11,331 results match your criteria expression pro-apoptotic

Benzofuranyl-2-imidazoles as imidazoline I receptor ligands for Alzheimer's disease.

Eur J Med Chem 2021 May 20;222:113540. Epub 2021 May 20.

Laboratory of Medicinal Chemistry (Associated Unit to CSIC), Department of Pharmacology, Toxicology and Medicinal Chemistry, Faculty of Pharmacy and Food Sciences, Institute of Biomedicine (IBUB), University of Barcelona, Av. Joan XXIII, 27-31, E-08028, Barcelona, Spain. Electronic address:

Recent findings unveil the pharmacological modulation of imidazoline I receptors (I-IR) as a novel strategy to face unmet medical neurodegenerative diseases. In this work, we report the chemical characterization, three-dimensional quantitative structure-activity relationship (3D-QSAR) and ADMET in silico of a family of benzofuranyl-2-imidazoles that exhibit affinity against human brain I-IR and most of them have been predicted to be brain permeable. Acute treatment in mice with 2-(2-benzofuranyl)-2-imidazole, known as LSL60101 (garsevil), showed non-warning properties in the ADMET studies and an optimal pharmacokinetic profile. Read More

View Article and Full-Text PDF

IMiDs uniquely synergize with TKIs to upregulate apoptosis of Philadelphia chromosome-positive acute lymphoblastic leukemia cells expressing a dominant-negative IKZF1 isoform.

Cell Death Discov 2021 Jun 11;7(1):139. Epub 2021 Jun 11.

Department of Pediatrics, Graduate School of Medicine, University of Yamanashi, Chuo, Yamanashi, Japan.

The long-term prognosis of Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph + ALL) is still unsatisfactory even after the emergence of tyrosine kinase inhibitors (TKIs) against chimeric BCR-ABL, and this is associated with the high incidence of genetic alterations of Ikaros family zinc finger 1 (IKZF1), most frequently the hemi-allelic loss of exons 4-7 expressing a dominant-negative isoform Ik6. We found that lenalidomide (LEN), a representative of immunomodulatory drugs (IMiDs), which have been long used for the treatment of multiple myeloma, specifically induced accumulation of Ik6 with the disappearance of functional isoforms within 24 h (i.e. Read More

View Article and Full-Text PDF

The novel AKT inhibitor Afuresertib suppresses human Merkel cell carcinoma MKL-1 cell growth.

Clin Exp Dermatol 2021 Jun 11. Epub 2021 Jun 11.

Department of Dermatology, McGovern Medical School at The University of Texas Health Science Center, Houston, TX, USA.

Merkel cell carcinoma (MCC) is a highly aggressive neuroendocrine neoplasm of the skin that is associated with exceedingly poor prognosis. The AKT/mTOR signaling pathway, which plays a pivotal role in the modulation of protein synthesis and cell survival, has been shown to be highly important for Merkel cell carcinogenesis. In the current study, our data indicate that AKT has important regulatory functions in MCC cells and that inhibition of AKT with the novel ATP-competitive AKT inhibitor, Afuresertib, has widespread effects on proliferative pathways. Read More

View Article and Full-Text PDF

Exploring the role and clinical implications of proteasome inhibition in medulloblastoma.

Pediatr Blood Cancer 2021 Jun 11:e29168. Epub 2021 Jun 11.

Department of Neurology, University of California, Irvine, California, USA.

Ubiquitin proteasome-mediated protein degradation has been implicated in posttranslational oncogenesis in medulloblastoma. Current research is evaluating the clinical implications of proteasome inhibition as a therapeutic target. In medulloblastoma cell lines, proteasome inhibitors induce apoptosis and inhibit cell proliferation via multiple pathways involving activation of caspase pathways, NFκB (nuclear factor kappa-light-chain-enhancer of activated B cells) pathway inhibition, reduced AKT/mTOR pathway activity, and pro-apoptotic protein expression. Read More

View Article and Full-Text PDF

Evaluation of pro-apoptotic potential of taxifolin against liver cancer.

PeerJ 2021 25;9:e11276. Epub 2021 May 25.

