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  1. Article ; Online: Terpene-Containing Analogues of Glitazars as Potential Therapeutic Agents for Metabolic Syndrome.

    Blokhin, Mikhail E / Kuranov, Sergey O / Khvostov, Mikhail V / Fomenko, Vladislav V / Luzina, Olga A / Zhukova, Natalia A / Elhajjar, Cham / Tolstikova, Tatiana G / Salakhutdinov, Nariman F

    Current issues in molecular biology

    2023  Volume 45, Issue 3, Page(s) 2230–2247

    Abstract: Metabolic syndrome is a complex of abnormalities involving impaired glucose and lipid metabolism, which needs effective pharmacotherapy. One way to reduce lipid and glucose levels associated with this pathology is the simultaneous activation of nuclear ... ...

    Abstract Metabolic syndrome is a complex of abnormalities involving impaired glucose and lipid metabolism, which needs effective pharmacotherapy. One way to reduce lipid and glucose levels associated with this pathology is the simultaneous activation of nuclear PPAR-alpha and gamma. For this purpose, we synthesized a number of potential agonists based on the pharmacophore fragment of glitazars with the inclusion of mono- or diterpenic moiety in the molecular structure. The study of their pharmacological activity in mice with obesity and type 2 diabetes mellitus (C57Bl/6
    Language English
    Publishing date 2023-03-08
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2000024-8
    ISSN 1467-3045 ; 1467-3037
    ISSN (online) 1467-3045
    ISSN 1467-3037
    DOI 10.3390/cimb45030144
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 5122: Show issues Location:
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  2. Article ; Online: Synthesis and In Vitro Study of Antiviral Activity of Glycyrrhizin Nicotinate Derivatives against HIV-1 Pseudoviruses and SARS-CoV-2 Viruses.

    Fomenko, Vladislav V / Rudometova, Nadezhda B / Yarovaya, Olga I / Rogachev, Artem D / Fando, Anastasia A / Zaykovskaya, Anna V / Komarova, Nina I / Shcherbakov, Dmitry N / Pyankov, Oleg V / Pokrovsky, Andrey G / Karpenko, Larisa I / Maksyutov, Rinat A / Salakhutdinov, Nariman F

    Molecules (Basel, Switzerland)

    2022  Volume 27, Issue 1

    Abstract: When developing drugs against SARS-CoV-2, it is important to consider the characteristics of patients with different co-morbidities. People infected with HIV-1 are a particularly vulnerable group, as they may be at a higher risk than the general ... ...

    Abstract When developing drugs against SARS-CoV-2, it is important to consider the characteristics of patients with different co-morbidities. People infected with HIV-1 are a particularly vulnerable group, as they may be at a higher risk than the general population of contracting COVID-19 with clinical complications. For such patients, drugs with a broad spectrum of antiviral activity are of paramount importance. Glycyrrhizinic acid (Glyc) and its derivatives are promising biologically active compounds for the development of such broad-spectrum antiviral agents. In this work, derivatives of Glyc obtained by acylation with nicotinic acid were investigated. The resulting preparation, Glycyvir, is a multi-component mixture containing mainly mono-, di-, tri- and tetranicotinates. The composition of Glycyvir was characterized by HPLC-MS/MS and its toxicity assessed in cell culture. Antiviral activity against three strains of SARS-CoV-2 was tested in vitro on Vero E6 cells by MTT assay. Glycyvir was shown to inhibit SARS-CoV-2 replication in vitro (IC
    MeSH term(s) Animals ; Antiviral Agents/chemical synthesis ; Antiviral Agents/pharmacology ; COVID-19/virology ; Chlorocebus aethiops ; Glycyrrhizic Acid/chemistry ; HIV Infections/drug therapy ; HIV Infections/virology ; HIV-1/drug effects ; HeLa Cells ; Humans ; In Vitro Techniques ; SARS-CoV-2/drug effects ; Vero Cells ; Virus Replication ; COVID-19 Drug Treatment
    Chemical Substances Antiviral Agents ; Glycyrrhizic Acid (6FO62043WK)
    Language English
    Publishing date 2022-01-04
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 1413402-0
    ISSN 1420-3049 ; 1431-5165 ; 1420-3049
    ISSN (online) 1420-3049
    ISSN 1431-5165 ; 1420-3049
    DOI 10.3390/molecules27010295
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Zs.MO 81: Show issues

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  3. Article ; Online: Biostability study, quantitation method and preliminary pharmacokinetics of a new antifilovirus agent based on borneol and 3-(piperidin-1-yl)propanoic acid.

