45,588 results match your criteria activity apoptotic

Discovery of novel class of histone deacetylase inhibitors as potential anticancer agents.

Bioorg Med Chem 2021 Jun 8;42:116251. Epub 2021 Jun 8.

Sharjah Institute for Medical Research, University of Sharjah, Sharjah 27272, United Arab Emirates; College of Pharmacy, University of Sharjah, Sharjah 27272, United Arab Emirates. Electronic address:

Selective inhibition of histone deacetylases (HDACs) is an important strategy in the field of anticancer drug discovery. However, lack of inhibitors that possess high selectivity toward certain HDACs isozymes is associated with adverse side effects that limits their clinical applications. We have initiated a collaborative initiatives between multi-institutions aimed at the discovery of novel and selective HDACs inhibitors. Read More

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Synthesis and biological evaluation of chalcone-polyamine conjugates as novel vectorized agents in colorectal and prostate cancer chemotherapy.

Eur J Med Chem 2021 May 28;222:113586. Epub 2021 May 28.

Université de Limoges, Laboratoire PEIRENE EA 7500, Faculté de Pharmacie, 2 Rue Du Dr Marcland, 87025, Limoges Cedex, France. Electronic address:

The aim of this study was to synthesize chalcone-polyamine conjugates in order to enhance bioavailability and selectivity of chalcone core towards cancer cells, using polyamine-based vectors. Indeed, it is well-known that polyamine transport system is upregulated in tumor cells. 3',4,4',5'-tetramethoxychalcone was selected as parent chalcone since it was found to be an efficient anti-proliferative agent on various cancer cells. Read More

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Spiraeoside extracted from red onion skin ameliorates apoptosis and exerts potent antitumor, antioxidant and enzyme inhibitory effects.

Food Chem Toxicol 2021 Jun 8:112327. Epub 2021 Jun 8.

Department of Stem Cell and Regenerative Biotechnology, Konkuk University, Seoul 05029, Republic of Korea. Electronic address:

Red onion skin waste (ROSW) was analyzed for extraction of naturally occurring 4'-O-glucoside of quercetin, spiraeoside (SPI) with promising biological activities. Reversed-phase high-performance liquid chromatography was used to determine the SPI content in three different solvent extracts of ROSW: water (12.2 mg/g), methanol (27. Read More

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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

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Effects of detraining on preconditioning exercise-induced neuroprotective potential after ischemic stroke in rats.

Brain Struct Funct 2021 Jun 10. Epub 2021 Jun 10.

Department of Systems Biology in Thromboregulation, Kagoshima University Graduate School of Medical and Dental Science, Kagoshima, Japan.

Preconditioning exercise prior to stroke exerts neuroprotection, which is an endogenous strategy that leads the brain cells to express several intrinsic factors and inhibits their apoptosis. However, it is unclear how long these benefits last after exercise cessation. The aim of this study was to investigate the effects of detraining on preconditioning exercise-induced neuroprotective potential after stroke. Read More

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MiR-124 and miR-506 are involved in the decline of protein C in children with extra-hepatic portal vein obstruction.

Sci Rep 2021 Jun 10;11(1):12320. Epub 2021 Jun 10.

Department of General Surgery, Capital Institute of Pediatrics, No. 2 Yabaolu Rd., Beijing, 100020, People's Republic of China.

The deficiency of protein C (PROC) can be partly rescued by Rex shunt through restoring portal blood flow in children with extra-hepatic portal venous obstruction (EHPVO). However, the decline of PROC is still found in some patients with a normal portal blood flow after Rex shunt. The aim of this study was to identify the candidate miRNAs involving in the decline of PROC and their mechanism. Read More

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TET2 Protects Against VSMC Apoptosis and Intimal Thickening in Transplant Vasculopathy.

Circulation 2021 Jun 11. Epub 2021 Jun 11.

Department of Medicine (Cardiovascular Medicine), Yale University School of Medicine, New Haven, CT.

