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Related Concept Videos

Pharmacogenetics of Phase I Enzymes: Cytochrome P450 Isozymes01:28

Pharmacogenetics of Phase I Enzymes: Cytochrome P450 Isozymes

Cytochrome P450 (CYP450) enzymes are a superfamily of heme-containing monooxygenases that play a pivotal role in Phase I drug metabolism by catalyzing oxidation and reduction reactions.These enzymes transform lipophilic xenobiotics into more hydrophilic metabolites, facilitating subsequent Phase II conjugation and eventual excretion. The CYP450 family is classified into families (e.g., CYP1–CYP3) and subfamilies (e.g., CYP2A, CYP2C), based on amino acid sequence homology.CYP450 isoenzymes,...
Pharmacokinetics: Drug–Drug Interactions01:25

Pharmacokinetics: Drug–Drug Interactions

Drug interactions occur when the pharmacological effect of one drug is altered by another substance, either enhancing or diminishing its activity. The drug whose activity is altered is known as the object drug, and the substance causing the alteration is called the agent drug or the precipitant. The net effects of these interactions are mostly undesirable, leading to decreased effectiveness or increased adverse effects. In rare cases, interactions can be beneficial, such as the enhanced...
Pharmacogenetics of Drug Metabolism: Overview01:27

Pharmacogenetics of Drug Metabolism: Overview

Genetic polymorphism in drug metabolism is crucial to the inter-individual variability observed in drug responses. Drug metabolism primarily involves the chemical modification of drugs and other xenobiotics to enhance their elimination by increasing their polarity. Two main classes of enzymes mediate this biotransformation process: Phase I enzymes, primarily cytochrome P450s, catalyze oxidation and reduction reactions, while other enzymes, such as esterases, mediate hydrolysis, and Phase II...
Drug Metabolism: Phase II Reactions01:14

Drug Metabolism: Phase II Reactions

Phase II reactions are essential for the detoxification and elimination of drugs from the body. These reactions involve the conjugation of parent drugs or their phase I metabolites with endogenous molecules, resulting in more hydrophilic drug conjugates. The primary conjugation reactions in this phase are sulfation and glucuronidation. Both sulfation and glucuronidation typically produce biologically inactive metabolites. However, in some cases involving prodrugs, active metabolites may be...
Drug toxicity: Drug–Drug Interaction01:30

Drug toxicity: Drug–Drug Interaction

Drug–drug interactions can precipitate toxicity through multiple mechanisms. Absorption interactions alter how drugs enter the body, exemplified when ranitidine increases the absorption of basic drugs, while cholestyramine decreases the levels of propranolol. Protein binding interactions occur when drugs share the same binding sites on plasma proteins. Drugs like aspirin and warfarin, when bound in excess, can lead to increased free drug concentrations, enhancing the potential for...
Drug toxicity: Idiosyncratic Reactions01:16

Drug toxicity: Idiosyncratic Reactions

Idiosyncratic drug reactions represent abnormal chemical responses that vary significantly among individuals, ranging from extreme sensitivity to low doses to insensitivity to high doses. These reactions often occur due to the drug's covalent binding with serum proteins, forming a foreign hapten that triggers an immunotoxicological response. The variability in drug reactions has a strong pharmacogenetic foundation, with genetic differences crucial in how individuals metabolize drugs. For...

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Related Experiment Video

Updated: Jun 10, 2026

Mass Spectrometry and Luminogenic-based Approaches to Characterize Phase I Metabolic Competency of In Vitro Cell Cultures
10:44

Mass Spectrometry and Luminogenic-based Approaches to Characterize Phase I Metabolic Competency of In Vitro Cell Cultures

Published on: March 28, 2017

Identification of cytochrome P450 (CYP) isoforms involved in the metabolism of corynoline, and assessment of its

Zhong-Ze Fang1, Yan-Yan Zhang, Guang-Bo Ge

  • 1Laboratory of Pharmaceutical Resource Discovery, Dalian Institute of Chemical Physics, Chinese Academy of Sciences, Dalian, 116023, China.

Phytotherapy Research : PTR
|July 20, 2010
PubMed
Summary

Corynoline, a plant alkaloid, is metabolized by CYP3A4 and CYP2C9 enzymes, potentially leading to herb-drug interactions. This study details its metabolic pathways and inhibitory effects on key drug-metabolizing enzymes.

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Last Updated: Jun 10, 2026

Mass Spectrometry and Luminogenic-based Approaches to Characterize Phase I Metabolic Competency of In Vitro Cell Cultures
10:44

Mass Spectrometry and Luminogenic-based Approaches to Characterize Phase I Metabolic Competency of In Vitro Cell Cultures

Published on: March 28, 2017

Area of Science:

  • Pharmacology
  • Drug Metabolism
  • Natural Products Chemistry

Background:

  • Corynoline, an isoquinoline alkaloid from Corydalis, exhibits diverse pharmacological activities.
  • Understanding its metabolism is crucial for predicting herb-drug interactions.

Purpose of the Study:

  • To investigate the metabolism of corynoline in human liver microsomes (HLMs).
  • To identify the specific cytochrome P450 (CYP) isoforms involved in corynoline metabolism.
  • To evaluate the inhibitory potential of corynoline on major CYP enzymes.

Main Methods:

  • Incubation of corynoline with HLMs and NADPH to identify metabolites.
  • Chemical inhibition studies and assays with recombinant CYP isoforms (CYP2C9, CYP3A4).
  • Enzyme kinetic analysis to determine inhibition types (competitive, noncompetitive) and constants (IC50, Ki).
  • Time-dependent inhibition (TDI) assays for CYP3A4 inactivation.

Main Results:

  • Two metabolites (M-1 and M-2) were identified, with CYP2C9 primarily forming M-1 and CYP3A4 forming M-2.
  • Corynoline potently inhibited CYP3A4 (IC50 = 3.3 µM) and CYP2C9 (IC50 = 31.5 µM).
  • Noncompetitive inhibition of CYP3A4 (Ki = 3.2 µM) and competitive inhibition of CYP2C9 (Ki = 6.3 µM) were observed.
  • Time-dependent inhibition of CYP3A4 by corynoline was confirmed with K(I) = 6.8 µM and k(inact) = 0.07 min⁻¹.

Conclusions:

  • Corynoline is metabolized by CYP2C9 and CYP3A4.
  • Corynoline exhibits significant inhibitory effects on CYP3A4 and CYP2C9, suggesting potential for herb-drug interactions.
  • The findings are important for the safe and effective clinical application of corynoline and related herbal medicines.