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  1. Article ; Online: Involvement of lysyl oxidase in the pathogenesis of arterial stiffness in chronic kidney disease.

    Sharma, Ravindra K / Kamble, Shyam H / Krishnan, Suraj / Gomes, Joshua / To, Brandon / Li, Shiyu / Liu, I-Chia / Gumz, Michelle L / Mohandas, Rajesh

    American journal of physiology. Renal physiology

    2023  Volume 324, Issue 4, Page(s) F364–F373

    Abstract: Patients with chronic kidney disease (CKD) are at increased risk for adverse cardiovascular events. CKD is associated with increases in arterial stiffness, whereas improvements in arterial stiffness correlate with better survival. However, arterial ... ...

    Abstract Patients with chronic kidney disease (CKD) are at increased risk for adverse cardiovascular events. CKD is associated with increases in arterial stiffness, whereas improvements in arterial stiffness correlate with better survival. However, arterial stiffness is increased early in CKD, suggesting that there might be additional factors, unique to kidney disease, that increase arterial stiffness. Lysyl oxidase (LOX) is a key mediator of collagen cross linking and matrix remodeling. LOX is predominantly expressed in the cardiovascular system, and its upregulation has been associated with increased tissue stiffening and extracellular matrix remodeling. Thus, this study was designed to evaluate the role of increased LOX activity in inducing aortic stiffness in CKD and whether β-aminopropionitrile (BAPN), a LOX inhibitor, could prevent aortic stiffness by reducing collagen cross linking. Eight-week-old male C57BL/6 mice were subjected to 5/6 nephrectomy (Nx) or sham surgery. Two weeks after surgery, mice were randomized to BAPN (300 mg/kg/day in water) or vehicle treatment for 4 wk. Aortic stiffness was assessed by pulse wave velocity (PWV) using Doppler ultrasound. Aortic levels of LOX were assessed by ELISA, and cross-linked total collagen levels were analyzed by mass spectrometry and Sircol assay. Nx mice showed increased PWV and aortic wall remodeling compared with control mice. Collagen cross linking was increased in parallel with the increases in total collagen in the aorta of Nx mice. In contrast, Nx mice that received BAPN treatment showed decreased cross-linked collagens and PWV compared with that received vehicle treatment. Our results indicated that LOX might be an early and key mediator of aortic stiffness in CKD.
    MeSH term(s) Animals ; Male ; Mice ; Aminopropionitrile/pharmacology ; Collagen ; Mice, Inbred C57BL ; Protein-Lysine 6-Oxidase ; Pulse Wave Analysis/methods ; Renal Insufficiency, Chronic ; Vascular Stiffness/physiology
    Chemical Substances Aminopropionitrile (151-18-8) ; Collagen (9007-34-5) ; Protein-Lysine 6-Oxidase (EC 1.4.3.13)
    Language English
    Publishing date 2023-02-24
    Publishing country United States
    Document type Journal Article ; Research Support, N.I.H., Extramural
    ZDB-ID 603837-2
    ISSN 1522-1466 ; 0363-6127
    ISSN (online) 1522-1466
    ISSN 0363-6127
    DOI 10.1152/ajprenal.00239.2022
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  2. Article: Pharmacokinetic Interaction of Kratom and Cannabidiol in Male Rats.

    Berthold, Erin C / Kamble, Shyam H / Kanumuri, Siva Rama Raju / Kuntz, Michelle A / Senetra, Alexandria S / Chiang, Yi-Hua / Mukhopadhyay, Sushobhan / McCurdy, Christopher R / Sharma, Abhisheak

    Pharmaceutics

    2024  Volume 16, Issue 3

    Abstract: Kratom and cannabidiol products are used to self-treat a variety of conditions, including anxiety and pain, and to elevate mood. Research into the individual pharmacokinetic properties of commercially available kratom and cannabidiol products has been ... ...