    Rogachev, Artem D / Putilova, Valentina P / Zaykovskaya, Anna V / Yarovaya, Olga I / Sokolova, Anastasiya S / Fomenko, Vladislav V / Pyankov, Oleg V / Maksyutov, Rinat A / Pokrovsky, Andrey G / Salakhutdinov, Nariman F

    Journal of pharmaceutical and biomedical analysis

    2021  Volume 199, Page(s) 114062

    Abstract: The stability of the new antifiloviral agent AS-358, which is a derivative of borneol and 3-(piperidin-1-yl)propanoic acid, was studied in the blood and blood plasma of rats in vitro. It was found that both in the blood and in the plasma stabilized by ... ...

    Abstract The stability of the new antifiloviral agent AS-358, which is a derivative of borneol and 3-(piperidin-1-yl)propanoic acid, was studied in the blood and blood plasma of rats in vitro. It was found that both in the blood and in the plasma stabilized by EDTA or heparin, the compound is rapidly hydrolyzed at the ester bond. When sodium fluoride was added to the whole blood, the decomposition of the compound was significantly slowed down, which made it possible to develop and validate a method for the quantitative determination of the agent in this matrix. The method was validated in terms of selectivity, calibration dependence, LLOQ, accuracy and precision, stability in an autosampler, recovery, and carry-over. A 8:2 v/v mixture of methanol containing 2-adamantylamine hydrochloride (internal standard, IS) with 0.2 M aqueous zinc sulfate was used for blood sample treatment and protein precipitation. Analysis was performed by HPLC-MS/MS using reversed phase chromatography. MS/MS detection was performed on a triple quadrupole mass spectrometer 6500 QTRAP (SCIEX) in multiple reaction monitoring (MRM) mode. The transitions 294.5→158.2/98.1 and 152.2→107.2/93.1 were monitored for AS-358 and the IS, respectively. The calibration curve was built in the concentration range of 1-500 ng/mL, the intra-day and inter-day accuracy and precision, carry-over and recovery were within the acceptable limits. The developed method was used for a preliminary study of the pharmacokinetics of the agent AS-358 after its oral administration to rats. It was shown that when the substance was administered at a dose of 200 mg/kg, its concentration in the blood of animals reached 550 ng/mL after 1 h, despite its instability in blood.
    MeSH term(s) Animals ; Camphanes ; Chromatography, High Pressure Liquid ; Propionates ; Rats ; Reproducibility of Results ; Tandem Mass Spectrometry
    Chemical Substances Camphanes ; Propionates ; isoborneol (L88RA8N5EG)
    Language English
    Publishing date 2021-04-03
    Publishing country England
    Document type Journal Article
    ZDB-ID 604917-5
    ISSN 1873-264X ; 0731-7085
    ISSN (online) 1873-264X
    ISSN 0731-7085
    DOI 10.1016/j.jpba.2021.114062
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    Zs.A 1850: Show issues Location:
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  4. Article ; Online: Globular chitosan treatment of bovine jugular veins: evidence of anticalcification efficacy in the subcutaneous rat model.

    Krasilnikova, Anna A / Sergeevichev, David S / Fomenko, Vladislav V / Korobeynikov, Alexander A / Vasilyeva, Maria B / Yunoshev, Alexander S / Karaskov, Alexander M / Pokushalov, Evgeny A

    Cardiovascular pathology : the official journal of the Society for Cardiovascular Pathology

    2017  Volume 32, Page(s) 1–7

    Abstract: Vascular xenografts are widely used in cardiovascular surgery as an alternative to autologous vessels and vascular allografts. Calcification is one of the main drawbacks of vascular grafts, especially among young patients and children. Among different ... ...

