A nature-inspired design yields a new class of steroids against trypanosomatids
This article belongs to the Special Issue Drug Discovery for Neglected Diseases
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| Altri autori: | , , , , , , , , , , , |
| Natura: | article |
| Lingua: | inglese |
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2019
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| Accesso online: | https://hdl.handle.net/20.500.12008/28675 |
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| _version_ | 1868890217429073920 |
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| author | Aguilera, Elena |
| author2 | Perdomo, Cintya Espíndola, Alejandra Corvo, Ileana Faral-Tello, Paula Robello Porto, Carlos Serna, Elva Benítez, Fátima Riveros, R. Torres, Susana Vera de Bilbao, N.I. Yaluff, Gloria Álvarez, Guzmán |
| author2_role | author author author author author author author author author author author author |
| author_browse | Aguilera, Elena Benítez, Fátima Corvo, Ileana Espíndola, Alejandra Faral-Tello, Paula Perdomo, Cintya Riveros, R. Robello Porto, Carlos Serna, Elva Torres, Susana Vera de Bilbao, N.I. Yaluff, Gloria Álvarez, Guzmán |
| author_facet | Aguilera, Elena Perdomo, Cintya Espíndola, Alejandra Corvo, Ileana Faral-Tello, Paula Robello Porto, Carlos Serna, Elva Benítez, Fátima Riveros, R. Torres, Susana Vera de Bilbao, N.I. Yaluff, Gloria Álvarez, Guzmán |
| author_role | author |
| collection | COLIBRI |
| dc.contributor.none.fl_str_mv | Aguilera Elena, Universidad de la República (Uruguay). Facultad de Ciencias. Instituto de Química Biológica. Perdomo Cintya, Universidad de la República (Uruguay). CENUR. Espíndola Alejandra, Universidad de la República (Uruguay). CENUR. Corvo Ileana, Universidad de la República (Uruguay). CENUR. Faral-Tello Paula, Instituto Pasteur (Montevideo). Robello Porto Carlos, Instituto Pasteur (Montevideo). Serna Elva Benítez F. Riveros R. Torres S. Vera de Bilbao N.I. Yaluff Gloria Álvarez Guzmán, Universidad de la República (Uruguay). CENUR. |
| dc.creator.none.fl_str_mv | Aguilera, Elena Perdomo, Cintya Espíndola, Alejandra Corvo, Ileana Faral-Tello, Paula Robello Porto, Carlos Serna, Elva Benítez, Fátima Riveros, R. Torres, Susana Vera de Bilbao, N.I. Yaluff, Gloria Álvarez, Guzmán |
| dc.date.none.fl_str_mv | 2019 2021-07-22T14:39:19Z 2021-07-22T14:39:19Z |
| dc.format.none.fl_str_mv | 22 h. application/pdf |
| dc.identifier.none.fl_str_mv | Aguilera, E, Perdomo, C, Espindola, A, y otros "A nature-inspired design yields a new class of steroids against trypanosomatids". Molecules. [en línea] 2019, 24(20): 3800. DOI: 10.3390/molecules24203800 1420-3049 https://hdl.handle.net/20.500.12008/28675 10.3390/molecules24203800 |
| dc.language.none.fl_str_mv | en eng |
| dc.publisher.none.fl_str_mv | MDPI |
| dc.relation.none.fl_str_mv | Molecules, 2019, 24(20): 3800 |
| dc.rights.none.fl_str_mv | info:eu-repo/semantics/openAccess Licencia Creative Commons Atribución (CC - By 4.0) |
| dc.source.none.fl_str_mv | reponame:COLIBRI instname:Universidad de la República instacron:Universidad de la República |
| dc.subject.none.fl_str_mv | Anti-T. cruzi activity in vitro and in vivo Anti-Leishmania spp. activity in vitro and in vivo Cytotoxicity and genotoxicity |
| dc.title.none.fl_str_mv | A nature-inspired design yields a new class of steroids against trypanosomatids |
| dc.type.none.fl_str_mv | Artículo info:eu-repo/semantics/article info:eu-repo/semantics/publishedVersion |
| description | This article belongs to the Special Issue Drug Discovery for Neglected Diseases |
| eu_rights_str_mv | openAccess |
| format | article |
| id | anni_e3cd1ee17da62d24495c4e0358831a4d |
| identifier_str_mv | Aguilera, E, Perdomo, C, Espindola, A, y otros "A nature-inspired design yields a new class of steroids against trypanosomatids". Molecules. [en línea] 2019, 24(20): 3800. DOI: 10.3390/molecules24203800 1420-3049 10.3390/molecules24203800 |
| instacron_str | Universidad de la República |
| institution | Universidad de la República |
| instname_str | Universidad de la República |
| language | eng |
| language_invalid_str_mv | en |
| network_acronym_str | anni |
| network_name_str | oai-lr-anni |
| oai_identifier_str | oai:colibri.udelar.edu.uy:20.500.12008/28675 |
| publishDate | 2019 |
| publishDateSort | 2019 |
| publisher.none.fl_str_mv | MDPI |
| reponame_str | COLIBRI |
| repository.mail.fl_str_mv | |