Atta-Ur-Rahman School of Applied Biosciences, National University of Sciences and Technology, Islamabad, Pakistan.

Liver cancer is the second most common cause of cancer-induced deaths worldwide. Liver cirrhosis and cancer are a consequence of the abnormal angio-architecture formation of liver and formation of new blood vessels. This angiogenesis is driven by overexpression of hypoxia-inducible factor 1-alpha (Hif1-) and vascular endothelial growth factor (VEGF). Read More

View Article and Full-Text PDF

Silica Nanoparticles Induce Hepatotoxicity by Triggering Oxidative Damage, Apoptosis, and Bax-Bcl2 Signaling Pathway.

Biol Trace Elem Res 2021 Jun 10. Epub 2021 Jun 10.

Laboratory of Toxicology-Microbiology and Environmental Health (17ES06), Faculty of Sciences of Sfax, University of Sfax, BP1171, 3000, Sfax, Tunisia.

The increase in the usage of silica nanoparticles (SiNPs) in the industrial and medical fields has raised concerns about their possible adverse effects on human health. The present study aimed to investigate the potential adverse effects of SiNPs at daily doses of 25 and 100 mg/kg body weight intraperitoneally (i.p. Read More

View Article and Full-Text PDF

Pepsin Digest of Gliadin Forms Spontaneously Amyloid-Like Nanostructures Influencing the Expression of Selected Pro-Inflammatory, Chemoattractant, and Apoptotic Genes in Caco-2 Cells: Implications for Gluten-Related Disorders.

Mol Nutr Food Res 2021 Jun 10:e2100200. Epub 2021 Jun 10.

Department of Chemistry, Organic Chemistry III, Bielefeld University, Universitätsstr. 25, Bielefeld, 33615, Germany.

Scope: Proteolysis-resistant gliadin peptides are intensely investigated in biomedical research related to Celiac Disease and gluten-related disorders. Herein, the first integrated supramolecular investigation of pepsin-digested gliadin peptides, p-gliadin, is presented in combination with its functional behavior in Caco-2 cell line.

Methods And Results: First, we investigated gliadin degradation by pepsin at pH 3, and the physicochemical properties of p-gliadin were compared with gliadin. Read More

View Article and Full-Text PDF

Pseudo-ginsenoside Rh2 Induces Protective Autophagy in Hepatocellular Carcinoma HepG2 Cells.

Recent Pat Anticancer Drug Discov 2021 Jun 6. Epub 2021 Jun 6.

Department of Pharmacology, School of Pharmaceutical Sciences, Jilin University, Changchun, 130021, Jilin Province, China.

Background: Pseudo-ginsenoside-Rh2 (pseudo-G-Rh2), a novel derivative of ginsenoside Rh2, is reported to exert a pro-apoptotic effect on various malignancies. However, whether this anti-cancer action of pseudo-G-Rh2 involves autophagy remains to be determined and explored.

Objectives: Investigation of pseudo-G-Rh2-induced apoptosis and autophagy and the underlying mechanism. Read More

View Article and Full-Text PDF

Rehabilitation training improves cognitive disorder after cerebrovascular accident by improving BDNF Bcl-2 and Bax expressions in regulating the JMK pathway.

Eur Rev Med Pharmacol Sci 2021 May;25(10):3807-3821

Department of Rehabilitation Medicine, The Second Affiliated Hospital of Qiqihar Medical University, Qiqihar, P.R. China.

Objective: To explore the effect of rehabilitation training on cognitive impairment after cerebrovascular accident and its potential mechanism.

Patients And Methods: 100 patients of cerebrovascular accident treated in our hospital from August 2018 to August 2019 were selected as the subjects, and 50 patients with physical examination were selected as healthy control group. The patients with cerebrovascular accident were randomly divided into control group (50 patients) and research group (50 patients). Read More

View Article and Full-Text PDF

Impact of Progesterone on Molecular Mechanisms of Preterm Premature Rupture of Membranes.

Reprod Sci 2021 Jun 9. Epub 2021 Jun 9.

