Additive In Vitro Antiplasmodial Effect of N-Alkyl and N-Benzyl-1,10-Phenanthroline Derivatives and Cysteine Protease Inhibitor E64
Joint Authors
Mustofa, Mustofa
Jumina, Jumina
Supargiyono, Supargiyono
Sholikhah, Eti Nurwening
Hadanu, Ruslin
Wijayanti, Mahardika Agus
Source
Malaria Research and Treatment
Issue
Vol. 2010, Issue 2010 (31 Dec. 2010), pp.1-8, 8 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2010-06-22
Country of Publication
Egypt
No. of Pages
8
Main Subjects
Abstract EN
Potential new targets for antimalarial chemotherapy include parasite proteases, which are required for several cellular functions during the Plasmodium falciparum life cycle.
Four new derivatives of N-alkyl and N-benzyl-1,10-phenanthroline have been synthesized.
Those are (1)-N-methyl-1,10-phenanthrolinium sulfate, (1)-N-ethyl-1,10-phenanthrolinium sulfate, (1)-N-benzyl-1,10-phenanthrolinium chloride, and (1)-N-benzyl-1,10-phenanthrolinium iodide.
Those compounds had potential antiplasmodial activity with IC50 values from 260.42 to 465.38 nM.
Cysteine proteinase inhibitor E64 was used to investigate the mechanism of action of N-alkyl and N-benzyl-1,10-phenanthroline derivatives.
A modified fixed-ratio isobologram method was used to study the in vitro interactions between the new compounds with either E64 or chloroquine.
The interaction between N-alkyl and N-benzyl-1,10-phenanthroline derivatives and E64 was additive as well as their interactions with chloroquine were also additive.
Antimalarial mechanism of chloroquine is mainly on the inhibition of hemozoin formation.
As the interaction of chloroquine and E64 was additive, the results indicated that these new compounds had a mechanism of action by inhibiting Plasmodium proteases.
American Psychological Association (APA)
Wijayanti, Mahardika Agus& Sholikhah, Eti Nurwening& Hadanu, Ruslin& Jumina, Jumina& Supargiyono, Supargiyono& Mustofa, Mustofa. 2010. Additive In Vitro Antiplasmodial Effect of N-Alkyl and N-Benzyl-1,10-Phenanthroline Derivatives and Cysteine Protease Inhibitor E64. Malaria Research and Treatment،Vol. 2010, no. 2010, pp.1-8.
https://search.emarefa.net/detail/BIM-479925
Modern Language Association (MLA)
Wijayanti, Mahardika Agus…[et al.]. Additive In Vitro Antiplasmodial Effect of N-Alkyl and N-Benzyl-1,10-Phenanthroline Derivatives and Cysteine Protease Inhibitor E64. Malaria Research and Treatment No. 2010 (2010), pp.1-8.
https://search.emarefa.net/detail/BIM-479925
American Medical Association (AMA)
Wijayanti, Mahardika Agus& Sholikhah, Eti Nurwening& Hadanu, Ruslin& Jumina, Jumina& Supargiyono, Supargiyono& Mustofa, Mustofa. Additive In Vitro Antiplasmodial Effect of N-Alkyl and N-Benzyl-1,10-Phenanthroline Derivatives and Cysteine Protease Inhibitor E64. Malaria Research and Treatment. 2010. Vol. 2010, no. 2010, pp.1-8.
https://search.emarefa.net/detail/BIM-479925
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-479925