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Hypericin: a potential antiglioma therapy

W T Couldwell1, R Gopalakrishna, D R Hinton

  • 1Department of Neurological Surgery, University of Southern California School of Medicine, Los Angeles.

Neurosurgery
|October 1, 1994
PubMed
Summary
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Hypericin, a plant-derived compound, shows promise as an antiglioma agent by inhibiting glioma cell growth and inducing apoptosis. Further clinical trials are suggested for this potential cancer treatment.

Area of Science:

  • Oncology
  • Pharmacology
  • Biochemistry

Background:

  • Hypericin, a plant-derived polycyclic aromatic dione, is under clinical evaluation for antiviral properties against human immunodeficiency virus (HIV).
  • Hypericin is recognized as a potent inhibitor of protein kinase C.
  • Gliomas are primary brain tumors with limited treatment options.

Purpose of the Study:

  • To investigate the potential of hypericin as an inhibitor of glioma cell growth.
  • To determine the mechanism of hypericin's effect on glioma cells, specifically whether it is cytostatic or cytocidal.
  • To assess the influence of visible light on hypericin's inhibitory effects.

Main Methods:

  • Treatment of established (U87) and low-passage (93-492) human glioma cell lines with varying concentrations of hypericin for 48 hours.

Related Experiment Videos

  • Measurement of [3H]thymidine uptake to assess glioma cell proliferation in the presence and absence of visible light.
  • Analysis of deoxyribonucleic acid (DNA) fragmentation using agarose gel electrophoresis to detect apoptosis.

    • Main Results:

    • Hypericin demonstrated dose-dependent inhibition of glioma cell growth, with significant effects observed at low micromolar concentrations.
    • A concentration of 10 mumol/L hypericin reduced [3H]thymidine uptake by 62% in U87 and 76% in 93-492 cell lines.
    • Visible light slightly enhanced hypericin's inhibitory effect in the A172 glioma cell line.
    • DNA analysis revealed a characteristic "ladder" pattern of oligonucleosome-sized fragments, indicating hypericin induces apoptosis (programmed cell death) in glioma cells.

    Conclusions:

    • Hypericin exhibits significant antiglioma activity in vitro by inhibiting proliferation and inducing apoptosis.
    • The established safety profile of hypericin supports its potential as a therapeutic agent for gliomas.
    • Clinical trials are warranted to evaluate hypericin's efficacy as an antiglioma drug.