Licochalcone a Exhibits Leishmanicidal Activity in vitro and in Experimental Model of Leishmania (Leishmania) Infantum
The efficacy of Licochalcone A (LicoA) and its two analogs were reported against Leishmania (Leishmania) amazonensis and Leishmania (Leishmania) infantum in vitro, and in experimental model of L. (L.) infantum in vitro. Initially, LicoA and its analogs were screened against promastigote forms of L....
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Frontiers Media S.A.
2020-12-01
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| Series: | Frontiers in Veterinary Science |
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| Online Access: | https://www.frontiersin.org/articles/10.3389/fvets.2020.00527/full |
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| author | Julia M. Souza Érica A. A. de Carvalho Ana Carolina B. B. Candido Rafael P. de Mendonça Maria Fernanda da Silva Renato L. T. Parreira Fernanda G. G. Dias Sérgio R. Ambrósio Andrea T. Arantes Ademar A. da Silva Filho Aline N. Nascimento Monique R. Costa Mirela I. Sairre Rodrigo C. S. Veneziani Lizandra G. Magalhães Lizandra G. Magalhães |
| author_facet | Julia M. Souza Érica A. A. de Carvalho Ana Carolina B. B. Candido Rafael P. de Mendonça Maria Fernanda da Silva Renato L. T. Parreira Fernanda G. G. Dias Sérgio R. Ambrósio Andrea T. Arantes Ademar A. da Silva Filho Aline N. Nascimento Monique R. Costa Mirela I. Sairre Rodrigo C. S. Veneziani Lizandra G. Magalhães Lizandra G. Magalhães |
| author_sort | Julia M. Souza |
| collection | DOAJ |
| description | The efficacy of Licochalcone A (LicoA) and its two analogs were reported against Leishmania (Leishmania) amazonensis and Leishmania (Leishmania) infantum in vitro, and in experimental model of L. (L.) infantum in vitro. Initially, LicoA and its analogs were screened against promastigote forms of L. (L.) amazonensis. LicoA was the most active compound, with IC50 values of 20.26 and 3.88 μM at 24 and 48 h, respectively. Against amastigote forms, the IC50 value of LicoA was 36.84 μM at 48 h. In the next step, the effectivity of LicoA was evaluated in vitro against promastigote and amastigote forms of L. (L.) infantum. Results demonstrated that LicoA exhibited leishmanicidal activity in vitro against promastigote forms with IC50 values of 41.10 and 12.47 μM at 24 and 48 h, respectively; against amastigote forms the IC50 value was 29.58 μM at 48 h. Assessment of cytotoxicity demonstrated that LicoA exhibited moderate mammalian cytotoxicity against peritoneal murine macrophages; the CC50 value was 123.21 μM at 48 h and showed about 30% of hemolytic activity at concentration of 400 μM. L. (L.) infantum-infected hamsters and treated with LicoA at 50 mg/kg for eight consecutive days was able to significantly reduce the parasite burden in both liver and spleen in 43.67 and 39.81%, respectively, when compared with negative control group. These findings suggest that chalcone-type flavonoids can be a promising class of natural products to be considered in the search of new, safe, and effective compounds capable to treat canine visceral leishmaniosis (CVL). |
| first_indexed | 2024-12-22T21:03:33Z |
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| institution | Directory Open Access Journal |
| issn | 2297-1769 |
| language | English |
| last_indexed | 2024-12-22T21:03:33Z |
| publishDate | 2020-12-01 |
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| series | Frontiers in Veterinary Science |
| spelling | doaj.art-d81a61290d4c4c848f2b3eb4621d1d402022-12-21T18:12:45ZengFrontiers Media S.A.Frontiers in Veterinary Science2297-17692020-12-01710.3389/fvets.2020.00527562820Licochalcone a Exhibits Leishmanicidal Activity in vitro and in Experimental Model of Leishmania (Leishmania) InfantumJulia M. Souza0Érica A. A. de Carvalho1Ana Carolina B. B. Candido2Rafael P. de Mendonça3Maria Fernanda da Silva4Renato L. T. Parreira5Fernanda G. G. Dias6Sérgio R. Ambrósio7Andrea T. Arantes8Ademar A. da Silva Filho9Aline N. Nascimento10Monique R. Costa11Mirela I. Sairre12Rodrigo C. S. Veneziani13Lizandra G. Magalhães14Lizandra G. Magalhães15Núcleo de Pesquisa em Ciências Exatas e Tecnológica, Universidade de Franca, Franca, BrazilNúcleo de Pesquisa em Ciências Exatas e Tecnológica, Universidade de Franca, Franca, BrazilNúcleo de Pesquisa em Ciências Exatas e Tecnológica, Universidade de Franca, Franca, BrazilPós Graduação em Ciência Animal, Universidade de