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Titolo:
IN-VIVO TRYPANOCIDAL ACTIVITIES OF NEW S-ADENOSYLMETHIONINE DECARBOXYLASE INHIBITORS
Autore:
BACCHI CJ; BRUN R; CROFT SL; ALICEA K; BUHLER Y;
Indirizzi:
PACE UNIV,HASKINS LABS,41 PK ROW NEW YORK NY 10038 PACE UNIV,DEPT BIOL NEW YORK NY 10038 SWISS TROP INST CH-4002 BASEL SWITZERLAND UNIV LONDON LONDON SCH HYG & TROP MED,DEPT MED PARASITOL LONDON WC1E 7HT ENGLAND
Titolo Testata:
Antimicrobial agents and chemotherapy
fascicolo: 6, volume: 40, anno: 1996,
pagine: 1448 - 1453
SICI:
0066-4804(1996)40:6<1448:ITAONS>2.0.ZU;2-I
Fonte:
ISI
Lingua:
ENG
Soggetto:
DL-ALPHA-DIFLUOROMETHYLORNITHINE; TRYPANOSOMA-BRUCEI-BRUCEI; METHYLGLYOXAL BIS(GUANYLHYDRAZONE); ORNITHINE DECARBOXYLASE; POLYAMINE METABOLISM; CHEMOTHERAPY; RHODESIENSE; COMBINATION; RESISTANCE; SURAMIN;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
31
Recensione:
Indirizzi per estratti:
Citazione:
C.J. Bacchi et al., "IN-VIVO TRYPANOCIDAL ACTIVITIES OF NEW S-ADENOSYLMETHIONINE DECARBOXYLASE INHIBITORS", Antimicrobial agents and chemotherapy, 40(6), 1996, pp. 1448-1453

Abstract

A series of novel aromatic derivatives based on the structure of methylglyoxal bis(guanylhydrazone) (MGBG) was examined for trypanocidal activities in human and veterinary trypanosomes of African origin, One agent, CGP 40215A, a bicyclic analog of MGBG which also resembles the diamidines diminazene (Berenil) and pentamidine, was curative of infections by 19 isolates of Trypanosoma brucei subspecies as well as a Trypanosoma congolense isolate, Several of these isolates were resistant to standard trypanocides, Curative doses were greater than or equal to 25 mg/kg of body weight/day for 3 days in these acute laboratory modelinfections, In addition, CGP 40215A also cured a model central nervous system infection in combination with the ornithine decarboxylase inhibitor DL-alpha-difluoromethylornithine (DFMO; Ornidyl, eflornithine),Curative combinations were 14 days of oral 2% DFMO (similar to 5 g/kg/day) plus 5, 10, or 25 mg/kg/day for 3 or 7 days given by intraperitoneal injection or with a miniosmotic pump, Combinations were most effective if CGP 40215A was given in the second half or at the end of the DFMO regimen, MGBG has modest activity as an inhibitor of trypanosome S-adenosylmethionine decarboxylase (50% inhibitory concentration [IC50], 130 mu M), while CGP 40215A was a more active inhibitor (IC50, 20 mu M). Preincubation of trypanosomes with CGP 40215A for 1 h caused a reduction in spermidine content (36%) and an increase in putrescine content (20%), indicating that one possible mechanism of its action may be inhibition of polyamine biosynthesis.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 20/01/21 alle ore 12:20:56