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Correlation study on methoxylation pattern of flavonoids and their heme-targeted antiplasmodial activity.

Abstract：

:A library of 33 polymethoxylated flavones (PMF) was evaluated for heme-binding affinity by biomimetic MS assay and in vitro antiplasmodial activity on two strains of P. falciparum. Stability of heme adducts was discussed using the dissociation voltage at 50% (DV50). No correlation was observed between the methoxylation pattern and the antiparasitic activity, either for the 3D7 chloroquine-sensitive or for the W2 chloroquine-resistant P. falciparum strains. However, in each PMF family an increased DV50 was observed for the derivatives methoxylated in position 5. Measurement of intra-erythrocytic hemozoin formation of selected derivatives was performed and hemozoin concentration was inversely correlated with heme-binding affinity. Kaempferol showed no influence on hemozoin formation, reinforcing the hypothesis that this compound may exert in vitro antiplasmodial activity mostly through other pathways. Pentamethoxyquercetin has simultaneously demonstrated a significant biological activity and a strong interaction with heme, suggesting that inhibition of hemozoin formation is totally or partially responsible for its antiparasitic effect.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Ortiz S,Vásquez-Ocmín PG,Cojean S,Bouzidi C,Michel S,Figadère B,Grougnet R,Boutefnouchet S,Maciuk A

doi

10.1016/j.bioorg.2020.104243

subject

Has Abstract

pub_date

2020-11-01 00:00:00

pages

104243

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(20)31541-8

journal_volume

104

pub_type

杂志文章

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