Database : HANSEN Search on : ANTIINFECCIOSOS/QUIM [Subject descriptor] References found : 2 [refine] Displaying: 1 .. 2   in format [Detailed]

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Id: 15629 Author: Salem, Isam Ismail; Steffan, Gerhard; Düzgünes, Nejat Title: Efficacy of clofazimine - modified cyclodextrin against Mycobacterium avium complex in human macrophages ..- Source: s.l; s.n; 2003. 10 p. graf. Abstract: Clofazimine, a water insoluble substituted iminophenazine derivative with anti-mycobacterial and anti-inflammatory activity, is recommended by the WHO for the treatment of leprosy. It is also active against disseminated Mycobacterium avium complex (MAC) disease in HIV-infected patients. Recently, we achieved a 4000-fold increase of clofazimine water solubility using a novel modified clofazimine-cyclodextrin complex synthesized and patented by our group [Wasserlösliche, Iminiophenazinderivate enthaltende pharmazeutische Zusammensetzungen, deren Herstellung und Verwendung, German Patent, DE19814814C2]. In this paper we examine the activity of this complex against MAC in human macrophages, and evaluate its cytotoxicity. MAC-infected macrophages were treated for 24h with free or complexed clofazimine. The in vitro minimum inhibitory concentrations of both free and complexed clofazimine were 0.1 microg/ml. Free and complexed clofazimine inhibited the growth of MAC inside macrophages to a similar extent, while modified cyclodextrin alone had no observable effects on MAC or macrophages. Complexed clofazimine was not toxic to cells at concentrations effective against MAC. The TD(50) of the modified cyclodextrin in THP-1 cell line was 297 microg/ml. (AU). Descriptors: ANTIINFECCIOSOS/quim ANTIINFECCIOSOS/farmacol ANTIINFECCIOSOS/tox CELULAS CULTIVADAS CLOFAZIMINA/quim CLOFAZIMINA/farmacol CLOFAZIMINA/tox MACROFAGOS/ef drogas TESTES DE SENSIBILIDADE MICROBIANA COMPLEXO MYCOBACTERIUM AVIUM/ef drogas ESTEROIS/quim ACIDO SUCCINICO Limits: ESTUDO COMPARATIVO HUMANO ANIMAL CAMUNDONGOS Electronic Medium: http://www.ilsl.br Location: BR191.1; 09082/s

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Id: 13945 Author: Salem, Isam Ismail; Steffan, Gerhard; Düzgünes, Nejat Title: Efficacy of clofazimine - modified cyclodextrin against Mycobacterium avium complex in human macrophages ..- Source: s.l; s.n; 2003. 10 p. graf. Abstract: Clofazimine, a water insoluble substituted iminophenazine derivative with anti-mycobacterial and anti-inflammatory activity, is recommended by the WHO for the treatment of leprosy. It is also active against disseminated Mycobacterium avium complex (MAC) disease in HIV-infected patients. Recently, we achieved a 4000-fold increase of clofazimine water solubility using a novel modified clofazimine-cyclodextrin complex synthesized and patented by our group [Wasserlösliche, Iminiophenazinderivate enthaltende pharmazeutische Zusammensetzungen, deren Herstellung und Verwendung, German Patent, DE19814814C2]. In this paper we examine the activity of this complex against MAC in human macrophages, and evaluate its cytotoxicity. MAC-infected macrophages were treated for 24h with free or complexed clofazimine. The in vitro minimum inhibitory concentrations of both free and complexed clofazimine were 0.1 microg/ml. Free and complexed clofazimine inhibited the growth of MAC inside macrophages to a similar extent, while modified cyclodextrin alone had no observable effects on MAC or macrophages. Complexed clofazimine was not toxic to cells at concentrations effective against MAC. The TD(50) of the modified cyclodextrin in THP-1 cell line was 297 microg/ml. (AU). Descriptors: ANTIINFECCIOSOS/quim ANTIINFECCIOSOS/farmacol ANTIINFECCIOSOS/tox CLOFAZIMINA/quim CLOFAZIMINA/farmacol CLOFAZIMINA/tox CELULAS CULTIVADAS MACROFAGOS/ef drogas MACROFAGOS/microbiol TESTES DE SENSIBILIDADE MICROBIANA COMPLEXO MYCOBACTERIUM AVIUM/ef drogas ESTEROIS/quim ACIDO SUCCINICO/quim Limits: ESTUDO COMPARATIVO HUMANO ANIMAL CAMUNDONGOS Electronic Medium: http://www.ilsl.br Location: BR191.1; 09082/s

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