A series of benzoylated and phenylsulfonylated amino acids are novel, low molecular weight, self-assembling molecules. At low pH, these compounds form microspheres that dissolve readily under neutral conditions. In a given synthetic series, those molecules with low aqueous solubility formed microspheres more readily than did the molecules possessing high water solubility, suggesting that the hydrophobicity of these compounds contributes to the ability to form microspheres. In addition, molecular modeling studies on selected compounds have shown that microsphere formation may depend also on various aromatic ring and dipole-dipole interactions, which could effect the extent and types of favorable stacking conformations between molecules. The microspheres prepared from these compounds have been used to effect the oral delivery of salmon calcitonin, a model protein drug, in both rodents and primates.

Tricetin is a type of flavonoid that plays an important role in anti-cancer activity. However, the protein targets and function mechanism of tricetin in HepG2 cells remain unclear, which greatly limits its clinical application. In this paper, tricetin was immobilized by 3D photo cross linking chip and the microfluidic environment was established. The SPR (surface plasmon resonance) technique was used to monitor the protein targets interacting with the tricetin on the surface of the chip. The target proteins captured by tricetin in HepG2 cell were identified by HPLC-MS (high performance liquid chromatography-mass pec trometry) method. Bioinformatics annotation and analysis of the obtained proteins showed that the VDR (vitamin D receptor) and PIM1 (Ser/Thr-protein kinase-1) were significantly enriched in the vitamin D receptor signalling pathway (Rich factor > 0.6), and thirty high affinity proteins mainly involved in pathways in Cancer, MAPK (mitogenactivated protein kinase) signalling pathway, TNF (tumour necrosis factor) signalling pathway, Osteoclast differentiation. Among them, four high score affinity target proteins, CYP1B1 (cytochrome P4501B1), VDR, PIM1 and GAA were screened by reverse molecular docking. Finally, the two target proteins, VDR and PIM1, which provided important theoretical support for tricetin in anti-liver cancer research were fully discussed.