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  1. Article ; Online: Complexation of the Antihypertensive Drug Olmesartan with Zn: In Vivo Antihypertensive and Cardiac Effects.

    Restrepo Guerrero, Andrés G / Martinez, Valeria R / Velez Rueda, Jorge O / Portiansky, Enrique L / De Giusti, Verónica / Ferrer, Evelina G / Williams, Patricia A M

    Biological trace element research

    2023  Volume 202, Issue 1, Page(s) 246–257

    Abstract: This study is based on the premise that the application of chemical synthesis strategies to structurally modify commercial drugs by complexation with biometals is a valid procedure to improve their biological effects. Our purpose is to synthesize a ... ...

    Abstract This study is based on the premise that the application of chemical synthesis strategies to structurally modify commercial drugs by complexation with biometals is a valid procedure to improve their biological effects. Our purpose is to synthesize a compound with greater efficacy than the original drug, able to enhance its antihypertensive and cardiac pharmacological activity. Herein, the structure of the coordination compound of Zn(II) and the antihypertensive drug olmesartan, [Zn(Olme)(H
    MeSH term(s) Rats ; Animals ; Male ; Antihypertensive Agents/pharmacology ; Antihypertensive Agents/therapeutic use ; Hypertension/drug therapy ; Rats, Inbred SHR ; Blood Pressure ; Hypertrophy, Left Ventricular/drug therapy ; Hypertrophy, Left Ventricular/prevention & control ; Zinc/pharmacology ; Zinc/therapeutic use
    Chemical Substances Antihypertensive Agents ; olmesartan (8W1IQP3U10) ; Zinc (J41CSQ7QDS)
    Language English
    Publishing date 2023-04-22
    Publishing country United States
    Document type Journal Article
    ZDB-ID 445336-0
    ISSN 1559-0720 ; 0163-4984
    ISSN (online) 1559-0720
    ISSN 0163-4984
    DOI 10.1007/s12011-023-03670-8
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: Improvement of the cardiovascular effect of methyldopa by complexation with Zn(II): Synthesis, characterization and mechanism of action.

    Actis Dato, Agustin B / Martinez, Valeria R / Velez Rueda, Jorge O / Portiansky, Enrique L / De Giusti, Verónica / Ferrer, Evelina G / Williams, Patricia A M

    Journal of trace elements in medicine and biology : organ of the Society for Minerals and Trace Elements (GMS)

    2023  Volume 81, Page(s) 127327

    Abstract: Background: the antihypertensive drug α-methyldopa (MD) stands as one of the extensively used medications for managing hypertension during pregnancy. Zinc deprivation has been associated with many diseases. In this context, the synthesis of a Zn ... ...

