Trypanosoma cruzi: in vitro activity of Epoxy-α-Lap, a derivative of α-lapachone, on trypomastigote and amastigote forms
Chagas disease is an endemic parasitic infection caused by Trypanosoma cruzi that affects 18–20 million people in Central and South America. Recently we described the Epoxy-α-Lap, an oxyran derivative of α-lapachone, which presents a low toxicity profile and a high inhibitory activity against T. cru...
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| Veröffentlicht in: | Experimental parasitology 2009-06, Vol.122 (2), p.91-96 |
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| creator | Bourguignon, S.C. Castro, H.C. Santos, D.O. Alves, C.R. Ferreira, V.F. Gama, I.L. Silva, F.C. Seguins, W.S. Pinho, R.T. |
| description | Chagas disease is an endemic parasitic infection caused by
Trypanosoma
cruzi that affects 18–20 million people in Central and South America. Recently we described the Epoxy-α-Lap, an oxyran derivative of α-lapachone, which presents a low toxicity profile and a high inhibitory activity against
T.
cruzi epimastigotes forms, the non-infective form of this parasite. In this work we described the trypanocidal effects of Epoxy-α-Lap on extracellular (trypomastigote) and intracellular (amastigote) infective forms of two
T. cruzi strains (Y and Colombian) known by their different infective profile. Our results showed that Epoxy-α-Lap is lethal to trypomastigote Y and Colombian strains (97% and 84%, respectively). Interestingly, Epoxy-α-Lap also showed a trypanocidal effect in human macrophage infected with
T. cruzi Y (85.6%) and Colombian (71.9%) strains amastigote forms. Similar effects were observed on
T. cruzi amastigote infected Vero cells (96.4% and 95.0%, respectively). Our results pointed Epoxy-α-Lap as a potential candidate for Chagas disease chemotherapy since it presents trypanocidal activity on all
T. cruzi forms with low) toxicity profile
. |
| doi_str_mv | 10.1016/j.exppara.2009.03.002 |
| format | Article |
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Trypanosoma
cruzi that affects 18–20 million people in Central and South America. Recently we described the Epoxy-α-Lap, an oxyran derivative of α-lapachone, which presents a low toxicity profile and a high inhibitory activity against
T.
cruzi epimastigotes forms, the non-infective form of this parasite. In this work we described the trypanocidal effects of Epoxy-α-Lap on extracellular (trypomastigote) and intracellular (amastigote) infective forms of two
T. cruzi strains (Y and Colombian) known by their different infective profile. Our results showed that Epoxy-α-Lap is lethal to trypomastigote Y and Colombian strains (97% and 84%, respectively). Interestingly, Epoxy-α-Lap also showed a trypanocidal effect in human macrophage infected with
T. cruzi Y (85.6%) and Colombian (71.9%) strains amastigote forms. Similar effects were observed on
T. cruzi amastigote infected Vero cells (96.4% and 95.0%, respectively). Our results pointed Epoxy-α-Lap as a potential candidate for Chagas disease chemotherapy since it presents trypanocidal activity on all
T. cruzi forms with low) toxicity profile
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Trypanosoma
cruzi that affects 18–20 million people in Central and South America. Recently we described the Epoxy-α-Lap, an oxyran derivative of α-lapachone, which presents a low toxicity profile and a high inhibitory activity against
T.
