Interactions between antiplasmodial 3,6-diamino-1'-dimethyl-9-anilinoacridine and hematin and concanamycin A.
Southeast Asian J Trop Med Public Health
;
2007 Nov; 38(6): 979-82
Article
in English
| IMSEAR
| ID: sea-34039
ABSTRACT
Antiplasmodial 9-anilinoacridine derivatives exert their effects either by inhibiting DNA topoisomerase (topo) II or by interfering with heme crystallization within the parasite acidic food vacuole. Previous studies have shown that analogs of 9-anilinoacridine containing 3,6-diamino substitutions (in the acridine ring) inhibit Plasmodium falciparum DNA topo II in situ, whereas those with a 3,6-diCl substitution act by inhibiting beta-hematin formation, a property also seen with 3,6-diamino-1'-dimethyl-9-anilinoacridine (DDAA). To understand this seemingly anomalous property of DDAA, studies of its interaction with hematin and localization within the parasite food vacuole were undertaken. A weak interaction with hematin was demonstrated spectroscopically. Antagonism of DDAA inhibition of Plasmodium falciparum growth in culture by concanamycin A, a macrolide antibiotic inhibitor of vacuolar H(+)-ATPase derived from Streptomyces sp, was equivocal.
Full text:
Available
Index:
IMSEAR (South-East Asia)
Main subject:
Antiviral Agents
/
Plasmodium falciparum
/
Amsacrine
/
Humans
/
Macrolides
/
Drug Interactions
/
Drug Therapy, Combination
/
Hemin
/
Animals
/
Antimalarials
Language:
English
Journal:
Southeast Asian J Trop Med Public Health
Year:
2007
Type:
Article
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