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  1. Article: Tyrame [N-(3-hydroxy-1:3:5(10)-estratrien-17β-yl)-4-hydroxy-phenethylamine], antithrombotic aminoestrogen that decreases microvesicle formation.

    Flores-García, Mirthala / Fernández-González, Juan M / León-Martínez, Mireille / Hernández-Ortega, Simón / Hernández-López, José R / Reyes-Munguía, Daniela / Sánchez-Sarabia, Hugo / Piña-Fragoso, Zeuz / Peña-Díaz, Aurora de la

    Gaceta medica de Mexico

    2022  Volume 157, Issue 6, Page(s) 588–593

    Abstract: Background: Estrogens that are used as contraceptives or in replacement therapy are associated with an increase in the risk for developing thrombosis, mainly during the first year of treatment and in women with associated risk factors.: Objective: To ...

    Title translation Tyrame [N-(3-hidroxi-1:3:5(10)-estratrien-17β-il)-4-hidroxi-fenetilamina], aminoestrógeno antitrombótico que disminuye la formación de microvesículas.
    Abstract Background: Estrogens that are used as contraceptives or in replacement therapy are associated with an increase in the risk for developing thrombosis, mainly during the first year of treatment and in women with associated risk factors.
    Objective: To synthesize, characterize and identify the anticoagulant, antiplatelet aggregation and microvesicle-reducing effect of the new aminoestrogen Tyrame.
    Material and methods: CD1 strain mice were used, which had Tyrame (0, 1 and 2 mg/100 g) subcutaneously administered. At 24 h, a blood sample was obtained to determine whole-blood clotting time, microvesicles concentration and inhibitory effect on platelet aggregation.
    Results: Blood clotting time increased up to 1.5 times in comparison with the control. Platelet aggregation inhibition had different magnitude depending on the agonist agent employed, and was complete with collagen. Both effects had a dose-dependent relationship. The microvesicles decreased up to six times with respect to the control.
    Conclusions: Tyrame reduces platelet aggregation and microvesicle formation, which emphasizes its potential therapeutic utility as an estrogen free of thrombotic effects.
    MeSH term(s) Animals ; Anticoagulants ; Fibrinolytic Agents/pharmacology ; Mice ; Phenethylamines/pharmacology ; Platelet Aggregation ; Thrombosis
    Chemical Substances Anticoagulants ; Fibrinolytic Agents ; Phenethylamines
    Language English
    Publishing date 2022-01-12
    Publishing country Mexico
    Document type Journal Article
    ZDB-ID 425456-9
    ISSN 0016-3813
    ISSN 0016-3813
    DOI 10.24875/GMM.M21000621
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Ua VI Zs.38: Show issues Location:
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  2. Article ; Online: Fibrinolytic Activity of Circulating Microvesicles Is Associated with Progression of Breast Cancer.

    Valente-Acosta, Benjamín / Flores-García, Mirthala / González-Zárate, Georgina / Gerson-Cwilich, Raquel / Maldonado-Méndez, Marai / Juárez-Vega, Guillermo / Anglés-Cano, Eduardo / Peña-Díaz, Aurora de la

    The Tohoku journal of experimental medicine

    2020  Volume 250, Issue 2, Page(s) 121–128

    Abstract: The fibrinolytic system plays an important role in breast cancer, favoring progression through extracellular-matrix degradation, angiogenesis, apoptosis and cellular proliferation. The expression of urokinase-type plasminogen activator (uPA) in breast ... ...

