有机硒化合物的抗炎及抗变态反应作用

 目的：有机硒化合物具有多种活性，为此研究3种合成的有机硒化合物的抗炎作用和抗变态反应作用,并分析构效关系。方法：药物对小鼠巴豆油性耳肿胀的影响;对组胺(histamine,His)、过敏性慢反应物质(slow-reacting substance of anaphylaxis SRS-A)所致离体豚鼠回肠收缩的影响;致敏豚鼠肺中SRS-A的提取及药物的拮抗实验。结果：3种化合物能不同程度地抑制小鼠巴豆油性耳肿胀(〖WTBX〗P＜0.05或P〖WTBZ〗＜0.01)。50%抑制离体豚鼠回肠收缩时的药物浓度(IC₅₀)分别为对His:1.25×10^-5,1.58×10^-4，1.25×10^-4 mol/L,对SRS-A:8.9×10^-6，1.25×10^-4，1.12×10^-4mol/L。致敏豚鼠肺释放SRS-A的抑制浓度:10^-4mol/L。结论：3药中9108对受体的拮抗作用最强。该类化合物的化学结构中苯环(B)邻位酯基取代的化合物具有强的受体拮抗作用。它们的抗炎及抗免疫作用与其对His及SRS-A的受体拮抗作用及SRS-A的阻释作用有关。

Effects of seleno-organic compounds on antinflammation and antiallergy

OBJECTIVE:To study effects of seleno-organic compounds 9108,9109 and 9110 on antinflammation and antiallergy.METHODS:Mouse ear edema induced by croton oil was inhibited.The contractions induced by histamine(His) and slow-reacting substance of anaphylaxis(SRS-A) in the guinea-pig ileum were inhibited.SRS-A was abstracted from isolated sensitized guinea-pig lung and SRS-A release was inhibited.RESULTS:Seleno-organic compounds were found to inhibit mouse ear edema induced by croton oil(P＜0.05 or P＜0.01) and the contractions induced by His and SRS-A in the guinea-pig ileum in dose-dependent manner.IC₅₀ values for His inhibition were 1.25×10^-5,1.58×10^-4 and 1.25×10^-4 mol/L,for SRS-A inhibition 8.9×10^-6,1.25×10^-4,and 1.12×10^-4 mol/L respectively.Seleno-organic compounds at dose of 10^-4 mol/L inhibited SRS-A release from isolated sensitized guinea-pig lung.CONCLUSION:These results indicate that these compounds possess antimmunoinflammatory effects and 9108 is the strongest receptor antagonist among the three compounds.This mdicates that esterification at the ortho-position of the phenyl-ring(B) exhibits strong receptor antagonistic action.Antagonism of His and SRS-A receptor and inhibition of SRS-A release may play an important role in the mechanism of antinflammatory actions of these compounds.