Preparation of derivates of Betulinic Acid, Steviol and Isosteviol and avaluation of Antitrypanosomal and Antimalarial Activities
Autor(a) principal: | |
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Data de Publicação: | 2016 |
Outros Autores: | , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Institucional da FIOCRUZ (ARCA) |
Texto Completo: | https://www.arca.fiocruz.br/handle/icict/20411 |
Resumo: | Universidade Federal do Paraná. Centro Politécnico. Departamento de Química. Curitiba, PR, Brasil. |
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Ullah, AsadBaratto, Leopoldo ClementePaula, Renata C.Silva, Luz Helena VillamizarSoares, Maurilio JoséOliveira, Brás H.2017-07-26T15:31:37Z2017-07-26T15:31:37Z2016ULLAH, Asad et al. Preparation of derivatives of Betulinic Acid, Steviol and Isosteviol and evaluation of Antitrypanosomal and Antimalarial Activities. Journal of the Brazilian Chemical Society, v. 27, n. 7, p. 1245-1253, 2016.1678-4790https://www.arca.fiocruz.br/handle/icict/2041110.5935/0103-5053.20160021engSociedade Brasileira de QuímicaÁcido betulínicoAntimalarialsBetulinic acidPlasmodium falciparumTrypanosoma cruziAntimaláricosPlasmodium falciparumTrypanosoma cruziAntimaláricosPlasmodium falciparumTrypanosoma cruziPreparation of derivates of Betulinic Acid, Steviol and Isosteviol and avaluation of Antitrypanosomal and Antimalarial Activitiesinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleUniversidade Federal do Paraná. Centro Politécnico. Departamento de Química. Curitiba, PR, Brasil.Universidade Federal do Paraná. Centro Politécnico. Departamento de Química. Curitiba, PR, Brasil.Universidade Federal de Minas Gerais, Faculdade de Farmácia. Belo Horizonte, MG, Brasil.Fundação Oswaldo Cruz. Instituto Carlos Chagas. Laboratório de Biologia Celular, Curitiba, PR, Brasil.Universidade Federal do Paraná. Centro Politécnico. Departamento de Química. Curitiba, PR, Brasil.Derivatives of steviol, isosteviol and betulinic acid were prepared and tested in vitro against Plasmodium falciparum W2 (chloroquine-resistant) and Trypanosoma cruzi. The best results against P. falciparum were found for the betulinic acid derivatives 3-[(2,4-dinitrophenyl)hydrazono]lup- 20(29)-en-28-oic acid and 3-hydroxy-20-[(2,4-dinitrophenyl)hydrazono]-29-norlupan-28-oic acid (values concentration in that the growth of the parasites is 50% inhibited, IC50 = 9.96, 6.45 and 21.06 µg mL-1, respectively). Isosteviol was inactive but its 4-nitro- and 2,4-dinitrophenylhydrazone showed moderate activity (IC50 = 17.50-22.58 µg mL-1). The derivatives of betulinic acid were more selective to the parasite when compared with hepatoblastoma HepG2 A16 cells. The results showed that nitrophenylhydrazone derivatives of lupane and beyerane terpenes are promising prototypes of antimalarial agents. Among the compounds tested against T. cruzi the oxime of isosteviol was active against both epimastigote and trypomastigote forms of the parasite.info:eu-repo/semantics/openAccessreponame:Repositório Institucional da FIOCRUZ (ARCA)instname:Fundação Oswaldo Cruz (FIOCRUZ)instacron:FIOCRUZLICENSElicense.txtlicense.txttext/plain; charset=utf-83074https://www.arca.fiocruz.br/bitstream/icict/20411/1/license.txt0271fb68963c017aa933c7aff60379f4MD51ORIGINALPreparation of Derivatives of Betulinic Acid, Steviol and Isosteviol and Evaluation.pdfPreparation of Derivatives of Betulinic Acid, Steviol and Isosteviol and Evaluation.pdfapplication/pdf308997https://www.arca.fiocruz.br/bitstream/icict/20411/2/Preparation%20of%20Derivatives%20of%20Betulinic%20Acid%2c%20Steviol%20and%20Isosteviol%20and%20Evaluation.pdf87fc9a94901bd5dff793c06d3a5ce40cMD52TEXTPreparation of Derivatives of Betulinic Acid, Steviol and Isosteviol and Evaluation.pdf.txtPreparation of Derivatives of Betulinic Acid, Steviol and Isosteviol and Evaluation.pdf.txtExtracted texttext/plain36376https://www.arca.fiocruz.br/bitstream/icict/20411/3/Preparation%20of%20Derivatives%20of%20Betulinic%20Acid%2c%20Steviol%20and%20Isosteviol%20and%20Evaluation.pdf.txt58a203b365ce6eef05da42ae352f8e9eMD53icict/204112019-11-23 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dc.title.pt_BR.fl_str_mv |
Preparation of derivates of Betulinic Acid, Steviol and Isosteviol and avaluation of Antitrypanosomal and Antimalarial Activities |
