LIVIVO - Das Suchportal für Lebenswissenschaften

switch to English language
Zurück zur letzten Suche Suchhistorie
Erweiterte Suche

Ihre letzten Suchen

  1. AU="Channabasavaiah, Jagadish Puralae"
  2. AU="Anselmi, Maurizio"
  3. AU="Chauhan, D."
  4. AU="Nicoll, Roger A"
  5. AU="Kwon, Young-Sam"
  6. AU="Mihwa Lee"
  7. AU="Yuanting Jin"
  8. AU="Ter Haar, Eva"
  9. AU="Wolin, Dan L"
  10. AU="Zhang, Tenan"
  11. AU="Piedrafita, Lídia"
  12. AU="Nandy, Ananya"
  13. AU="Bansemer, Sven"
  14. AU="Kochetov, O"
  15. AU="Liu, Fen"

Suchergebnis

Treffer 1 - 3 von insgesamt 3

Suchoptionen

  1. Artikel ; Online: Differential effects of dietary polyphenols on oral pharmacokinetics of cyclin-dependent kinase inhibitors in rats: a mechanistic framework for in vitro-in vivo extrapolation.

    Patil, Prajakta Harish / Desai, Mrunal Pradeep / Birangal, Sumit / Gautham Shenoy, G / Channabasavaiah, Jagadish Puralae

    The Journal of pharmacy and pharmacology

    2023  Band 76, Heft 2, Seite(n) 93–105

    Abstract: Objectives: Cyclin-dependent kinase inhibitors are subject to rapid first-pass metabolism, and their oral absorption is hindered by intestinal CYP3A4 and P-gp. The present study investigates the impact of dietary polyphenols on the oral pharmacokinetics ...

    Abstract Objectives: Cyclin-dependent kinase inhibitors are subject to rapid first-pass metabolism, and their oral absorption is hindered by intestinal CYP3A4 and P-gp. The present study investigates the impact of dietary polyphenols on the oral pharmacokinetics of palbociclib and ribociclib, considering their potential as modulators of CYP3A4 and P-gp.
    Methods: Therefore, potential inhibitory effects of dietary polyphenols on drug metabolism and efflux of these drugs were investigated using molecular docking; in vitro preclinical assay using rat liver microsomes and Caco-2 cell monolayers; in vivo, pharmacokinetic parameters were determined in rats pretreated with dietary polyphenols.
    Key findings: Curcumin and quercetin have the highest binding affinities to the PXR's AF-2 region cluster. Curcumin and quercetin significantly inhibited both intestinal efflux and CYP3A4-mediated metabolism of palbociclib and ribociclib (P < .05). In rats pretreated with curcumin, Cmax of palbociclib exhibited a 5.13% increase, while the AUC0-24h of ribociclib showed a significant increase of 18.83% (P < .05). Quercetin administration, notably, impedes the pharmacokinetics of palbociclib. However, the pharmacokinetics of ribociclib remains unaffected by quercetin.
    Conclusions: In conclusion, the utilization of curcumin as a bioenhancer can enhance the bioavailability of dual substrates of P-gp and CYP3A4.
    Mesh-Begriff(e) Humans ; Rats ; Animals ; Cytochrome P-450 CYP3A/metabolism ; Caco-2 Cells ; Curcumin/pharmacology ; Quercetin/pharmacology ; Molecular Docking Simulation ; ATP Binding Cassette Transporter, Subfamily B, Member 1/metabolism ; Administration, Oral ; Cyclin-Dependent Kinases/metabolism ; Aminopyridines ; Purines
    Chemische Substanzen ribociclib (TK8ERE8P56) ; Cytochrome P-450 CYP3A (EC 1.14.14.1) ; Curcumin (IT942ZTH98) ; Quercetin (9IKM0I5T1E) ; ATP Binding Cassette Transporter, Subfamily B, Member 1 ; Cyclin-Dependent Kinases (EC 2.7.11.22) ; Aminopyridines ; Purines
    Sprache Englisch
    Erscheinungsdatum 2023-12-12
    Erscheinungsland England
    Dokumenttyp Journal Article
    ZDB-ID 3107-0
    ISSN 2042-7158 ; 0022-3573 ; 0373-1022
    ISSN (online) 2042-7158
    ISSN 0022-3573 ; 0373-1022
    DOI 10.1093/jpp/rgad115
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

