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Phase I biotransformation reactions are integral to drug metabolism, predominantly involving oxidative, reductive, and hydrolytic transformations. Chief among these are oxidative reactions, which enhance the hydrophilicity of xenobiotics and introduce polar functional groups to facilitate their elimination from the body.
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Hydrolysis, a cornerstone of phase I biotransformation reactions, uses water to cleave chemical bonds. This process is pivotal in drug metabolism, generating more polar metabolites that can be easily excreted.
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Methylation is a phase II biotransformation process involving the attachment of a methyl group to a substrate. Enzymes known as methyltransferases orchestrate this reaction.
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Evaluating kratom alkaloids using PHASE.

Christopher R Ellis1, Rebecca Racz1, Naomi L Kruhlak1

  • 1Division of Applied Regulatory Science, Office of Clinical Pharmacology, Office of Translational Sciences, Center for Drug Evaluation and Research, United States Food and Drug Administration, Silver Spring, Maryland, United States of America.

Plos One
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Summary
This summary is machine-generated.

Kratom alkaloids were computationally analyzed for opioid receptor binding, revealing structural similarities to controlled opioids. This study provides a method to assess kratom

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Area of Science:

  • Pharmacology
  • Toxicology
  • Computational Chemistry

Background:

  • Kratom is promoted for opioid indications in the US without FDA approval.
  • Kratom contains numerous alkaloids, with limited data on most beyond mitragynine and 7-hydroxymitragynine.
  • Understanding kratom's alkaloid pharmacology is crucial for risk assessment.

Purpose of the Study:

  • To apply the Public Health Assessment via Structural Evaluation (PHASE) protocol to predict in silico binding profiles for 25 kratom alkaloids.
  • To facilitate the risk evaluation of kratom by understanding its alkaloid interactions with key receptors.
  • To experimentally verify the in silico predictions for a subset of kratom alkaloids.

Main Methods:

  • Utilized the PHASE protocol for in silico analysis of 25 kratom alkaloids.
  • Predicted binding profiles across opioid, adrenergic, and serotonin receptors.
  • Experimentally validated in silico findings using radioligand binding assays for selected alkaloids.

Main Results:

  • Kratom alkaloids exhibit structural similarities to controlled opioids.
  • Several kratom alkaloids demonstrate binding affinity for opioid, adrenergic, and serotonin receptors.
  • Mitragynine and 7-hydroxymitragynine were identified as potent binders at the mu opioid receptor.

Conclusions:

  • The PHASE protocol effectively identifies potential safety signals for kratom alkaloids.
  • In silico binding profiles can prioritize compounds for experimental safety evaluation.
  • This approach aids in the comprehensive risk assessment of botanical substances like kratom.