In vitro evaluation of the cytotoxic and trypanocidal activities of Ampelozizyphus amazonicus (Rhamnaceae)



Document title: In vitro evaluation of the cytotoxic and trypanocidal activities of Ampelozizyphus amazonicus (Rhamnaceae)
Journal: Brazilian journal of medical and biological research
Database: PERIÓDICA
System number: 000350341
ISSN: 0100-879X
Authors: 1
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2
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Institutions: 1Universidade do Amazonas, Departamento de Quimica, Manaus, Amazonas. Brasil
2Universidade de Ribeirao Preto, Unidade de Biotecnologia Vegetal, Ribeirao Preto, Sao Paulo. Brasil
3Universidade de Sao Paulo, Faculdade de Ciencias Farmaceuticas, Ribeirao Preto, Sao Paulo. Brasil
Year:
Season: May
Volumen: 40
Number: 5
Pages: 663-670
Country: Brasil
Language: Inglés
Document type: Artículo
Approach: Experimental, aplicado
English abstract Ampelozizyphus amazonicus Ducke is a tree commonly found in the Amazon region and an extract of its stem bark is popularly used as an antimalarial and anti-inflammatory agent and as an antidote to snake venom. Ursolic acid; five lupane type triterpenes: betulin, betulinic acid, lupenone, 3ß-hydroxylup-20(29)-ene-27,28-dioic acid, and 2a,3ß-dihydroxylup-20(29)-ene-27,28-dioic acid, and three phytosteroids: stigmasterol, sitosterol and campesterol, have been isolated from stem extracts of A. amazonicus Ducke. Their structures were characterized by spectral data including COSY and HMQC. In an in vitro biological screening of the isolated compounds, 3ß-hydroxylup-20(29)-ene-27,28-dioic acid was cytotoxic against the SKBR-3 human adenocarcinoma cell line (1 to 10 mg/mL), while 2a,3ß-dihydroxylup-20(29)-ene-27,28-dioic acid exhibited cytotoxicity against both SKBR-3 human adenocarcinoma and C-8161 human melanoma tumor cell lines (>0.1 mg/mL). In the present study, different extracts and some fractions of this plant were also investigated for trypanocidal activity due to the presence of pentacyclic triterpenes. The triterpene classes are potent against Trypanosoma cruzi. The bioassays were carried out using blood collected from Swiss albino mice by cardiac puncture during the parasitemic peak (7th day) after infection with the Y strain of T. cruzi. The results obtained showed that A. amazonicus is a potential source of bioactive compounds since its extracts and fractions isolated from it exhibited in vitro parasite lysis against trypomastigote forms of T. cruzi at concentrations >100 µg/mL. Fractions containing mainly betulin, lupenone, 3ß-hydroxylup-20(29)-ene-27,28-dioic acid, and 2a,3ß-dihydroxylup-20(29)-ene-27,28-dioic acid showed more activity than crude extracts
Disciplines: Medicina
Keyword: Farmacología,
Fitoquímica,
Triterpenos pentacíclicos,
Actividad citotóxica,
Actividad tripanocida,
Ampelozizyphus amazonicus,
Rhamnaceae
Keyword: Medicine,
Pharmacology,
Phytochemistry,
Pentacyclic triterpenes,
Cytotoxic activity,
Trypanocidal activity,
Ampelozizyphus amazonicus,
Rhamnaceae
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