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Related Experiment Videos

Bisandrographolide from Andrographis paniculata activates TRPV4 channels.

Paula L Smith1, Katherine N Maloney, Randy G Pothen

  • 1Department of Cardiology, Howard Hughes Medical Institute, Children's Hospital, Boston, Massachusetts 02115, USA.

The Journal of Biological Chemistry
|August 11, 2006
PubMed
Summary

Researchers identified bisandrographolide A (BAA) from Andrographis paniculata as a potent activator of TRPV4 channels. This discovery offers new insights into plant-derived compounds targeting transient receptor potential channels.

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Area of Science:

  • Pharmacology
  • Molecular Biology
  • Natural Products Chemistry

Background:

  • Transient receptor potential (TRP) channels are crucial in sensory perception and are modulated by plant-derived compounds like capsaicin and menthol.
  • Existing research highlights plant compounds' interaction with TRP channels, necessitating further exploration for novel activators or blockers.

Purpose of the Study:

  • To identify novel plant-derived compounds that modulate TRP channels, specifically focusing on TRPV3 and TRPV4.
  • To characterize the activity of bisandrographolide A (BAA), a compound isolated from Andrographis paniculata, on various TRPV channel subtypes.

Main Methods:

  • Screening of 50 Chinese herbal plant extracts using calcium-imaging assays to detect activity on TRPV3 and TRPV4 channels.
  • Fractionation of active extracts and purification of bisandrographolide A (BAA) for detailed pharmacological characterization.

Related Experiment Videos

  • Electrophysiological recordings in cell lines (HEK293T, 308 cells) to assess BAA's effect on TRPV4 channel activity in whole-cell and outside-out patch configurations.

    • Main Results:

    • An extract from Andrographis paniculata demonstrated potent activation of TRPV4 channels.
    • Purified bisandrographolide A (BAA) selectively activated TRPV4 channels with an EC50 of 790-950 nm, showing no significant activity on TRPV1, TRPV2, or TRPV3.
    • BAA induced TRPV4 currents in keratinocytes and HEK293T cells, confirming its membrane-delimited activation mechanism. Andrographolide, a related compound, did not affect TRPV4 activity.

    Conclusions:

    • Bisandrographolide A (BAA) is identified as a specific activator of TRPV4 channels.
    • The findings suggest that BAA's activation of TRPV4 channels may contribute to the traditional medicinal effects attributed to Andrographis extract.
    • This research expands the understanding of plant-derived modulators of TRP channels and their potential therapeutic applications.