Antimalarial Activity of Potential Inhibitors of Plasmodium falciparum Lactate Dehydrogenase Enzyme Selected by Docking Studies
2011

Antimalarial Activity of Inhibitors for Plasmodium falciparum Lactate Dehydrogenase

Sample size: 50 publication 10 minutes Evidence: moderate

Author Information

Author(s): Julia Penna-Coutinho, Wilian Augusto Cortopassi, Aline Alves Oliveira, Tanos Celmar Costa França, Antoniana Ursine Krettli

Primary Institution: Faculdade de Medicina, Universidade Federal de Minas Gerais

Hypothesis

Can potential inhibitors of PfLDH effectively reduce malaria parasite growth?

Conclusion

The study confirmed that molecular docking studies are a valuable strategy for discovering new antimalarial drugs, with posaconazole showing the most promise.

Supporting Evidence

  • Posaconazole was the most active compound against P. falciparum.
  • Itraconazole and atorvastatin also showed activity but were less effective than posaconazole.
  • The compounds were selected based on their similarity to NADH and docking scores.
  • All three compounds reduced parasitemia in treated mice compared to untreated controls.
  • The study suggests that existing drugs can be repurposed for malaria treatment.

Takeaway

Researchers tested some existing drugs to see if they could help fight malaria by blocking a key enzyme in the parasite. They found that one drug, posaconazole, worked really well.

Methodology

The study used molecular docking to select 50 compounds, which were then tested for antimalarial activity against P. falciparum in vitro and in mice.

Potential Biases

Potential bias in selecting compounds based on docking scores rather than empirical data.

Limitations

The study was limited by the availability of purified compounds for testing.

Participant Demographics

Mice infected with P. berghei were used for in vivo testing.

Statistical Information

P-Value

<5 µM

Statistical Significance

p<0.05

Digital Object Identifier (DOI)

10.1371/journal.pone.0021237

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