TAILIEUCHUNG - Báo cáo khoa học: Multi-targeted activity of maslinic acid as an antimalarial natural compound

Most drugs against malaria that are available or under development target a single process of the parasite infective cycle, favouring the appearance of resistant mutants which are easily spread in areas under chemotherapeutic treatments. | IFEBS Journal Multi-targeted activity of maslinic acid as an antimalarial natural compound Carlos Moneriz1 4 Jordi Mestres2 Jose M. Bautista1 3 Amalia Diez1 3 and Antonio Puyet1 3 1 Departamento de Bioquimica y Biologia Molecular IV Facultad de Veterinaria Universidad Complutense de Madrid Spain 2 Chemogenomics Laboratory Research Unit on BiomedicalInformatics GRIB Institut Municipald Investigacio Medica and Universitat Pompeu Fabra Barcelona Spain 3 Instituto de Investigacion delHospital12 de Octubre Universidad Complutense de Madrid Spain 4 Departamento de Bioquimica Facultad de Medicina Universidad de Cartagena Colombia Keywords apicomplexa merozoite surface protein metalloprotease inhibition PfSUBI phospholipase plasmodium Correspondence A. Puyet Departamento de Bioquimica y Biologia Molecular IV Facultad de Veterinaria Universidad Complutense de Madrid E28040 Madrid Spain Fax 34 913 943 824 Tel 34 913 943 827 E-mail apuyet@ Received 21 April 2011 revised 14 June 2011 accepted 17 June 2011 doi Most drugs against malaria that are available or under development target a single process of the parasite infective cycle favouring the appearance of resistant mutants which are easily spread in areas under chemotherapeutic treatments. Maslinic acid MA is a low toxic natural pentacyclic triterpene for which a wide variety of biological and therapeutic activities have been reported. Previous work revealed that Plasmodium falciparum erythrocytic cultures were inhibited by MA which was able to hinder the maturation from ring to schizont stage and as a consequence prevent the release of merozoites and the subsequent invasion. We show here that MA effectively inhibits the proteolytic processing of the merozoite surface protein complex probably by inhibition of PfSUB1. In addition MA was also found to inhibit metalloproteases of the M16 family by a non-chelating mechanism suggesting the possible hindrance of plasmodial .

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