    Abstract Kratom and cannabidiol products are used to self-treat a variety of conditions, including anxiety and pain, and to elevate mood. Research into the individual pharmacokinetic properties of commercially available kratom and cannabidiol products has been performed, but there are no studies on coadministration of these products. Surveys of individuals with kratom use history indicate that cannabidiol use is one of the strongest predictors of both lifetime and past month kratom use. The purpose of this study was to determine if there are changes in pharmacokinetic properties when commercially available kratom and cannabidiol products are administered concomitantly. It was found that with concomitant administration of cannabidiol, there was a 2.8-fold increase in the exposure of the most abundant kratom alkaloid, mitragynine, and increases in the exposure of other minor alkaloids. The results of this work suggest that with cannabidiol coadministration, the effects of kratom may be both delayed and increased due to a delay in time to reach maximum plasma concentration and higher systemic exposure of the psychoactive alkaloids found in kratom.
    Language English
    Publishing date 2024-02-24
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2527217-2
    ISSN 1999-4923
    ISSN 1999-4923
    DOI 10.3390/pharmaceutics16030318
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  3. Article ; Online: UPLC-MS/MS method for the quantification of MCI-77, a novel sigma-1 receptor ligand, and its application to pharmacokinetic studies.

    Popa, Raluca / Kamble, Shyam H / Kanumuri, Raju S / King, Tamara I / Berthold, Erin C / Intagliata, Sebastiano / Sharma, Abhisheak / McCurdy, Christopher R

    Journal of chromatography. B, Analytical technologies in the biomedical and life sciences

    2022  Volume 1196, Page(s) 123187

    Abstract: Sigma-1 receptors are involved in pain modulation, particularly in cases of nerve injury and neuropathic pain. High-affinity ligands with improved pharmacokinetic profiles are needed to further investigate the properties of these receptors and their ... ...

    Abstract Sigma-1 receptors are involved in pain modulation, particularly in cases of nerve injury and neuropathic pain. High-affinity ligands with improved pharmacokinetic profiles are needed to further investigate the properties of these receptors and their potential as a therapeutic target. The novel compound MCI-77 is one such selective sigma-1 receptor ligand, and the purpose of this study was to characterize its preclinical pharmacokinetic parameters. An ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method was developed and validated to quantify MCI-77 in mouse plasma and brain homogenate. The method was validated for sensitivity, selectivity, linearity, accuracy, precision, stability, and dilution integrity. The method has a linearity range of 2-200 ng/mL, a short run-time of 3.2 min, and requires a low sample volume of 25 µL. A simple protein precipitation procedure was used for compound extraction. Samples were run on an Acquity UPLC BEH C
    MeSH term(s) Animals ; Chromatography, High Pressure Liquid/methods ; Chromatography, Liquid/methods ; Ligands ; Mice ; Receptors, sigma ; Reproducibility of Results ; Tandem Mass Spectrometry/methods ; Sigma-1 Receptor
    Chemical Substances Ligands ; Receptors, sigma
    Language English
    Publishing date 2022-03-05
    Publishing country Netherlands
    Document type Journal Article
    ZDB-ID 1180823-8
    ISSN 1873-376X ; 0378-4347 ; 1570-0232 ; 1387-2273
    ISSN (online) 1873-376X
    ISSN 0378-4347 ; 1570-0232 ; 1387-2273
    DOI 10.1016/j.jchromb.2022.123187
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  4. Article: UPLC-MS/MS method for the quantification of MCI-77, a novel sigma-1 receptor ligand, and its application to pharmacokinetic studies

    Popa, Raluca / Kamble, Shyam H. / Kanumuri, Raju S. / King, Tamara I. / Berthold, Erin C. / Intagliata, Sebastiano / Sharma, Abhisheak / McCurdy, Christopher R.

    Journal of chromatography. 2022 Apr. 30, v. 1196

    2022  

    Abstract: Sigma-1 receptors are involved in pain modulation, particularly in cases of nerve injury and neuropathic pain. High-affinity ligands with improved pharmacokinetic profiles are needed to further investigate the properties of these receptors and their ... ...

