24,796 results match your criteria induction apoptotic


Novel Benzyloxyphenyl Pyrimidine-5-Carbonitrile Derivatives as Potential Apoptotic Antiproliferative Agents.

Anticancer Agents Med Chem 2021 Jun 11. Epub 2021 Jun 11.

Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig, 44519. Egypt.

Background: Pyrimidine-5-carbonitrile had a broad spectrum of biological activities such as antiviral, antioxidant and anticancer activity. Among similar compounds, monastrol being the most prominent due to cell-permeant inhibitor of mitosis therefore, we investigated the new Pyrimidine-5-carbonitrile as a cytotoxic agent for p53 pathway.

Objective: Several new benzyloxyphenyl pyrimidine-5-carbonitrile derivatives were designed, synthesized, characterized, and their cytotoxicity was evaluated. Read More

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DNA binding ability and cytotoxicity, cell cycle arrest and apoptosis inducing properties of a benzochromene derivative against K562 human leukemia cells.

Nucleosides Nucleotides Nucleic Acids 2021 Jun 15:1-22. Epub 2021 Jun 15.

Department of Biology, Faculty of Natural Sciences, University of Tabriz, Tabriz, Iran.

Chromene and its derivatives are generally spread in nature. Heterocylic-based compounds like chromenes have displayed pharmacological activities. Chromene derivatives are critical due to some biological features such as anticancer activity. Read More

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From triazolophthalazines to triazoloquinazolines: A bioisosterism-guided approach toward the identification of novel PCAF inhibitors with potential anticancer activity.

Bioorg Med Chem 2021 Jun 5;42:116266. Epub 2021 Jun 5.

Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy (Boys), Al-Azhar University, Nasr City 11884, Cairo, Egypt; Pharmaceutical Chemistry Department, Faculty of Pharmacy, Horus University - Egypt, International Coastal Road, 34518 New Damietta, Egypt. Electronic address:

Inhibition of PCAF bromodomain has been validated as a promising strategy for the treatment of cancer. In this study, we report the bioisosteric modification of the first reported potent PCAF bromodomain inhibitor, L-45 to its triazoloquinazoline bioisosteres. Accordingly, three new series of triazoloquinazoline derivatives were designed, synthesized, and assessed for their anticancer activity against a panel of four human cancer cells. Read More

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Natural Phytochemicals as Novel Therapeutic Strategies to Prevent and Treat Parkinson's Disease: Current Knowledge and Future Perspectives.

Oxid Med Cell Longev 2021 25;2021:6680935. Epub 2021 May 25.

Department of Applied Life Science, Graduate School, BK21 Program, Konkuk University, Chungju 27478, Republic of Korea.

Parkinson's disease (PD) is the second-most common neurodegenerative chronic disease affecting both cognitive performance and motor functions in aged people. Yet despite the prevalence of this disease, the current therapeutic options for the management of PD can only alleviate motor symptoms. Research has explored novel substances for naturally derived antioxidant phytochemicals with potential therapeutic benefits for PD patients through their neuroprotective mechanism, targeting oxidative stress, neuroinflammation, abnormal protein accumulation, mitochondrial dysfunction, endoplasmic reticulum stress, neurotrophic factor deficit, and apoptosis. Read More

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Doxorubicin/Nucleophosmin Binding Protein-Conjugated Nanoparticle Enhances Anti-leukemia Activity in Acute Lymphoblastic Leukemia Cells and .

Front Pharmacol 2021 28;12:607755. Epub 2021 May 28.

Department of Hematology, Fujian Institute of Hematology, Fujian Provincial Key Laboratory of Hematology, Fujian Medical University Union Hospital, Fuzhou, China.

