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| 1 | Phosphomonoester Phosphoethanolamine Induces Apoptosis in Human Chronic Myeloid Leukemia Cells显示文摘Background:Leukemia is a type of cancer that starts in the blood or blood-forming tissues.It results from the clonal proliferation of hematopoietic cells in the bone marrow and/or lymphoid tissues,which subsequently reach the peripheral circulation and can infiltrate other systems.There are many different kinds of leukemia,and treatments are different for each one.Chronic leukemia is with a slower growing than acute leukemia but could be just as life-threatening.Phospholipids are antitumor analogs,such as synthetic phosphoethanolamine,which is a phosphorylated compound capable of controlling cellular proliferation and inducing apoptosis in several types of tumor cells.Methods:K562 and K562-Lucena(MDR+)human chronic myeloid leukemia cells were treated with synthetic phosphoethanolamine(Pho-s).The viability was evaluated by sulforhodamine B(SRB)assay and cell cycle phases,apoptosis,markers expression,and mitochondrial potential were assessed by flow cytometry.Results:Tumor cells formed clusters in suspension and decreased significantly viability.The concentrations for IC50%were obtained.Pho-s treated were 43.1 mM(K562)and 145.9 mM(K562-Lucena MDR+)in a period of 24 hours.Pho-s induced changes in the distribution of cell population phases of cell cycle which showed an increase in fragmented DNA and increased markers expression envolved apoptosis pathways a decrease in the G1/G0 phase.Discussion:Treatment of K562 and K562-Lucena(MDR+)chronic myeloid leukemia cells with Pho-s showed dose and time dependent cytotoxic effects.This cytotoxicity induced a decrease in proliferative capacity,mitochondrial electrical potential,and consequently release of cytochrome C;inhibition of Bcl-2 family protein expression,increase in pro-apoptotic family members Bad and Bax,dependent on p53 expression.Conclusion:This study presented a significant therapeutic potential of Phos-s in this type of leukemia through the apoptotic effects on tumor cells independently of the molecular resistance profile(MDR+). | Thais de Oliveira Conceicao Manuela Garcia Laveli da Silva Durvanei Augusto Maria | 2019 | Journal of Pharmacy and Pharmacology2019，7，7： | 3 |
| 2 | Meclizine Chloridrate and Methyl-β-Cyclodextrin Associated with Monophosphoester Synthetic Phosphoethanolamine Modulating Proliferative Potential in Triple-Negative Breast Cancer Cells显示文摘Synthetic phosphoethanolamine(Pho-s)is a monophosphoester ester with anti-inflammatory and pro-apoptotic properties.Meclizine chloridrate(MC)is a histamine H1 receptor blocker that is also able to inhibit cellular respiration.However,MC does not inhibit cellular respiration in isolated mitochondria such as antimycin and rotenone.Methyl-β-cyclodextrin(MβCD)belongs to theβ-cyclodextrin family,which is capable of removing cholesterol from the plasma membrane.The aim of this study was to evaluate the proliferative effects of meclizine chloridrate and methyl-β-cyclodextrin compounds associated with synthetic phosphoethanolamine in a triple-negative human breast tumor line,MDA-MB-231 Cell viability of the tumor line and normal cells FN1 was evaluated by MTT colorimetric test;the production of free radicals was determined by lipoperoxidation(LPO)test;and the percentage of cell cycle phases and proliferative index was evaluated by flow cytometry.Cell viability demonstrated a significant decrease with the treatments of MβCD,MC and Pho-s associated with MC.The production of free radicals decreases significantly in all treatments.In addition,a significant increase of DNA fragment and decrease in G0/G1 cell cycle phase were observed in cellular percentage with concentrations of 20 and 30 mM of Pho-s in association with MC and MβCD,respectively. | Manuela Garcia Laveli da Silva Luciana Bastianelli Knop Durvanei Augusto Maria | 2019 | Journal of Pharmacy and Pharmacology2019，7，7： | 2 |
| 3 | 2-aminoethyl Dihydrogen Phosphate as a Modulator of Proliferative and Apoptotic Effects in Breast Cancer Cell Lines显示文摘Background: Breast cancer is a type of cancer that affects more women throughout the world, in developing anddeveloped countries. 