    Abstract Sigma-1 receptors are involved in pain modulation, particularly in cases of nerve injury and neuropathic pain. High-affinity ligands with improved pharmacokinetic profiles are needed to further investigate the properties of these receptors and their potential as a therapeutic target. The novel compound MCI-77 is one such selective sigma-1 receptor ligand, and the purpose of this study was to characterize its preclinical pharmacokinetic parameters. An ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method was developed and validated to quantify MCI-77 in mouse plasma and brain homogenate. The method was validated for sensitivity, selectivity, linearity, accuracy, precision, stability, and dilution integrity. The method has a linearity range of 2–200 ng/mL, a short run-time of 3.2 min, and requires a low sample volume of 25 µL. A simple protein precipitation procedure was used for compound extraction. Samples were run on an Acquity UPLC BEH C₁₈ column (1.7 μm, 2.1 × 50 mm) following a gradient elution method using a mobile phase consisting of water containing 0.1% (v/v) formic acid and acetonitrile. The method was applied to the analysis of plasma and brain homogenate samples from preclinical pharmacokinetic studies in CD-1 mice. MCI-77 exhibited high systemic clearance (8.5 ± 0.3 L/h/kg) and extensive tissue distribution indicated by a high volume of distribution (20.1 ± 0.3 L/kg). The concentration levels were consistently higher in brain samples than in plasma (brain/plasma AUC ratio 2.9), indicating its ability to cross the blood–brain barrier.
    Keywords acetonitrile ; blood-brain barrier ; brain ; formic acid ; ligands ; mice ; nerve tissue ; pain ; pharmacokinetics ; tandem mass spectrometry ; therapeutics ; tissue distribution
    Language English
    Dates of publication 2022-0430
    Publishing place Elsevier B.V.
    Document type Article
    ISSN 1570-0232
    DOI 10.1016/j.jchromb.2022.123187
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  5. Article ; Online: Comparative Pharmacokinetics of Commercially Available Cannabidiol Isolate, Broad-Spectrum, and Full-Spectrum Products.

    Berthold, Erin C / Kamble, Shyam H / Kanumuri, Siva Rama Raju / Kuntz, Michelle A / Senetra, Alexandria S / Chiang, Yi-Hua / McMahon, Lance R / McCurdy, Christopher R / Sharma, Abhisheak

    European journal of drug metabolism and pharmacokinetics

    2023  Volume 48, Issue 4, Page(s) 427–435

    Abstract: Background and objectives: A wide variety of products containing cannabidiol (CBD) are available on the commercial market. One of the most common products, CBD oil, is administered to self-treat a variety of conditions. These oils are available as CBD ... ...

    Abstract Background and objectives: A wide variety of products containing cannabidiol (CBD) are available on the commercial market. One of the most common products, CBD oil, is administered to self-treat a variety of conditions. These oils are available as CBD isolate, broad-spectrum [all terpenes and minor cannabinoids except Δ-9-tetrahydrocannabinol (THC)], or full-spectrum (all terpenes and minor cannabinoids with THC < 0.3% dried weight) products. A systematic pharmacokinetic study was performed to determine whether there are differences in the pharmacokinetic parameters and systemic exposure of CBD after oral dosing as an isolate, broad-spectrum, or full-spectrum product.
    Methods: Male and female Sprague Dawley rats were treated with a single, equivalent oral dose of CBD delivered as isolate, broad-spectrum, or full-spectrum product. An additional study using an in-house preparation of CBD isolate plus 0.2% THC was performed. A permeability assay was also conducted to investigate whether the presence of THC alters the intestinal permeability of CBD.
    Results: There was an increase in the oral bioavailability of CBD (12% and 21% in male and female rats, respectively) when administered as a full-spectrum product compared with the isolate and broad-spectrum products. There was no difference in the bioavailability of CBD between the commercially available full-spectrum formulation (3.1% CBD; containing 0.2% THC plus terpenes and other minor cannabinoids) versus the in-house preparation of CBD full-spectrum (CBD isolate 3.2% plus 0.2% THC isolate). In vitro permeability assays demonstrated that the presence of THC increases permeability of CBD while also decreasing efflux through the gut wall.
    Conclusions: The presence of 0.2% THC increased the oral bioavailability of CBD in male and female rats, indicating that full-spectrum products may produce increased effectiveness of CBD due to a greater exposure available systemically.
    MeSH term(s) Male ; Female ; Rats ; Animals ; Cannabidiol ; Dronabinol ; Rats, Sprague-Dawley ; Cannabinoids ; Biological Availability
    Chemical Substances Cannabidiol (19GBJ60SN5) ; Dronabinol (7J8897W37S) ; Cannabinoids
    Language English
    Publishing date 2023-06-19
    Publishing country France
    Document type Journal Article
    ZDB-ID 196729-0
    ISSN 2107-0180 ; 0398-7639 ; 0378-7966
    ISSN (online) 2107-0180
    ISSN 0398-7639 ; 0378-7966
    DOI 10.1007/s13318-023-00839-3
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  6. Article ; Online: Metabolism of Speciociliatine, an Overlooked Kratom Alkaloid for its Potential Pharmacological Effects.

