1921
Volume 75, Issue 4
  • ISSN: 0002-9637
  • E-ISSN: 1476-1645

Abstract

Artemisinins show the potential for neurotoxicity in preclinical studies. Artemisone is a leading candidate of second-generation semi-synthetic artemisinin derivatives for antimalarial therapy devoid of neurotoxicity. Artemisone showed 3–5-fold higher activity (50% effective concentration (EC) = 0.14 nmol/L, EC = 2.55 nmol/L) than artesunate against fresh isolates from Gabon and a high-activity correlation indicates a shared drug target.

Loading

Article metrics loading...

/content/journals/10.4269/ajtmh.2006.75.637
2006-10-01
2017-09-25
Loading full text...

Full text loading...

/deliver/fulltext/14761645/75/4/0750637.html?itemId=/content/journals/10.4269/ajtmh.2006.75.637&mimeType=html&fmt=ahah

References

  1. Adjuik M, Babiker A, Garner P, Olliaro P, Taylor W, White N; International Artemisinin Study Group., 2004. Artesunate combinations for treatment of malaria: meta-analysis. Lancet 363 : 9–17.
  2. Kremsner PG, Krishna S, 2004. Antimalarial combinations. Lancet 364 : 285–294.
  3. Ashley EA, White NJ, 2005. Artemisinin-based combinations. Curr Opin Infect Dis 18 : 531–536.
  4. Leonardi E, Gilvary G, White NJ, Nosten F, 2001. Severe allergic reactions to oral artesunate: a report of two cases. Trans R Soc Trop Med Hyg 95 : 182–183.
  5. Genovese RF, Nguyen HA, Mog SR, 2001. Effects of arteether on an auditory radial-arm maze task in rats. Physiol Behav 73 : 87–91.
  6. Genovese RF, Newman DB, Brewer TG, 2000. Behavioral and neural toxicity of the artemisinin antimalarial, arteether, but not artesunate and artelinate, in rats. Pharmacol Biochem Behav 67 : 37–44.
  7. Panossian LA, Garga NI, Pelletier D, 2005. Toxic brainstem encephalopathy after artemisinin treatment for breast cancer. Ann Neurol 58 : 812–813.
  8. Toovey S, Jamieson A, 2004. Audiometric changes associated with the treatment of uncomplicated falciparum malaria with co-artemether. Trans R Soc Trop Med Hyg 98 : 261–267.
  9. Haynes RK, Fugmann B, Stetter J, Rieckmann K, Heilmann HD, Chan HW, Cheung MK, Lam WL, Wong HN, Croft SL, Vivas L, Rattray L, Steward L, Peters W, Robinson BL, Edstein MD, Kotecka B, Kyle DE, Beckermann B, Gerisch M, Radtke M, Schmuck G, Steinke W, Wollborn U, Schmeer K, Römer A, 2006. Artemisone: a highly active antimalarial drug of the artemisinin class. Angew Chem Int Ed Engl 45 : 2082–2088.
  10. Borrmann S, Binder RK, Adegnika AA, Missinou MA, Issifou S, Ramharter M, Wernsdorfer WH, Kremsner PG, 2002. Reassessment of the resistance of Plasmodium falciparum to chloroquine in Gabon: implications for the validity of tests in vitro vs. in vivo. Trans R Soc Trop Med Hyg 96 : 660–663.
  11. Ramharter M, Wernsdorfer WH, Kremsner PG, 2004. In vitro activity of quinolines against Plasmodium falciparum in Gabon. Acta Trop 90 : 55–60.
  12. Uhlemann AC, Ramharter M, Lell B, Kremsner PG, Krishna S, 2005. Amplification of Plasmodium falciparum multidrug resistance gene 1 in isolates from Gabon. J Infect Dis 192 : 1830–1835.
  13. Noedl H, Wernsdorfer WH, Miller RS, Wongsrichanalai C, 2002. Histidine-rich protein II: a novel approach to malaria drug sensitivity testing. Antimicrob Agents Chemother 46 : 1658–1664.
  14. Lietchfield JT, Wilcoxon F, 1949. A simplified method of evaluating dose-effect experiments. J Pharmacol Exp Ther 96 : 99–113.
  15. World Health Organization, 2001. The Use of Antimalarial Drugs. Report of an Informal Consultation. Geneva: World Health Organization. WHO/CDS/RBM/2001.33.
  16. Facts on ACTs (ArtemisininBased Combination Therapies. Accessed February 1, 2006. Available from http://www.rbm.who.int/cmc_upload/0/000/015/364/RBMInfosheet_9.htm
  17. Hutagalung R, Htoo H, Nwee P, Arunkamomkiri J, Zwang J, Carrara VI, Ashley E, Singhasivanon P, White N, Nosten F, 2006. A case-control auditory evaluation of patients treated with artemether-lumefantrine. Am J Trop Med Hyg 74 : 211–214.
  18. Eckstein-Ludwig U, Webb RJ, van Goethem ID, East JM, Lee AG, Kimura M, O’Neill PM, Bray PG, Ward SA, Krishna S, 2003. Artemisinins target the SERCA of Plasmodium falciparum. Nature 424 : 957–961.
  19. Uhlemann AC, Cameron A, Eckstein-Ludwig U, Fischbarg J, Iserovich P, Zuniga FA, East M, Lee A, Brady L, Haynes RK, Krishna S, 2005. A single amino acid residue can determine the sensitivity of SERCAs to artemisinins. Nat Struct Mol Biol 12 : 628–629.
http://instance.metastore.ingenta.com/content/journals/10.4269/ajtmh.2006.75.637
Loading
/content/journals/10.4269/ajtmh.2006.75.637
Loading

Data & Media loading...

  • Received : 18 Apr 2006
  • Accepted : 06 Jun 2006

Most Cited This Month

This is a required field
Please enter a valid email address
Approval was a Success
Invalid data
An Error Occurred
Approval was partially successful, following selected items could not be processed due to error