In vitro antimalarial activity of hyperforin, a prenylated acylphloroglucinol. A structure-activity study

Luisella Verotta, Giovanni Appendino, Ezio Bombardelli, Reto Brun

Risultato della ricerca: Contributo su rivistaArticolo in rivistapeer review

Abstract

The antimalarial activity of hyperforin, a phenol-like compound that can be easily absorbed orally, and a series of derivatives variously modified on the cyclohexatrienone system was investigated. Hyperforin was active against Plasmodium falciparum with an IC50 value in the micromolar range, and the activity was not critically dependent on either its phenol-like sensitivity to autooxidation or the presence of unsaturation on the prenyl residues. Related phloroglucinols like the hop β-acids and the enantiomers of usnic acid showed only marginal activity, suggesting that hyperforin is a new antimalarial chemotype.

Lingua originaleInglese
pagine (da-a)1544-1548
Numero di pagine5
RivistaBioorganic and Medicinal Chemistry Letters
Volume17
Numero di pubblicazione6
DOI
Stato di pubblicazionePubblicato - 15 mar 2007
Pubblicato esternamente

Fingerprint

Entra nei temi di ricerca di 'In vitro antimalarial activity of hyperforin, a prenylated acylphloroglucinol. A structure-activity study'. Insieme formano una fingerprint unica.

Cita questo