Characterization of the Sweet Taste Properties of Cyclodextrins and Their Derivatives and Their Underlying Molecular Mechanisms

Cyclodextrins (CDs) are cyclic oligosaccharides with versatile functions and applications. However, knowledge about their taste properties and underlying molecular mechanisms is still quite limited. In this research, the sweet tastes of α-, β-, and γ-CDs were re-evaluated by a sensory test, and their efficacy to activate the human sweet taste receptor Tas1R2/Tas1R3 was examined with a cell-based assay. The results indicate that CDs are orthodox sweet taste ligands that activate human Tas1R2/Tas1R3. Furthermore, the sweet taste properties of the five derivatives of CDs were also clarified. Moreover, CDs could be classified as a primitive group of sweeteners based on the species-dependent sweet taste. Lastly, it is suggested that the organization of AH, B, and X glucophores in CDs is responsible for their interaction with human Tas1R2/Tas1R3, while the molecular compatibility of the integral configuration is essential for their sweetening power. Our findings provide novel insights for a deeper understanding of the structure–activity relationships of these important biomolecules.