The Chemotherapeutic Action of Phenanthridine Compounds

Goodwin, L. G.; Goss, M. D.; Lock, J. A.; Walls, L. P.

doi:10.1111/j.1476-5381.1950.tb01013.x

Cited by 10 publications

(8 citation statements)

References 12 publications

(1 reference statement)

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“…That the bile should be a major route of ethidium excretion is in accordance with the findings of Schanker & Soloman (1963), Schanker (1968) and Nayak & Schanker (1969) who presented evidence for the active transport of tertiary and quarternary ammonium compounds into the bile of rats. Biliary excretion of phenanthridines has also been reported by other workers (Goodwin, Goss & Lock, 1950;Taylor, 1960a;MacGregor & Clarkson, 1971. In rabbits with cannulated bile ducts, no drug was found in the faeces and the rate of appearance of radioactivity in the bile over the first 12 h following treatment was approximately the same as was found in the faeces of uncannulated ethidium-treated rabbits.…”

Section: Discussionsupporting

confidence: 81%

Ethidium bromide: pharmacokinetics and efficacy against trypanosme infections in rabbits and calves

Gilbert

Newton

1982

Parasitology

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[14C]ethidium bromide has been used to determine drug levels in tissues and body fluids of rabbits and calves following intramuscular injection. Uninfected and Trypanosoma brucei- or Trypanosoma congolense-infected animals were studied. Blood and tissue fluid level reached a maximum with 1 h and then fell rapidly; after 96 h 80-90% of the radioactivity injected had been excreted, approximately one third in urine and two thirds in faeces. By 1 h after injection of 1 mg [14C]ethidium/kg into a T. congolense-infected calf, 70-80% of the radioactivity in blood was found to be bound to trypanosomes. Doses of 1 or 10 mg/kg were found not to be curative for T congolense or T. brucei infections in rabbits: drug treatment resulted in a period of sub-patent parasitaemia which was always followed by a relapse. Examination of the prophylactic action of ethidium in rabbits showed that the drug extended the pre-patent period following trypanosome inoculation but provided no absolute protection. A period of "apparent' prophylaxis observed after drug treatment of infected rabbits has been correlated with the presence of anti-trypanosome IgG in the serum.

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Section: Discussionsupporting

confidence: 81%

Ethidium bromide: pharmacokinetics and efficacy against trypanosme infections in rabbits and calves

Gilbert

Newton

1982

Parasitology

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“…The first of these drugs has been shown to be active Goodwin, Goss, Lock, and Walls, 1950) when given during the incubation period, but not against an established infection, whereas 3C47 is active under both conditions. It seems probable from this evidence that although 6C46 is toxic to the blood forms of the parasite, it is either inactive against the intracellular forms, or does not penetrate readily enough to produce a concentration lethal to the enclosed parasites.…”

Section: Resultsmentioning

confidence: 99%

“…The effects of drugs upon T. cruzi in tissue culture The method of maintaining T. cruzi in tissue culture was similar to that described by Hawking (1946), with a modification in the method of infection. Explants from the hearts of embryo rats were placed in a thick suspension of T. cruzi in serum-Tyrode mixture.…”

Section: Absorption Of Drugs By Trypanosomesmentioning

confidence: 99%

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The Chemotherapeutic Action of Phenanthridine Compounds

1950

British Journal of Pharmacology and Chemotherapy

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“…2: 7-Dicarbethoxyamino Phenanthridinium Compounds (Table V).-It has been reported previously that interference with the primary amino groups in the 2: 7-positions greatly reduces trypanocidal activity against African species of trypanosomes, though such compounds may possess activity against the South American T. cruzi (Goodwin et al, 1950). I have prepared and tested a number of such compounds.…”

Section: Resultsmentioning

confidence: 99%

Trypanocidal Action of Phenanthridine Compounds: Further 2:7‐diamino Phenanthridinium Compounds

Woolfe¹

1956

British Journal of Pharmacology and Chemotherapy

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Woolfe (1952) showed that the trypanocidal activity of dimidium bromide (2: 7-diamino-10-methyl-9-phenyl-phenanthridinium bromide; I) was influenced by changing the quaternary group, and later (Woolfe, 1956) (Woolfe, 1952) were used, and drugs were given in single doses subcutaneously to mice. The Median Curative Dose (CD5O) was estimated as the dose necessary to remove parasites from the peripheral blood of 50% of infected mice for a period of not less than one month. Active drugs were compared with dimidium (activity taken as 1) on the basis of the CD5O. RESULTS2 : 7-Diamino-9-phenyl-phenanthridinium Compounds (Table I).-I previously (Woolfe, 1952) discussed the effect of n-alkyl and of allyl-quaternating groups. I have now tried a number of quaternating groups containing hetero-atoms, and in the TABLE I

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The Chemotherapeutic Action of Phenanthridine Compounds

Cited by 10 publications

References 12 publications

Ethidium bromide: pharmacokinetics and efficacy against trypanosme infections in rabbits and calves

Ethidium bromide: pharmacokinetics and efficacy against trypanosme infections in rabbits and calves

The Chemotherapeutic Action of Phenanthridine Compounds

Trypanocidal Action of Phenanthridine Compounds: Further 2:7‐diamino Phenanthridinium Compounds

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