Preparation of derivates of Betulinic Acid, Steviol and Isosteviol and avaluation of Antitrypanosomal and Antimalarial Activities

Detalhes bibliográficos
Autor(a) principal: Ullah, Asad
Data de Publicação: 2016
Outros Autores: Baratto, Leopoldo Clemente, Paula, Renata C., Silva, Luz Helena Villamizar, Soares, Maurilio José, Oliveira, Brás H.
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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spelling 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 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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
instname_str Fundação Oswaldo Cruz (FIOCRUZ)
instacron_str FIOCRUZ
institution FIOCRUZ
reponame_str Repositório Institucional da FIOCRUZ (ARCA)
collection Repositório Institucional da FIOCRUZ (ARCA)
bitstream.url.fl_str_mv https://www.arca.fiocruz.br/bitstream/icict/20411/1/license.txt
https://www.arca.fiocruz.br/bitstream/icict/20411/2/Preparation%20of%20Derivatives%20of%20Betulinic%20Acid%2c%20Steviol%20and%20Isosteviol%20and%20Evaluation.pdf
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