Protective Effect Of A Novel α-Melanocyte-Stimulating Hormone Analogue On Mouse Model For Endotoxic Shock

Objective To design MC1 and MC5 receptor-selective α-MSH analogues, and evaluate their protective effect on the mouse model for endotoxic shock. Methods The software of Insight â…¡ was used to design α-MSH analogues, which were synthesized by GL Biochem Limited Company. THP-1 cells were incubated with α-MSH or synthetic peptides while stimulation with LPS. The supernatant concentration of TNF-α was tested by ELISA kit. K_i values of α-MSH and synthetic peptides with human MC1, MC3, MC4, and MC5 receptors were obtained in competition with [¹²⁵I]NDP-MSH for affinity studies. The cyclic AMP level was tested by [³H]-cyclic AMP kit. Endotoxic shock was modeled by endotoxic injection of 6...