| Author | Ullah, Asad | |
| Author | Baratto, Leopoldo Clemente | |
| Author | Paula, Renata C. | |
| Author | Silva, Luz Helena Villamizar | |
| Author | Soares, Maurilio José | |
| Author | Oliveira, Brás H. | |
| Access date | 2017-07-26T15:31:37Z | |
| Available date | 2017-07-26T15:31:37Z | |
| Document date | 2016 | |
| Citation | 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. | pt_BR |
| ISSN | 1678-4790 | pt_BR |
| URI | https://www.arca.fiocruz.br/handle/icict/20411 | |
| Language | eng | pt_BR |
| Publisher | Sociedade Brasileira de Química | pt_BR |
| Rights | open access | pt_BR |
| Subject in Portuguese | Ácido betulínico | pt_BR |
| Title | Preparation of derivates of Betulinic Acid, Steviol and Isosteviol and avaluation of Antitrypanosomal and Antimalarial Activities | pt_BR |
| Type | Article | pt_BR |
| DOI | 10.5935/0103-5053.20160021 | pt_BR |
| Abstract | 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. | pt_BR |
| Affilliation | Universidade Federal do Paraná. Centro Politécnico. Departamento de Química. Curitiba, PR, Brasil. | pt_BR |
| Affilliation | Universidade Federal do Paraná. Centro Politécnico. Departamento de Química. Curitiba, PR, Brasil. | pt_BR |
| Affilliation | Universidade Federal de Minas Gerais, Faculdade de Farmácia. Belo Horizonte, MG, Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Carlos Chagas. Laboratório de Biologia Celular, Curitiba, PR, Brasil. | pt_BR |
| Affilliation | Universidade Federal do Paraná. Centro Politécnico. Departamento de Química. Curitiba, PR, Brasil. | pt_BR |
| Subject | Antimalarials | pt_BR |
| Subject | Betulinic acid | pt_BR |
| Subject | Plasmodium falciparum | pt_BR |
| Subject | Trypanosoma cruzi | pt_BR |
| Subject in Spanish | Antimaláricos | pt_BR |
| Subject in Spanish | Plasmodium falciparum | pt_BR |
| Subject in Spanish | Trypanosoma cruzi | pt_BR |
| DeCS | Antimaláricos | pt_BR |
| DeCS | Plasmodium falciparum | pt_BR |
| DeCS | Trypanosoma cruzi | pt_BR |
