000			02815na a2200253 4500
003			H12O
005			20210625062802.0
008			130622s2011 xxx||||| |||| 00| 0 eng d
040			_cH12O
041			_aeng
100			_91902 _aBautista, José M. _eInstituto de Investigación i+12
100			_aDíez, Amalia _91901 _eInstituto de Investigación i+12
100			_aPuyet, Antonio _91900 _eInstituto de Investigación i+12
245	0	0	_aMulti-targeted activity of maslinic acid as an antimalarial natural compound: maslinic acid targets on Plasmodium falciparum _h[artículo]
260			_bFEBS Journal, _c2011
300			_a278(16):2951-2961.
500			_aFormato Vancouver: Moneriz C, Mestres J, Bautista JM, Diez A, Puyet A. Multi-targeted activity of maslinic acid as an antimalarial natural compound. FEBS J. 2011;278(16):2951-61.
501			_aPMID: 21689375
504			_aContiene 60 referencias
520			_aMost 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 metalloproteases belonging to that family, such as falcilysin and apicoplast peptide-processing proteases. Finally, in silico target screening was used to search for other potential binding targets that may have remained undetected. Among the targets identified, the method recovered two for which experimental activity could be confirmed, and suggested several putative new targets to which MA could have affinity. One of these unreported targets, phospholipase A2, was shown to be partially inhibited by MA. These results suggest that MA may behave as a multi-targeted drug against the intra-erythrocytic cycle of Plasmodium, providing a new tool to investigate the synergistic effect of inhibiting several unrelated processes with a single compound, a new concept in antimalarial research.
710			_9625 _aInstituto de Investigación imas12
856			_uhttp://pc-h12o-es.m-hdoct.a17.csinet.es/pdf/pc/5/pc5813.pdf _ySolicitar documento
942			_n0 _2ddc _cART
999			_c5813 _d5813