    Kamble, Shyam H / Berthold, Erin C / Kanumuri, Siva Rama Raju / King, Tamara I / Kuntz, Michelle A / León, Francisco / Mottinelli, Marco / McMahon, Lance R / McCurdy, Christopher R / Sharma, Abhisheak

    The AAPS journal

    2022  Volume 24, Issue 5, Page(s) 86

    Abstract: Speciociliatine, a diastereomer of mitragynine, is an indole-based alkaloid found in kratom (Mitragyna speciosa). Kratom has been widely used for the mitigation of pain and opioid dependence, as a mood enhancer, and/or as an energy booster. ... ...

    Abstract Speciociliatine, a diastereomer of mitragynine, is an indole-based alkaloid found in kratom (Mitragyna speciosa). Kratom has been widely used for the mitigation of pain and opioid dependence, as a mood enhancer, and/or as an energy booster. Speciociliatine is a partial µ-opioid agonist with a 3-fold higher binding affinity than mitragynine. Speciociliatine has been found to be a major circulating alkaloid in humans following oral administration of a kratom product. In this report, we have characterized the metabolism of speciociliatine in human and preclinical species (mouse, rat, dog, and cynomolgus monkey) liver microsomes and hepatocytes. Speciociliatine metabolized rapidly in monkey, rat, and mouse hepatocytes (in vitro half-life was 6.6 ± 0.2, 8.3 ± 1.1, 11.2 ± 0.7 min, respectively), while a slower metabolism was observed in human and dog hepatocytes (91.7 ± 12.8 and > 120 min, respectively). Speciociliatine underwent extensive metabolism, primarily through monooxidation and O-demethylation metabolic pathways in liver microsomes and hepatocytes across species. No human-specific or disproportionate metabolites of speciociliatine were found in human liver microsomes. The metabolism of speciociliatine was predominantly mediated by CYP3A4 with minor contributions by CYP2D6.
    MeSH term(s) Animals ; Dogs ; Humans ; Macaca fascicularis ; Mice ; Microsomes, Liver/metabolism ; Mitragyna/chemistry ; Mitragyna/metabolism ; Rats ; Secologanin Tryptamine Alkaloids/chemistry ; Secologanin Tryptamine Alkaloids/metabolism ; Secologanin Tryptamine Alkaloids/pharmacology
    Chemical Substances Secologanin Tryptamine Alkaloids ; mitragynine (EP479K822J)
    Language English
    Publishing date 2022-07-19
    Publishing country United States
    Document type Journal Article ; Research Support, N.I.H., Extramural
    ISSN 1550-7416
    ISSN (online) 1550-7416
    DOI 10.1208/s12248-022-00736-8
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  7. Article ; Online: Bioanalytical method development and pharmacokinetics of MCI-92, a sigma-1 receptor ligand.

