scholarly journals Effects of Cyclamen trochopteranthum on hepatic drug-metabolizing enzymes

2011 ◽  
Vol 63 (3) ◽  
pp. 545-555 ◽  
Author(s):  
Sevki Arslan ◽  
Ozden Ozgun ◽  
Gurbet Celik ◽  
Asli Semiz ◽  
Olcay Dusen ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Mrna Level ◽  
Drug Metabolizing Enzymes ◽  
Mrna Levels ◽  
Rt Pcr ◽  
Metabolizing Enzymes ◽  
Hepatic Drug ◽  
Tuber Extract ◽  
Different Doses

The modulatory effects of the Cyclamen trochopterantum tuber extract on hepatic drug-metabolizing enzymes, including aniline 4-hydroxylase (A4H; CYP2E1), ethoxyresorufin O-deethylase (EROD; CYP1A), methoxyresorufin O-demethylase (MROD; CYP1A), caffeine N-demethylase (C3ND; CYP1A2) aminopyrene N-demethylase (APND; CYP2C6), and erythromycin N-demethylase (ERND; CYP3A1), were examined in vivo in rats. The activities of all of these enzymes were induced by the cyclamen extract. In addition, Western-blot and RT-PCR results clearly showed that CYP2E1, CYP1A1/CYP1A2 and CYP2C6 protein and mRNA levels were substantially increased by four different doses of cyclamen. Although, the CYP3A1 protein level was increased significantly, the mRNA level was not changed. These results indicate that cyclamen tuber extract might have a potential not only to inhibit and/or induce the metabolism of certain co-administered drugs but also influence the development of toxicity and carcinogenesis due to the induction of the cytochrome P450-dependent drug-metabolizing enzymes.

Changes of Transporters and Drug-metabolizing Enzymes in Nephrotic Syndrome

2020 ◽  
Vol 21 (5) ◽  
pp. 368-378
Author(s):  
Yaqian Dong ◽  
Linna Gong ◽  
Xianyuan Lu ◽  
Mingguang Ye ◽  
Yu Lin ◽  
...  
Keyword(s):  
Drug Disposition ◽  
Mrna Level ◽  
Hepatic Function ◽  
Clinical Findings ◽  
Drug Metabolizing Enzymes ◽  
Mrna Levels ◽  
Pharmacokinetics And Pharmacodynamics ◽  
Metabolizing Enzymes ◽  
Adriamycin Nephropathy ◽  
Clinical Drugs

Background: Drug-metabolizing enzymes and transporters play key roles in drug disposition and drug interactions. The alterations of their expression will influence drug pharmacokinetics and pharmacodynamics. However, the changes in the expression of enzymes and transporters in the disease state are still unclear. Objective: Our study was to investigate the changes in the expression of main enzymes and drug transporters distributed in Adriamycin nephropathy rat liver, kidney, and intestine. Methods: An intravenous injection with a single dose of Adriamycin (6mg/kg) was made to establish Adriamycin nephropathy (AN) model and normal groups were injected with normal saline. Serum was collected for lipid metabolism, renal, and hepatic function measurement. The real-time PCR and western blot were applied to determine the mRNA and protein expression of drug enzymes and transporters. Results: In the kidney, a greater expression of Mdr1, Mrp2, Mrp4 Oat2 and Oct2 mRNA was found in AN rats as compared with control rats. In the liver, the expression of Bcrp mRNA was more doubled or tripled than control groups and downregulation of Mdr1, Mrp2, Mrp4 and Bsep gene expression was found in AN rats. Besides, we observed a downward trend of Cyp1a2, Cyp3a4 and Cyp2c9 mRNA levels in AN groups. In the duodenum, the expression of Mdr1 and Mrp3 mRNA level was decreased, while Bcrp and Mrp2 mRNA were increased. Conclusion: The changes in drug-metabolizing enzymes and transporters expression in AN rats were clarified, which may be beneficial for understanding the altered pharmacokinetics and pharmacodynamics of clinical drugs and reduce unexpected clinical findings for nephropathy patients.

Phenotyping of drug-metabolizing enzymes in adults: a review of in-vivo cytochrome P450 phenotyping probes

2000 ◽  
Vol 10 (3) ◽  
pp. 187-216 ◽  
Author(s):  
Daniel S. Streetman ◽  
Joseph S. Bertino ◽  
Anne N. Nafziger
Keyword(s):  
Cytochrome P450 ◽  
Drug Metabolizing Enzymes ◽  
Metabolizing Enzymes

scholarly journals Effect of 4-(4-Chlorobenzyl)pyridine on Rat Hepatic Microsomal Cytochrome P450 and Drug-Metabolizing Enzymes in Vivo and in Vitro.

2001 ◽  
Vol 24 (5) ◽  
pp. 505-509 ◽  
Author(s):  
Yasuna KOBAYASHI ◽  
Naomi OHSHIRO ◽  
Tadanori SASAKI ◽  
Shogo TOKUYAMA ◽  
Takashi TOBE ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Drug Metabolizing Enzymes ◽  
Metabolizing Enzymes ◽  
Microsomal Cytochrome ◽  
Microsomal Cytochrome P450

scholarly journals Chirality Matters: Biological Activity of Optically Pure Silybin and Its Congeners

2021 ◽  
Vol 22 (15) ◽  
pp. 7885
Author(s):  
Vladimír Křen
Keyword(s):  
Neurological Diseases ◽  
Biological Effects ◽  
Drug Metabolizing Enzymes ◽  
Metabolizing Enzymes ◽  
Biological Targets ◽  
Molecular Effects ◽  
Anisotropic Systems ◽  
Specific Activities ◽  
Optically Pure

This review focuses on the specific biological effects of optically pure silymarin flavo-nolignans, mainly silybins A and B, isosilybins A and B, silychristins A and B, and their 2,3-dehydro derivatives. The chirality of these flavonolignans is also discussed in terms of their analysis, preparative separation and chemical reactions. We demonstrated the specific activities of the respective diastereomers of flavonolignans and also the enantiomers of their 2,3-dehydro derivatives in the 3D anisotropic systems typically represented by biological systems. In vivo, silymarin flavonolignans do not act as redox antioxidants, but they play a role as specific ligands of biological targets, according to the “lock-and-key” concept. Estrogenic, antidiabetic, anticancer, antiviral, and antiparasitic effects have been demonstrated in optically pure flavonolignans. Potential application of pure flavonolignans has also been shown in cardiovascular and neurological diseases. Inhibition of drug-metabolizing enzymes and modulation of multidrug resistance activity by these compounds are discussed in detail. The future of “silymarin applications” lies in the use of optically pure components that can be applied directly or used as valuable lead structures, and in the exploration of their true molecular effects.

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