Title |
Two series of new semisynthetic triterpene derivatives: differences in anti-malarial activity, cytotoxicity and mechanism of action
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Published in |
Malaria Journal, March 2013
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DOI | 10.1186/1475-2875-12-89 |
Pubmed ID | |
Authors |
Gloria NS da Silva, Nicole RG Maria, Desirée C Schuck, Laura N Cruz, Miriam S de Moraes, Myna Nakabashi, Cedric Graebin, Grace Gosmann, Célia RS Garcia, Simone CB Gnoatto |
Abstract |
The discovery and development of anti-malarial compounds of plant origin and semisynthetic derivatives thereof, such as quinine (QN) and chloroquine (CQ), has highlighted the importance of these compounds in the treatment of malaria. Ursolic acid analogues bearing an acetyl group at C-3 have demonstrated significant anti-malarial activity. With this in mind, two new series of betulinic acid (BA) and ursolic acid (UA) derivatives with ester groups at C-3 were synthesized in an attempt to improve anti-malarial activity, reduce cytotoxicity, and search for new targets. In vitro activity against CQ-sensitive Plasmodium falciparum 3D7 and an evaluation of cytotoxicity in a mammalian cell line (HEK293T) are reported. Furthermore, two possible mechanisms of action of anti-malarial compounds have been evaluated: effects on mitochondrial membrane potential (ΔΨm) and inhibition of β-haematin formation. |
X Demographics
Geographical breakdown
Country | Count | As % |
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United Kingdom | 2 | 67% |
Unknown | 1 | 33% |
Demographic breakdown
Type | Count | As % |
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Members of the public | 2 | 67% |
Unknown | 1 | 33% |
Mendeley readers
Geographical breakdown
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United Kingdom | 1 | 1% |
Brazil | 1 | 1% |
Unknown | 73 | 97% |
Demographic breakdown
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Student > Master | 16 | 21% |
Student > Ph. D. Student | 14 | 19% |
Student > Bachelor | 8 | 11% |
Student > Doctoral Student | 6 | 8% |
Professor > Associate Professor | 4 | 5% |
Other | 13 | 17% |
Unknown | 14 | 19% |
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Biochemistry, Genetics and Molecular Biology | 3 | 4% |
Other | 4 | 5% |
Unknown | 17 | 23% |