| repository.name.fl_str_mv | |
| repository_id_str | |
| rights_invalid_str_mv | Licencia Creative Commons Atribución (CC - By 4.0) |
| spelling | A nature-inspired design yields a new class of steroids against trypanosomatidsAguilera, ElenaPerdomo, CintyaEspíndola, AlejandraCorvo, IleanaFaral-Tello, PaulaRobello Porto, CarlosSerna, ElvaBenítez, FátimaRiveros, R.Torres, SusanaVera de Bilbao, N.I.Yaluff, GloriaÁlvarez, GuzmánAnti-T. cruzi activity in vitro and in vivoAnti-Leishmania spp. activity in vitro and in vivoCytotoxicity and genotoxicityThis article belongs to the Special Issue Drug Discovery for Neglected DiseasesChagas disease and Leishmaniasis are neglected endemic protozoan diseases recognized as public health problems by the World Health Organization. These diseases affect millions of people around the world however, efficient and low-cost treatments are not available. Different steroid molecules with antimicrobial and antiparasitic activity were isolated from diverse organisms (ticks, plants, fungi). These molecules have complex structures that make de novo synthesis extremely difficult. In this work, we designed new and simpler compounds with antiparasitic potential inspired in natural steroids and synthesized a series of nineteen steroidal arylideneketones and thiazolidenehydrazines. We explored their biological activity against Leishmania infantum, Leishmania amazonensis, and Trypanosoma cruzi in vitro and in vivo. We also assayed their genotoxicity and acute toxicity in vitro and in mice. The best compound, a steroidal thiosemicarbazone compound 8 (ID_1260) was active in vitro (IC50 200 nM) and in vivo (60% infection reduction at 50 mg/kg) in Leishmania and T. cruzi. It also has low toxicity in vitro and in vivo (LD50 >2000 mg/kg) and no genotoxic effects, being a promising compound for anti-trypanosomatid drug development.MDPIAguilera Elena, Universidad de la República (Uruguay). Facultad de Ciencias. Instituto de Química Biológica.Perdomo Cintya, Universidad de la República (Uruguay). CENUR.Espíndola Alejandra, Universidad de la República (Uruguay). CENUR.Corvo Ileana, Universidad de la República (Uruguay). CENUR.Faral-Tello Paula, Instituto Pasteur (Montevideo).Robello Porto Carlos, Instituto Pasteur (Montevideo).Serna ElvaBenítez F.Riveros R.Torres S.Vera de Bilbao N.I.Yaluff GloriaÁlvarez Guzmán, Universidad de la República (Uruguay). CENUR.2021-07-22T14:39:19Z2021-07-22T14:39:19Z2019Artículoinfo:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersion22 h.application/pdfAguilera, E, Perdomo, C, Espindola, A, y otros "A nature-inspired design yields a new class of steroids against trypanosomatids". Molecules. [en línea] 2019, 24(20): 3800. DOI: 10.3390/molecules242038001420-3049https://hdl.handle.net/20.500.12008/2867510.3390/molecules24203800reponame:COLIBRIinstname:Universidad de la Repúblicainstacron:Universidad de la RepúblicaenengMolecules, 2019, 24(20): 3800Las obras depositadas en el Repositorio se rigen por la Ordenanza de los Derechos de la Propiedad Intelectual de la Universidad de la República.(Res. Nº 91 de C.D.C. de 8/III/1994 – D.O. 7/IV/1994) y por la Ordenanza del Repositorio Abierto de la Universidad de la República (Res. Nº 16 de C.D.C. de 07/10/2014)info:eu-repo/semantics/openAccessLicencia Creative Commons Atribución (CC - By 4.0)oai:colibri.udelar.edu.uy:20.500.12008/286752026-04-14T10:09:42Z |
| spellingShingle | A nature-inspired design yields a new class of steroids against trypanosomatids Aguilera, Elena Anti-T. cruzi activity in vitro and in vivo Anti-Leishmania spp. activity in vitro and in vivo Cytotoxicity and genotoxicity |
| status_str | publishedVersion |
| title | A nature-inspired design yields a new class of steroids against trypanosomatids |
| title_full | A nature-inspired design yields a new class of steroids against trypanosomatids |
| title_fullStr | A nature-inspired design yields a new class of steroids against trypanosomatids |
| title_full_unstemmed | A nature-inspired design yields a new class of steroids against trypanosomatids |
| title_short | A nature-inspired design yields a new class of steroids against trypanosomatids |
| title_sort | A nature-inspired design yields a new class of steroids against trypanosomatids |
| topic | Anti-T. cruzi activity in vitro and in vivo Anti-Leishmania spp. activity in vitro and in vivo Cytotoxicity and genotoxicity |
| url | https://hdl.handle.net/20.500.12008/28675 |