    Abstract The fibrinolytic system plays an important role in breast cancer, favoring progression through extracellular-matrix degradation, angiogenesis, apoptosis and cellular proliferation. The expression of urokinase-type plasminogen activator (uPA) in breast cancer tissue is widely recognized as an unfavorable prognostic factor. However, fibrinolytic activity associated with uPA cannot be reliably measured in the blood because of the rapid inhibition of uPA by plasminogen activator inhibitor-1 (PAI-1). By contrast, circulating microvesicles (Mvs) in peripheral blood protect bound enzymes from inhibition. Mvs are extracellular vesicles, released from various types of cells, and their size fluctuates between 100 and 1,000 nm. Mvs carry DNA, RNA, miRNA, and proteins, thereby serving as a source of horizontal communication between cells. We investigated whether fibrinolytic activity on circulating Mvs reflects breast cancer progression. The study population consisted of 13 patients with breast cancer and 13 healthy women. The cancer patients included 4 patients in remission, 3 patients with locally advanced cancer, and 6 with metastatic disease. Mvs were isolated from peripheral blood, quantified by a protein concentration method, and their fibrinolytic potential was measured by their capacity to generate plasmin. Although the quantity of Mvs found in patients with cancer and healthy individuals was similar, plasmin generated on Mvs was twice the amount in patients with metastasis than in healthy women (P < 0.05), underlying the value of this distinctive parameter. The data suggest that in breast cancer patients, higher fibrinolytic activity of circulating Mvs could be related to progression and metastasis of breast cancer.
    MeSH term(s) Adult ; Breast Neoplasms/drug therapy ; Breast Neoplasms/metabolism ; Breast Neoplasms/pathology ; Cell-Derived Microparticles/metabolism ; Disease Progression ; Female ; Fibrinolysin/metabolism ; Fibrinolysis ; Fluorescence ; Humans ; Middle Aged ; Urokinase-Type Plasminogen Activator/metabolism
    Chemical Substances Fibrinolysin (EC 3.4.21.7) ; Urokinase-Type Plasminogen Activator (EC 3.4.21.73)
    Language English
    Publishing date 2020-02-27
    Publishing country Japan
    Document type Journal Article
    ZDB-ID 123477-8
    ISSN 1349-3329 ; 0040-8727
    ISSN (online) 1349-3329
    ISSN 0040-8727
    DOI 10.1620/tjem.250.121
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article ; Online: The matrix metalloproteinase 2-1575 gene polymorphism is associated with the risk of developing myocardial infarction in Mexican patients.

    Pérez-Hernández, Nonanzit / Vargas-Alarcón, Gilberto / Martínez-Rodríguez, Nancy / Martínez-Ríos, Marco Antonio / Peña-Duque, Marco Antonio / Peña-Díaz, Aurora de la / Valente-Acosta, Benjamín / Posadas-Romero, Carlos / Medina, Aida / Rodríguez-Pérez, José Manuel

    Journal of atherosclerosis and thrombosis

    2012  Volume 19, Issue 8, Page(s) 718–727

    Abstract: Aim: Was to evaluate the role of seven matrix metalloproteinase (MMP) polymorphisms in the genetic susceptibility to develop myocardial infarction in Mexican individuals.: Methods: Seven polymorphisms in the MMP genes were genotyped by 5' exonuclease ...

