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首页> 外文期刊>Chemical and Pharmaceutical Bulletin >Supramolecular Complex of Methyl-β-cyclodextrin with Adamantane-Grafted Hyaluronic Acid as a Novel Antitumor Agent
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Supramolecular Complex of Methyl-β-cyclodextrin with Adamantane-Grafted Hyaluronic Acid as a Novel Antitumor Agent

机译:甲基-β-环糊精与金刚烷接枝的透明质酸作为新型抗肿瘤剂的超分子复合物

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摘要

Methyl-β-cyclodextrin (M-β-CyD) exhibits cytotoxic activity, and has the potentials as an antitumor agent. However, a tumor-selectivity of M-β-CyD is low, leading to low antitumor activity and the adverse effects. Meanwhile, hyaluronic acid (HA) is known as a promising tumor targeting ligand, because various cancer cells overexpress CD44, a HA-binding glycoprotein. In the present study, to develop a tumor-selective delivery system for M-β-CyD, we designed a supramolecular complex of M-β-CyD with adamantane-grafted HA (Ad-HA/M-β-CyD) and evaluated it as a tumor-selective antitumor agent. M-β-CyD formed a stable complex with Ad-HA ( K c
机译:甲基-β-环糊精(M-β-CyD)表现出细胞毒活性,并具有作为抗肿瘤药的潜力。然而,M-β-CyD的肿瘤选择性低,导致低的抗肿瘤活性和不良作用。同时,透明质酸(HA)被称为有前途的肿瘤靶向配体,因为各种癌细胞都过表达CD44(HA结合糖蛋白)。在本研究中,为了开发M-β-CyD的肿瘤选择性递送系统,我们设计了M-β-CyD与金刚烷移植的HA(Ad-HA /M-β-CyD)的超分子复合物,并对其进行了评估作为肿瘤选择性抗肿瘤药。 M-β-CyD与Ad-HA形成稳定的复合物(K c ?M ?1 )。此外,Ad-HA /M-β-CyD形成带有ca的带负电荷的纳米粒子。粒径为140?nm,表明抗肿瘤药具有良好的理化性质。 Ad-HA /M-β-CyD在人类结肠癌细胞系HCT116细胞(CD44(+))中通过CD44介导的内体途径显示出优异的细胞毒性活性。另外,Ad-HA /M-β-CyD的细胞毒性活性是通过凋亡诱导的。这些结果表明,Ad-HA /M-β-CyD具有作为肿瘤选择性超分子抗肿瘤剂的潜力。

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