The effects of 1,7-bis(p-aminophenoxy)heptane (153C51) on glucose utilization by Schistosoma mansoni

Watts, Stuart D.M.

doi:10.1016/0306-4492(78)90082-5

Cited by 5 publications

(7 citation statements)

References 15 publications

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“…Drug preparation and administration, mouse infection and maintenance, and the collection of adult schistosomes were performed as described previously (Watts, 1978) unless specified otherwise.…”

Section: Methodsmentioning

confidence: 99%

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Lysosomes and tegument pathology in the chemotherapy of schistosomiasis with 1,7 -bis(p-aminophenoxy)heptane(153C51)

Watts¹,

Orpin²,

MacCormick³

1979

Parasitology

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SUMMARYOne therapeutic oral dose (400 mg/kg) of 153C51 administered to infested mice caused pathological changes in the dorsal region of the tegument of maleSchistosoma mansoniduring the period 3–24 h after treatment. These changes occurred prior to the ‘hepatic shift’. At the ultrastructural level they consisted of a gradual accumulation in the tegument epidermis of numerous membranous inclusions with the characteristics of residual lysosomes and changes in the localization of acid phosphatase, a lysosomal enzyme. It seemed likely that these changes were due to inhibition or exhaustion of enzyme in the epidermis, followed by re-synthesis of enzyme in the cell bodies and its export to the epidermis. The elimination of hydrolytic activity from lysosomes in the epidermis would explain the accumulation of residual lysosomes. Drug- treated parasites retained their disguise of host red blood cell ghost antigens as shown by indirect fluorescent antibody-labelling and, therefore, it seemed unlikely that immunological factors could be important in producing the tegument pathology.

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Section: Methodsmentioning

confidence: 99%

“…To date, the nature of the metabolic lesion initiating this shift remains uncertain. Previous suggestions that 153C51 and a related secondary amine stressed schistosomes by inhibiting glucose transport (Standen, 1962;Bueding, 1962) have been discounted by recent experiments (Watts, 1978).…”

Section: Introductionmentioning

confidence: 97%

Lysosomes and tegument pathology in the chemotherapy of schistosomiasis with 1,7 -bis(p-aminophenoxy)heptane(153C51)

Watts¹,

Orpin²,

MacCormick³

1979

Parasitology

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“…Both Edwards et al (1981) and Rew et al (1983) demonstrated differential effects of the drug on surface properties of immature and adult flukes, and the former workers considered that tegumental damage is the primary drug effect which may lead to a small but insignificant decrease in glucose uptake. This postulate is supported by the effects of 1, 1-bis (p-aminophenoxy) heptane on S. mansoni (Watts, 1978) but it is, nevertheless, difficult to reconcile the conflicting data on glucose transport and the action of diamphenethide-amine.…”

Section: Other Classes Of Anthelmintic Drugsmentioning

confidence: 99%

“…Thus hycanthone causes gross lesions on the surface of the male of S. mansoni involving flattening or complete loss of the tubercles (Senft & Hillman, 1976): the effects of hycanthone on the female are directed preferentially towards the vitellaria and intestine. Similarly, the schistosomicidal properties of BW484C, a 5-nitro-4-thiazoline, and 153C51, an aminophenoxy heptane, are a reflection of selective damage to the male tegument; the former compound facilitates hepatic shift and host phagocyte attack (Watts, 1978(Watts, , 1986Watts, Orpin & McCormick, 1979). With these and other compounds damage to the tegument of the male schistosome appears to be restricted to the dorso-lateral surface and no indication of morphological changes to the surface of the gynaecophoral canal has been obtained.…”

Section: Anthelmintic Drugs Digeneamentioning

confidence: 99%

The interactions between drugs and the parasite surface

Chappell

1988

Parasitology

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SUMMARYThe interrelationships between drugs and parasite surfaces are considered under the headings of (a) effects on membrane transport, (b) drug uptake mechanisms and (c) effects on surface morphology and function: praziquantel is discussed under a separate heading. The range of chemotherapeutic compounds that cause permeability changes and concomitant morphological disruption is discussed in terms of mode of drug action. Interpretation of the available data renders it difficult to identify the primary mode of action in the drugs considered. Drug uptake mechanisms are known for relatively few compounds; drug resistance as a function of drug acquisition is discussed. The role of the parasite surface as a specific drug target is argued.

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“…Subcurative doses of amoscanate also damage the tegument (Voge & Bueding, 1980) as does the experimental schistosomicide 1,7,-bis (p-aminophenoxy) heptane (Oyerinde, 1976;Watts, Orpin & MacCormick, 1979). However, earlier reports that 1,7-bis {jpaminophenoxy) heptane acts by inhibition of glucose uptake have been discounted (Watts, 1978). The biochemical changes induced by these drugs which damage the tegument are not known.…”

Section: Hycanthone and Oxamniquinementioning

confidence: 99%

Recent advances in schistosome biochemistry

Coles

1984

Parasitology

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The effects of 1,7-bis(p-aminophenoxy)heptane (153C51) on glucose utilization by Schistosoma mansoni

Cited by 5 publications

References 15 publications

Lysosomes and tegument pathology in the chemotherapy of schistosomiasis with 1,7 -bis(p-aminophenoxy)heptane(153C51)

Lysosomes and tegument pathology in the chemotherapy of schistosomiasis with 1,7 -bis(p-aminophenoxy)heptane(153C51)

The interactions between drugs and the parasite surface

Recent advances in schistosome biochemistry

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