The use of Receptor Binding, a Very Specific, High Capacity Screening Method, in the Identification of Biologically Active Components from Natural Sources

Abstract

Nature has been a rich source of valuable drugs despite the fact that the exploration of natural sources has been largely guided by toxicology and ethnopharmacology. Most traditional medicines have been found by coincidence, or by trial and error, not by systematic research. Thus it is very likely that the majority of useful drugs in nature so far have escaped discovery. This, together with the fact that only a minute fraction of natural sources has been partially explored, leads to the conclusion that natural product research has barely begun. In vitro mechanistic screening techniques such as receptor binding, are very selective and sensitive analytical methods. In recent years, they have been highly automated and converted to high throughput screening procedures making them extremely powerful tools in drug research. Recent developments in synthetic organic chemistry, collected under the broad term ‘combinatorial chemistry’ result in an unprecedented output of new compounds which are subjected to high throughput screening procedures. Thus, natural product research is obliged to make use of these new possibilities, or is doomed to fade away.