公开(公告)号：EP2337560B1

公开(公告)日：2014-01-22

申请号：EP09806250.8

申请日：2009-08-14

申请人： Universidade Federal Do Pará

发明人： SANTOS, Alberdan Silva ,  SILVA, Edilene Oliveira da ,  NASCIMENTO, José Luiz Martins do ,  ALVES, Cláudio Naum ,  RODRIGUES, Ana Paula Drumond ,  CARVALHO, Antônio Sérgio da Costa

IPC分类号： A61K31/351 ,  A61P33/02

CPC分类号： C07D309/40 ,  A61K31/351 ,  A61K31/366 ,  Y02A50/409

摘要： The present invention refers to the use of HMP (a secondary metabolite obtained from Aspergillus fungi) as an agent that intensifies the mechanism of macrophage activation, leading to the death of L. (Leishmania) amazonensis, the etiologic agent of cutaneous leishmaniasis. The main mechanism of action of this agent is the activation of the microbicidal activity of host cells, through increased superoxide production, number of lysosomes, actin and microtubule filament polymerization and increased spreading, typical of activated cells. Additionally, HMP represents a molecule of easy acquisition, presents an efficient combat mechanism with no adverse reactions and capacity to inhibit the development of promastigotes and amastigotes forms. Finally, results suggest HMP to be a potential candidate for use against cutaneous leishmaniasis at a minimal concentration of 50 μg/mL.

公开(公告)号：EP2337560A1

公开(公告)日：2011-06-29

申请号：EP09806250.8

申请日：2009-08-14

申请人： Universidade Federal Do Pará

发明人： SANTOS, Alberdan Silva ,  SILVA, Edilene Oliveira da ,  NASCIMENTO, José Luiz Martins do ,  ALVES, Cláudio Naum ,  RODRIGUES, Ana Paula Drumond ,  CARVALHO, Antônio Sérgio da Costa

IPC分类号： A61K31/351 ,  A61P33/02

CPC分类号： C07D309/40 ,  A61K31/351 ,  A61K31/366 ,  Y02A50/409

摘要： The present invention refers to the use of HMP (a secondary metabolite obtained from Aspergillus fungi) as an agent that intensifies the mechanism of macrophage activation, leading to the death of L. (Leishmania) amazonensis, the etiologic agent of cutaneous leishmaniasis. The main mechanism of action of this agent is the activation of the microbicidal activity of host cells, through increased superoxide production, number of lysosomes, actin and microtubule filament polymerization and increased spreading, typical of activated cells. Additionally, HMP represents a molecule of easy acquisition, presents an efficient combat mechanism with no adverse reactions and capacity to inhibit the development of promastigotes and amastigotes forms. Finally, results suggest HMP to be a potential candidate for use against cutaneous leishmaniasis at a minimal concentration of 50 μg/mL.

摘要翻译： 本发明涉及使用HMP（从曲霉属真菌获得的次级代谢物）作为增强巨噬细胞活化机制的药剂，导致L.（利什曼原虫）亚马逊杆菌（皮肤利什曼病的病原体）的死亡。 该作用剂的主要作用机理是通过增加超氧化物的产生，溶酶体的数量，肌动蛋白和微管丝聚合以及活化细胞的典型增加的扩散来激活宿主细胞的杀微生物活性。 此外，HMP代表了一种容易获得的分子，呈现出高效的作战机制，没有不良反应，并且具有抑制前鞭毛体和无鞭毛体形式发育的能力。 最后，结果表明HMP是在50μg/ mL的最低浓度下用于抵抗皮肤利什曼病的潜在候选物。