Laser activation of anthracycline-related drugs combines chemotherapy
with photoablation for improved treatment. Hypericin, a structurally r
elated anthraquinone, was tested for laser activation and cytotoxicity
in human cancer cells. Viability of P3 squamous cell carcinoma cells
incubated with 1 to 20 mu g/mL hypericin was reduced by more than 95%
after 1 minute exposure at 4 degrees C to an argon laser (514 nm, 5 W)
, a KTP-532 laser (532 nm, 5 W), or a 20-A xenon lamp. Viability was r
educed over 90% in six human carcinoma, sarcoma, and melanoma cell lin
es by this combined treatment, but only trace toxicity was seen after
separate exposure to hypericin or light alone. These results show that
hypericin is a sensitive agent for phototherapy of human cancer cells
in vitro and indicate that this drug may be useful for tumor targetin
g via minimally invasive imaging-guided laser fiberoptics.