    Popa, Raluca / Kamble, Shyam H / Kanumuri, Raju S / King, Tamara I / Berthold, Erin C / Intagliata, Sebastiano / Sharma, Abhisheak / McCurdy, Christopher R

    Journal of pharmaceutical and biomedical analysis

    2020  Volume 191, Page(s) 113610

    Abstract: Sigma-1 receptors are found throughout the nervous system and play a role in regulating nociception. They are highly expressed in nerve injury, making them a potential target for the treatment of neuropathic pain. Although sigma-1 receptor antagonists ... ...

    Abstract Sigma-1 receptors are found throughout the nervous system and play a role in regulating nociception. They are highly expressed in nerve injury, making them a potential target for the treatment of neuropathic pain. Although sigma-1 receptor antagonists have been shown to have anti-nociceptive and anti-allodynic effects, improved selectivity of these ligands is needed to further investigate their potential to treat neuropathic pain. MCI-92 is a novel, selective sigma-1 receptor ligand developed to address this need. A sensitive and rapid ultra-performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) method was developed and validated for the quantification of MCI-92 in mouse plasma and brain homogenate. A structural analog of the analyte, MCI-147, was used as the internal standard (IS). The chromatographic separation was achieved on an Acquity UPLC BEH C
    MeSH term(s) Animals ; Chromatography, High Pressure Liquid ; Chromatography, Liquid ; Ligands ; Mice ; Rats ; Rats, Sprague-Dawley ; Receptors, sigma ; Reproducibility of Results ; Tandem Mass Spectrometry ; Sigma-1 Receptor
    Chemical Substances Ligands ; Receptors, sigma
    Language English
    Publishing date 2020-09-13
    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.2020.113610
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  8. Article ; Online: Adolescent nicotine and tobacco smoke exposure enhances nicotine self-administration in female rats.

    Chellian, Ranjithkumar / Behnood-Rod, Azin / Wilson, Ryann / Kamble, Shyam H / Sharma, Abhisheak / McCurdy, Christopher R / Bruijnzeel, Adriaan W

    Neuropharmacology

    2020  Volume 176, Page(s) 108243

    Abstract: Most people start experimenting with tobacco products or e-cigarettes in early adolescence and become habitual smokers in late adolescence or adulthood. These studies investigated if exposure to tobacco smoke or nicotine during early and mid-adolescence ... ...

    Abstract Most people start experimenting with tobacco products or e-cigarettes in early adolescence and become habitual smokers in late adolescence or adulthood. These studies investigated if exposure to tobacco smoke or nicotine during early and mid-adolescence affects nicotine intake in late adolescence and early adulthood. Male and female rats were exposed to tobacco smoke from low- and high-nicotine SPECTRUM cigarettes or nicotine (0.3 mg/kg, twice a day) from postnatal day (P) 24-42. The self-administration sessions started at P55. The rats self-administered nicotine for 14-15 days under a fixed-ratio 1 schedule, and on the first day, the maximum number of infusions was twenty. Exposure to smoke from high, but not low, nicotine cigarettes during adolescence increased nicotine self-administration in female but not male rats. Adolescent treatment with nicotine facilitated nicotine self-administration. On the first day of nicotine self-administration, nicotine-treated rats reached the maximum number of infusions before the saline-treated control rats. Nicotine intake was also higher in the nicotine-treated female rats than in the saline-treated females. There was no sex difference in nicotine intake in controls when the data from the studies were combined. Smoke exposure led to a dose-dependent increase in plasma nicotine and cotinine levels in adolescent rats. Exposure to smoke from high-nicotine cigarettes and 0.3 mg/kg of nicotine led to plasma nicotine and cotinine levels that are similar to those in tobacco users. These findings indicate that in females, but not males, exposure to nicotine during adolescence may facilitate smoking and e-cigarette use later in life.
    MeSH term(s) Age Factors ; Animals ; Behavior, Addictive/blood ; Behavior, Addictive/chemically induced ; Behavior, Addictive/psychology ; Female ; Inhalation Exposure/adverse effects ; Male ; Nicotine/administration & dosage ; Nicotine/blood ; Nicotinic Agonists/administration & dosage ; Nicotinic Agonists/blood ; Rats ; Self Administration ; Tobacco Smoke Pollution/adverse effects
    Chemical Substances Nicotinic Agonists ; Tobacco Smoke Pollution ; Nicotine (6M3C89ZY6R)
    Language English
    Publishing date 2020-07-20
    Publishing country England
    Document type Journal Article ; Research Support, N.I.H., Extramural ; Research Support, U.S. Gov't, P.H.S.
    ZDB-ID 218272-5
    ISSN 1873-7064 ; 0028-3908
    ISSN (online) 1873-7064
    ISSN 0028-3908
    DOI 10.1016/j.neuropharm.2020.108243
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  9. Article: Exploring 1-adamantanamine as an alternative amine moiety for metabolically labile azepane ring in newly synthesized benzo[