Coronary allograft vasculopathy (CAV) is a devastating sequelae of heart transplant in which arterial intimal thickening limits coronary blood flow. There are currently no targeted therapies to prevent or reduce this pathology that leads to transplant failure. Vascular smooth muscle cell (VSMC) phenotypic plasticity is critical in CAV neointima formation. Read More

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Evidences for the mechanism of Shenmai injection antagonizing doxorubicin-induced cardiotoxicity.

Phytomedicine 2021 May 21;88:153597. Epub 2021 May 21.

Hangzhou Medical college, Hangzhou, China. Electronic address:

Background: Doxorubicin (DOX) is a widely used antitumor drug. However, its clinical application is limited for its serious cardiotoxicity. The mechanism of DOX-induced cardiotoxicity is attributed to the increasing of cell stress in cardiomyocytes, then following autophagic and apoptotic responses. Read More

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Complement System in Alcohol-Associated Liver Disease.

Immunol Lett 2021 Jun 7. Epub 2021 Jun 7.

Institute of Biomedical Sciences, University of São Paulo, Brazil.

Innate immunity contributes effectively to the development of Alcohol-Associated Liver Disease (ALD). Particularly, human studies and murine models of ALD have shown that Complement activation plays an important role during the initial and later stages of ALD. The Complement System may contribute to the pathogenesis of this disease since it has been shown that ethanol-derived metabolic products activate the Complement cascade on liver membranes, leading to hepatocellular damage. Read More

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Immunomodulatory and cytotoxic activities of euphol.

Life Sci 2021 Jun 7:119700. Epub 2021 Jun 7.

Laboratory of Phytotherapy, Phytotherapy Technology and Chemistry of Natural Products, State University of Ponta Grossa, Ponta Grossa, Brazil.

Aims: This study evaluated the effect of euphol isolated from Euphorbia umbellata (Pax) Bruyns latex on the activation of complement pathways (classical (CP), alternative (AP) and lectin (LP)), neutrophil chemotaxis, cytotoxic activity, cell morphology and death in HRT-18 and 3T3 cells lines.

Main Methods: CP and AP were assessed using hemolytic assays and ELISA for LP; neutrophil chemotaxis was performed using Boyden's chamber; cytotoxicity was evaluated by neutral red methodology and characteristics of cell death were assessed by cell morphology with hematological staining.

Key Findings: Although euphol increased CP activation (38% at a concentration of 976. Read More

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Elucidation of Rutin role in inducing caspase dependent apoptosis via HPV-E6 and E7 downregulation in cervical cancer HeLa cells.

Biosci Rep 2021 Jun 10. Epub 2021 Jun 10.

Lucknow University, Lucknow, India.

Over the recent few years rutin has gained wider attention in exhibiting inhibitory potential against several oncotargets for inducing apoptotic and antiproliferative activity in several human cancer cells. Several deregulated signaling pathways are implicated in cancer pathogenesis. Therefore we have inclined our research towards exploring the anticancerous efficacy of a very potent phytocompound for modulating the incontinent expression of these two crucial E6 and E7 oncogenes. Read More

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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

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Modulation of DNA damage response by targeting ATM kinase using newly synthesized di-phenoxy acetamide (DPA) analogs to induce anti-neoplasia.

Pharmacol Rep 2021 Jun 9. Epub 2021 Jun 9.

Molecular Biomedicine Laboratory, Postgraduate Department of Studies and Research in Biotechnology, Sahyadri Science College, Kuvempu University, Shivamogga, Karnataka, India.

Background: Imbalance and instability in the structure of the DNA have become major characteristics of cancer. In response to DNA damage, DNA damage response (DDR) protein, ataxia telangiectasia mutated (ATM), plays a pivotal role in the modulation of regulatory regions responsible for inhibition of apoptosis, thereby neoplastic progression.

Methods: A new series of DPA (7a-t) were synthesized, characterized. Read More

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Tanshinones induce tumor cell apoptosis via directly targeting FHIT.

Sci Rep 2021 Jun 9;11(1):12217. Epub 2021 Jun 9.

Center for Chemical Biology, Institute of Interdisciplinary Integrative Medicine Research, Shanghai University of Traditional Chinese Medicine, Shanghai, China.

