| Full text | |
| Author(s): Show less - |
Ferreira, Leticia T.
[1]
;
Venancio, Vinicius P.
[2]
;
Kawano, Taila
[2, 3]
;
Abrao, Lailah C. C.
[2, 3]
;
Tavella, Tatyana A.
[1]
;
Almeida, Ludimila D.
[4]
;
Pires, Gabriel S.
[4]
;
Bilsland, Elizabeth
[4]
;
Sunnerhagen, Per
[5]
;
Azevedo, Luciana
[6]
;
Talcott, Stephen T.
[2]
;
Mertens-Talcott, Susanne U.
[2]
;
Costa, Fabio T. M.
[1]
Total Authors: 13
|
| Affiliation: | [1] Univ Campinas UNICAMP, Lab Trop Dis Prof Dr Luiz Jacintho da Silva, Dept Genet Evolut Microbiol & Immunol, BR-13083970 Campinas, SP - Brazil
[2] Texas A&M Univ, Dept Nutr & Food Sci, College Stn, TX 77843 - USA
[3] Univ Fed Alfenas, Fac Pharmaceut Sci, BR-37130001 Alfenas, MG - Brazil
[4] Univ Campinas UNICAMP, Synthet Biol Lab, Dept Struct & Funct Biol, Inst Biol, BR-13083970 Campinas, SP - Brazil
[5] Univ Gothenburg, Dept Chem & Mol Biol, SE-40530 Gothenburg - Sweden
[6] Univ Fed Alfenas, Lab Nutr & Toxicol Anal Vivo LANTIN, Fac Nutr, Alfenas, MG - Brazil
Total Affiliations: 6
|
| Document type: | Journal article |
| Source: | ACS OMEGA; v. 4, n. 13, p. 15628-15635, SEP 24 2019. |
| Web of Science Citations: | 0 |
| Abstract | |
Malaria remains a major detrimental parasitic disease in the developing world, with more than 200 million cases annually. Widespread drug-resistant parasite strains push for the development of novel antimalarial drugs. Plant-derived natural products are key sources of antimalarial molecules. Euterpe oleracea Martius ({''}acai{''}) originates from Brazil and has anti-inflammatory and antineoplasic properties. Here, we evaluated the antimalarial efficacy of three phenolic fractions of acai; total phenolics (1), nonanthocyanin phenolics (2), and total anthocyanins (3). In vitro, fraction 2 moderately inhibited parasite growth in chloroquine-sensitive (HB3) and multiresistant (Dd2) Plasmodium falciparum strains, while none of the fractions was toxic to noncancer cells. Despite the limited activity in vitro, the oral treatment with 20 mg/kg of fraction 1 reduced parasitemia by 89.4% in Plasmodium chabaudi-infected mice and prolonged survival. Contrasting in vitro and in vivo activities of 1 suggest key antiplasmodial roles for polyphenol metabolites rather than the fraction itself. Finally, we performed haploinsufficiency chemical genomic profiling (HIP) utilizing heterozygous Saccharomyces cerevisiae deletion mutants to identify molecular mechanisms of acai fractions. HIP results indicate proteostasis as the main cellular pathway affected by fraction 2. These results open avenues to develop acai polyphenols as potential new antimalarial candidates. (AU) | |
| FAPESP's process: | 15/03553-6 - Engineering yeast cells for drug discovery |
| Grantee: | Elizabeth Bilsland |
| Support Opportunities: | Research Grants - Young Investigators Grants |
| FAPESP's process: | 17/01986-8 - Determination of substrate specificity of plasma membrane transporters from Saccharomyces cerevisiae and Homo sapiens |
| Grantee: | Ludimila Dias Almeida |
| Support Opportunities: | Scholarships in Brazil - Doctorate |
| FAPESP's process: | 17/18611-7 - Development of new tools for search and validation of molecular targets for therapy against Plasmodium vivax |
| Grantee: | Fabio Trindade Maranhão Costa |
| Support Opportunities: | Research Projects - Thematic Grants |
| FAPESP's process: | 17/50400-6 - Advancing academic partnership in the discovery of anti malarial microbial metabolites of botanicals |
| Grantee: | Fabio Trindade Maranhão Costa |
| Support Opportunities: | Regular Research Grants |
| FAPESP's process: | 18/07007-4 - Identification of new antimalarial treatments through a target-centred "drug repositioning" approach |
| Grantee: | Elizabeth Bilsland |
| Support Opportunities: | Regular Research Grants |