Health beneficial activity screening

Our bioanalytical methods assess interference with cellular pathways that govern normal cell growth and differentiation. Some chemicals can interfere with these pathways. If this interference is strong and in an inappropriate uncontrolled context, like environmental or occupational exposure, this is unwanted and the basis of toxicity assessment.  The main difference between health beneficial and toxic compounds is that the former compounds interact with these pathways in a more subtle manner, at lower therapeutic rather than toxic doses. Thus, these pathways often are equally important in the discovery of health beneficial compounds. An important asset of a druggable molecule is that it can enter the body and reach its target. Most CALUX® assays are targeted by molecules with druggable properties, and by assessing entry into cells and major metabolic conversions already information on important barriers is obtained.

Bioactive mixtures screening in e.g. plants and biomass

Using our quantitative high throughput CALUX panel we can rapidly evaluate the bioactivity profile of natural compound mixtures in samples of interest such as plants, fungi and biomass. Depending on the desired application, we can select the assay panel, and if needed the extraction method in such a way that we focus on the desired activity. If there are no data on safe human use, we in parallel, can already at this early stage assess potential toxicity of the same sample. Observed activities of natural compound mixtures  can be compared to f compounds with known health effects or toxicity profiles, thereby assessing the uniqueness of the activity profile.

Identification of bioactive compounds  in mixtures using effect-directed analysis

If a desired activity profile is obtained, indicating the presence of bioactive compounds with a positive health effect, as a next step the compound(s) responsible for this bioactivity can be purified through a stepwise fractionation coupled to bioactivity testing of the obtained active mixtures. This effect-directed analysis is continued until a relatively pure biologically active fraction is obtained that can be subjected to chemical analytics to identify the compound(s) of interest. If successful, the CALUX methods already provide important information on its mode-of-action, while follow-up studies using suitable cell types can complement this knowledge. The identification of the compound, together with the assessment of its mode of action, and if possible combined with historic use of the crude sample can then form the basis of a health claim.

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For further information, please see the relevant references section, or contact Harrie Besselink or Bart van der Burg.