department of Microbiology, Faculty of Sciences, University of Granada, 18071 Granada, Spain.

MamC-mediated biomimetic magnetic nanoparticles (BMNPs) have emerged as one of the most promising nanomaterials due to their magnetic features (superparamagnetic character and large magnetic moment per particle), their novel surface properties determined by MamC, their biocompatibility and their ability as magnetic hyperthermia agents. However, the current clinical application of magnetic hyperthermia is limited due to the fact that, in order to be able to reach an effective temperature at the target site, relatively high nanoparticle concentration, as well as high magnetic field strength and/or AC frequency are needed. In the present study, the potential of BMNPs to increase the temperature upon irradiation of a laser beam in the near infrared, at a wavelength at which tissues become partially transparent, is explored. Read More

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Feasibility of Developing Radiotracers for MDM2: Synthesis and Preliminary Evaluation of an F-Labeled Analogue of the MDM2 Inhibitor SP-141.

Pharmaceuticals (Basel) 2021 Apr 13;14(4). Epub 2021 Apr 13.

Department of Radiology, Duke University Medical Center, Durham, NC 27710, USA.

Murine double minute 2 (MDM2), a negative regulator of the p53 tumor suppressor protein, is overexpressed in several human cancers. Herein we investigate the feasibility of developing F-labeled compounds based on the small molecule inhibitor SP-141 for imaging tumor MDM2 expression levels with positron emission tomography (PET). Three nonradioactive fluorinated SP-141 analogues, -, were synthesized, and their binding to the MDM2 protein was analyzed by surface plasmon resonance (SPR). Read More

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The Importance of Platelet Glycoside Residues in the Haemostasis of Patients with Immune Thrombocytopaenia.

J Clin Med 2021 Apr 13;10(8). Epub 2021 Apr 13.

Hematology Unit, La Paz University Hospital-IdiPAZ, Paseo de la Castellana 261, 28046 Madrid, Spain.

Loss of sialic acid from the carbohydrate side chains of platelet glycoproteins can affect platelet clearance, a proposed mechanism involved in the etiopathogenesis of immune thrombocytopaenia (ITP). We aimed to assess whether changes in platelet glycosylation in patients with ITP affected platelet counts, function, and apoptosis. This observational, prospective, and transversal study included 82 patients with chronic primary ITP and 115 healthy controls. Read More

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Biological Properties of Essential Oils from Boiss.

Plants (Basel) 2021 Apr 16;10(4). Epub 2021 Apr 16.

Nutrition and Bromatology Group, Department of Analytical and Food Chemistry, Faculty of Food Science and Technology, University of Vigo-Ourense Campus, E32004 Ourense, Spain.

This study describes the chemical composition, antitumor, antioxidant, and antimicrobial activities of the plant Boiss. Essential oils (EOs) were collected in different periods (before, during, and after flowering stage) from the El-Guetfa region, M'sila, Algeria. The EOs extraction was achieved using three distinguishing techniques: hydro (Clevenger trap), steam, and microwave distillations, targeting different aerial parts of the plant (stems, flowers, and leaves). Read More

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Multiple Roles of Black Raspberry Anthocyanins Protecting against Alcoholic Liver Disease.

Molecules 2021 Apr 16;26(8). Epub 2021 Apr 16.

School of Functional Food and Wine, Shenyang Pharmaceutical University, Shenyang 110016, China.

This study aimed to investigate the protective effect of black raspberry anthocyanins (BRAs) against acute and subacute alcoholic liver disease (ALD). Network analysis and docking study were carried out to understand the potential mechanism. Thereafter, the serum biochemical parameters and liver indexes were measured, the histopathological changes of the liver were analyzed in vivo. Read More

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Low P66shc with High SerpinB3 Levels Favors Necroptosis and Better Survival in Hepatocellular Carcinoma.

Biology (Basel) 2021 Apr 23;10(5). Epub 2021 Apr 23.

Department of Medicine, University of Padua, Via Giustiniani, 2, 35128 Padua, Italy.

Cell proliferation and escape from apoptosis are important pathological features of hepatocellular carcinoma (HCC), one of the tumors with the highest mortality rate worldwide. The aim of the study was to evaluate the expression of the pro-apoptotic p66shc and the anti-apoptotic SerpinB3 in HCCs in relation to clinical outcome, cell fate and tumor growth. p66shc and SerpinB3 were evaluated in 67 HCC specimens and the results were correlated with overall survival. Read More

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