Acute lymphoblastic leukemia (ALL) is an aggressive malignancy. Adults with ALL have more than 50% relapse rates. We have previously validated that overexpression of nucleophosmin (NPM) is involved in the multidrug resistance (MDR) development during ALL; and a synthetically engineered recombinant NPM binding protein (NPMBP) has been developed in our group; NPMBP and doxorubicin (DOX) can be conjugated in a nanoparticle-based drug delivery system named DOX-PMs-NPMBP to counteract MDR during ALL. Read More

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Extracts Exert Anti-Breast-Cancer Bioactivity through the Apoptosis Induction Dependent on Mitochondrial Reactive Oxygen Species and Caspase Activation.

Nutr Cancer 2021 Jun 12:1-13. Epub 2021 Jun 12.

School of Food and Biological Engineering, Engineering Research Center of Bio-process, Ministry of Education, Hefei University of Technology, Hefei, Anhui, China.

Puffballs are a class of fungi widely distributed worldwide and associated with various bioactivities. This research mainly showed the antitumor bioactivity of extracts from (CL), which is a common variety of puffballs. NMR and high-performance liquid chromatography methods are used to characterize the extracts. Read More

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Tea tree oil extract causes mitochondrial superoxide production and apoptosis as an anticancer agent, promoting tumor infiltrating neutrophils cytotoxic for breast cancer to induce tumor regression.

Biomed Pharmacother 2021 Jun 11;140:111790. Epub 2021 Jun 11.

School of Pharmacy and Medical Science, Menzies Health Institute of Queensland, Griffith University, Gold Coast Campus, Southport, Queensland 4222, Australia. Electronic address:

The antitumor activity of the tea tree oil (TTO) derived product, Melaleuca Alternifolia Concentrate (MAC) was characterized mechanistically at the molecular and cellular level. MAC was analyzed for its anticancer activity against human prostate (LNCaP) and breast (MCF-7) cancer cell lines growing in vitro. MAC (0. Read More

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Design, synthesis and evaluation of new quinazolin-4-one derivatives as apoptotic enhancers and autophagy inhibitors with potent antitumor activity.

Eur J Med Chem 2021 Jun 5;222:113609. Epub 2021 Jun 5.

Drug Design and Discovery Lab, Zewail City of Science and Technology, Giza, 12578, Egypt; Biomedical Sciences Program, University of Science and Technology, Zewail City of Science and Technology, Giza, 12578, Egypt. Electronic address:

This work presents the design and synthesis of a series of new quinazolin-4-one derivatives, based on the established effectiveness of quinazoline-based small molecules as anticancer agents. Synthesized compounds were more potent against MCF-7 than A-549 with low to submicromolar ICs. Compound 17 exhibited the best IC being equipotent with the positive control doxorubicin (IC 0. Read More

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Unfolding the Apoptotic Mechanism of Antioxidant Enriched-Leaves of Tabebuia pallida (Lindl.) Miers in EAC Cells and Mouse Model.

J Ethnopharmacol 2021 Jun 9:114297. Epub 2021 Jun 9.

Department of Pharmacy, University of Rajshahi, Rajshahi-6205, Bangladesh. Electronic address:

Ethnopharmacological Relevance: Tabebuia pallida (Lindl.) Miers (T. pallida) is a well-known native Caribbean medicinal plant. Read More

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Electrospun meshes intrinsically promote M2 polarization of microglia under hypoxia and offer protection from hypoxia-driven cell death.

Biomed Mater 2021 Jun 11. Epub 2021 Jun 11.

Department of Chemical Engineering, Indian Institute of Technology Hyderabad, IITH Main Road, Near NH 65, Kandi, Sangareddy, Hyderabad, Telanagana, Hyderabad, 502205, INDIA.

