open access

https://hdl.handle.net/2115/96203

Molecular structure of enzyme-synthesized amylose-like chimeric isomaltomegalosaccharides and their encapsulation of the sulfasalazine prodrug

英語

Synchrotron X-ray

2024-11-13

Elsevier

Carbohydrate Polymers

349

122956

The glucoconjugation between linear chimeric α-(1→4)- and α-(1→6)-glucosidic segments exhibits functional properties throughout their structure. In this study, we enzymatically synthesized three new series of chimeric nonreducing isomaltomegalosaccharides (N-IMS-n/m), each featuring a constant n, α-(1→4)-segment (DP = 22–25) at the nonreducing terminal, and varying m, α-(1→6)-main chain lengths (DP = 7–53). The synthesized compounds—N-IMS-25/7, N-IMS-24/19, and N-IMS-22/53—were compared to amylose (DP = 28) and previous samples of N-IMS-15/35 and D-IMS-28.3/13/3. D-IMS refers to a sugar with double α-(1→4)-segments at both the nonreducing and reducing ends. The binding affinity to the aromatic prodrug sulfasalazine (SZ) was assessed using a 4phase-solubility assay, followed by freeze-thawing. Wide-angle X-ray scattering revealed B-type crystalline patterns in bulk, and the crystallinity generally reduced with the increasing α-(1→6) segment. Interestingly, the B-type crystal structure was maintained even after SZ encapsulation, in contrast to the more common transition to V-type crystals upon drug encapsulation. Multi-angle dynamic light scattering and small-angle X-ray scattering revealed an intricate solution-state morphology, both in the absence and presence of SZ. Glucoconjugation aids in maintaining structural organization and integrity, even after the incorporation of the large SZ molecule.

学術雑誌論文

Accepted Manuscript

Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International

© <2024>. This manuscript version is made available under the CC-BY-NC-ND 4.0 license http://creativecommons.org/licenses/by-nc-nd/4.0/

0144-8617