cruzi epimastigotes forms, the non-infective form of this parasite. In this work we described the trypanocidal effects of Epoxy-α-Lap on extracellular (trypomastigote) and intracellular (amastigote) infective forms of two
T. cruzi strains (Y and Colombian) known by their different infective profile. Our results showed that Epoxy-α-Lap is lethal to trypomastigote Y and Colombian strains (97% and 84%, respectively). Interestingly, Epoxy-α-Lap also showed a trypanocidal effect in human macrophage infected with
T. cruzi Y (85.6%) and Colombian (71.9%) strains amastigote forms. Similar effects were observed on
T. cruzi amastigote infected Vero cells (96.4% and 95.0%, respectively). Our results pointed Epoxy-α-Lap as a potential candidate for Chagas disease chemotherapy since it presents trypanocidal activity on all
T. cruzi forms with low) toxicity profile
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Pathogenesis</subject><subject>Macrophages - parasitology</subject><subject>Naphthoquinones - chemistry</subject><subject>Naphthoquinones - pharmacology</subject><subject>Protozoa</subject><subject>Trypanocidal Agents - pharmacology</subject><subject>Trypanocidal effect</subject><subject>Trypanosoma cruzi</subject><subject>Trypanosoma cruzi - drug effects</subject><subject>Trypanosoma cruzi - growth & development</subject><subject>Vero Cells</subject><subject>α -Lapachone</subject><issn>0014-4894</issn><issn>1090-2449</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2009</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkEuO1DAQhi0EYpqBI4C8gdUklB3nYTYjNBoeUktshrVVcSrgVhIHO92anltxEc6EWx0xS1Z-1Fd_lT7GXgvIBYjq_S6n-3nGgLkE0DkUOYB8wjYCNGRSKf2UbQCEylSj1QV7EeMOABoh1XN2IbRsSqjVhj3cheOMk49-RG7D_sF94G7iB7cEz9EuLt2O3Pf8dvb3x-zP72yL8xVH3lFwB0x1OlXT_4Az2p9-oivuJ76k2BQZF_fDL8Rx6jg-PnsfxviSPetxiPRqPS_Z90-3dzdfsu23z19vPm4zq2qxZKirGlVR16rUkJYuVNpdFAStVbonjbJtaylEbztpVVO1LTWAVLaV0qJEUVyyd-fcOfhfe4qLGV20NAw4kd9HI6GspKqrBJZn0AYfY6DezMGNGI5GgDlJNzuzSjcn6QYKk6SnvjfrgH07UvfYtVpOwNsVwGhx6ANO1sV_nBSqgUKfgq7PHCUdB0fBROtostS5QHYxnXf_WeUvTkSlIg</recordid><startdate>20090601</startdate><enddate>20090601</enddate><creator>Bourguignon, S.C.</creator><creator>Castro, H.C.</creator><creator>Santos, D.O.</creator><creator>Alves, C.R.</creator><creator>Ferreira, V.F.</creator><creator>Gama, I.L.</creator><creator>Silva, F.C.</creator><creator>Seguins, W.S.</creator><creator>Pinho, R.T.</creator><general>Elsevier Inc</general><general>Elsevier</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>M7N</scope></search><sort><creationdate>20090601</creationdate><title>Trypanosoma cruzi: in vitro activity of Epoxy-α-Lap, a derivative of α-lapachone, on trypomastigote and amastigote forms</title><author>Bourguignon, S.C. ; Castro, H.C. ; Santos, D.O. ; Alves, C.R. ; Ferreira, V.F. ; Gama, I.L. ; Silva, F.C. ; Seguins, W.S. ; Pinho, R.T.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c471t-a967a437745905073428513e0bc49fe9a2bb7211fcd2c486bbe80ae5b64915a13</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2009</creationdate><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>Cells, Cultured</topic><topic>Cercopithecus aethiops</topic><topic>Dose-Response Relationship, Drug</topic><topic>Epoxy Compounds - pharmacology</topic><topic>Epoxy-α-Lap</topic><topic>Fibroblasts - parasitology</topic><topic>Fundamental and applied biological sciences. Psychology</topic><topic>Humans</topic><topic>Life Cycle Stages - drug effects</topic><topic>Life cycle. Host-agent relationship. Pathogenesis</topic><topic>Macrophages - parasitology</topic><topic>Naphthoquinones - chemistry</topic><topic>Naphthoquinones - pharmacology</topic><topic>Protozoa</topic><topic>Trypanocidal Agents - pharmacology</topic><topic>Trypanocidal effect</topic><topic>Trypanosoma cruzi</topic><topic>Trypanosoma cruzi - drug effects</topic><topic>Trypanosoma cruzi - growth & development</topic><topic>Vero Cells</topic><topic>α -Lapachone</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Bourguignon, S.C.