Formation of Higher Structural Levels in λ-Carrageenan Induced by the Antimalarial Drug Chloroquine,ACS Macro Letters

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Formation of Higher Structural Levels in λ-Carrageenan Induced by the Antimalarial Drug Chloroquine
ACS Macro Letters ( IF 5.1 ) Pub Date : 2020-08-26 , DOI: 10.1021/acsmacrolett.0c00501
Michael Diener ₁ , Jozef Adamcik ₁ , Raffaele Mezzenga _{1,

2}

Affiliation

The linear polysaccharide λ-carrageenan is the only one among the carrageenans not forming secondary, tertiary, and quaternary structures in the presence of inorganic ions. Chloroquine (CQ) is a well-established antimalaria drug also recently discussed in therapeutics against the COVID-19 pandemic. The interaction of this polysaccharide–ionic drug pair was investigated by combining UV–vis spectrophotometry and atomic force microscopy (AFM) imaging. A decrease of the UV peak assigned to free CQ and the occurrence of isosbestic points indicate the formation of complexes. High-resolution AFM height images revealed an increasing height of the single polysaccharide chains in the random coil state upon addition of CQ, indicating the formation of a secondary structure, followed by higher hierarchical aggregates. The disappearance of higher-ordered structures and the recovery of polysaccharide chains with primary structure were observed by introducing inorganic cations (Na⁺, K⁺, Ca²⁺), replacing the condensed CQ and paving the way to reversible ion-induced drug release.

中文翻译：

抗疟药氯喹诱导的 λ-角叉菜胶中更高结构水平的形成

线性多糖 λ-角叉菜胶是唯一一种在无机离子存在下不形成二级、三级和四级结构的角叉菜胶。氯喹 (CQ) 是一种行之有效的抗疟疾药物，最近也在针对 COVID-19 大流行的治疗中进行了讨论。通过结合紫外-可见分光光度法和原子力显微镜 (AFM) 成像来研究这种多糖-离子药物对的相互作用。分配给游离 CQ 的 UV 峰的减少和等吸光点的出现表明复合物的形成。高分辨率 AFM 高度图像显示，在添加 CQ 后，无规卷曲状态的单个多糖链的高度增加，表明形成了二级结构，随后是更高层次的聚集体。⁺ , K ⁺ , Ca ²⁺ )，取代浓缩的 CQ 并为可逆的离子诱导药物释放铺平了道路。

更新日期：2020-09-15

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