水溶性柱[6]芳烃超分子包封提高喜树碱类抗肿瘤药物的溶解度和生物活性
Improved Solubility and Bioactivity of Camptothecin Family Antitumor Drugs with Supramolecular Encapsulation by Water-Soluble Pillar[6]arene.
作者信息
Liu Yamin, Chen Xi, Ding Jiaming, Yu Lin, Ma Da, Ding Jiandong
机构信息
Department of Chemistry and State Key Laboratory of Molecular Engineering of Polymers, Department of Macromolecular Science, Fudan University, 220 Handan Road, Shanghai 200433, China.
出版信息
ACS Omega. 2017 Aug 31;2(8):5283-5288. doi: 10.1021/acsomega.7b01032.
Water-soluble pillar[6]arene (WP6) was used to solubilize camptothecin family antitumor drugs. In the presence of WP6, the solubility of camptothecin (CPT) and 10-hydroxycamptothecin (HCPT) was enhanced by 380 and 40 times, respectively. The solubility enhancement is proved to be the result of the host-guest encapsulation by WP6. WP6 has a low cytotoxicity against normal MC 3T3-E1 cells, whereas the bioactivity of CPT and HCPT is substantially improved as a result of the solubility enhancement.
水溶性柱[6]芳烃（WP6）被用于增溶喜树碱类抗肿瘤药物。在WP6存在的情况下，喜树碱（CPT）和10-羟基喜树碱（HCPT）的溶解度分别提高了380倍和40倍。溶解度的提高被证明是WP6主客体包封的结果。WP6对正常MC 3T3-E1细胞具有低细胞毒性，而CPT和HCPT的生物活性由于溶解度的提高而得到显著改善。
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