Department of Obstetrics & Gynecology, Uijeongbu St. Mary's Hospital, College of Medicine, The Catholic University of Korea, 271, Cheonbo-Ro, Uijeongbu-si, Gyeonggi-do, Uijeongbu-si, Republic of Korea.

The role and mechanisms of progesterone in preterm premature rupture of membranes (PPROM) remains unclear. This study aims to investigate the molecular mechanisms of action of progesterone in pre-labor full-term fetal amniotic membrane cells with and without stimulation by microbial, pro-inflammatory, or thrombogenic agents. Fetal amniotic membranes were collected from 30 women with a normal singleton pregnancy undergoing elective cesarean section at term prior to the onset of labor. Read More

View Article and Full-Text PDF

Neuroprotective Effects of Sodium Butyrate through Suppressing Neuroinflammation and Modulating Antioxidant Enzymes.

Neurochem Res 2021 Jun 9. Epub 2021 Jun 9.

Department of Integrated Biosciences, Graduate School of Konkuk University, Chungju, 27478, Korea.

The discovery of effective therapeutic agents against neurodegenerative diseases (NDDs) remains challenging. Neurotoxicity, inflammations, and oxidative stress are associating factors of NDDs. Sodium butyrate (NaB) is a short-chain fatty acid found in diet and produced in the gut that reportedly protects cancer, inflammation, obesity and so on. Read More

View Article and Full-Text PDF

Use of melatonin as an inhibitor of apoptotic process for cryopreservation of zebrafish (Danio rerio) embryos.

Braz J Biol 2021 2;82:e241081. Epub 2021 Jun 2.

Universidade Estadual de Maringá - UEM, Departamento de Zootecnia, Maringá, PR, Brasil.

This study investigated the use of melatonin to arrest the effects of apoptosis in vitrified zebrafish (D. rerio) embryos. Dechorionated embryos at 22-24 somite-stage were divided (n = 60/treatment) into a non-vitrified (Control Group, 0 M melatonin) and vitrified treatments with 0 M (T1), 1 µM (T2) and 1 mM of melatonin (T3). Read More

View Article and Full-Text PDF

[Effect of Competitive Antagonist of Transmembrane Glutamine Flux V-9302 on Apoptosis of Acute Myeloid Leukemia Cell Lines HL-60 and KG-1].

Zhongguo Shi Yan Xue Ye Xue Za Zhi 2021 Jun;29(3):685-689

Department of Hematology, School of Medicine, South China University of Technology, Guangzhou 510006, Guangdong Province,China,E-mail:

Objective: To investigate the effect of V-9302 (an antagonist of transmembrane glutamine flux) on the proliferation and apoptosis of acute myeloid leukemia cells HL-60 and KG-1.

Methods: HL-60 and KG-1 cells at logarithmic phase were treated by different concentrations of V-9302. CCK-8 assay was used to detect the proliferation of the cells. Read More

View Article and Full-Text PDF

Platelet Mitochondria Transplantation Rescues Hypoxia/Reoxygenation-Induced Mitochondrial Dysfunction and Neuronal Cell Death Involving the FUNDC2/PIP3/Akt/FOXO3a Axis.

Cell Transplant 2021 Jan-Dec;30:9636897211024210

Department of Neurology, Guangdong Second Provincial General Hospital, Guangzhou, Guangdong, China.

Mitochondrial transplantation emerges as a novel therapeutic solution for ischemia/reperfusion injury (IRI) in various tissues. Platelets have recently been used in mitochondrial transplantation as readily-available donors of small-size platelet mitochondria (plt-mito). Interestingly, FUN14 Domain Containing 2 (FUNDC2), a protein highly-expressed in the outer membrane (OMM) of plt-mito, has been identified to maintain platelet survival under hypoxic condition. Read More

View Article and Full-Text PDF

Neat1 decreases neuronal apoptosis after oxygen and glucose deprivation.

Neural Regen Res 2022 Jan;17(1):163-169

Department of Neurosurgery, First Affiliated Hospital of Chongqing Medical University, Chongqing, China.

