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

dc.creatorUllah, Asad
dc.creatorBaratto, Leopoldo Clemente
dc.creatorPaula, Renata C.
dc.creatorSilva, Luz Helena Villamizar
dc.creatorSoares, Maurilio José
dc.creatorOliveira, Brás H.
dc.date2017-07-26T15:31:37Z
dc.date2017-07-26T15:31:37Z
dc.date2016
dc.date.accessioned2023-09-26T23:46:06Z
dc.date.available2023-09-26T23:46:06Z
dc.identifierULLAH, 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.identifier1678-4790
dc.identifierhttps://www.arca.fiocruz.br/handle/icict/20411
dc.identifier10.5935/0103-5053.20160021
dc.identifier.urihttps://repositorioslatinoamericanos.uchile.cl/handle/2250/8893996
dc.descriptionDerivatives 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.
dc.formatapplication/pdf
dc.languageeng
dc.publisherSociedade Brasileira de Química
dc.rightsopen access
dc.subjectÁcido betulínico
dc.subjectAntimalarials
dc.subjectBetulinic acid
dc.subjectPlasmodium falciparum
dc.subjectTrypanosoma cruzi
dc.subjectAntimaláricos
dc.subjectPlasmodium falciparum
dc.subjectTrypanosoma cruzi
dc.subjectAntimaláricos
dc.subjectPlasmodium falciparum
dc.subjectTrypanosoma cruzi
dc.titlePreparation of derivates of Betulinic Acid, Steviol and Isosteviol and avaluation of Antitrypanosomal and Antimalarial Activities
dc.typeArticle


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