Synthesis and Anti-tumor Activity of Novel Amino Acid Glyceroglycolipid†

Abstract

Glyceroglycolipids have been identified as one of the most important anticancer drug. In this work,novel amino acid glyceroglycolipids were synthesized through the esterification of glycosylglycerol and N-acyl amino acid and characterized by means of~1 H NMR and ESI-MS. The anti-tumor activities against human breast cancer cell line,human liver cancer cell line and chronic myeloid leukemia cell line in vitro were tested by MTT method. The preliminary results demonstrated that compounds 27( IC_(50)= 3. 53,4. 71,4. 13 μmol/L),28( IC_(50)= 4. 35,4. 57,5. 79 μmol/L),31( IC_(50)= 3. 91,3. 73,4. 54 μmol/L) and32( IC_(50)= 5. 17,5. 52,5. 93 μmol/L) exhibited significant anti-tumor activities. The preliminary studies on the structure-activity relationship showed that when the acyl was decanoyl or lauroyl,good activity was exhibited in all the eight different kinds of glycosyl diacylglycerols. The preliminary prediction of this type of compound had certain inhibitory effect on the growth of tumor cells,they are non-toxic to normal cells. Such novel amino acid glyceroglycolipids as antineoplastic drugs or excellent surfactants could be widely investigated in the future.