Ahmad Moghis U, Ali Shoukath M, Ahmad Ateeq, Sheikh Saifuddin, Chen Paul, Ahmad Imran
Jina Pharmaceuticals Inc., 28100 N Ashley Circle, Suite 103, Libertyville, IL 60048, USA.
Nia Life Sciences, 28100 N Ashley Circle, Suite 102, Libertyville, IL 60048, USA.
Chem Phys Lipids. 2015 Feb;186:30-8. doi: 10.1016/j.chemphyslip.2014.10.003. Epub 2014 Nov 13.
A new synthetic methodology for cationic glycolipids using p-aminophenyl-α-D-mannopyranoside (PAPM) and p-aminophenyl-α-D-galactopyranoside (PAPG) with spacer in between the quaternary nitrogen atom and the sugar unit is developed. In addition, a new class of neutral glycolipid conjugates, such as PAPM-lipids or PAPG-lipids conjugates was also synthesized for targeting drugs to receptors. The precipitation-inhibition assay showed that conjugate of PAPM inhibited the concanavalin A and invertase aggregation. This binding inhibition study of a synthesized compound suggests that conjugates of PAPM can be potentially used to target mannose receptors. In addition, a higher transfection was obtained by mixing PAPM with pSV-β-gal reporter gene and incubating with mannose binding protein/receptor expressing A549 cells. The coexistence of both mannose group and a net positive charge may result in improved transfection efficiency in cells expressing mannose binding proteins/receptors.
