The Role of Oxidative Drug Metabolizing Enzymes in Liver and Lung Specific Toxicity

1999 ◽  
pp. 173-182
Author(s):  
Richard M. Philpot
Keyword(s):  
Drug Metabolizing Enzymes ◽  
Metabolizing Enzymes

Role of Citrus Limonoid as a Possible Bioavailability Enhancer

2020 ◽  
Vol 859 ◽  
pp. 132-138
Author(s):  
Nusara Piyapolrungroj ◽  
Panadda Phattanawasin ◽  
Uthai Sotanaphun ◽  
May Phyu Thein Maw
Keyword(s):  
Drug Absorption ◽  
Oral Delivery ◽  
The Body ◽  
Drug Metabolizing Enzymes ◽  
Dependent Manner ◽  
Drug Bioavailability ◽  
Concentration Dependent Manner ◽  
Metabolizing Enzymes ◽  
Calcein Am

The oral delivery is the most practical route to deliver drugs into the body, however drug-metabolizing enzymes and drug transporters can play important roles in modulating drug absorption. This study intended to find a natural bioenhancer for improving drug bioavailability. Two limonoids, including limonin deepoxy and nomilin, isolated from pomelo pulp were studied and the inhibition effects on human CYP3A4 and P-gp were investigated. Testosterone 6β-hydroxylation was performed in recombinant human CYP3A4 to discover the effects on CYP activity. Daunorubicin transport in Caco-2 and calcein-AM uptake in LLC-PK1 and LLC-GA5-COL300 were conducted to evaluate the effects on P-gp function. The results show that both limonin deepoxy and nomilin could inhibit CYP3A4 and only nomilin exhibited mechanism-based inhibition. Nomilin was able to inhibit human P-gp in the concentration-dependent manner. Taken together, nomilin demonstrated strong activities on both CYP3A4 and P-gp, indicating that nomilin could possibly be used as a bioavailability enhancer.

scholarly journals Application of a novel regulatable Cre recombinase system to define the role of liver and gut metabolism in drug oral bioavailability

2015 ◽  
Vol 465 (3) ◽  
pp. 479-488 ◽  
Author(s):  
Colin J. Henderson ◽  
Lesley A. McLaughlin ◽  
Maria Osuna-Cabello ◽  
Malcolm Taylor ◽  
Ian Gilbert ◽  
...  
Keyword(s):  
Mouse Model ◽  
Oral Bioavailability ◽  
Drug Disposition ◽  
Single Agent ◽  
Cre Recombinase ◽  
Drug Metabolizing Enzymes ◽  
Relative Role ◽  
Metabolizing Enzymes ◽  
Gut Metabolism

We describe a mouse model where the functions of key drug-metabolizing enzymes are deleted in liver or liver and gut by application of a single agent, allowing the relative role of each tissue in drug disposition to be established.

scholarly journals The role of the microbiome and psychosocial stress in the expression and activity of drug metabolizing enzymes in mice

2020 ◽  
Vol 10 (1) ◽  
Author(s):  
Nina Zemanová ◽  
Pavel Anzenbacher ◽  
Iveta Zapletalová ◽  
Lenka Jourová ◽  
Petra Hermanová ◽  
...  
Keyword(s):  
Psychosocial Stress ◽  
Drug Metabolizing Enzymes ◽  
Metabolizing Enzymes ◽  
Expression And Activity
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