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Titolo:
Inhibitory and lytic effects of phenothiazine derivatives and related tricyclic neuroleptic compounds, on Entamoeba histolytica HK9 and HMI trophozoites
Autore:
Ondarza, RN; Hernandez, E; Iturbe, A; Hurtado, G;
Indirizzi:
Natl Publ Hlth Inst, Ctr Res Infect Dis, Cuernavaca 62508, Morelos, MexicoNatl Publ Hlth Inst Cuernavaca Morelos Mexico 62508 2508, Morelos, Mexico Natl Autonomous Univ Mexico, Fac Med, Dept Biochem, Mexico City 04510, DF,Mexico Natl Autonomous Univ Mexico Mexico City DF Mexico 04510 04510, DF,Mexico
Titolo Testata:
BIOTECHNOLOGY AND APPLIED BIOCHEMISTRY
, volume: 32, anno: 2000,
parte:, 1
pagine: 61 - 67
SICI:
0885-4513(200008)32:<61:IALEOP>2.0.ZU;2-N
Fonte:
ISI
Lingua:
ENG
Soggetto:
TRYPANOTHIONE REDUCTASE; GLUTATHIONE METABOLISM; ANTIDEPRESSANT DRUGS; LEISHMANIA; EUKARYOTE;
Keywords:
chlorpromazine; clomipramine; potential anti-amoebic drug; potential anti-leishmanial drug; potential anti-trypanosomal drug;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Agriculture,Biology & Environmental Sciences
Life Sciences
Citazioni:
12
Recensione:
Indirizzi per estratti:
Indirizzo: Ondarza, RN Olivar Padres 941, Mexico City 01780, DF, Mexico Olivar Padres 941 Mexico City DF Mexico 01780 780, DF, Mexico
Citazione:
R.N. Ondarza et al., "Inhibitory and lytic effects of phenothiazine derivatives and related tricyclic neuroleptic compounds, on Entamoeba histolytica HK9 and HMI trophozoites", BIOT APP B, 32, 2000, pp. 61-67

Abstract

It has been shown previously that tricyclic neuroleptics like clomipramineand chlorpromazine have lethal effects on Leishmania donovani and L. major, and other studies indicate that the phenothiazine inhibitors of trypanothione reductase are potential anti-trypanosomal and anti-leishmanial drugs, With this in mind and our original observation on the presence of trypanothione in Entamoeba histolytica HK9, we examined the possible inhibitory effects of various phenothiazine and tricyclic derivatives on this human parasite. We found that drugs like clomipramine (KD002), the most potent in vitroinhibitor of trypanothione reductase among 30 tricyclic compounds tested, at 25 mu M after 24 h of culture under aerobic conditions, caused a substantial decrease in the number of E. histolytica HK9 trophozoites, from approx, 15 x 10(6) to 5.37 x 10(6) cells, and at 100 mu M to 0.8 x 10(6) cells, Asubstantial inhibitory effect on cell proliferation could also be demonstrated with metronidazol (used clinically against amoebiasis). Under similar experimental conditions other tricyclic and phenothiazine derivatives (OFKs), designed originally to inhibit the trypanothione reductase of trypanosomatides, had an inhibitory effect of 16 to 95%, For comparison, similar results were obtained using clomipramine and a phenothiazine derivative (OFK006) with Trypanosoma cruzi and Crithidia luciliae, except that with the latter the inhibitory effect of clomipramine was less dramatic. Experiments comparing two E. histolytica strains showed that normal cell proliferation under anaerobiosis was higher in strain HK9 than in HMI, which is highly virulent, but that metronidazol and clomipramine were less effective against HMI. Two other drugs tested, diphenydramine (KD005) and a phenothiazine derivative (OFK008), also had significant but lower inhibitory effects on both strains. The inhibitory activity on cell proliferation and the lytic effects on this human parasite by the tricyclic compounds clomipramine, chlorpromazine and others, as well as by the phenothiazine derivatives, indicate that they can be considered potential anti-amoebic agents.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 04/04/20 alle ore 21:45:38