牡丹皮抗内毒素活性研究

目的对传统中药牡丹皮(Paeonia suffruticosa Andr,PSA)抗内毒素(LPS)活性组分进行定向分离及体内外活性评价。方法利用生物传感器、硅胶柱层析、聚酰胺层析、离子交换-HPLC等技术对牡丹皮进行活性组分的定向分离。通过活性组分对LPS介导RAW264.7分泌细胞因子的抑制实验、对LPS和热灭活大肠杆菌攻击小鼠的保护实验,评价所得活性组分对内毒素的拮抗作用。结果从牡丹皮水提取物中分离到一个与Lipid A具有较高结合活性的组分(PSA-3),PSA-3在体外能抑制LPS介导的RAW264.7细胞释放TNF-α(P45μg<0.05,P90、180μg<0.01),对致死剂量LPS攻击小鼠的保护率为50%(P<0.01),对致死剂量热灭活大肠杆菌攻击小鼠的保护率为50%(P<0.05),而低结合活性PSA-1组分则不具有抑制作用,对LPS和热灭活大肠杆菌(HK-E.coli)攻击小鼠也无保护效果。结论从牡丹皮中分离到一个与Lipid A具有较高结合活性的组分,该组分在体内外对LPS均具有一定的拮抗作用。

Antiendotoxin bioactivities of Paeonia suffruticosa Andr

Objective To isolate the antiendotoxin active components（LPS） from Paeonia suffruticosa Andr（PSA） using biosensor and purification technology and assess their bioactivities in vitro and in vivo.Methods LPS were isolated from PSA using biosensor,silica gel column chromatography,polyamide chromatography,and IEC-HPLC.Inhibitory effect of LPS on antiendotoxin-mediated secretion of cytokines from RAW264.7 and protective effect of LPS on mice against antiendotoxin and heat killed E.coli（HK-E.coli） were studied.Results PSA-3,an antiendotoxin active component with a high binding activity to lipid A,isolated from PSA,could inhibit TNF-α release from LPS-mediated RAW264.7（P₄5 μg <0.05,P₉0,180 μg <0.01）.The protective efficiency of PSA-3 on mice was 50% against lethal LPS dose（P<0.01）and lethal HK-E.coli dose,respectively（P<0.05）.PSA-1 with a lower binding activity to lipid A had no inhibitory and protective effect on mice against LPS and HK-E.coli.Conclusion PSA-3,a component isolated from PSA,has a high binding activity to lipid A and an antagonistic effect on LPS both in vivo and in vitro.