scholarly journals 5. FLAVIN-CONTAINING MONOOXYGENASES (FMO) ARE PHASE I ENZYMES OF XENOBIOTIC BIOTRANSFORMATION. NOMENCLATURE, STRUCTURE, MOLECULAR DIVERSITY, FUNCTION, PARTICIPATION IN THE FUNCTIONING OF THE BIOTRANSFORMATION SYSTEM. A COMPARISON WITH CYTOCHROMES Р450 (A

2020 ◽  
pp. 5
Author(s):  
Лев Павлович Смирнов ◽  
Lev Smirnov
Keyword(s):  
Phase I ◽  
Molecular Diversity ◽  
System A ◽  
Xenobiotic Biotransformation ◽  
Phase I Enzymes ◽  
Biotransformation System

scholarly journals ORGANIC ANION TRANSPORTERS. MOLECULAR DIVERSITY, STRUCTURE, CONTRIBUTION TO THE FUNCTIONING OF THE XENOBIOTIC BIOTRANSFORMATION SYSTEM IN ANIMALS (A REWIEW)

2017 ◽  
pp. 28
Author(s):  
Лев Павлович Смирнов ◽  
Ирина Викторовна Суховская ◽  
Екатерина Витальевна Борвинская ◽  
Lev Smirnov ◽  
Irina Sukhovskaya ◽  
...  
Keyword(s):  
Molecular Diversity ◽  
Organic Anion ◽  
Organic Anion Transporters ◽  
Anion Transporters ◽  
Xenobiotic Biotransformation ◽  
Diversity Structure ◽  
Biotransformation System

scholarly journals Detoxification of the tricyclic antidepressant opipramol and its analog – IS-noh by UGT enzymes before and after activation by phase I enzymes in rat liver microsomes

2021 ◽  
Author(s):  
Anna Mieszkowska ◽  
Koleta Hemine ◽  
Anna Skwierawska ◽  
Ewa Augustin ◽  
Zofia Mazerska
Keyword(s):  
Phase I ◽  
Rat Liver ◽  
Phase Ii ◽  
Oxidation Product ◽  
Liver Microsomes ◽  
Correct Selection ◽  
Rat Liver Microsomes ◽  
Recombinant Enzymes ◽  
Data Set ◽  
Phase I Enzymes

AbstractThe present studies were carried out to evaluate the simultaneous one-pot metabolism of opipramol (IS-opi) and analog (IS-noh) by phase I and phase II enzymes present in rat liver microsomes (RLM) as an alternative to separate testing with recombinant enzymes. This approach allows for more time-saving and cost-effective screening of the metabolism of newly discovered drugs. We also considered that the lack of results for phase II, including UGT, often creates problems in correct selection of valuable compounds. Moreover, microsomes data set is richer in the contest and provides medical scientist to determine also the susceptibility of drugs to undergo phase I and then phase II. In the present work, we have shown that IS-noh was metabolized in vitro by phase I enzymes to the oxidation product, which was next transformed with UGTs to glucuronide. The results showed also that the previously known oxidation product of opipramol was changed to previously no reported glucuronidation product by UDP-glucuronosyltransferases. In addition, unlike IS-noh, opipramol did not prove to be the substrate for UGTs. Therefore, tricyclic antidepressants depending on the structure can trigger a different response after contact with UGT enzymes. Some will metabolize directly with UGTs, others only after activation by phase I enzymes.

scholarly journals Coumarins and P450s, Studies Reported to-Date

Molecules ◽  
2019 ◽  
Vol 24 (8) ◽  
pp. 1620 ◽  
Author(s):  
Maryam Foroozesh ◽  
Jayalakshmi Sridhar ◽  
Navneet Goyal ◽  
Jiawang Liu
Keyword(s):  
Cytochrome P450 ◽  
Phase I ◽  
Cytochrome P450 Enzymes ◽  
Endogenous Compounds ◽  
Pharmacology And Toxicology ◽  
Xenobiotic Compounds ◽  
Phase I Enzymes

Cytochrome P450 enzymes (CYPs) are important phase I enzymes involved in the metabolism of endogenous and xenobiotic compounds mainly through mono-oxygenation reactions into more polar and easier to excrete species. In addition to their role in detoxification, they play important roles in the biosynthesis of endogenous compounds and the bioactivation of xenobiotics. Coumarins, phytochemicals abundant in food and commonly used in fragrances and cosmetics, have been shown to interact with P450 enzymes as substrates and/or inhibitors. In this review, these interactions and their significance in pharmacology and toxicology are discussed in detail.

scholarly journals The degree of anthropogenic load, gene polymorphism of the xenobiotic biotransformation system and congenital malformations as links in the same chain

2021 ◽  
Vol 100 (7) ◽  
pp. 658-662
Author(s):  
Olga N. Gulyaeva ◽  
Anna G. Zhukova ◽  
Anastasiya S. Kazitskaya ◽  
Faina A. Luzina ◽  
Marina V. Alekseeva ◽  
...  
Keyword(s):  
Gene Polymorphism ◽  
Pregnant Women ◽  
Congenital Malformations ◽  
The Body ◽  
Anthropogenic Load ◽  
Chemical Pollution ◽  
The South ◽  
Gstm1 Gene ◽  
Xenobiotic Biotransformation ◽  
Biotransformation System

Introduction. According to epidemiological observations, the level of congenital malformations in children is associated with the degree of chemical pollution of the environment and certain forms of genes of the I and II phases of the xenobiotic biotransformation system. The study aimed to determine and compare the index of anthropogenic load with the probability of occurrence of congenital malformations of the fetus in combination with gene polymorphisms of I and II phases of the xenobiotic biotransformation system in women living in different administrative territories in the South of Kuzbass. Material and methods. The level of air pollution in the cities of the South of the Kemerovo region (Kuzbass) was established. Prenatal screening of 1,426 pregnant women at the term of 15-18 weeks in the cities of the South of Kuzbass was carried out. The Real Time-PCR method was used to determine the gene polymorphism of the xenobiotic biotransformation system (CYP1A2, GSTM1) in 53 women of Novokuznetsk who gave birth to newborns with congenital malformations. Results. In the cities of the South of Kuzbass, with a critical and high degree of pollution of atmospheric air and waterways, many women are at risk of congenital malformations in offsprings. The A/A CYP1A2*1F genotype in combination with the deletion polymorphism of the GSTM1 gene in the mother is reliably associated with the occurrence of congenital malformations in offsprings (χ2 - 4.72; р - 0.030; OR - 5.56; CI - 1.05-29.32), and the C/ACYP1A2*1F genotype in combination with the normal functioning GSTM1 “+” gene is associated with resistance to the development of congenital malformations (χ2 - 12.53; p - <0.001; OR - 0.11; CI - 0.03-0.4 ). Conclusion. Against the background of an increasingly unfavourable ecological situation in Kuzbass and raising the number of newborns with congenital malformations, it is essential to include in the algorithm for early prenatal diagnosis the determination of the forms of genes of different phases of the xenobiotic metabolism system to elaborate an algorithm for reducing the xenobiotic load on the body of pregnant women during critical periods of fetal organogenesis.

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