Promising Aculeatin Derivatives PDF Print E-mail

New Weapons against Malaria

Aculeatins belong to a novel family of molecules recently isolated from the plant Amonum aculeatum commonly used in Papua New Guinea as a traditional medicine to treat fever and malaria. Researchers at the Molecular Pharmacochemistry department, University Joseph Fourier, have developed a unique synthesis pathway giving access to a wide range of aculeatin derivatives. This highly flexible diversity-oriented approach enables the synthesis of numerous and complex derivatives, some of which already demonstrate enhanced anti-plasmodium activities and reduced cell toxicity. This new method of synthesis can result in opportunities regarding both the molecular optimization of aculeatins, as well as an understanding of their mode of action.

Key features

  • Novel aculeatin derivatives with low toxicity towards human cell lines
  • Acute anti plasmodium and anti toxoplasmosis activities evidenced in vitro

Benefits

The technology has the potential to produce a wide range of derivatives, enabling a clear understanding of structure-activity relationships (SAR). By establishing a critical mass where sufficient numbers of molecules are available, followed by an in-depth analysis of the structure-activity relationship, the identification ol lead compounds is made possible.

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The Plasmodium falciparum parasite causes Malaria, one of the world's most common infectious disease killing over one million people each year, mainly in sub-tropical climates.


Key laboratory results

  • High efficiency in terms of parasite inhibitiion (in vitro assays)
- IC50 on Plasmodium falciparum as low as 80-90nM
- IC50 on Toxoplasma gondii under 180nM
  • Ability to cure plasmodium infected erythrocytes within one hour of exposure (ex vivo assays)
  • Low toxicity levels in human blood cells (IC50 reaching 9-11µM)

anti plasmodium effect.jpg

Intellectual Property

Covered by French Patent # 07/06929 (October 3, 2007)

Technology Status

Floralis is currently looking for partners to further develop this exciting technology which demonstrates significant potential in the development og highly promising molecules with malaria inhibiting properties.

Contacts

Mathieu TILQUIN
(Technology Transfer)
+33 (0)4 76 00 78 41
This e-mail address is being protected from spambots. You need JavaScript enabled to view it

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