A cyclodextrin-based macrocyclic oligosaccharide cavitand with a dual functionality limits the collagen...

β-Cyclodextrin (β-CD), a macrocyclic oligosaccharide cavitand, is a well-known candidate for drug delivery and formulation. In this study, we extended the application of β-CD using a β-cyclodextrin sulfate (β-CDS) as a possible therapeutic for fibrotic diseases caused by excess deposition of collagen fibrils. We have strategically chosen β-CDS, which mimics the natural existence of dermatan sulfate in the extracellular matrix, for limiting collagen fibrillation. The hydrophobic nature of the inner core β-CDS is expected to form an inclusion complex with hydrophobic side chain amino acids with the simultaneous action of forming an ionic bond through a negative charge on sulfate group with positively charged amino acids side chain in collagen. Various results suggested that such dual action not only limited the collagen fibrillation but also reduced the fibril size formed in the presence of β-CDS. The contemporary results thus indicate that β-CDS can be explored as a therapeutic molecule in fibrotic diseases.