Yang Xue, Zhao Wenxuan, Wang Ziyi, Huang Ying, Lee Simon M Y, Tao Zhu, Wang Ruibing
State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Taipa, Macau SAR, China.
State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Taipa, Macau SAR, China; Key Laboratory of Macrocyclic and Supramolecular Chemistry of Guizhou Province, Guizhou University, Guiyang 550025, China.
Food Chem Toxicol. 2017 Oct;108(Pt B):510-518. doi: 10.1016/j.fct.2017.01.003. Epub 2017 Jan 9.
Hemimethyl-substituted cucurbit[7]uril (HMeCB[7]), a derivative of cucurbit[7]uril (CB[7]) with nearly identical host-guest complexation properties to that of the parent, has significant potential in biomedical sciences due to its superior solubility in water. Its toxicity profile has been investigated in this work, including its developmental and organ-specific toxicities, with both in vivo zebrafish models and a relevant in vitro cellular model. These results demonstrated that HMeCB[7] has negligible developmental toxicity at concentrations up to 3.2 mM and very moderate cardiotoxicity and hepatotoxicity at concentrations of ≥0.8 mM, and is thus generally less toxic than the parent CB[7]. Our results suggest that HMeCB[7] may be a promising candidate of excipient in medicinal and pharmaceutical research fields.
半甲基取代的葫芦[7]脲（HMeCB[7]）是葫芦[7]脲（CB[7]）的衍生物，其主客体络合性质与母体几乎相同，由于其在水中具有优异的溶解性，在生物医学领域具有巨大潜力。在这项工作中，利用体内斑马鱼模型和相关的体外细胞模型，对其毒性特征进行了研究，包括发育毒性和器官特异性毒性。这些结果表明，HMeCB[7]在浓度高达3.2 mM时发育毒性可忽略不计，在浓度≥0.8 mM时具有非常适度的心脏毒性和肝毒性，因此总体毒性低于母体CB[7]。我们的结果表明，HMeCB[7]可能是医药和制药研究领域中一种有前途的辅料候选物。