2-AEH2P is a phospholipid analog of cellular membrane, which makes it different from existing molecules fortheir absorption, stability and display anti-inflammatory, anti-proliferative and pro-apoptotic properties. Methods: MCF-7 humanbreast adenocarcinoma cells were treated with 2-AEH2P. The viability and adhesion cells were evaluated by MTT assay. Cell cyclephases, apoptosis, markers and mitochondrial potential were assessed by flow cytometry. Morphological ultrastructural analyzeswere performed by laser confocal microscopy. Results: MCF-7 Tumor cells acquired round shapes, lost cytoplasmic expansions,formed clusters in suspension and decreased significantly viability. There were changes in the morphology, membrane fragmentationand loss of cytoplasmic projection. The obtained concentrations for IC50% were 37.2;25.8;1.8 mM for periods of 24, 48 and 72 h,respectively. Changes in the distribution of cell population phases of the cell cycle showed an increase in fragmented DNA and anincrease in the G2/M phase. The expression β-gal showed proliferative reduction induced by 2-AEH2P. Laser confocal microscopyshowed changes in the mitochondrial membrane and alteration in distribution. Proliferative index of MCF-7 tumor cells treated with2-AEH2P decreased significantly when compared to fibroblast normal cells. The compound 2-AEH2P is a phospholipid withantiproliferative potential and apoptosis modulator. | Manuela Garcia Laveli da Silva Laertty Garcia de Sousa Cabral Monique Gonçalves Alves Thais deOliveira Conceição Henrique Hesse Rosa Andrea Nogueira Laiso Daniel da Conceição Rabelo Durvanei Augusto Maria | 2021 | Journal of Pharmacy and Pharmacology2021，9，3： | 1 |
| 4 | Bcl-2 family proteins and cytoskeleton changes involved in DM-1 cytotoxic effect on melanoma cells显示文摘 | Fernanda Fai?o-Flores José Agustín Quincoces Suarez Vanessa Soto-Cerrato Margarita Espona-Fiedler Ricardo Pérez-Tomás Durvanei Augusto Maria | 2013 | Tumor Biology2013，，2： | 1 |
| 5 | Clinical Oncology Translational Study Phase-1 with Antitumor Phosphorylethanolamine(2-AEH_(2)P)in Dogs with Neoplasms显示文摘The animal has the potential to serve as a clinical model for human disease,due to striking similarities and homologies in diseases.Early clinical development of a new drug may influence its final destination,and a careful and thoughtful approach to Phase-1 clinical trials is essential.Phosphorylethanolamine(2-AEH2P)is a new cytostatic phospholipid agent that,unlike most chemotherapeutic drugs used today,does not target DNA or cytoskeleton,but act on the cell membrane.Studies carried out by our group have shown several effects of 2-AEH2P controlling the progression of the cell cycle,in the alterations of the mitochondrial electrical potential capable of inducing apoptosis and autophagy in several types of human and animal tumor cells.The aim of this study is to establish the recommended safety dose of a 2-AEH2P monophosphoester,in dogs with tumor following the Phase 1 study model proposed by Fibonacci.The Phase-1 study following the Fibonacci model,2-AEH2P was safe at all staggered doses up to 150 mg/Kg for 8 weeks.Intravenous administration in staggered doses according to the Fibonacci model,showed that the drug is safe,no advent of mortality during the study period or acute toxicity were observed.It is not a drug with hemolytic properties or that induces anemia.It does not lead to changes in liver and renal functions and was able to modulate leukocyte production.2-AEH2P is new compound with antitumor potential,being useful for future veterinary and human tumors,as a combination of chemotherapeutic agents. | Olivia Gonçalves de Almeida Leitão da Cunha Lucas Campos de SáRodrigues Daniel da Conceição Rabelo Rosa Andrea Nogueira Laiso Sergio Mestieri Chammas Laertty Garcia de Sousa Cabral Durvanei Augusto Maria | 2021 | Journal of Pharmacy and Pharmacology2021，9，5： | 0 |
| 6 | The Antiproliferative and Pro-apoptotic Role of 2-aminoethyl dihydrogen Phosphate in Triple-negative Breast Tumor Cells显示文摘Antineoplastic phospholipids are a new class of antitumor agents.These molecules interact with the plasma membrane,changing numerous pathways that induce cell death,with high selectivity for cancer cells.A representative of this class of antineoplastic agents is 2-aminoethyl dihydrogen phosphate(2-AEH2P).It is present in high intracellular concentrations in various tissues and organelles with antitumor,antiproliferative and pro-apoptotic action.Therefore,4T1 triple-negative tumor cells were treated in different concentrations in order to assess the cytotoxic potential and its effects on the modulation of cell death pathways in association with the chemotherapeutic drug Paclitaxel.2-AEH2P promoted cytotoxicity in tumor cells and significant morphological changes,however,it did not cause these effects in normal cells.There was positive regulation of proteins involved in the intrinsic pathway of cell death by apoptosis and regulation of the phases of cell cycle progression.Furthermore,structural and distribution changes in mitochondria,as well as decreased cell density and regression of the cytoskeleton were observed.The 2-AEH2P demonstrated a modulatory potential of apoptotic pathways inducing cell death,being a new compound with antitumor properties. | Antenor Pereira Bonfim Neto Laertty Garcia de Sousa Cabral Thalles Anthony Duarte Oliveira JulioCarlstron Pacheco Monique Gonçalves Alves Mercedes Reyes Hernández Rosa Andreia Nogueira Laiso Durvanei Augusto Maria | 2021 | Journal of Pharmacy and Pharmacology2021，9，4： | 0 |
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