关键词: 关键词：华游蛇PLIγ，sPLA2，分子对接，炎症

Abstract: Objective To design a mimic peptide based on Sinonatrix percarinata PLIγ sequence and to explore its inhibitory activity on PLA2. Methods Sinonatrix percarinata PLIγ gene was cloned by RT-PCR and aligned with other published PLIγ sequences. Based on the results, a 19aa peptide was designed derived from Sinonatrix percarinata PLIγ. Molecular docking was then achieved to investigate the interaction between the 19aa peptide and sPLA2 by Auto-dock software. Experimental validation was conducted by agarose plate method, and anti-hemorrhagic activity against snake venom sPLA2 on mice skin was tested as well. Arachidonic acid content in LPS induced Raw264.7 cells was assayed to evaluate the 19aa peptide inhibitory effect on mammal sPLA2 enzyme. Results The mimic 19aa peptide with the sequence as PGLPLSYPNGGGGSVAFRS, behaved dominant pharmacological inhibitive properties to enzymatic activity and hemorrhage toxicity of sPLA2. It also significantly reduced arachidonic acid content in the LPS induced Raw264.7 inflammatory cells with an IC50 of 86.3μmol/L, probably by inhibiting the mammal sPLA2. Conclusion The designed 19aa mimic peptide showed similar pharmacological properties with natural Sinonatrix percarinata PLIγ, indicates its anti-inflammatory and anti-hemorrhage potential.

Key words: Key words: Sinonatrix percarinata PLIγ, sPLA2, molecular docking, inflammatory