The liposoluble tanshinones are bioactive components in Salvia miltiorrhiza and are widely investigated as anti-cancer agents, while the molecular mechanism is to be clarified. In the present study, we identified that the human fragile histidine triad (FHIT) protein is a direct binding protein of sodium tanshinone IIA sulfonate (STS), a water-soluble derivative of Tanshinone IIA (TSA), with a Kd value of 268.4 ± 42. Read More

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Methoxy and bromo scans on -(5-methoxyphenyl) methoxybenzenesulphonamides reveal potent cytotoxic compounds, especially against the human breast adenocarcinoma MCF7 cell line.

J Enzyme Inhib Med Chem 2021 Dec;36(1):1029-1047

Laboratorio de Química Orgánica y Farmacéutica, Departamento de Ciencias Farmacéuticas, Facultad de Farmacia, Universidad de Salamanca, Salamanca, Spain.

Thirty seven -(5-methoxyphenyl)-4-methoxybenzenesulphonamide with methoxy or/and bromo substitutions (series 1-4) and with different substituents on the sulphonamide nitrogen have been synthesised. 21 showed sub-micromolar cytotoxicity against HeLa and HT-29 human tumour cell lines, and were particularly effective against MCF7. The most potent series has 2,5-dimethoxyanilines, especially the 4-brominated compounds -. Read More

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December 2021

[Effectiveness of TRB3 on human hepatocellular carcinoma cells proliferation, apoptosis and migration].

Zhonghua Gan Zang Bing Za Zhi 2021 May;29(5):439-445

Department of Hepatobiliary Surgery, Affiliated Min da Hospital of Hubei Institute for Nationalities, Enshi 445000, China.

To explore the regulatory role and mechanism of tribbles pseudokinase 3 (TRB3) on hepatocarcinoma (HCC) cells proliferation, apoptosis and migration. Immunohistochemistry and Western blot were used to detect TRB3 expression in cancerous and adjacent cancerous liver tissues of HCC patients. TRB3 expression was detected in vitro in HepG2 and Huh7 hepatocarcinoma cell lines. Read More

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Resveratrol activates PI3K/AKT to reduce myocardial cell apoptosis and mitochondrial oxidative damage caused by myocardial ischemia/reperfusion injury.

Acta Histochem 2021 Jun 6;123(5):151739. Epub 2021 Jun 6.

Department of Cardiovascular Surgery, The First Affiliated Hospital of Nanjing Medical University, Nanjing, 210029, China. Electronic address:

Resveratrol is a kind of iPolyphenols widely existing in herbal medicine. Here we aim to investigate whether resveratrol can reduce the degree of myocardial ischemia/reperfusion (IR) injury and inhibit the development of oxidative stress, and elucidate the molecular mechanism of resveratrol in protecting myocardial cells. The primary rat cardiomyocytes were used to establish an ischemia/reperfusion model in vitro, and a series of routine biochemical experiments were conducted to explore the antioxidant and anti-apoptotic effects of resveratrol in myocardial ischemia-reperfusion injury. Read More

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Formulated Chinese medicine Shaoyao Gancao Tang reduces NLRP1 and NLRP3 in Alzheimer's disease cell and mouse models for neuroprotection and cognitive improvement.

Aging (Albany NY) 2021 Jun 9;13. Epub 2021 Jun 9.

Department of Life Science, National Taiwan Normal University, Taipei 11677, Taiwan.

Amyloid β (Aβ) plays a major role in the neurodegeneration of Alzheimer's disease (AD). The accumulation of misfolded Aβ causes oxidative stress and inflammatory damage leading to apoptotic cell death. Traditional Chinese herbal medicine (CHM) has been widely used in treating neurodegenerative diseases by reducing oxidative stress and neuroinflammation. Read More

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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

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Transglutaminase 2 promotes tumorigenicity of colon cancer cells by inactivation of the tumor suppressor p53.

Oncogene 2021 Jun 8. Epub 2021 Jun 8.

Goethe University Hospital Frankfurt, Department of Medicine, Hematology/Oncology, Frankfurt am Main, Germany.

