Bioassay-guided fractionation of the organic extract obtained from stem barks of the African plant Lophira lanceolata has led to the isolation of seven biflavonoids, including the new α'-chlorolophirone E (5) and 5'-chlorolophirone D (6). Among the isolated compounds, the bichalcone lophirone E was identified as a potent gametocytocidal agent with an IC50 value in the nanomolar range and negligible cytotoxicity (selectivity index = 570). Lophirone E proved to be about 100 times more active against P. falciparum stage V gametocytes than on asexual blood stages, thus exhibiting a unique stage-specific activity profile. The isolation of structural analogues allowed to draw preliminary structure-activity relationships, identifying the critical positions on the chemical scaffold of lophirone E.
Identification of a potent and selective gametocytocidal antimalarial agent from the stem barks of Lophira lanceolata
Habluetzel, Annette;
2019-01-01
Abstract
Bioassay-guided fractionation of the organic extract obtained from stem barks of the African plant Lophira lanceolata has led to the isolation of seven biflavonoids, including the new α'-chlorolophirone E (5) and 5'-chlorolophirone D (6). Among the isolated compounds, the bichalcone lophirone E was identified as a potent gametocytocidal agent with an IC50 value in the nanomolar range and negligible cytotoxicity (selectivity index = 570). Lophirone E proved to be about 100 times more active against P. falciparum stage V gametocytes than on asexual blood stages, thus exhibiting a unique stage-specific activity profile. The isolation of structural analogues allowed to draw preliminary structure-activity relationships, identifying the critical positions on the chemical scaffold of lophirone E.File | Dimensione | Formato | |
---|---|---|---|
Bioorganic Chemistry 93 (2019) 103321 p.1-6.pdf
solo gestori di archivio
Descrizione: Articolo principale
Tipologia:
Versione Editoriale
Licenza:
NON PUBBLICO - Accesso privato/ristretto
Dimensione
728.64 kB
Formato
Adobe PDF
|
728.64 kB | Adobe PDF | Visualizza/Apri Richiedi una copia |
Bioorganic Chemistry 93 (2019) 103321 Supplementary material.pdf
solo gestori di archivio
Descrizione: Appendix A. Supplementary material
Tipologia:
Altro materiale allegato
Licenza:
NON PUBBLICO - Accesso privato/ristretto
Dimensione
600.51 kB
Formato
Adobe PDF
|
600.51 kB | Adobe PDF | Visualizza/Apri Richiedi una copia |
I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.