    Zusatzmaterialien

    Kategorien

    Verfügbar in ZB MED Köln/Königswinter

    Uf I Zs.149: Hefte anzeigen Standort:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
    ab Jg. 2022: Lesesaal (EG)

    Über subito bestellen

    Dieser Service ist kostenpflichtig (siehe Lieferbedingungen von subito). Bestellungen, die einen Artikel nebst Supplementary Material umfassen, werden grundsätzlich wie mehrfache Bestellungen bearbeitet. Gebühren fallen in diesen Fällen für jede einzelne Bestellung an.

  2. Artikel ; Online: Molecular Insights into the Mechanism of Modulatory Effects of Proton Pump Inhibitors on P-glycoprotein Mediated Drug Transport of Palbociclib and Ribociclib.

    Desai, Mrunal Pradeep / Harish Patil, Prajakta / Vullendula, Sai Krishna Anand / Birangal, Sumit / Shenoy, G Gautham / Rao, Mahadev / Dengale, Swapnil Jayant / Bhat, Krishnamurthy / Channabasavaiah, Jagadish Puralae

    Current drug metabolism

    2023  Band 24, Heft 6, Seite(n) 458–465

    Abstract: Background: Palbociclib and ribociclib are substrates of efflux transporter P-glycoprotein which plays a key role in absorption and transport of these drugs. Proton pump inhibitors, when co-administered with them are known to show inhibitory effect on P- ...

    Abstract Background: Palbociclib and ribociclib are substrates of efflux transporter P-glycoprotein which plays a key role in absorption and transport of these drugs. Proton pump inhibitors, when co-administered with them are known to show inhibitory effect on P-glycoprotein.
    Objective: Therefore, this study aims to investigate the role of proton pump inhibitors in inhibition of P-glycoprotein mediated efflux of palbociclib and ribociclib.
    Method: A combined approach of molecular docking and
    Results: Molecular docking studies revealed that omeprazole, rabeprazole and pantoprazole bound to the ATP site of nucleotide binding domain with binding energies of -27.53, -29.56 and -38.44 Kcal/mol respectively. In
    Conclusion: The experimental evidence presented highlights the fact that proton pump inhibitors have potential to inhibit P-glycoprotein, giving rise to drug interactions with palbociclib and ribociclib. Hence, monitoring is required while proton pump inhibitors and cyclin-dependent kinase inhibitors are being co-administered to avoid adverse events.
    Sprache Englisch
    Erscheinungsdatum 2023-08-14
    Erscheinungsland Netherlands
    Dokumenttyp Journal Article
    ZDB-ID 2064815-7
    ISSN 1875-5453 ; 1389-2002
    ISSN (online) 1875-5453
    ISSN 1389-2002
    DOI 10.2174/1389200224666230815122312
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

    Zusatzmaterialien

    Kategorien

    Verfügbar in ZB MED Köln/Königswinter

    Zs.A 5584: Hefte anzeigen Standort:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (2.OG)
    ab Jg. 2022: Lesesaal (EG)

    Über subito bestellen

    Dieser Service ist kostenpflichtig (siehe Lieferbedingungen von subito). Bestellungen, die einen Artikel nebst Supplementary Material umfassen, werden grundsätzlich wie mehrfache Bestellungen bearbeitet. Gebühren fallen in diesen Fällen für jede einzelne Bestellung an.

