| Full text | |
| Author(s): |
Barrosa, Kaidu H.
[1]
;
Pinto, Erika G.
[2, 3]
;
Tempone, Andre G.
[2]
;
Martins, Euder Glendes A.
[4]
;
Lago, Joao Henrique G.
[1]
Total Authors: 5
|
| Affiliation: | [1] Univ Fed Sao Paulo, Inst Ciencias Ambientais Quim & Farmaceut, BR-09972270 Sao Paulo - Brazil
[2] Adolfo Lutz Inst, Ctr Parasitol & Micol, Sao Paulo - Brazil
[3] Univ Sao Paulo, Inst Med Trop Sao Paulo, Sao Paulo - Brazil
[4] Univ Sao Paulo, Dept Bot, Inst Biociencias, Sao Paulo - Brazil
Total Affiliations: 4
|
| Document type: | Journal article |
| Source: | Planta Medica; v. 80, n. 15, p. 1310-1314, OCT 2014. |
| Web of Science Citations: | 8 |
| Abstract | |
Bioactivity-guided fractionation of the MeOH extract from the leaves of Alchornea glandulosa afforded a newguanidine alkaloid named alchornedine, as well as two other inactive derivatives (pteroginine and pteroginidine). The structure of alchornedine, which shows a very rare ring system, was elucidated based on NMR, IR, and MS spectral analyses. This compound displayed antiprotozoal activity against Trypanosoma cruzi (Y strain). By using the MTT assay, the trypomastigotes showed an IC50 value of 93 mu g/mL (443 mu M), a similar effectiveness to the standard drug benznidazole. Alchornedine also showed activity against the intracellular amastigotes, with an IC50 value of 27 mu g/mL (129 mu M). Using benznidazole as a standard drug, this guanidine alkaloid was approximately 3-fold more effective against the intracellular form of T. cruzi. The mammalian cytotoxicity of alchornedine was verified against NCTC cells and demonstrated an IC50 of 50 mu g/mL (237 mu M), but this compound demonstrated a selective elimination of parasites inside macrophages without affecting the morphology of the host cells. Alchornedine was effective against both clinical forms of T. cruzi and could be used as a scaffold for future drug design studies against American trypanosomiasis. (AU) | |
| FAPESP's process: | 11/51739-0 - Sustainable use of biodiversity in Atlantic Forest remnants in São Paulo: evaluation, isolation and molecular characterization of bioactive secondary metabolites in plant species |
| Grantee: | João Henrique Ghilardi Lago |
| Support Opportunities: | BIOTA-FAPESP Program - Regular Research Grants |