Antiplasmodial activity and cytotoxicity, isolation of active alkaloids, and dereplication of Xylopia sericea leaves ethanol extract by UPLC-DAD-ESI-MS/MS.
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Date
2019
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Abstract
Objectives: To assess the antiplasmodial activity of the ethanol extract of Xylopia
sericea leaves, Annonaceae, often associated with antimalarial use and to perform
a bioguided isolation of active compounds.
Methods: Dereplication of ethanol extract by the UPLC-DAD-ESI-MS/MS technique allowed the identification of the major constituents, isolation and identification of alkaloids. The antiplasmodial and cytotoxic activity of the extract,
fractions and isolated compounds was evaluated against the chloroquine-resistant
W2 strain Plasmodium falciparum and HepG2 cells, respectively.
Key findings: Ethanol extract showed high reduction of parasitemia as well as
moderate cytotoxicity (86.5 3.0% growth inhibition at 50 lg/ml and CC50
72.1 5.1 lg/ml, respectively). A total of eight flavonoids were identified, and
two aporphine alkaloids, anonaine and O-methylmoschatoline, were isolated.
Anonaine disclosed significant antiplasmodial effect and moderate cytotoxicity
(IC50 23.2 2.7 lg/ml, CC50 38.3 2.3 lg/ml, SI 1.6) while O-methylmoschatoline was not active against P. falciparum and showed a low cytotoxicity
(33.5 1.9% growth inhibition at 50 lg/ml, CC50 274.4 0.5 lg/ml).
Conclusions: Characterization of Xylopia sericea leaves ethanol extract by UPLCDAD-ESI-MS/MS as well as its antiplasmodial activity and the occurrence of
anonaine and O-methylmoschatoline in this Xylopia species are reported by the
first time.
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Keywords
Extract dereplication, Flavonoids
Citation
GONTIJO, D. da C. et al. Antiplasmodial activity and cytotoxicity, isolation of active alkaloids, and dereplication of Xylopia sericea leaves ethanol extract by UPLC-DAD-ESI-MS/MS. Journal of Pharmacy and Pharmacology, v. 71, n. 2, p. 260-269, fev. 2019. Disponível em: <https://onlinelibrary.wiley.com/doi/full/10.1111/jphp.13029>. Acesso em: 25 fev. 2019.