Abstract
Toll-like receptor 4, commonly expressed in innate immune cells, is considered as one of promising molecular targets for immune – modulating drugs, because it can be activated to regulate immune response by ligand interaction. Our previous report shows that glycolipids with serine coupled with lipid amine to mimic phytosphingosine of □-GalCer, a bioactive glycolipid, can activate immune system via TLR4. Herein, we used amide bond formation to synthesize sixty new galactosyl serine derivatives efficiently. Moreover, we modified the sugar moiety of galactosyl serine derivatives, to achieve the synthesis of 14 different compounds. The assay results, tested in Dr. Shu-Ling Fu’s Laboratory, show that galactosyl serine lipids with lipid amine containing C11 and fatty acid containing C12 as well as four compounds with modified sugar moiety can activate human epithelial cell via TLR4. The results suggest that these derivatives are immune modulators and may serve as potential immunoadjuvant in immunotherapy.