Mechanism of action of psicofuranine.
نویسنده
چکیده
Psicofuranine is a new antibiotic which was first described by Schroeder and Hoeksema (1959), Eble et al. (1959), and Vavra et al. (1959). It has good antibacterial activity in vivo (Lewis et al., 1959) and antitumor activity (Evans and Gray, 1959), but it shows no activity in vitro when assayed by conventional methods. The activity in vitro was demonstrated using the special media and assay techniques described by Hanka et al. (1959). Psicofuranine resembles closely Angustmycin C described by Yulnsten (1958); the latter was reported biologically and optically inactive however. The structural similarity of psicofuranine (figure 1) to adenosine suggested an antimetabolite mode of action. Therefore, studies were made for the reversal of inhibitory activity of psicofuranine by compounds containing purine and pyrimidine bases, and the results are reported herein.
منابع مشابه
Inhibition of Parental and Mutant Xanthosine 5'-phosphate Aminases by Psicofuranine.
The antibiotic psicofuranine (9-n-psicofuranosy-6-aminopurine) causes a guanine deficiency in enteric bacteria (1) through inhibition of xanthosine 5’-phosphate (XMP) aminase (2), an enzyme essential for guanine nucleotide synthesis (3). A study of the mechanism of the inhibition was undertaken as a preliminary to the biochemical analysis of psicofuranine-resistant mutants of Escherichiu coli B...
متن کاملInhibition of Parental and Mutant Xanthosine S-Phosphate Aminases by Psicofuranine*
The antibiotic psicofuranine (9-n-psicofuranosy-6-aminopurine) causes a guanine deficiency in enteric bacteria (1) through inhibition of xanthosine 5’-phosphate (XMP) aminase (2), an enzyme essential for guanine nucleotide synthesis (3). A study of the mechanism of the inhibition was undertaken as a preliminary to the biochemical analysis of psicofuranine-resistant mutants of Escherichiu coli B...
متن کاملFormation of an adenyl xanthosine monophosphate intermediate by xanthosine 5'-phosphate aminase and its inhibition by psicofuranine.
The amination of xanthosine 5’-phosphate and its inhibition by psicofuranine was examined with substrate amounts of purified xanthosine St-phosphate aminase from Escherichia coli. In the absence of NH,, incubation of the enzyme with adenosine triphosphate-8-i4C and XMP-8J4C for 10 min results in the conversion of ATP to AMP without concomitant formation of guanosine monophosphate. Shorter perio...
متن کاملStudies with psicofuranine in the tumor-bearing rat.
The effects of the antitumor agent, psicofuranine, have been investigated in rats with subcutaneously transplanted Walker 256 adenocarcinomas. Administration of the drug at 500 mg/kg/day for 1 week caused a marked regression and a sharp drop in utilization of phosphate-P m uptake in the tumors. Longer treatment also produced significant decreases in phosphate uptake by host tissues. I t was pos...
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Xylazine hydrochloride, α2 adrenoceptor agonist, is an analgesic, sedative, tranquilizer, and muscle relaxant agent in veterinary medicine which is mostly used as in pre-anesthesia in veterinary medicine. One of the main adverse effects of xylazine which limits application of this medication in small animal veterinary practice (mostly in cats) is nausea and vomiting which can end up with aspira...
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ورودعنوان ژورنال:
- Journal of bacteriology
دوره 80 شماره
صفحات -
تاریخ انتشار 1960