Despite a high clinical need for the treatment of colorectal carcinoma (CRC) as the second leading cause of cancer-related deaths, targeted therapies are still limited. The multifunctional enzyme Transglutaminase 2 (TGM2), which harbors transamidation and GTPase activity, has been implicated in the development and progression of different types of human cancers. However, the mechanism and role of TGM2 in colorectal cancer are poorly understood. Read More

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Detecting retinal cell stress and apoptosis with DARC: Progression from lab to clinic.

Prog Retin Eye Res 2021 Jun 5:100976. Epub 2021 Jun 5.

Western Eye Hospital Imperial College Healthcare NHS Trust, London, UK; ICORG, Imperial College, London, UK.

DARC (Detection of Apoptosing Retinal Cells) is a retinal imaging technology that has been developed within the last 2 decades from basic laboratory science to Phase 2 clinical trials. It uses ANX776 (fluorescently labelled Annexin A5) to identify stressed and apoptotic cells in the living eye. During its development, DARC has undergone biochemistry optimisation, scale-up and GMP manufacture and extensive preclinical evaluation. Read More

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Targeting the SHP2 phosphatase promotes vascular damage and inhibition of tumor growth.

EMBO Mol Med 2021 Jun 8:e14089. Epub 2021 Jun 8.

Laboratory of Cellular Oncology, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, MD, USA.

The tyrosine phosphatase SHP2 is oncogenic in cancers driven by receptor-tyrosine-kinases, and SHP2 inhibition reduces tumor growth. Here, we report that SHP2 is an essential promoter of endothelial cell survival and growth in the remodeling tumor vasculature. Using genetic and chemical approaches to inhibit SHP2 activity in endothelial cells, we show that SHP2 inhibits pro-apoptotic STAT3 and stimulates proliferative ERK1/2 signaling. Read More

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alpha-Tocopherol supplementation reduces inflammation and apoptosis in high cholesterol mediated nonalcoholic steatohepatitis.

Biofactors 2021 Jun 8. Epub 2021 Jun 8.

Department of Biochemistry, Faculty of Medicine, Genetic and Metabolic Diseases Research and Investigation Center (GEMHAM), Marmara University, Istanbul, Turkey.

Inflammation and apoptosis signaling are crucial steps in the progression from nonalcoholic fatty liver disease (NAFLD) to nonalcoholic steatohepatitis (NASH). Alpha-tocopherol, the most active form of vitamin E, is an important modulator of signaling mechanisms, but its involvement to cholesterol-induced NASH pathogenesis remains poorly defined. Herein we have reported a novel effect of α-tocopherol in the transition from hepatic steatosis to NASH. Read More

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Quantitative spectrofluorometric assay detecting nuclear condensation and fragmentation in intact cells.

Sci Rep 2021 Jun 7;11(1):11921. Epub 2021 Jun 7.

Department of Biological and Biochemical Sciences, Faculty of Chemical Technology, University of Pardubice, Studentska 573, 532 10, Pardubice, Czech Republic.

At present, nuclear condensation and fragmentation have been estimated also using Hoechst probes in fluorescence microscopy and flow cytometry. However, none of the methods used the Hoechst probes for quantitative spectrofluorometric assessment. Therefore, the aim of the present study was to develop a spectrofluorometric assay for detection of nuclear condensation and fragmentation in the intact cells. Read More

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Effect of supplementation of medium with Bauhinia forficata recombinant lectins on expression of oxidative stress genes during in vitro maturation of bovine oocytes.

Reprod Toxicol 2021 Jun 7;103:64-70. Epub 2021 Jun 7.

Programa de Pós-Graduação em Biotecnologia (PPGB), Grupo de Pesquisa em Oncologia Celular e Molecular, Laboratório de Biotecnologia do Câncer, Centro de Desenvolvimento Tecnológico, Universidade Federal de Pelotas, Pelotas, 96010-610, RS, Brazil. Electronic address:

The lectin of Bauhinia forficata (nBfL) is a protein able to bind reversibly to N-acetylgalactosamine, performing several functions and one of them is the antiproliferative activity in tumor cells, but its effects have not yet been evaluated in female gametes. The objective of the present study was to determine the additional effect of B. forficata recombinants lectins in the medium of maturation in vitro of bovine oocytes in expression of genes related to oxidative stress pathways. Read More

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Induction of monoamine oxidase A-mediated oxidative stress and impairment of NRF2-antioxidant defence response by polyphenol-rich fraction of Bergenia ligulata sensitizes prostate cancer cells in vitro and in vivo.