</creatorcontrib><creatorcontrib>Castro, H.C.</creatorcontrib><creatorcontrib>Santos, D.O.</creatorcontrib><creatorcontrib>Alves, C.R.</creatorcontrib><creatorcontrib>Ferreira, V.F.</creatorcontrib><creatorcontrib>Gama, I.L.</creatorcontrib><creatorcontrib>Silva, F.C.</creatorcontrib><creatorcontrib>Seguins, W.S.</creatorcontrib><creatorcontrib>Pinho, R.T.</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Algology Mycology and Protozoology Abstracts (Microbiology C)</collection><jtitle>Experimental parasitology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Bourguignon, S.C.</au><au>Castro, H.C.</au><au>Santos, D.O.</au><au>Alves, C.R.</au><au>Ferreira, V.F.</au><au>Gama, I.L.</au><au>Silva, F.C.</au><au>Seguins, W.S.</au><au>Pinho, R.T.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Trypanosoma cruzi: in vitro activity of Epoxy-α-Lap, a derivative of α-lapachone, on trypomastigote and amastigote forms</atitle><jtitle>Experimental parasitology</jtitle><addtitle>Exp Parasitol</addtitle><date>2009-06-01</date><risdate>2009</risdate><volume>122</volume><issue>2</issue><spage>91</spage><epage>96</epage><pages>91-96</pages><issn>0014-4894</issn><eissn>1090-2449</eissn><coden>EXPAAA</coden><abstract>Chagas disease is an endemic parasitic infection caused by
Trypanosoma
cruzi that affects 18–20 million people in Central and South America. Recently we described the Epoxy-α-Lap, an oxyran derivative of α-lapachone, which presents a low toxicity profile and a high inhibitory activity against
T.
cruzi epimastigotes forms, the non-infective form of this parasite. In this work we described the trypanocidal effects of Epoxy-α-Lap on extracellular (trypomastigote) and intracellular (amastigote) infective forms of two
T. cruzi strains (Y and Colombian) known by their different infective profile. Our results showed that Epoxy-α-Lap is lethal to trypomastigote Y and Colombian strains (97% and 84%, respectively). Interestingly, Epoxy-α-Lap also showed a trypanocidal effect in human macrophage infected with
T. cruzi Y (85.6%) and Colombian (71.9%) strains amastigote forms. Similar effects were observed on
T. cruzi amastigote infected Vero cells (96.4% and 95.0%, respectively). Our results pointed Epoxy-α-Lap as a potential candidate for Chagas disease chemotherapy since it presents trypanocidal activity on all
T. cruzi forms with low) toxicity profile
.</abstract><cop>Amsterdam</cop><pub>Elsevier Inc</pub><pmid>19285074</pmid><doi>10.1016/j.exppara.2009.03.002</doi><tpages>6</tpages><oa>free_for_read</oa></addata></record> |
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| ispartof | Experimental parasitology, 2009-06, Vol.122 (2), p.91-96 |
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| subjects | Animals Biological and medical sciences Cells, Cultured Cercopithecus aethiops Dose-Response Relationship, Drug Epoxy Compounds - pharmacology Epoxy-α-Lap Fibroblasts - parasitology Fundamental and applied biological sciences. Psychology Humans Life Cycle Stages - drug effects Life cycle. Host-agent relationship. Pathogenesis Macrophages - parasitology Naphthoquinones - chemistry Naphthoquinones - pharmacology Protozoa Trypanocidal Agents - pharmacology Trypanocidal effect Trypanosoma cruzi Trypanosoma cruzi - drug effects Trypanosoma cruzi - growth & development Vero Cells α -Lapachone |
| title | Trypanosoma cruzi: in vitro activity of Epoxy-α-Lap, a derivative of α-lapachone, on trypomastigote and amastigote forms |
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