Di Perri T, Auteri A
Department of Special Medical Pathology, University of Siena, Italy.
Int Angiol. 1988 Apr-Jun;7(2 Suppl):11-5.
Activation of the complement system during the early phase of inflammation is partly responsible for increased vascular permeability, white blood cell margination and stimulation of phagocytosis. The aim of this study was to evaluate the anti-inflammatory action of S 5682 in terms of inactivation of the serum complement system. Serum complement was measured by the method of Mayer modified. In vitro, S 5682 was tested on human and rabbit sera with increasing concentrations from 10 to 5.10(-8) g in the presence of different complement pathways activators. In vivo, serum anticomplement activity was evaluated is the N.Z. rabbit after administration of a single dose (100 mg/kg) of S 5682. In vitro, the anticomplement action of S 5682 was effective, starting at the concentration 1.10(-9) g for both classical (IC50 = 6.19.10(-9) g) and alternative pathways (IC50 = 7.69.10(-9) g). This dose-dependent anticomplement action was statistically significant (p less than 0.01) and involved fraction Clq and C3. In vivo, there was a statistically significant decrease (p less than 0.01) of complement activation which reached a maximum of 74%, 180 minutes after the administration of S 5682. This decrease was still significant after 5 hours (p greater than 0.01). These data suggest that the anti-oedematous effect of S 5682 can be partly explained by anti-inflammatory properties in relation with an anticomplement action.
炎症早期补体系统的激活部分导致血管通透性增加、白细胞靠边和吞噬作用受刺激。本研究的目的是根据血清补体系统的失活情况评估S 5682的抗炎作用。血清补体采用改良的Mayer法测定。在体外，在不同补体途径激活剂存在的情况下，用浓度从10到5×10⁻⁸ g递增的S 5682对人血清和兔血清进行测试。在体内，在给新西兰兔单次注射剂量为100 mg/kg的S 5682后评估血清抗补体活性。在体外，S 5682的抗补体作用有效，对于经典途径（IC50 = 6.19×10⁻⁹ g）和替代途径（IC50 = 7.69×10⁻⁹ g），起始浓度为1×10⁻⁹ g。这种剂量依赖性抗补体作用具有统计学意义（p小于0.01），涉及C1q和C3成分。在体内，补体激活有统计学意义的降低（p小于0.01），在注射S 5682后180分钟达到最大降幅74%。5小时后这种降低仍然显著（p大于0.01）。这些数据表明，S 5682的抗水肿作用部分可由与抗补体作用相关的抗炎特性来解释。