In this study, we offer new insights into the contrasting effects of electrospun fiber orientation on microglial polarization under normoxia and hypoxia and establish for the first time, the intrinsically protective roles of electrospun meshes against hypoxia-induced microglial responses. First, resting microglia were cultured under normoxia on poly(caprolactone) (PCL) fibers possessing two distinctly different fiber orientations. Matrix-guided differences in cell shape/orientation and differentially expressed Rho GTPases (RhoA, Rac1, Cdc42) were well-correlated with the randomly oriented fibers inducing a predominantly pro-inflammatory phenotype and the aligned fibers sustaining a resting phenotype. 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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Transcriptional Changes in CD16+ Monocytes May Contribute to the Pathogenesis of COVID-19.

Front Immunol 2021 24;12:665773. Epub 2021 May 24.

Department of Pathology, Albert Einstein College of Medicine, Bronx, NY, United States.

The COVID-19 pandemic has caused more than three million deaths globally. The severity of the disease is characterized, in part, by a dysregulated immune response. CD16+ monocytes are innate immune cells involved in inflammatory responses to viral infections, and tissue repair, among other functions. Read More

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A glutathione-responsive polyphenol - Constructed nanodevice for double roles in apoptosis and ferroptosis.

Colloids Surf B Biointerfaces 2021 Jun 4;205:111902. Epub 2021 Jun 4.

Key Laboratory of Biomedical Polymers of Ministry of Education, College of Chemistry and Molecular Science, Wuhan University, Wuhan, 430072, PR China. Electronic address:

Combination chemotherapy regimens have been put forward to achieve a synergistic effect and reduce drug doses for the clinical applications of cancer treatment. One of the principal approaches for killing cancer cells involves triggering apoptotic cell death with anti-cancer drugs. Nevertheless, the efficacy of apoptosis induction in tumors is often restricted on account of intrinsic or acquired resistance of cancer cells to apoptosis. 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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Hyperbaric oxygen suppressed tumor progression through the improvement of tumor hypoxia and induction of tumor apoptosis in A549-cell-transferred lung cancer.

Sci Rep 2021 Jun 8;11(1):12033. Epub 2021 Jun 8.

Department of Biochemistry, National Defense Medical Center, Taipei, Taiwan, ROC.

Tumor cells have long been recognized as a relative contraindication to hyperbaric oxygen treatment (HBOT) since HBOT might enhance progressive cancer growth. However, in an oxygen deficit condition, tumor cells are more progressive and can be metastatic. HBOT increasing in oxygen partial pressure may benefit tumor suppression. Read More

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Effect of the standard herbal preparation, STW5, treatment on dysbiosis induced by dextran sodium sulfate in experimental colitis.

BMC Complement Med Ther 2021 Jun 8;21(1):168. Epub 2021 Jun 8.

Department of Pharmacology and Toxicology, Faculty of Pharmacy, Cairo University, Kasr El-Aini Street, Cairo, 11562, Egypt.

Background: The standardized herbal preparation, STW 5, is effective clinically in functional gastrointestinal disorders and experimentally in ulcerative colitis (UC). The present study explores whether the beneficial effect of STW 5 involves influencing the intestinal microbiota.

Methods: UC was induced in Wistar rats by feeding them 5% dextran sodium sulfate (DSS) in drinking water for 7 days. 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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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 5;172:136-151. Epub 2021 Jun 5.

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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Effects of morphine and NeuroAid on the expression levels of GluN2A and GluN3A in the hippocampus and striatum of rats.

Iran J Basic Med Sci 2021 Apr;24(4):469-475

Cognitive and Neuroscience Research Center (CNRC), Amir-Almomenin Hospital, Tehran Medical Sciences, Islamic Azad University, Tehran, Iran.

Objectives: NMDA glutamatergic receptors are heteromeric receptors with various subunits. GluN2A and GluN3A subunits specify the functional heterogeneity of NMDA receptors. These subunits play a key role in the induction of LTP and synaptic plasticity. Read More

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Alternative approaches to overcome chemoresistance to apoptosis in cancer.

Adv Protein Chem Struct Biol 2021 9;126:91-122. Epub 2021 Mar 9.

