Poor water-solubility of hydrophobic drugs greatly hampers drug design and creats delivery problems.The traditional way to improve the solubility is to add hydrotropes or excipients to supress aggregations.Here,a nove...Poor water-solubility of hydrophobic drugs greatly hampers drug design and creats delivery problems.The traditional way to improve the solubility is to add hydrotropes or excipients to supress aggregations.Here,a novel mechanisim has been proposed based on supramolecular interactions and demonstrated with a small molecule,pvromellitic diimide(PD).This compound contains thymine-like ‘face’ and can interact with adenines through Wat-son-Crick and Hoogsteen hydrogen-bonding.Given the high water solubility of poly adenines[poly(A)],it is expectec that poly(A)will greatly increase the PD solubility.Indeed,such an increased solubility was confirmed by ultraviolet-visible spectroscopy(UV-Vis)and polyacrylamide gel electrophoresis(PAGE)analysis.We believe that this strategy could be used to improve the solubility of other similar hydrophobic molecules.展开更多
基金Supported by the National Natural Science Foundation of China(No.21974111)the Chongqing Research Program of Basic Research and Frontier Technology,China(No.cstc2018jcyjAX0482)+2 种基金the Venture&Innovation Support Program for Chongqing Overseas Returnees,China(No.cx2018088)the Sichuan Applied Basic Research Project,China(No.2019YJ0603)the Sichuan Financial Innovation Capacity Improvement Project,China(No.2016GYSH-016).
文摘Poor water-solubility of hydrophobic drugs greatly hampers drug design and creats delivery problems.The traditional way to improve the solubility is to add hydrotropes or excipients to supress aggregations.Here,a novel mechanisim has been proposed based on supramolecular interactions and demonstrated with a small molecule,pvromellitic diimide(PD).This compound contains thymine-like ‘face’ and can interact with adenines through Wat-son-Crick and Hoogsteen hydrogen-bonding.Given the high water solubility of poly adenines[poly(A)],it is expectec that poly(A)will greatly increase the PD solubility.Indeed,such an increased solubility was confirmed by ultraviolet-visible spectroscopy(UV-Vis)and polyacrylamide gel electrophoresis(PAGE)analysis.We believe that this strategy could be used to improve the solubility of other similar hydrophobic molecules.