    Intagliata, Sebastiano / Agha, Hebaalla / Kopajtic, Theresa A / Katz, Jonathan L / Kamble, Shyam H / Sharma, Abhisheak / Avery, Bonnie A / McCurdy, Christopher R

    Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents

    2020  Volume 29, Issue 9, Page(s) 1697–1706

    Abstract: In this work we report the structure-activity relationships, binding properties, and metabolic stability studies of a series of benzo[ ...

    Abstract In this work we report the structure-activity relationships, binding properties, and metabolic stability studies of a series of benzo[
    Language English
    Publishing date 2020-07-08
    Publishing country United States
    Document type Journal Article
    ZDB-ID 1116702-6
    ISSN 1054-2523
    ISSN 1054-2523
    DOI 10.1007/s00044-020-02597-2
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  10. Article: In Vitro Antioxidant and Anti-Glycation Activity of Resveratrol and Its Novel Triester with Trolox

    Intagliata, Sebastiano / Spadaro, Angelo / Lorenti, Miriam / Panico, Annamaria / Siciliano, Edy A / Barbagallo, Sabrina / Macaluso, Benito / Kamble, Shyam H / Modica, Maria N / Montenegro, Lucia

    Antioxidants. 2020 Dec. 24, v. 10, no. 1

    2020  

    Abstract: Resveratrol (RSV) is well known for its many beneficial activities, but its unfavorable physicochemical properties impair its effectiveness after systemic and topical administration; thus, several strategies have been investigated to improve RSV efficacy. ...

    Abstract Resveratrol (RSV) is well known for its many beneficial activities, but its unfavorable physicochemical properties impair its effectiveness after systemic and topical administration; thus, several strategies have been investigated to improve RSV efficacy. With this aim, in this work, we synthesized a novel RSV triester with trolox, an analogue of vitamin E with strong antioxidant activity. The new RSV derivative (RSVTR) was assayed in vitro to evaluate its antioxidant and anti-glycation activity compared to RSV. RSVTR chemical stability was assessed at pH 2.0, 6.8, and 7.2 and different storage temperatures (5 °C, 22 °C, and 37 °C). An influence of pH stronger than that of temperature on RSVTR half-life values was pointed out, and RSVTR greatest stability was observed at pH 7.2 and 5 °C. RSVTR showed a lower antioxidant ability compared to RSV (determined by the oxygen radical absorbance capacity assay) while its anti-glycation activity (evaluated using the Maillard reaction) was significantly greater than that of RSV. The improved ability to inhibit the glycation process was attributed to a better interaction of RSVTR with albumin owing to its increased topological polar surface area value and H-bond acceptor number compared to RSV. Therefore, RSVTR could be regarded as a promising anti-glycation agent worthy of further investigations.
    Keywords Maillard reaction ; albumins ; antioxidants ; assays ; glycation ; half life ; oxygen radical absorbance capacity ; pH ; resveratrol ; storage temperature ; surface area ; topical application ; topology ; vitamin E
    Language English
    Dates of publication 2020-1224
    Publishing place Multidisciplinary Digital Publishing Institute
    Document type Article
    Note NAL-light
    ZDB-ID 2704216-9
    ISSN 2076-3921
    ISSN 2076-3921
    DOI 10.3390/antiox10010012
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