title |
Preparation of derivates of Betulinic Acid, Steviol and Isosteviol and avaluation of Antitrypanosomal and Antimalarial Activities |
spellingShingle |
Preparation of derivates of Betulinic Acid, Steviol and Isosteviol and avaluation of Antitrypanosomal and Antimalarial Activities Ullah, Asad Ácido betulínico Antimalarials Betulinic acid Plasmodium falciparum Trypanosoma cruzi Antimaláricos Plasmodium falciparum Trypanosoma cruzi Antimaláricos Plasmodium falciparum Trypanosoma cruzi |
title_short |
Preparation of derivates of Betulinic Acid, Steviol and Isosteviol and avaluation of Antitrypanosomal and Antimalarial Activities |
title_full |
Preparation of derivates of Betulinic Acid, Steviol and Isosteviol and avaluation of Antitrypanosomal and Antimalarial Activities |
title_fullStr |
Preparation of derivates of Betulinic Acid, Steviol and Isosteviol and avaluation of Antitrypanosomal and Antimalarial Activities |
title_full_unstemmed |
Preparation of derivates of Betulinic Acid, Steviol and Isosteviol and avaluation of Antitrypanosomal and Antimalarial Activities |
title_sort |
Preparation of derivates of Betulinic Acid, Steviol and Isosteviol and avaluation of Antitrypanosomal and Antimalarial Activities |
author |
Ullah, Asad |
author_facet |
Ullah, Asad Baratto, Leopoldo Clemente Paula, Renata C. Silva, Luz Helena Villamizar Soares, Maurilio José Oliveira, Brás H. |
author_role |
author |
author2 |
Baratto, Leopoldo Clemente Paula, Renata C. Silva, Luz Helena Villamizar Soares, Maurilio José Oliveira, Brás H. |
author2_role |
author author author author author |
dc.contributor.author.fl_str_mv |
Ullah, Asad Baratto, Leopoldo Clemente Paula, Renata C. Silva, Luz Helena Villamizar Soares, Maurilio José Oliveira, Brás H. |
dc.subject.other.pt_BR.fl_str_mv |
Ácido betulínico |
topic |
Ácido betulínico Antimalarials Betulinic acid Plasmodium falciparum Trypanosoma cruzi Antimaláricos Plasmodium falciparum Trypanosoma cruzi Antimaláricos Plasmodium falciparum Trypanosoma cruzi |
dc.subject.en.pt_BR.fl_str_mv |
Antimalarials Betulinic acid Plasmodium falciparum Trypanosoma cruzi |
dc.subject.es.pt_BR.fl_str_mv |
Antimaláricos Plasmodium falciparum Trypanosoma cruzi |
dc.subject.decs.pt_BR.fl_str_mv |
Antimaláricos Plasmodium falciparum Trypanosoma cruzi |
description |
Universidade Federal do Paraná. Centro Politécnico. Departamento de Química. Curitiba, PR, Brasil. |
publishDate |
2016 |
dc.date.issued.fl_str_mv |
2016 |
dc.date.accessioned.fl_str_mv |
2017-07-26T15:31:37Z |
dc.date.available.fl_str_mv |
2017-07-26T15:31:37Z |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/article |
format |
article |
status_str |
publishedVersion |
dc.identifier.citation.fl_str_mv |
ULLAH, Asad et al. Preparation of derivatives of Betulinic Acid, Steviol and Isosteviol and evaluation of Antitrypanosomal and Antimalarial Activities. Journal of the Brazilian Chemical Society, v. 27, n. 7, p. 1245-1253, 2016. |
dc.identifier.uri.fl_str_mv |
https://www.arca.fiocruz.br/handle/icict/20411 |
dc.identifier.issn.pt_BR.fl_str_mv |
1678-4790 |
dc.identifier.doi.pt_BR.fl_str_mv |
10.5935/0103-5053.20160021 |
identifier_str_mv |
ULLAH, Asad et al. Preparation of derivatives of Betulinic Acid, Steviol and Isosteviol and evaluation of Antitrypanosomal and Antimalarial Activities. Journal of the Brazilian Chemical Society, v. 27, n. 7, p. 1245-1253, 2016. 1678-4790 10.5935/0103-5053.20160021 |
url |
https://www.arca.fiocruz.br/handle/icict/20411 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
dc.publisher.none.fl_str_mv |
Sociedade Brasileira de Química |
publisher.none.fl_str_mv |
Sociedade Brasileira de Química |
dc.source.none.fl_str_mv |
reponame:Repositório Institucional da FIOCRUZ (ARCA) instname:Fundação Oswaldo Cruz (FIOCRUZ) instacron:FIOCRUZ |
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Fundação Oswaldo Cruz (FIOCRUZ) |
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FIOCRUZ |
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FIOCRUZ |
reponame_str |
Repositório Institucional da FIOCRUZ (ARCA) |
collection |
Repositório Institucional da FIOCRUZ (ARCA) |
bitstream.url.fl_str_mv |
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