In vivo biological activity of the components of haematoporphyrin derivative.

摘要: The in vivo biological activity of various fractions and components haematoporphyrin derivative (HpD) have been determined by measuring the depth necrosis implanted tumours mice exposed to light after administration standard doses porphyrins dissolved alkali. In this assay, haematoporphyrin, hydroxyethylvinyldeuteroporphyrin protoporphyrin are inactive, but mono- di-acetates (which major HpD) acetoxyethylvinyldeuteroporphyrin active. However, situation appears be more complex than this. normal method for preparing HpD injection involves an alkali treatment which causes hydrolysis elimination acetoxy functions, only recognized products (haematoporphyrin, protoporphyrin) inactive assay. It is concluded that active component here a porphyrin, possibly dimer or oligomer, retained on column during separation HPLC. This conclusion supported observations (i) crude material obtained from spent without further treatment, (ii) develops over 30 min, when diacetates treated with sodium bicarbonate aqueous DMSO. advantages working pure substance (e.g. diacetate) rather mixture stressed.