Synthesis and Antiplasmodial Activity of Betulinic Acid and Ursolic Acid Analogues
Abstract
:1. Introduction
2. Results and Discussion
2.1. Chemical Synthesis
2.2. Antiplasmodial Assay
2.3. Cytotoxicity Assay
Compounds | IC50 (µM) P. falciparum 3D7 | IC50 (µM) HEK293T | Selectivity Index (SI) 48 h | |
---|---|---|---|---|
24 h | 48 h | |||
1 | 18 | - | - | - |
1a | 4 | >100 | >100 | - |
1b | 5 | 4 | 4 | 0.8 |
1c | 0.220 | 4 | 4 | 18 |
2 | 36 | - | - | - |
2a | 14 | - | - | - |
2b | 15 | - | - | - |
2c | 0.175 | 4 | 4 | 23 |
2.4. Infected Erythrocytes: Loading with the Calcium Indicator Fluo4/AM
3. Experimental
3.1. General
3.2. Plant Material and Isolation of Triterpenes
3.3. Chemical Synthesis
3.4. Antiplasmodial Assay
3.5. Cytotoxicity Assay
3.6. Infected Erythrocytes: Loading with the Calcium Indicator Fluo4/AM
3.7. Statistical Analysis
4. Conclusions
Acknowledgements
- Sample Availability: Samples of the compounds are available from the authors.
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Innocente, A.M.; Silva, G.N.S.; Cruz, L.N.; Moraes, M.S.; Nakabashi, M.; Sonnet, P.; Gosmann, G.; Garcia, C.R.S.; Gnoatto, S.C.B. Synthesis and Antiplasmodial Activity of Betulinic Acid and Ursolic Acid Analogues. Molecules 2012, 17, 12003-12014. https://doi.org/10.3390/molecules171012003
Innocente AM, Silva GNS, Cruz LN, Moraes MS, Nakabashi M, Sonnet P, Gosmann G, Garcia CRS, Gnoatto SCB. Synthesis and Antiplasmodial Activity of Betulinic Acid and Ursolic Acid Analogues. Molecules. 2012; 17(10):12003-12014. https://doi.org/10.3390/molecules171012003
Chicago/Turabian StyleInnocente, Adrine M., Gloria N. S. Silva, Laura Nogueira Cruz, Miriam S. Moraes, Myna Nakabashi, Pascal Sonnet, Grace Gosmann, Célia R. S. Garcia, and Simone C. B. Gnoatto. 2012. "Synthesis and Antiplasmodial Activity of Betulinic Acid and Ursolic Acid Analogues" Molecules 17, no. 10: 12003-12014. https://doi.org/10.3390/molecules171012003