    Abstract Aim: Was to evaluate the role of seven matrix metalloproteinase (MMP) polymorphisms in the genetic susceptibility to develop myocardial infarction in Mexican individuals.
    Methods: Seven polymorphisms in the MMP genes were genotyped by 5' exonuclease TaqMan genotyping assays in 300 patients with myocardial infarction and 300 healthy unrelated controls.
    Results: A similar distribution of MMP2-1306 (rs243865), MMP2-790 (rs243864), MMP2-735 (rs22850553), MMP7-153(rs11568819), MMP7-181(rs11568818), and MMP12-82(rs2276109) polymorphisms was observed in both studied groups. On the other hand, patients showed increased frequencies of MMP2-1575 A allele and AA genotype when compared to controls (pC= 0.001; OR= 1.58 and pC= 0.036; OR= 2.37, respectively). According to the dominant model, individuals with AG+AA genotypes had a 1.65-fold increased risk of developing the disease (p= 0.002). After adjusting for known risk factors, we found a significant contribution of gender, BMI, smoking habit, diabetes mellitus, and hypertension to the inheritance model. In this analysis, individuals with the-1575 AA genotype had a 4.23-fold increased risk of developing MI (p= 0.003). On the other hand, an association of the MMP12-82 polymorphism with the extent of coronary artery disease (CAD) was observed. In our study, it was possible to distinguish two risk haplotypes and one protective haplotype for this disease in the MMP2 gene.
    Conclusions: The results suggest that the MMP2-1575 (rs243866) gene polymorphism could be involved in the risk of developing myocardial infarction in Mexican individuals.
    MeSH term(s) Case-Control Studies ; Female ; Genetic Predisposition to Disease ; Genotype ; Haplotypes ; Humans ; Male ; Matrix Metalloproteinase 2/genetics ; Mexico/epidemiology ; Middle Aged ; Myocardial Infarction/epidemiology ; Myocardial Infarction/etiology ; Polymorphism, Single Nucleotide/genetics ; Prognosis ; Risk Factors
    Chemical Substances MMP2 protein, human (EC 3.4.24.24) ; Matrix Metalloproteinase 2 (EC 3.4.24.24)
    Language English
    Publishing date 2012-06-27
    Publishing country Japan
    Document type Comparative Study ; Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2011474-6
    ISSN 1880-3873 ; 1340-3478
    ISSN (online) 1880-3873
    ISSN 1340-3478
    DOI 10.5551/jat.11817
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Zs.A 5192: Show issues Location:
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  4. Article: The structures and inhibitory effects of Buame [N-(3-hydroxy-1,3,5(10)-estratrien-17β-yl)-butylamine] and Diebud [N,N′-bis-(3-hydroxy-1,3,5(10)-estratrien-17β-yl)-1,4-butanediamine] on platelet aggregation

    Flores-García, Mirthala / Fernández-G, Juan M / León-Martínez, Mireille / Hernández-Ortega, Simón / Pérez-Méndez, Oscar / Correa-Basurto, José / Carreón-Torres, Elizabeth / Tolentino-López, Luis E / Ceballos-Reyes, Guillermo Manuel / Peña-Díaz, Aurora de la

    Steroids. 2012 Apr., v. 77, no. 5

    2012  

    Abstract: Compounds with estrogenic effects that also inhibit platelet aggregation might be useful in reducing thrombotic events associated with estrogenic therapy. In this study, two aminoestrogens, Buame [N-(3-hydroxy-1,3,5(10)-estratrien-17β-yl)-butylamine] and ...

    Abstract Compounds with estrogenic effects that also inhibit platelet aggregation might be useful in reducing thrombotic events associated with estrogenic therapy. In this study, two aminoestrogens, Buame [N-(3-hydroxy-1,3,5(10)-estratrien-17β-yl)-butylamine] and Diebud [N,N′-bis-(3-hydroxy-1,3,5(10)-estratrien-17β-yl)-1,4-butanediamine], were synthesized and characterized using common analytical methods and spectrophotometric analyses. The location and orientation of these molecules on the estrogenic receptor α (ERα) were also evaluated. Platelet inhibitory effects were elucidated ADP-induced platelet aggregation and ADP- and collagen-induced ATP release. Molecular docking demonstrated that Buame can reach and bind to the ERα in the ligand binding domain (LBD) similar to 17β-estradiol (co-crystallized ligand). On the other hand, Diebud binds only to the surface of ERα due to its high molecular volume compared to 17β-estradiol and Buame.
    Keywords adenosine diphosphate ; adenosine triphosphate ; analytical methods ; estradiol ; estrogenic properties ; molecular models ; platelet aggregation ; therapeutics
    Language English
    Dates of publication 2012-04
    Size p. 512-520.
    Publishing place Elsevier Inc.
    Document type Article
    ZDB-ID 80312-1
    ISSN 1878-5867 ; 0039-128X
    ISSN (online) 1878-5867
    ISSN 0039-128X
    DOI 10.1016/j.steroids.2012.01.010
    Database NAL-Catalogue (AGRICOLA)

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