Studies have shown that downregulation of nuclear-enriched autosomal transcript 1 (Neat1) may adversely affect the recovery of nerve function and the increased loss of hippocampal neurons in mice. Whether Neat1 has protective or inhibitory effects on neuronal cell apoptosis after secondary brain injury remains unclear. Therefore, the effects of Neat1 on neuronal apoptosis were observed. Read More

View Article and Full-Text PDF
January 2022

Antioxidant and anti-apoptotic prophylactic effect of silymarin against lead-induced hepatorenal toxicity in rats.

Environ Sci Pollut Res Int 2021 Jun 8. Epub 2021 Jun 8.

Department of Biotechnology, College of Science, Taif University, P.O. Box 11099, Taif, 21944, Saudi Arabia.

This study assessed prophylactic potentials of silymarin against lead-induced hepatorenal toxicity in rats with the respect to its antioxidant and anti-apoptotic activities. Forty male albino rats were distributed into four groups. Control group is provided with distilled water. Read More

View Article and Full-Text PDF

Suppresses Cell Proliferation and Apoptosis via Regulation of SIRT1/PGC-1α/NRF2 Axis in Pancreatic Cancer.

Cell J 2021 Jul 26;23(2):199-210. Epub 2021 May 26.

Department of Gastrointestinal Surgery, The Central Hospital of Hengyang City, Hengyang 421001, P.R.China.Email:

Objective: Our study aimed to investigate function and mechanism of in proliferation and apoptosis of pancreatic cancer (PC) cells by regulating NAD+-dependent histone deacetylase sirtulin 1 (SIRT1).

Materials And Methods: This experimental study included two PC cell lines AsPC-1 and PANC-1 in which expression levels of and were manipulated. The level of was detected by reverse transcription quantitative polymerase chain reaction (RT-qPCR) method. Read More

View Article and Full-Text PDF

Estradiol and 1α,25(OH) vitamin D share plasma membrane downstream signal transduction through calcium influx and genomic activation in immature rat testis.

Theriogenology 2021 May 30;172:36-46. Epub 2021 May 30.

Laboratório de Hormônios & Transdução de Sinais, Departamento de Bioquímica, Centro de Ciências Biológicas, Universidade Federal de Santa Catarina, Florianópolis, Santa Catarina, Brazil. Electronic address:

The aim of this study was to investigate the rapid response pathway and gene and protein expression profiles of the rat testis in response to estradiol (E) and 1α,25(OH) vitamin D (1,25-D), to understand how they mediate their effects on the first spermatogenic wave. To do this, we compared the effects of 1,25-D and E on calcium(Ca) uptake and the involvement of estrogen receptors (ESR) in their rapid responses. Additionally, we studied the downstream signal transduction effects of 1,25-D and E on cyclin A1/B1 and cellular cycle protein expression. Read More

View Article and Full-Text PDF

Laurus nobilis ethanolic extract attenuates hyperglycemia and hyperinsulinemia-induced insulin resistance in HepG2 cell line through the reduction of oxidative stress and improvement of mitochondrial biogenesis - possible implication in pharmacotherapy.

Mitochondrion 2021 Jun 3. Epub 2021 Jun 3.

National Medicines Institute, Chełmska 30/34, 00-725 Warsaw, Poland.

The aim of this study was to establish the potential effect of Laurus nobilis ethanolic extract on improving insulin sensitivity and protecting liver cells from apoptosis, mitochondrial dysfunction, oxidative stress (OS), and inflammation; all of which considered as major alterations occurring during insulin resistance (IR) as well as diabetes onset, in hyperinsulinemic and hyperglycemic-induced HepG2 cell line. Thereby, L. nobilis ethanolic extract has been first chemically characterized using LC-MS/MS technique. Read More

View Article and Full-Text PDF

Cushing syndrome and glucocorticoids: T-cell lymphopenia, apoptosis and rescue by IL-21.

J Allergy Clin Immunol 2021 Jun 2. Epub 2021 Jun 2.

Immunology Service, Department of Laboratory Medicine, NIH Clinical Center, NIH, Bethesda, MD, USA, 20892. Electronic address:

Background: Pediatric endogenous Cushing syndrome is mainly caused by pituitary corticotropin-producing adenomas and most glucocorticoid-dependent effects progressively regress upon tumor removal. Endogenous Cushing syndrome reproduces long-term high-dose glucocorticoid therapy, representing a clean, natural and unbiased model in which to study glucocorticoid bona-fide effects on immunity.

