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The complex of Hypocrellin A with Al(3+) is prepared in water solution by a facile method. The water-solubility and stability of complexes are improved. Irradiation of Al(3+)-HA complex results in higher efficient generation of singlet oxygen ((1)O2) and photocleavage ability to CT DNA than HA. In vitro studies have illustrated that the Al(3+)-HA complex has anti-cancer activity.

We first synthesized and characterized a monomer ruthenium complex of hypocrellin B (HB) by chelation with Ru(bpy)2Cl2 (in which bpy = 2,2′-bipyridine). It possesses the photosensitizing properties and can be applied in photodynamic therapy (PDT). The chemiluminescence assays indicated that the photodamage ability of the complex is stronger than that of HB.

An amorphous formulation of hypocrellin A for photodynamic therapy is reported which can provide stable aqueous dispersion of such hydrophobic photosensitizers. In vitro studies have demonstrated the active uptake of amorphous formulation of hypocrellin A into the mitochondria of tumor cells. Compared with Tween-80 micelle embedded hypocrellin A, low dark-toxicity but similar light-toxicity of the amorphous one to drug impregnated tumor cells was observed. Thus, the potential of using amorphous formulation of hypocrellin A as drug delivery system for photodynamic therapy has been demonstrated.