On the nature of ‘haematoporphyrin derivative’

Bonnett, Raymond; Ridge, Richard J.; Scourides, Panayiotis A.; Berenbaum, M. C.

doi:10.1039/p19810003135

Cited by 107 publications

(53 citation statements)

References 1 publication

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Full details of the preparation and fractionation using high-pressure liquid chromatography (HPLC) are given in Bonnett et al (1981) which also records the preparation of authen- 1) and measurement of the depth of necrosis usually presented no great difficulty if measurements were made over the centre of the tumour, where the skin surface was at right angles to thle light beam. About 600 tumours -were used in the w-ork summarized lhere.…”

Section: Methodsmentioning

confidence: 99%

“…The separation of the major components of HpD on a preparative scale by HPLC has been described (Bonnett et al, 1981) and a typical separation is shown, with the components and fractions identified, in Fig. 2.…”

Section: Chrormatographic Separationmentioning

confidence: 99%

“…Under these conditions the simple porphyrin acetates do not survive, but haematoporphyrin (1), hydroxyethylvinyldeuteroporphyrin (4 and 5), and protoporphyrin (9) are the major recognized constituents (Bonnett et al, 1980). These compounds, prepared by standard methods, were tested in a separate series of experiments.…”

Section: Chrormatographic Separationmentioning

confidence: 99%

“…It is a complex mixture, and it is clearly important to identify the components responsible for its anti-tumour effects in vivo and to use these in a pure form. HpD has therefore been fractionated by preparative high-pressure liquid chromatography (Bonnett et al, 1978(Bonnett et al, , 1980(Bonnett et al, , 1981 and we now report the activities of the various components, as judged by an in vivo assay using a transplantable mouse tumour.…”

mentioning

confidence: 99%

See 3 more Smart Citations

In vivo biological activity of the components of haematoporphyrin derivative

Berenbaum¹,

Bonnett²,

Scourides³

1982

Br J Cancer

167

View full text Add to dashboard Cite

Summary.-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.

show abstract

Section: Methodsmentioning

confidence: 99%

Section: Chrormatographic Separationmentioning

confidence: 99%

Section: Chrormatographic Separationmentioning

confidence: 99%

mentioning

confidence: 99%

See 2 more Smart Citations

In vivo biological activity of the components of haematoporphyrin derivative

Berenbaum¹,

Bonnett²,

Scourides³

1982

Br J Cancer

167

View full text Add to dashboard Cite

show abstract

“…The photosensitiser most widely used at present is "haematoporphyrin derivative" (HpD), a complex mixture of porphyrins (Bonnett et al, 1980(Bonnett et al, , 1981Berenbaum et al, 1982). HpD is excited at a number of discrete wavebands, most intensely by violet light at 400-410nm (the Soret band), and with much less (and decreasing) intensity by bands at 500-505nm, 535-540nm, 565-575 nm and 620-635 nm.…”

mentioning

confidence: 99%

Wavelength and light-dose dependence in tumour phototheraphy with haematoporphyrin derivative

Gemert¹,

Berenbaum²,

Gijsbers³

1985

Br J Cancer

101

View full text Add to dashboard Cite

Summary Red light (c. 630 nm) is almost universally used in tumour phototherapy as it is the most penetrating of the porphyrin excitation wavebands. However, measurements of tumour attenuation of light of different wavelengths and of the excitation spectrum of haematoporphyrin derivative in vitro suggested that green light might be more efficient than red in destroying thin tumours. Experimentally, we confirmed this for tumours up to -1.2mm thick, a depth exceeding that of most carcinomas-in-situ. The superiority of green light over red in terms of the illumination time required to produce equivalent depths of necrosis may extend to greater depths (3-4 mm) if the former is produced by an argon laser and the latter by an argon-pumped dye laser.The relation between depth of necrosis zn and light dose D is shown to be zn=a x 'n(D/lA) where 0A iS the attenuation coefficient for light at wavelength A and 0A the threshold light dose for producing necrosis at that wavelength. This logarithmic relationship suggests that it may be difficult to eradicate large tumours merely by increasing the light dose, and indicates the need for other approaches.

show abstract

Pharmaceutical development and medical applications of porphyrin-type macrocycles

Mody

2000

J. Porphyrins Phthalocyanines

View full text Add to dashboard Cite

The current state of pharmaceutical development of porphyrin-type macrocycles in medicine is highlighted. Currently, several porphyrinoid-based drugs are under various stages of development as phototherapeutic agents, X-ray radiation enhancers and boron neutron capture agents. These compounds represent a burgeoning class of pharmacological agents that are potentially useful in an array of treatment areas.

show abstract

On the nature of ‘haematoporphyrin derivative’

Cited by 107 publications

References 1 publication

In vivo biological activity of the components of haematoporphyrin derivative

In vivo biological activity of the components of haematoporphyrin derivative

Wavelength and light-dose dependence in tumour phototheraphy with haematoporphyrin derivative

Pharmaceutical development and medical applications of porphyrin-type macrocycles

Contact Info

Product

Resources

About