  3. Artikel ; Online: A pilot randomized controlled trial to compare the effectiveness of two 14-day primaquine regimens for the radical cure of vivax malaria in South India.

    Saravu, Kavitha / Tellapragada, Chaitanya / Kulavalli, Shrivathsa / Xavier, Wilbin / Umakanth, Shashikiran / Brahmarouphu, Gouthami / Srinivas, Navyasree Kola / Channabasavaiah, Jagadish Puralae / Bava, Anzil / Saadi, Abdul Vahab / Guddattu, Vasudev / Satyamoorthy, Kapaettu / Bhat, Krishnamurthy

    Malaria journal

    2018  Band 17, Heft 1, Seite(n) 321

    Abstract: Background: Radical cure of Plasmodium vivax malaria requires treatment with a blood schizonticide and a hypnozoitocide (primaquine) to eradicate the dormant liver stages. There has been uncertainty about the operational effectiveness and optimum dosing ...

    Abstract Background: Radical cure of Plasmodium vivax malaria requires treatment with a blood schizonticide and a hypnozoitocide (primaquine) to eradicate the dormant liver stages. There has been uncertainty about the operational effectiveness and optimum dosing of the currently recommended 14-day primaquine (PQ) course.
    Methods: A two centre, randomized, open-label, two arm study was conducted in South India. Patients were randomized to receive either high dose (0.5 mg base/kg body weight) or conventional dose (0.25 mg/kg) PQ for 14 days. Plasma concentrations of PQ and carboxyprimaquine (CPQ) on the 7th day of treatment were measured by reverse phase high performance liquid chromatography. Study subjects were followed up for 6 months. Recurrent infections were genotyped using capillary fragment length polymorphism of two PCR-amplified microsatellite markers (MS07 and MS 10).
    Results: Fifty patients were enrolled. Baseline characteristics and laboratory features did not differ significantly between the groups. Mean age of the study population was 42 ± 16.0 years. Recurrences 80-105 days later occurred in 4 (8%) patients, two in each the groups. All recurrences had the same microsatellite genotype as that causing the index infection suggesting all were relapses. One relapse was associated with low CPQ concentrations suggesting poor adherence.
    Conclusions: This small pilot trial supports the effectiveness of the currently recommended lower dose (0.25 mg/kg/day) 14 day PQ regimen for the radical cure of vivax malaria in South India. Trial registration Clinical Trials Registry-India, CTRI/2017/03/007999. Registered 3 March 2017, http://ctri.nic.in/Clinicaltrials/regtrial.php?modid=1&compid=19&EncHid=82755.86366 .
    Mesh-Begriff(e) Adult ; Aged ; Antimalarials/therapeutic use ; Dose-Response Relationship, Drug ; Female ; Humans ; India ; Malaria, Vivax/drug therapy ; Male ; Middle Aged ; Pilot Projects ; Plasmodium vivax/drug effects ; Primaquine/therapeutic use ; Recurrence ; Young Adult
    Chemische Substanzen Antimalarials ; Primaquine (MVR3634GX1)
    Sprache Englisch
    Erscheinungsdatum 2018-09-03
    Erscheinungsland England
    Dokumenttyp Journal Article ; Randomized Controlled Trial
    ISSN 1475-2875
    ISSN (online) 1475-2875
    DOI 10.1186/s12936-018-2472-5
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

    Zusatzmaterialien

    Kategorien

    Über subito bestellen

    Dieser Service ist kostenpflichtig (siehe Lieferbedingungen von subito). Bestellungen, die einen Artikel nebst Supplementary Material umfassen, werden grundsätzlich wie mehrfache Bestellungen bearbeitet. Gebühren fallen in diesen Fällen für jede einzelne Bestellung an.

    Fernleihe an ZB MED

    Sie können sich den gewünschten Titel als lokale Nutzerin oder lokaler Nutzer von ZB MED direkt an den Standort Köln schicken lassen.

Zum Seitenanfang