Inhibitory Activity of Ferroquine, versus Chloroquine, against Western Kenya Plasmodium falciparum Field Isolates Determined by a SYBR Green I In Vitro Assay
| Autor: | Fredrick L. Eyase, Hoseah M. Akala, Jacob D. Johnson, Douglas S. Walsh |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2011 |
| Předmět: |
clone (Java method)
Metallocenes Plasmodium falciparum Drug Resistance Protozoan Proteins Drug resistance Microbial Sensitivity Tests Polymorphism Single Nucleotide chemistry.chemical_compound Antimalarials Parasitic Sensitivity Tests Chloroquine Virology parasitic diseases medicine Humans Ferrous Compounds Malaria Falciparum IC50 biology Wild type Membrane Transport Proteins Articles biology.organism_classification medicine.disease Kenya Infectious Diseases chemistry SYBR Green I Aminoquinolines Parasitology Malaria medicine.drug |
| Popis: | Ferroquine (FQ), a chloroquine (CQ) analog, is being developed to treat persons with Plasmodium falciparum malaria. In 146 P. falciparum field isolates from western Kenya, we measured 50% inhibitory concentrations (IC50; nM) of CQ and FQ by a SYBR Green I in vitro assay. Reference clones included W2 (CQ resistant) and D6 (CQ sensitive). Mutation analysis was done for P. falciparum CQ-resistance transporter gene (Pfcrt K76T). Median IC50 values for FQ were lower than CQ for field isolates and the W2 clone (both P < 0.05). The Pfcrt mutation (76T), which was detected in > 80% of isolates, conferred higher CQ IC50 values (P < 0.05) and modestly lower FQ IC50 values (P < 0.05), versus Pfcrt wild type (K76). FQ is more potent than CQ against CQ-resistant P. falciparum field isolates and the W2 clone, and is less affected by Pfcrt 76T. These findings support the notion that FQ could be useful in treating persons with P. falciparum malaria. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|