The limitations of conventional techniques hinder the identification of natural compounds
with anticancer potential in terms of speed, throughput, sensitivity, and the capability
of continuous monitoring of relevant biological effects. Novel label‐free optical
biosensors represent new opportunities in the discovery of drug candidates, eliminating
these difficulties. Our study monitored the anti‐adhesive effects of 11 isolated pure
natural compounds (representing four different structural frameworks) and four crude
extracts, obtained from plant and fungal sources. The resonant waveguide grating (RWG)
method (using an evanescent field‐based label‐free optical biosensor) and a combined
miniaturized holographic microscope technique were applied to investigate the effects
of pure compounds and crude extracts on cancerous (HeLa) and healthy (preosteoblast)
model cells in real time. The adhesion kinetics on fibronectin‐coated surfaces and
the morphological parameters on polystyrene surfaces were studied using these model
cells in the presence and absence of compounds and extracts. The introduced biosensor
method also investigated their interaction with the fibronectin surface. This methodology
enables continuous, high‐sensitivity parallel measurements, facilitating the identification
of natural compounds with anticancer potential while also providing insights into
their mechanism of action. The interaction of the aryltetralin lignans deoxypodophyllotoxin
and angeloyl podophyllotoxin with fibronectin was confirmed as a key mechanism behind
their non‐selective anti‐adhesive effects. In contrast, the selective adhesion inhibitory
effects of the neolignan balanophonin and the alkaloid vermelhotin against HeLa cells
were unrelated to fibronectin interaction.