    Abstract Background: the antihypertensive drug α-methyldopa (MD) stands as one of the extensively used medications for managing hypertension during pregnancy. Zinc deprivation has been associated with many diseases. In this context, the synthesis of a Zn coordination complex [Zn(MD)(OH)(H
    Methods: ZnMD was synthesized and physicochemically characterized. Fluorescence spectral studies were conducted to examine the binding of both, the ligand and the metal with bovine serum albumin (BSA). MD, ZnMD, and ZnCl
    Results: The complex exhibited a moderate affinity for binding with BSA showing a spontaneous interaction (indicated by negative ΔG values) and moderate affinity (determined by affinity constant values). The binding process involved the formation of Van der Waals forces and hydrogen bonds. Upon treatment with MD and ZnMD, a reduction in the systolic blood pressure in SHR was observed, being ZnMD more effective than MD (122 ± 8.1 mmHg and 145 ± 5.6 mmHg, at 8th week of treatment, respectively). The ZnMD treatment prevented myocardial hypertrophy, improved the heart function and reduced the cardiac fibrosis, as evidenced by parameters such as left ventricular mass, fractional shortening, and histological studies. In contrast, MD did not show noticeable differences in these parameters. ZnMD regulates negatively the oxidative damage by reducing levels of ROS and lipid peroxidation, as well as the cardiac NAD(P)H oxidase, and increasing SOD1 expression, while MD did not show significant effect. Moreover, cardiac nitric oxide levels were greater in the ZnMD therapy compared to MD treatment.
    Conclusion: Both MD and ZnMD have the potential to be transported by albumin. Our findings provide important evidence suggesting that this complex could be a potential therapeutic drug for the treatment of hypertension and cardiac hypertrophy and dysfunction.
    MeSH term(s) Rats ; Animals ; Antihypertensive Agents/therapeutic use ; Methyldopa/pharmacology ; Methyldopa/therapeutic use ; Reactive Oxygen Species/metabolism ; Superoxide Dismutase-1 ; Nitric Oxide/metabolism ; Hypertension/drug therapy ; Blood Pressure ; Rats, Inbred SHR ; Myocytes, Cardiac/metabolism ; Cardiomegaly ; NADPH Oxidases ; Zinc/pharmacology ; Zinc/therapeutic use
    Chemical Substances Antihypertensive Agents ; Methyldopa (56LH93261Y) ; Reactive Oxygen Species ; Superoxide Dismutase-1 (EC 1.15.1.1) ; Nitric Oxide (31C4KY9ESH) ; NADPH Oxidases (EC 1.6.3.-) ; Zinc (J41CSQ7QDS)
    Language English
    Publishing date 2023-10-21
    Publishing country Germany
    Document type Journal Article
    ZDB-ID 1236267-0
    ISSN 1878-3252 ; 1611-602X ; 0946-672X
    ISSN (online) 1878-3252 ; 1611-602X
    ISSN 0946-672X
    DOI 10.1016/j.jtemb.2023.127327
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 2279: Show issues Location:
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    Jg. 1995 - 2021: Lesesall (2.OG)
    ab Jg. 2022: Lesesaal (EG)

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  3. Article ; Online: Effect of the structural modification of Candesartan with Zinc on hypertension and left ventricular hypertrophy.

    Martinez, Valeria R / Martins Lima, Augusto / Stergiopulos, Nikolaous / Velez Rueda, Jorge O / Islas, Maria S / Griera, Mercedes / Calleros, Laura / Rodriguez Puyol, Manuel / Jaquenod de Giusti, Carolina / Portiansky, Enrique L / Ferrer, Evelina G / De Giusti, Verónica / Williams, Patricia A M

    European journal of pharmacology

    2023  Volume 946, Page(s) 175654

    Abstract: Hypertension is the most common cause of left ventricular hypertrophy, contributing to heart failure progression. Candesartan (Cand) is an angiotensin receptor antagonist widely used for hypertension treatment. Structural modifications were previously ... ...

    Abstract Hypertension is the most common cause of left ventricular hypertrophy, contributing to heart failure progression. Candesartan (Cand) is an angiotensin receptor antagonist widely used for hypertension treatment. Structural modifications were previously performed by our group using Zinc (ZnCand) as a strategy for improving its pharmacological properties. The measurements showed that ZnCand exerts a stronger interaction with the angiotensin II receptor, type 1 (AT
    MeSH term(s) Animals ; Rats ; Antihypertensive Agents/chemistry ; Antihypertensive Agents/pharmacology ; Biphenyl Compounds/pharmacology ; Blood Pressure ; Hypertension/complications ; Hypertension/drug therapy ; Hypertrophy, Left Ventricular/drug therapy ; Matrix Metalloproteinase 2 ; Myocytes, Cardiac ; Rats, Inbred SHR ; Tetrazoles/pharmacology ; Tetrazoles/therapeutic use ; Zinc/pharmacology
    Chemical Substances Antihypertensive Agents ; Biphenyl Compounds ; candesartan (S8Q36MD2XX) ; Matrix Metalloproteinase 2 (EC 3.4.24.24) ; Tetrazoles ; Zinc (J41CSQ7QDS)
    Language English
    Publishing date 2023-03-15
    Publishing country Netherlands
    Document type Journal Article
    ZDB-ID 80121-5
    ISSN 1879-0712 ; 0014-2999
    ISSN (online) 1879-0712
    ISSN 0014-2999
    DOI 10.1016/j.ejphar.2023.175654
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 522: Show issues Location:
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