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Related Experiment Videos

Modulation of Pgp function by boswellic acids.

Claudia-Carolin Weber1, Karen Reising, Walter E Müller

  • 1Institute of Pharmacology, ZAFES, Biocenter, University of Frankfurt, Germany.

Planta Medica
|June 15, 2006
PubMed
Summary
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Boswellia serrata

Area of Science:

  • Pharmacology
  • Neuroscience
  • Natural Products Chemistry

Background:

  • Boswellic acids from Boswellia serrata are important for treating inflammatory conditions and cerebral edema.
  • Drug penetration into the brain is crucial for central nervous system-acting drugs.
  • P-glycoprotein (Pgp) significantly influences drug disposition and clinical efficacy.

Purpose of the Study:

  • To investigate the influence of Boswellia serrata extract and its main components on P-glycoprotein (Pgp) transport activity.
  • To assess the cerebral pharmacokinetics of boswellic acids and their interaction with Pgp at the blood-brain barrier.

Main Methods:

  • In vitro assays using a Pgp-expressing human lymphocytic leukaemia cell line (VLB cells) and porcine brain capillary endothelial cells (PBCEC cells).

Related Experiment Videos

  • Calcein acetoxymethyl ester (calcein-AM) was used as a Pgp substrate to measure transport inhibition.
  • Evaluation of the modulatory effects of Boswellia serrata extract (H15®) and individual boswellic acids on Pgp activity.

    • Main Results:

    • The Boswellia extract and keto-boswellic acids (11-keto-beta-boswellic acid and acetyl-11-keto-beta-boswellic acid) inhibited Pgp transport activity in both cell models at micromolar concentrations.
    • Boswellic acids lacking a keto group did not modulate Pgp activity.
    • The brain/plasma ratio for keto-boswellic acids was relatively low, suggesting limited Pgp inhibition relevance at the blood-brain barrier.

    Conclusions:

    • Boswellia serrata extract and its keto derivatives inhibit Pgp-mediated transport in vitro.
    • While Pgp inhibition at the blood-brain barrier may not significantly impact brain availability of other Pgp substrates due to low plasma levels, interactions at the gastrointestinal level are possible.
    • Further research is needed to fully elucidate the clinical implications of Pgp modulation by Boswellia serrata.