Franca, Franca, BrazilPós Graduação em Ciência Animal, Universidade de Franca, Franca, BrazilNúcleo de Pesquisa em Ciências Exatas e Tecnológica, Universidade de Franca, Franca, BrazilPós Graduação em Ciência Animal, Universidade de Franca, Franca, BrazilNúcleo de Pesquisa em Ciências Exatas e Tecnológica, Universidade de Franca, Franca, BrazilCentro Tecnológico Agropecuário, Batatais, BrazilDepartamento de Ciências Farmacêuticas, Universidade Federal de Juiz de Fora, Juiz de Fora, BrazilCentro de Ciências Naturais e Humanas, Universidade Federal Do ABC, Santo André, BrazilCentro de Ciências Naturais e Humanas, Universidade Federal Do ABC, Santo André, BrazilCentro de Ciências Naturais e Humanas, Universidade Federal Do ABC, Santo André, BrazilNúcleo de Pesquisa em Ciências Exatas e Tecnológica, Universidade de Franca, Franca, BrazilNúcleo de Pesquisa em Ciências Exatas e Tecnológica, Universidade de Franca, Franca, BrazilPós Graduação em Ciência Animal, Universidade de Franca, Franca, BrazilThe efficacy of Licochalcone A (LicoA) and its two analogs were reported against Leishmania (Leishmania) amazonensis and Leishmania (Leishmania) infantum in vitro, and in experimental model of L. (L.) infantum in vitro. Initially, LicoA and its analogs were screened against promastigote forms of L. (L.) amazonensis. LicoA was the most active compound, with IC50 values of 20.26 and 3.88 μM at 24 and 48 h, respectively. Against amastigote forms, the IC50 value of LicoA was 36.84 μM at 48 h. In the next step, the effectivity of LicoA was evaluated in vitro against promastigote and amastigote forms of L. (L.) infantum. Results demonstrated that LicoA exhibited leishmanicidal activity in vitro against promastigote forms with IC50 values of 41.10 and 12.47 μM at 24 and 48 h, respectively; against amastigote forms the IC50 value was 29.58 μM at 48 h. Assessment of cytotoxicity demonstrated that LicoA exhibited moderate mammalian cytotoxicity against peritoneal murine macrophages; the CC50 value was 123.21 μM at 48 h and showed about 30% of hemolytic activity at concentration of 400 μM. L. (L.) infantum-infected hamsters and treated with LicoA at 50 mg/kg for eight consecutive days was able to significantly reduce the parasite burden in both liver and spleen in 43.67 and 39.81%, respectively, when compared with negative control group. These findings suggest that chalcone-type flavonoids can be a promising class of natural products to be considered in the search of new, safe, and effective compounds capable to treat canine visceral leishmaniosis (CVL).https://www.frontiersin.org/articles/10.3389/fvets.2020.00527/fullcutaneous leishmaniasisvisceral leishmaniasiscanine visceral leishmaniasislicochalcone Aleishmanicidal activity |
| spellingShingle | Julia M. Souza Érica A. A. de Carvalho Ana Carolina B. B. Candido Rafael P. de Mendonça Maria Fernanda da Silva Renato L. T. Parreira Fernanda G. G. Dias Sérgio R. Ambrósio Andrea T. Arantes Ademar A. da Silva Filho Aline N. Nascimento Monique R. Costa Mirela I. Sairre Rodrigo C. S. Veneziani Lizandra G. Magalhães Lizandra G. Magalhães Licochalcone a Exhibits Leishmanicidal Activity in vitro and in Experimental Model of Leishmania (Leishmania) Infantum Frontiers in Veterinary Science cutaneous leishmaniasis visceral leishmaniasis canine visceral leishmaniasis licochalcone A leishmanicidal activity |
| title | Licochalcone a Exhibits Leishmanicidal Activity in vitro and in Experimental Model of Leishmania (Leishmania) Infantum |
| title_full | Licochalcone a Exhibits Leishmanicidal Activity in vitro and in Experimental Model of Leishmania (Leishmania) Infantum |
| title_fullStr | Licochalcone a Exhibits Leishmanicidal Activity in vitro and in Experimental Model of Leishmania (Leishmania) Infantum |
| title_full_unstemmed | Licochalcone a Exhibits Leishmanicidal Activity in vitro and in Experimental Model of Leishmania (Leishmania) Infantum |
| title_short | Licochalcone a Exhibits Leishmanicidal Activity in vitro and in Experimental Model of Leishmania (Leishmania) Infantum |
| title_sort | licochalcone a exhibits leishmanicidal activity in vitro and in experimental model of leishmania leishmania infantum |
| topic | cutaneous leishmaniasis visceral leishmaniasis canine visceral leishmaniasis licochalcone A leishmanicidal activity |
| url | https://www.frontiersin.org/articles/10.3389/fvets.2020.00527/full |
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