飯匙倩心臟毒以輔{23406a}作化學修飾

Abstract

吾人合成三種輔?(NAD)的衍生物，第一種先用碘醋酸接於第一個氮上面，經過置換重整於第六個碳上的氨基；再接上6個碳帶雙氨基的作腳。第二種則藉溴分子接上輔?，再由六碳腳取代，第三種則用過碘酸使六碳腳接上?醣基(Ribose)。 輔?衍生物與臺灣眼鏡蛇心臟毒結合；第三種衍生物結合後的?物，原本期望以還原型態的NAD衍生物作為蛇毒的標示，來研究心臟蛇毒對紅血球細胞膜作用的機轉。 第二種衍生物與蛇毒結合後用來作輔?循環的免疫分析，輔?與蛇毒結合後，尚存5﹪的活性，而這輔?的活性，會受到蛇毒抗體的抑制，然而用在測定紅血球懸浮液中蛇毒殘餘量時，受到細胞內自然存在輔?的幹擾。 第一種衍生物接上蛇毒，發現有兩種不同的?物，這可能是接上蛇毒分子上僅存的兩個天丙胺酸上，這兩種?物仍具有溶解紅血球細胞膜的作用。

I synthesized two NAD analogs, namely N6-[(6-aminohexyl)-carbamoylmethyl]-NAD+ and 8-(6-aminohexyl)-amino-NAD+. These two analogs were individually coupled to cardiotoxin in the presence of 1-Ethyl-3-(3-dimethyl-aminopropyl)carbodiimide. Products having various ratio of NAD to cardiotoxin were isolated and purified. Like their parent toxin, those cardiotoxin derivatives exhibited hemolytical activity, which was enhanced synergistically by phospholipase A2. The cardiotoxin derivative showed immunoaffinity to cardiotoxin antibody. However, the NAD moiety of the derivative remained only 5% of coenzyme activity.