Objectives: To perform extensive immunologic studies in otherwise healthy pediatric patients with endogenous Cushing syndrome before and 6-13 months after tumor resection, as well as in in-vitro glucocorticoid-treated control cells. Read More

View Article and Full-Text PDF

Caprine parainfluenza virus type 3 N protein promotes viral replication via inducing apoptosis.

Vet Microbiol 2021 May 24;259:109129. Epub 2021 May 24.

Institute of Veterinary Medicine, Jiangsu Academy of Agricultural Sciences, Key Laboratory of Veterinary Diagnosis, Jiangsu Academy of Agricultural Sciences, Key Laboratory of Veterinary Biological Engineering and Technology, Ministry of Agriculture, Nanjing, 210014, China; Institute of Life Sciences, School of Food and Biological Engineering, Jiangsu University, Zhenjiang, 212013, China; College of Veterinary Medicine, Nanjing Agricultural University, Nanjing, 210095, China. Electronic address:

Caprine parainfluenza virus type 3 (CPIV3) is one of the most important viral respiratory pathogens of goat. Accumulating evidence demonstrates that apoptosis is a cellular mechanism for the host response to pathogens, and it participates in regulating viral replication. However, there is little study on CPIV3-induced host cells apoptosis. Read More

View Article and Full-Text PDF

Iodoacetic acid affects Estrous Cyclicity, ovarian gene expression, and hormone levels in mice.

Biol Reprod 2021 Jun 3. Epub 2021 Jun 3.

Department of Comparative Biosciences, University of Illinois, Urbana, IL, USA.

Iodoacetic acid (IAA) is a water disinfection byproduct that is an ovarian toxicant in vitro. However, information on the effects of IAA on ovarian function in vivo was limited. Thus, we determined whether IAA exposure affects estrous cyclicity, steroidogenesis, and ovarian gene expression in mice. Read More

View Article and Full-Text PDF

Potential targeting of Hep3B liver cancer cells by lupeol isolated from Avicennia marina.

Arch Pharm (Weinheim) 2021 Jun 4:e2100120. Epub 2021 Jun 4.

Research Institute for Medical and Health Sciences, University of Sharjah, Sharjah, UAE.

Medicinal plants are valuable sources of different active constituents that are known to have important pharmacological activities including anticancer effects. Lupeol, a pentacyclic triterpenoid, present in many medicinal plants, has a wide range of biological activities. Although the anticancer activity of lupeol was reported, the published data are inconsistent and the clear mechanism of action has never been assigned. Read More

View Article and Full-Text PDF

Jaspine B Hydrochloride-induced Apoptosis in HeLa Cells Is Associated With Disrupted Sphingolipid Metabolism and Ceramide Overload.

Anticancer Res 2021 Jun;41(6):2875-2883

Department of Pharmacology, Faculty of Medicine, P.J. Šafárik University, Košice, Slovak Republic;

Background/aim: A series of experiments on HeLa cells were conducted to provide new information concerning the anti-cancer properties of jaspine B hydrochloride (JBH).

Materials And Methods: HeLa cells treated with 0.5 μmol/l JBH for 24, 48, and 72 h underwent flow cytometric analysis of the cell cycle, and measurement of phosphatidylserine externalization, mitochondrial membrane potential (MMP), casp-3 activation, cleavage of PARP, ceramide levels, aSMase activity, and Bcl-2 release. Read More

View Article and Full-Text PDF

Histone deacetylase 2 selective inhibitors: A versatile therapeutic strategy as next generation drug target in cancer therapy.

Pharmacol Res 2021 Jun 1;170:105695. Epub 2021 Jun 1.

