Abstract
The in vivo biological activity of various fractions and components of haematoporphyrin derivative (HpD) have been determined by measuring the depth of necrosis of implanted tumours in mice exposed to light after the administration of standard doses of porphyrins dissolved in alkali. In this assay, haematoporphyrin, hydroxyethylvinyldeuteroporphyrin and protoporphyrin are inactive, but the mono- and di-acetates of haematoporphyrin (which are major components of HpD) and acetoxyethylvinyldeuteroporphyrin are active. However, the situation appears to be more complex than this. The normal method for preparing HpD for injection involves an alkali treatment which causes hydrolysis and elimination of the acetoxy functions, and the only recognized products (haematoporphyrin, hydroxyethylvinyldeuteroporphyrin and protoporphyrin) are inactive in the in vivo assay. It is concluded that the active component here is a porphyrin, possibly a dimer or oligomer, which is retained on the column during the normal separation by HPLC. This conclusion is supported by the observations that (i) the crude material obtained from the spent column is active without further alkali treatment, and (ii) activity develops over 30 min, when HpD or the mono- or diacetates of haematoporphyrin are treated with sodium bicarbonate in aqueous DMSO. The advantages of working with a pure substance (e.g. haematoporphyrin diacetate) rather than a mixture (HpD) are stressed.
This is a preview of subscription content, access via your institution
Access options
Subscribe to this journal
Receive 24 print issues and online access
$259.00 per year
only $10.79 per issue
Buy this article
- Purchase on Springer Link
- Instant access to full article PDF
Prices may be subject to local taxes which are calculated during checkout
Similar content being viewed by others
Rights and permissions
About this article
Cite this article
Berenbaum, M., Bonnett, R. & Scourides, P. In vivo biological activity of the components of haematoporphyrin derivative. Br J Cancer 45, 571–581 (1982). https://doi.org/10.1038/bjc.1982.94
Issue Date:
DOI: https://doi.org/10.1038/bjc.1982.94
This article is cited by
-
Photodynamic therapy with mTHPC and polyethylene glycol-derived mTHPC: a comparative study on human tumour xenografts
British Journal of Cancer (1999)
-
Characterization of a murine model for the rapid assessment of acute photodynamic response in tumour and muscle
Lasers in Medical Science (1997)
-
Tetra(m-hydroxyphenyl)chlorin clinical photodynamic therapy of early bronchial and oesophageal cancers
Lasers in Medical Science (1996)
-
In vitro and in vivo photodynamic effects of a new photosensitizer: Tetra(m-hydroxyphenyl)chlorin
Lasers in Medical Science (1994)
-
Selectivity ofmeso-tetra(hydroxyphenyl)porphyrins and chlorins and of photofrin II in causing photodamage in tumour, skin, muscle and bladder. The comcept of cost-benefit in analysing the results
Lasers in Medical Science (1993)