Intermolecular complexation of low-molecular-weight succinoglycans directs solubility enhancement of pindolol

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• 作者：Kyoungtea Kim^a ; Eunae Cho^a ; Jae Min Choi^a ; Hwanhee Kim^a ; Ahri Jang^a ; Youngjin Choi^b ; Im Soon Lee^c ; Jae-Hyuk Yu^d ; ^e ; Seunho Jung^a ; ^{shjung@konkuk.ac.kr" class="auth_mail}
• 关键词：Low-molecular-weight succinoglycans ; Sinorhizobium meliloti ; Pindolol ; Solubility enhancement ; Cyclodextrin ; Complexation
• 刊名：Carbohydrate Polymers
• 出版年：15 June, 2014
• 年：2014
• 卷：106
• 期：Complete
• 页码：101-108
• 全文大小：1843 K

文摘

The low-molecular-weight succinoglycans isolated from Sinorhizobium meliloti are repeating octasaccharide units consisting of monomers, dimers, and trimers. Pindolol is a beta-blocker used to treat cardiovascular disorders. We investigated the formation of complexes between pindolol and low-molecular-weight succinoglycan monomers (SGs). Even though SGs have a linear structure, the solubility of pindolol in the presence of SGs was increased up to 7-fold compared with methyl-尾-cyclodextrin reported as the best solubilizer of pindolol. Complexation of SGs with pindolol was confirmed by nuclear magnetic resonance, Fourier-transform infrared spectroscopy, differential scanning calorimetry, and scanning electron microscopy. Formation constants of complexes were determined from phase solubility diagrams. Conformation of complex was suggested based on a molecular docking study. The present study indicated that formation of pindolol/SGs complexes not only resulted in increased pindolol solubility but also could be useful for improving its clinical application as it did not affect cell viability.