| Status | 已發表Published |
| Supramolecular Alleviation of Hepatotoxicity of Arecoline (Areca alkaloid) by a Synthetic Receptor | |
Li, S. ; Yang, X.; Yin, H.; Kuok, J.; Wang, R. 
| |
| 2017-05-01 | |
| Source Publication | 3rd MESMAP
 |
| Abstract | Objective / Purpose: Areca nut has been recognised as the fourth most addictive self-administered psychoactive substance. Arecoline, the major active phytochemical in Areca nut that has been well studied for its beneficial role in various diseases including neurological disorders and cardiovascular diseases, has shown profound links with serious hepatotoxicity. This study was aimed to develop a supramolecular formulation of arecoline with reduced liver toxicity. Material and Methods: 1H NMR titration was conducted to investigate binding sites between cucurbit[7]uril (CB[7]) and arecoline in aqueous solution. ITC experiments were employed to determine the binding ratio, binding constant, as well as the thermodynamic parameters during the arecoline-CB[7] complexation process. Molecular modeling and ESI-MS were also employed to confirm encapsulations of arecoline inside CB[7]. The hepatotoxicity of arecoline in the absence and in the presence of CB[7] was evaluated using MTT assay with L02, a healthy human liver cell line. Results: our results showed that CB[7] formed 1:1 host-guest inclusion complexes with arecoline, driven by both enthalpy and entropy, with a binding constant of ~ 104. The hepatotoxicity of arecoline was significantly alleviated in vitro, upon its encapsulation by CB[7], as evaluated by MTT assay of a healthy human liver cell line L02. Conclusion / Discussion: Our results not only provide a novel supramolecular arecoline formulation for alleviated toxicity and improved safety, but also bring CB[7] further to potential application as a novel pharmaceutical excipient. |
| Keyword | Hepatotoxicity Arecoline Cucurbituril |
| Language | 英語English |
| The Source to Article | PB_Publication |
| PUB ID | 31833 |
| Document Type | Conference paper |
| Collection | Institute of Chinese Medical Sciences |
| Corresponding Author | Wang, R. |
| Recommended Citation GB/T 7714 | Li, S.,Yang, X.,Yin, H.,et al. Supramolecular Alleviation of Hepatotoxicity of Arecoline (Areca alkaloid) by a Synthetic Receptor[C], 2017. |
| APA | Li, S.., Yang, X.., Yin, H.., Kuok, J.., & Wang, R. (2017). Supramolecular Alleviation of Hepatotoxicity of Arecoline (Areca alkaloid) by a Synthetic Receptor. 3rd MESMAP. |
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