    Abstract Vascular xenografts are widely used in cardiovascular surgery as an alternative to autologous vessels and vascular allografts. Calcification is one of the main drawbacks of vascular grafts, especially among young patients and children. Among different anticalcification approaches, chitosan emerges as a highly promising candidate due to its versatility, natural origin, and biocompatibility. We investigated the anticalcification efficacy of globular chitosan ("Chitozol") as it demonstrated the improved rate of water solubility as compared with conventional linear macromolecules of chitosan. In addition, we supposed that compact globular form of "Chitozol" molecules could provide effective penetration of extracellular matrix of bovine jugular veins (BJVs). Our results revealed that "Chitozol" treatment mitigated calcification in the experimental groups as compared to the control groups (without any treatment, conventional treatment with glutaraldehyde, and commercially available Contegra conduit). Different concentrations of "Chitozol" (0.3% and 3%), as well as different incubation times (15 and 30min), were equally effective in the prevention of calcification. In addition, "Chitozol" treatment with decellularization of BJVs demonstrated slightly improved stress-strain properties of unimplanted samples. Thus, the filling of fresh BJV with globular chitosan is proposed as a promising emerging treatment for the mitigation of calcific degeneration in BJVs xenografts.
    MeSH term(s) Animals ; Calcinosis/prevention & control ; Cattle ; Chitosan/pharmacology ; Disease Models, Animal ; Heterografts/drug effects ; Heterografts/pathology ; Jugular Veins/transplantation ; Rats
    Chemical Substances Chitosan (9012-76-4)
    Language English
    Publishing date 2017-09-14
    Publishing country United States
    Document type Journal Article
    ZDB-ID 1134600-0
    ISSN 1879-1336 ; 1054-8807
    ISSN (online) 1879-1336
    ISSN 1054-8807
    DOI 10.1016/j.carpath.2017.08.003
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Zs.A 3572: Show issues Location:
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  5. Article ; Online: Globular chitosan prolongs the effective duration time and decreases the acute toxicity of botulinum neurotoxin after intramuscular injection in rats.

    Sergeevichev, David S / Krasilnikova, Anna A / Strelnikov, Artem G / Fomenko, Vladislav V / Salakhutdinov, Nariman F / Romanov, Alexander B / Karaskov, Alexander M / Pokushalov, Evgeny A / Steinberg, Jonathan S

    Toxicon : official journal of the International Society on Toxinology

    2018  Volume 143, Page(s) 90–95

    Abstract: Botulinum neurotoxin (BoNT) is used for an increasing number of neurological and non-neurological indications and disorders. Since the duration of action of this neurotoxin is limited, the goal of the work was to improve the pharmacological time course ... ...

    Abstract Botulinum neurotoxin (BoNT) is used for an increasing number of neurological and non-neurological indications and disorders. Since the duration of action of this neurotoxin is limited, the goal of the work was to improve the pharmacological time course of BoNT. We explored the effect of several polysaccharides on the duration of action of BoNT/A1 in rat electromyography. The formulation of BoNT/A1 containing globular chitosan increased the threshold stimulation intensity almost 2 times in 30 days after injection if compared with the baseline threshold. However, conventional linear chitosan, heparin and hyaluronic acid did not have such an effect. In addition, we compared the effectiveness of different doses of BoNT/A1 (25, 50, 75, and 100 U) with globular chitosan and compared the acute toxicity of this formulation with that of BoNT/A1 in physiological saline after intramuscular injection. The results demonstrated that the dose 25 U of BoNT/A1 with globular chitosan was both effective and safe for animals after intramuscular injection. The assessed median lethal dose (LD
    MeSH term(s) Animals ; Botulinum Toxins, Type A/administration & dosage ; Botulinum Toxins, Type A/pharmacology ; Chitosan/administration & dosage ; Chitosan/pharmacology ; Drug Compounding ; Hamstring Muscles/drug effects ; Injections, Intramuscular ; Lethal Dose 50 ; Male ; Neuromuscular Agents/administration & dosage ; Neuromuscular Agents/pharmacology ; Rats, Wistar ; Time Factors
    Chemical Substances Neuromuscular Agents ; Chitosan (9012-76-4) ; Botulinum Toxins, Type A (EC 3.4.24.69)
    Language English
    Publishing date 2018-01-31
    Publishing country England
    Document type Journal Article
    ZDB-ID 204479-1
    ISSN 1879-3150 ; 0041-0101
    ISSN (online) 1879-3150
    ISSN 0041-0101
    DOI 10.1016/j.toxicon.2018.01.013
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Zs.A 501: Show issues Location:
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