Department of Cancer Biology, College of Medicine and Life Sciences, University of Toledo Health Science Campus, Toledo, OH, United States. Electronic address:

Apoptosis, or programmed cell death, is a form of regulated cell death (RCD) that is essential for organogenesis and homeostatic maintenance of normal cell populations. Apoptotic stimuli activate the intrinsic and/or extrinsic pathways to induce cell death due to perturbations in the intracellular and extracellular microenvironments, respectively. In patients with cancer, the induction of apoptosis by anticancer drugs and radiation can produce cancer cell death. Read More

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Bone marrow mesenchymal stem cells and their derived exosomes resolve doxorubicin-induced chemobrain: critical role of their miRNA cargo.

Stem Cell Res Ther 2021 Jun 5;12(1):322. Epub 2021 Jun 5.

Department of Biochemistry, Faculty of Pharmacy, Ain Shams University, Cairo, 11566, Egypt.

Background: Doxorubicin (DOX), a widely used chemotherapeutic agent, can cause neurodegeneration in the brain, which leads to a condition known as chemobrain. In fact, chemobrain is a deteriorating condition which adversely affects the lives of cancer survivors. This study aimed to examine the potential therapeutic effects of bone marrow mesenchymal stem cells (BMSCs) and their derived exosomes (BMSCs-Exo) in DOX-induced chemobrain in rat models. Read More

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A KMT2A-AFF1 gene regulatory network highlights the role of core transcription factors and reveals the regulatory logic of key downstream target genes.

Genome Res 2021 Jun 4. Epub 2021 Jun 4.

University of Oxford, MRC Weatherall Institute of Molecular Medicine

Regulatory interactions mediated by transcription factors (TFs) make up complex networks that control cellular behavior. Fully understanding these gene regulatory networks (GRNs) offers greater insight into the consequences of disease-causing perturbations than can be achieved by studying single TF binding events in isolation. Chromosomal translocations of the lysine methyltransferase 2A (KMT2A) produce KMT2A fusion proteins such as KMT2A-AFF1, causing poor prognosis acute lymphoblastic leukemias (ALLs) that sometimes relapse as acute myeloid leukemias (AMLs). Read More

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Molecular targets for the management of gastrointestinal cancer using melatonin, a natural endogenous body hormone.

Biomed Pharmacother 2021 Jun 1;140:111782. Epub 2021 Jun 1.

Noncommunicable Diseases Research Center, Neyshabur University of Medical Sciences, Neyshabur, Iran. Electronic address:

Gastrointestinal cancer is one of the most common cancers globally. Melatonin, a natural endogenous body hormone, has been of interest for years, due to its anti-cancer characteristics, such as antiproliferative, antimetastatic, and cytotoxic as well as apoptotic induction. Through regulating several proteins such as melatonin upregulated mRNAs and proteins of downregulated Bcl-2-associated X protein (Bax), and B-cell lymphoma 2 (Bcl-2), as well as cytoplasmic protein such as calcium-binding proteins calmodulin or tubulin, and nuclear receptors, including RORα/RZR, and acts by non-receptor-regulated mechanisms, melatonin can exert anti-cancer efficacy. Read More

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Psiadin and plectranthone selectively inhibit colorectal carcinoma cells proliferation via modulating cyclins signaling and apoptotic pathways.

PLoS One 2021 4;16(6):e0252820. Epub 2021 Jun 4.

Department of Microbiology and Immunology, Faculty of Medicine, Kuwait University, Safat, Kuwait.

Three scarce terpenes, psiadin, plectranthone and saudinolide, were obtained after chromatographic isolation and purification from the aerial parts of the respective plants. Their identities were established based on their spectral data. Their anticancer effects against two human colorectal carcinoma cell lines, CCL233 and CCL235, along with the potential molecular mechanisms of action, were explored. Read More

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Dichloromethane fraction of Moringa oleifera leaf methanolic extract selectively inhibits breast cancer cells (MCF7) by induction of apoptosis via upregulation of Bax, p53 and caspase 8 expressions.

