2 edition of interrelation of hycanthone and related motagenic antischistosomal compounds with DNA found in the catalog.
interrelation of hycanthone and related motagenic antischistosomal compounds with DNA
Ph.D. thesis. Typescript.
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The intercalation of hycanthone and related mutagenic antischistosomal compounds with DNA. Author: Jahargir, M. ISNI: Awarding Body: University of Bradford Current Institution: University of Bradford Date of Award: Availability of Full Text.
43 Mutation Research, 55 () Elsevier/North-Holland Biomedical Press GENETIC ACTIVITIES OF HYCANTHONE AND SOME OTHER ANTISCHISTOSOMAL DRUGS TONG-MAN ONG * National InstiCited by: 1.
Mutat Res. ;55(1) Genetic activities of hycanthone and some other antischistosomal drugs. Ong TM. PMID: [PubMed - indexed for MEDLINE]Cited by: The antischistosomal activity of hycanthone is believed to be due to its ability to bind covalently with DNA by a reaction sequence very similar to that described for oxamniquine (Chapter 11).
Lucanthone (25) is oxidized in the biophase to form hycanthone (26), which is transformed into the ester (85) in the presence of kinase or sulphotransferase.
Life Sciences, Vol. 37, pp. Pergamon Press Printed in the U.S.A. EVIDENCE FOR THE MODE OF ANTISCHISTOSOMAL ACTION OF HYCANTHONE 0. Cioli*, L.
Pica-Mattoccia*, S. Rosenbergt and S. Archert *Institute of Cell Biology, 18/A Via Romagnosi,Rome, Italy tCogswell Laboratory, Chemistry Department, Rensselaer Polytechnic Institute Troy, NY Cited by: Abstract.
Hycanthone-sensitive and hycanthone-resistant schistosomes (which are also sensitive and resistant to oxamniquine) were exposed in vitro to tritium-lCited by: In order to separate the desired antischistosomal action of the compound from the undesirable side-effects, a number of structural analogues of hycanthone and lucanthone (a related antischistosomal drug) were synthesized by Dr.
ELSLAGER at Parke-Davis Co.; these are benzothiopyranoindazole compounds indicated as "IA-3", "IA-4", "IA-5" and "IA-6".Cited by: 6.
Mutation Research, 31 () Elsevier Scientific Publishing Company, Amsterdam-Printed in The Netherlands $7 MICROSOMAL ACTIVATION TO MUTAGENS OF ANTISCHISTOSOMAL METHYL THIOXANTHENONES AND INITIAL TESTS ON A POSSIBLY NON-MUTAGENIC ANALOGUE* PHILIP E.
HARTMANa, PETER B. HULBERTb,c, ERNEST BUEDINGb AND Cited by: Hycanthone is the schistosomicide approved by the FDA in It is a metabolite of hone interferes with parasite nerve function, resulting in paralysis and death.
This agent also intercalates into DNA and inhibits RNA synthesis in vitro and shows potential antineoplastic Number: Abstract. Mice infected with Schistosoma mansoni were given an intramuscular injection of a single 80 mg/kg dose of randomly tritiated hycanthone.
The uptake of the drug in male and female worms, as well as its concentration in the red blood cells and plasma of the mice, was followed for a period of 24 by: Many of these compounds have been shown to be carcinogenic and mutagenic.
Examples include the food preservative AF-2, the food fumigant ethylene dibromide, the antischistosome drug hycanthone, several hair-dye additives, and the industrial compound vinyl chloride; all are potent, and some have subsequently been subjected to government control.
Hycanthone: AFrameshift Mutagen Abstract. Rapid spot-test screening of antischistosomal agents reveals that hy-canthone is a potent frameshift mutagen while the closely related compound, miracil D, is nonmutagenic in Salmonella.
Both hycanthone and miracil D are frameshift mutagens for T4 bacteriophage during growth in Escherichia coli. Over. "N-Oxidation at the diethylamino group of hycanthone, of lucanthone, and of two chlorbenzothiopyranoindazoles resulted in a marked reduction in mutagenic activity, while antischistosomal activity was retained or even enhanced.
Introduction of chlorine into the 8-position of benzothiopyranoindazoles reduced acute toxicity but had no effect on. On a per mole basis, hycanthone is the least toxic and mutagenic, whereas IA-3 is the most toxic and mutagenic compound among the six closely related agents.
In general, compounds. Pica-Mattoccia, L., Archer, S., and Cioli, D.,Hycanthone resistance in schistosomes correlates with the lack of an enzymatic activity which produces the covalent binding of hycanthone to parasite macromolecules, Mol. Biochem.
Abstract. This review focuses on two synthetic compounds, the most widely studied in a large series of congeners and derivatives, which have been employed extensively in the treatment of human schistosomiasis, have attracted modest interest in experimental cancer chemotherapy, and have become useful probes in the examination of some aspects of molecular biology.
The mutagenic activities of the TV-oxides of lucanthone, IA-4 and IA-3 were all much lower when compared with hycanthone, that of IA-3 TV-oxide being less than 1% of hycanthone while its antischistosomal activity is at least twice that of hycanthone.
Indeed, due to its efficacy against all forms of human schistosomiasis , PZQ has largely supplanted other antischistosomal compounds, such as oxamniquine (OXA) (Fig.
2), a tetrahydroquinoline. A family of nine mutagenic derivatives was characterized for the first time in the history of opium use, which is known to have been inhaled and smoked since ancient times. These compounds share a common 3-hydroxyphenanthrene ring system to which a heterocyclic five-membered ring system is attached.
Centennial Reflections – a distinguished parasitologist reflects on a paper published in their field in Parasitology years ago. A paper entitled “Bilharziasis in Natal”, published in Parasitology in by Dr F.
Cawston, provides a window on the state of knowledge at the time (Cawston, ). He was a British physician and zoologist practising in. The compound was shown to stimulate glucose utilization and lactic acid porduction. Cytotoxic- ity of hadacidin and 2-deoxy-D-glucose was potentiated in KB cells by diaminopurine.
The compound was administered in growth medium and cultures were observed for four to five days for cytopathology and for 48 hours for biochemical determinations.Frameshift Mutations Frameshift Mutations Roth, J R Since the original descriptions of frameshift mutations in T4 (1, 2), a large body of literature has accumulated characterizing such mutations and the mutagens which induce them.
A model suggested by Streisinger (3) accounts for some aspects of the data. In spite of these advances, many .Oxamniquine has generally been reported to lack mutagenic activity as determined by various assay methods including cytogenetic, dominant lethal, and host mediated assays; however, as high concentrations, evidence of weak mutagenic activity has been reported as determined by the Ames mutagenic assay with or without metabolic activation.