In Vivo Study of the Effect of Antiviral Acyclic Nucleotide Phosphonate /R)-9-[2-(phosphonomethoxy)propyl}adenine(PMPA, tenofovir) and Its Prodrug Tenofovir Disoproxil Fumarate on rat microsomal Cytochrome P450

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15110%2F08%3A00007584" target="_blank" >RIV/61989592:15110/08:00007584 - isvavai.cz</a>

Alternative codes found

RIV/68378041:_____/08:00315836 RIV/61388963:_____/08:00315836

Result on the web

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DOI - Digital Object Identifier

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Result language

angličtina

Original language name

In Vivo Study of the Effect of Antiviral Acyclic Nucleotide Phosphonate /R)-9-[2-(phosphonomethoxy)propyl}adenine(PMPA, tenofovir) and Its Prodrug Tenofovir Disoproxil Fumarate on rat microsomal Cytochrome P450

Original language description

The total content of rat liver microsomal cytochrome P450 (CYP) significantly decreased after repeated i.p. administration of the antiviral agent tenofovir ((R)?9?[2? (phosphonomethoxy)propyl]adenine) and tenofovir disoproxil at a daily dose 25 mg.kg-1.The content of liver microsomal protein however did not change. The decrease of the CYP content was accompanied by concomitant increase of the amount of inactive CYP form, cytochrome P420. This effect was confirmed by a parallel study of the activities of selected CYP forms, CYP2E1 (p-nitrophenol hydroxylation) and CYP1A2 (7-ethoxyresorufin deethylation). The activity (expressed relatively to the protein content) of both CYP forms decreased significantly following the decrease of the total CYP. On the other hand, the CYP2E1 activity expressed relatively to the (decreasing) total CYP content remained unchanged. CYP1A2 activity however decreased as well when calculated relatively to the total native CYP content indicating lower stability

Czech name

In vivo studie vlivu antivirálního acyklického nukleotidfosfonátu (R)-9-[2-(fosfonomethoxy)propyl]adenin (PMPA, tenofovir) a jeho prodrug tenofovir disoproxil fumarátu na mikrosomální cytochrom P450 u potkana.

Czech description

Celkový obsah jaterních mikrosomálních cytochromů P450 (CYP) se výrazně snížil po opakovaném i.p. podání antivirální látky tenofoviru ((R)?9?[2? (fosfonomethoxy)propyl]adenin) a tenofoviru disoproxilu při denní dávce 25 mg.kg-1. Zároveň vzrostl obsah neaktivní formy CYP, tj. cytochromu P420. Bylo zjištěno, že v přítomnosti tenofoviru došlo k významné inaktivaci některých forem mikrosomálních jaterních CYP (vznik P420), ale celkový obsah CYP (vztaženo na množství proteinu) zůstal nezměněn.

Type

J_x - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)

CEP classification

FR - Pharmacology and apothecary chemistry

OECD FORD branch

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Project

<a href="/en/project/1M0508" target="_blank" >1M0508: New Antivirals and Antineoplastics</a><br>

Continuities

Z - Vyzkumny zamer (s odkazem do CEZ)

Publication year

2008

Confidentiality

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Name of the periodical

Physiological Research

ISSN

0862-8408

e-ISSN

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Volume of the periodical

57

Issue of the periodical within the volume

5

Country of publishing house

CZ - CZECH REPUBLIC

Number of pages

7

Pages from-to

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UT code for WoS article

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EID of the result in the Scopus database

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