Mol Biol Rep 2021 Jun 4. Epub 2021 Jun 4.

Advanced Medical and Dental Institute, Universiti Sains Malaysia, Bertam, 13200, Kepala Batas, Penang, Malaysia.

Moringa oleifera is a well-known medicinal plant which has anti-cancer and other biological activities. This research aims to determine the cytotoxic and apoptotic effect of M. oleifera leave extract on the breast cancer (MCF7) cells. Read More

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Apoptotic DNase network: Mutual induction and cooperation among apoptotic endonucleases.

J Cell Mol Med 2021 Jun 4. Epub 2021 Jun 4.

University of Arkansas for Medical Sciences, Little Rock, AR, USA.

DNA fragmentation produced by apoptotic DNases (endonucleases) leads to irreversible cell death. Although apoptotic DNases are simultaneously induced following toxic/oxidative cell injury and/or failed DNA repair, the study of DNases in apoptosis has generally been reductionist in approach, focusing on individual DNases rather than their possible cooperativity. Coordinated induction of DNases would require a mechanism of communication; however, mutual DNase induction or activation of DNases by enzymatic or non-enzymatic mechanisms is not currently recognized. Read More

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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

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Candidalysin triggers epithelial cellular stresses that induce necrotic death.

Cell Microbiol 2021 Jun 3:e13371. Epub 2021 Jun 3.

Centre for Host-Microbiome Interactions, Faculty of Dentistry, Oral & Craniofacial Sciences, King's College London, London, UK.

Candida albicans is a common opportunistic fungal pathogen that causes a wide range of infections from superficial mucosal to hematogenously disseminated candidiasis. The hyphal form plays an important role in the pathogenic process by invading epithelial cells and causing tissue damage. Notably, the secretion of the hyphal toxin candidalysin is essential for both epithelial cell damage and activation of mucosal immune responses. Read More

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Enhanced G1 arrest and apoptosis via MDM4/MDM2 double knockdown and MEK inhibition in wild-type colon and gastric cancer cells with aberrant KRAS signaling.

Oncol Lett 2021 Jul 25;22(1):558. Epub 2021 May 25.

Department of Gastroenterology, Institute of Clinical Medicine, Graduate School of Comprehensive Human Sciences, University of Tsukuba, Tsukuba, Ibaraki 305-8575, Japan.

Murine double minute homolog 2 (MDM2) is an oncoprotein that induces p53 degradation via ubiquitin-ligase activity. MDM4 cooperates with MDM2-mediated p53 degradation, directly inhibiting p53 transcription by binding to its transactivation domain. Our previous study reported that the simultaneous inhibition of MDM2 and MDM4 using nutlin-3 (an inhibitor of the MDM2-p53 interaction) and chimeric small interfering RNA with DNA-substituted seed arms (named chiMDM2 and chiMDM4) more potently activated p53 than the MDM2 or MDM4 inhibitor alone and synergistically augmented antitumor effects in various types of cancer cells with the wild-type (wt) . Read More

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The effects of Benjakul extract and its isolated compounds on cell cycle arrest and apoptosis in human non-small cell lung cancer cell line NCI-H226.

Res Pharm Sci 2021 Apr 5;16(2):129-140. Epub 2021 Mar 5.

Faculty of Pharmacy and Pharmaceutical Sciences, University of Alberta, Edmonton, Canada.

Background And Purpose: Benjakul, a traditional Thai formulation for cancer treatment, is composed of five plants. This study aimed to assess the cytotoxicity of Benjakul, its five plants, and its isolated compounds against non-small cell lung cancer (NSCLC) by the sulforhodamine B (SRB) assay.

Experimental Approach: Analyses of cell cycle and membrane asymmetry changes were performed with different fluorescent dyes and analyzed by flow cytometry in NCI-H226 cells. Read More

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