Department of Biophysics, Manipal School of Life Sciences, MAHE, Manipal, India. Electronic address:

Acetylation and deacetylation of histone and several non-histone proteins are the two important processes amongst the different modes of epigenetic modulation that are involved in regulating cancer initiation and development. Abnormal expression of histone deacetylases (HDACs) is often reported in various types of cancers. Few pan HDAC inhibitors have been approved for use as therapeutic interventions for cancer treatment including vorinostat, belinostat and panobinostat. Read More

View Article and Full-Text PDF

Potential Role of Hsp70 and Activated NK Cells for Prediction of Prognosis in Glioblastoma Patients.

Front Mol Biosci 2021 17;8:669366. Epub 2021 May 17.

Department of Radiation Oncology, School of Medicine, Technical University Munich (TUM), Munich, Germany.

Despite rapid progress in the treatment of many cancers, glioblastoma remains a devastating disease with dismal prognosis. The aim of this study was to identify chaperone- and immune-related biomarkers to improve prediction of outcome in glioblastoma. Depending on its intra- or extracellular localization the major stress-inducible heat shock protein 70 (Hsp70) fulfills different tasks. Read More

View Article and Full-Text PDF

USP8 is a Novel Therapeutic Target in Melanoma Through Regulating Receptor Tyrosine Kinase Levels.

Cancer Manag Res 2021 24;13:4181-4189. Epub 2021 May 24.

Department of Oncology, Xiangyang No.1 People's Hospital, Hubei University of Medicine, Xiangyang, Hubei, People's Republic of China.

Introduction: The hyperactivation of receptor tyrosine kinase (RTK)-mediated pathways plays an important role in melanoma progression and resistance to therapy. The ubiquitin-specific protease 8 (USP8) is a deubiquitinating enzyme and its inhibition induces degradation of RTKs. This work explored the expression and role of USP8 in melanoma. Read More

View Article and Full-Text PDF

Tormentic acid induces anticancer effects in cisplatin-resistant human cervical cancer cells mediated via cell cycle arrest, ROS production, and targeting mTOR/PI3K/AKT signalling pathway.

J BUON 2021 Mar-Apr;26(2):643

Department of Oncology, Second Hospital of Shanxi Medical University, Taiyuan, Shanxi 030000, China.

Purpose: Tormentic acid has been shown to exert remarkable anti-cancer potential against different cancer cell types. In this study, the anti-cancer potential of tormentic acid was examined in cisplatin-resistant cervical cancer cells (HeLa cells). Further, the effects of tormentic acid on cell cycle, reactive oxygen species (ROS) production, and mTOR/PI3K/AKT signalling pathway were evaluated as well. Read More

View Article and Full-Text PDF

8a, a New Acridine Antiproliferative and Pro-Apoptotic Agent Targeting HDAC1/DNMT1.

Int J Mol Sci 2021 May 24;22(11). Epub 2021 May 24.

Li Dak Sum Yip Yio Chin Kenneth Li Marine Biopharmaceutical Research Center, College of Food and Pharmaceutical Sciences, Ningbo University, Ningbo 315800, China.

Epigenetic therapy using histone deacetylase (HDAC) inhibitors has become an attractive project in new drug development. However, DNA methylation and histone acetylation are important epigenetic ways to regulate the occurrence and development of leukemia. Given previous studies, -(2-aminophenyl)benzamide acridine (), as a histone deacetylase 1 (HDAC1) inhibitor, induces apoptosis and shows significant anti-proliferative activity against histiocytic lymphoma U937 cells. Read More

View Article and Full-Text PDF

Opa1 Deficiency Promotes Development of Retinal Vascular Lesions in Diabetic Retinopathy.

Int J Mol Sci 2021 May 31;22(11). Epub 2021 May 31.

Department of Medicine, Boston University School of Medicine, Boston, MA 02118, USA.

This study investigates whether reduced optic atrophy 1 () level promotes apoptosis and retinal vascular lesions associated with diabetic retinopathy (DR). Four groups of mice: wild type (WT) control mice, streptozotocin (STZ)-induced diabetic mice, mice, and diabetic mice were used in this study. 16 weeks after diabetes onset, retinas were assessed for Opa1 and Bax levels by Western blot analysis, and retinal networks were examined for acellular capillaries (AC) and pericyte loss (PL). Read More

View Article and Full-Text PDF