Zhang Jianghong, Yan Xu, Tian Yunpeng, Li Wanyun, Wang Haiyang, Li Qinbin, Li Yufei, Li Zhu, Wu Ting
Xiamen Nuokangde Biological Technology Co., Ltd., Xiamen 361006, China.
School of Chemistry, Sun Yat-Sen University, Guangzhou 510275, China.
ACS Omega. 2020 Mar 16;5(12):6494-6499. doi: 10.1021/acsomega.9b04120. eCollection 2020 Mar 31.
A new melatonin sulfonate derivative sodium 4-(3-(2-acetamidoethyl)-5-methoxy-1-indol-1-yl) butane-1-sulfonate (MLTBS) with higher water solubility (695 times) and lower cytotoxicity than natural melatonin (MLT) was synthesized, yet with the same sleep aid function. The poor solubility of MLT in water has been improved with a simple chemical reaction, which solves the poor solubility of melatonin in water, overcoming the safety problem caused by adding organic reagents such as dimethyl sulfoxide (DMSO) and ethanol to increase the solubility. Moreover, the modified MLT still has the same sleep aid effect as the natural MLT and higher biological safety. As a novel potential drug for sleep aid, the new MLT derivative could also flourish the application and research of this molecule in medicine and biology.
合成了一种新的褪黑素磺酸盐衍生物4-(3-(2-乙酰氨基乙基)-5-甲氧基-1-吲哚-1-基)丁烷-1-磺酸钠(MLTBS)，其水溶性比天然褪黑素(MLT)高695倍，细胞毒性更低，但具有相同的助眠功能。通过简单的化学反应改善了MLT在水中的溶解性差的问题，解决了褪黑素在水中的溶解性差的问题，克服了添加二甲基亚砜(DMSO)和乙醇等有机溶剂来增加溶解度所带来的安全问题。此外，改性后的MLT仍具有与天然MLT相同的助眠效果和更高的生物安全性。作为一种新型的潜在助眠药物，这种新的MLT衍生物也可以促进该分子在医学和生物学中的应用和研究。
