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Using a peptide segment to covalently conjugate doxorubicin and taxol for the study of drug combination effect

机译：使用肽段将阿霉素和紫杉醇共价偶联以研究药物联合作用

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Doxorubicin (Dox) and Taxol can be covalently bonded to the same peptide segment via proper structural modification. Doxorubicin-maleimide derivative links to peptide via Michael addition reaction and Taxol-Succi-NHS active ester connects to the same peptide backbone through ester-amide exchange reaction. Enzymatic transformation, as an inherent biological process, is applied here to trigger the formation of nanofiber networks from the as prepared hydrogelator precursor. The precursor which loads equal molar ratio of Dox and Taxol can self-assemble to form a red stable hydrogel after dephosphorylation reaction catalyzed by alkaline phosphatase (ALP). This hydrogel could maintain sustained release of drugs and show strong anticancer effect. This work, as a new strategy to build a codelivery system of covalently linked Dox and Taxol, owns the potential to serve as an injectable hydrogel for therapeutic applications.
机译：阿霉素（Dox）和紫杉醇可通过适当的结构修饰共价键合至同一肽段。阿霉素-马来酰亚胺衍生物通过迈克尔加成反应连接至肽，而紫杉醇-琥珀-NHS活性酯通过酯-酰胺交换反应连接至相同的肽主链。作为固有的生物学过程，在此应用酶转化来触发由制备的水凝胶剂前体形成纳米纤维网络。负载相等的Dox和紫杉醇摩尔比的前体在碱性磷酸酶（ALP）催化的脱磷酸反应后可以自组装形成红色稳定的水凝胶。这种水凝胶可以维持药物的持续释放，并显示出强大的抗癌作用。这项工作作为建立共价连接的Dox和Taxol的代码传递系统的新策略，具有作为治疗应用的可注射水凝胶的潜力。

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