Free Radic Biol Med 2021 Jun 4. Epub 2021 Jun 4.

Division of Molecular Medicine, Bose Institute, Kolkata, India. Electronic address:

Prostate cancer (PCa) is a major cause of mortality and morbidity in men. Available therapies yield limited outcome. We explored anti-PCa activity in a polyphenol-rich fraction of Bergenia ligulata (PFBL), a plant used in Indian traditional and folk medicine for its anti-inflammatory and antineoplastic properties. Read More

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Curcumin loaded chitosan-protamine nanoparticles revealed antitumor activity via suppression of NF-κB, proinflammatory cytokines and Bcl-2 gene expression in the breast cancer cells.

J Pharm Sci 2021 Jun 4. Epub 2021 Jun 4.

Department of Pharmaceutical Biotechnology, College of Biotechnology, Misr University for Science and Technology P. O. Box 77, Giza, Egypt.

Nano drug delivery has been recently used to enhance the stability and bioavailability of chemotherapeutic agents. In this study, Chitosan/protamine nanocarrier was synthesized and used to encapsulate curcumin (CUR). The physicochemical properties of the empty carrier (CHPNPs) and curcumin-containing carrier (CU-CHPNPs) were characterized by TEM imaging, Zetasizer, and FT-IR spectroscopy. Read More

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4-thiazolidinone-based derivatives do not affect differentiation of mouse embryo fibroblasts (3T3-L1 cell line) into adipocytes.

Chem Biol Interact 2021 Jun 4:109538. Epub 2021 Jun 4.

Department of Lifestyle Disorders and Regenerative Medicine, Medical College, University of Information Technology and Management in Rzeszow, Sucharskiego 2, 35-225 Rzeszow, Poland.

Nowadays, diabetes mellitus type 2 (T2DM) is a serious problem in western European societies and in the United States. Thiazolidinediones (TZDs) are a broad group of compounds used to decrease insulin resistance in TDM2. To date, it has been believed that TZDs act mainly through activation of peroxisome proliferator-activated receptor gamma (PPARγ). Read More

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Peptide-based delivery vectors with pre-defined geometrical locks.

RSC Med Chem 2020 Nov 13;11(11):1303-1313. Epub 2020 Aug 13.

Department of Biosciences and Bioengineering, Indian Institute of Technology Guwahati Guwahati-781039 Assam India

Design of peptide-based targeted delivery vectors with attributes of specificity and selective cellular targeting by fixing their topology and resulting electrostatic fingerprint is the objective of this study. We formulated our peptide design platform by utilizing the possibilities of side-chain induced geometric restrictions in a typical peptide molecule. Conceptually, we locked the conformation of the RGD/NGR motif of tumor homing peptides (THPs) by mutating glycine in these motifs with d-proline and tailed the peptides with a syndiotactic amphipathic segment for cellular penetration. Read More

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November 2020

Pharmacological Mechanisms Underlying the Therapeutic Effects of Danhong Injection on Cerebral Ischemia.

Evid Based Complement Alternat Med 2021 21;2021:5584809. Epub 2021 May 21.

Institute of Basic Research in Clinical Medicine, China Academy of Chinese Medical Sciences, Beijing 100700, China.

Background: Although Danhong injection (DHI) has been proved to be curative, the mechanism of its action against ischemia stroke (IS) is not clear. Here, we explored the therapeutic basis of DHI by network pharmacology.

Methods: Putative targets and activity scores for each compound in DHI were obtained from the Traditional Chinese Medicine System Pharmacology Database, Encyclopedia of Traditional Chinese Medicine, and Quantitative Structure Activity Relationships. Read More

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