Siebert G, Schönharting M, Ott M, Surjana S
Hoppe Seylers Z Physiol Chem. 1975 Jun;356(6):855-60. doi: 10.1515/bchm2.1975.356.s1.855.
Colchicine and some of its metabolites and derivatives were investigated regarding their inhibitory action against alkaline phosphatases from E. coli and calf intestine, and against acid phosphatase from potato. Colchicine itself was essentially ineffective, also its metabolites O2-demethyl- and O3-demethylcolchicine. The metabolite O10-demethylcolchicine (= colchiceine) was found to be a powerful, non-competitive inhibitor for all three phosphatases with Ki in the range of 0.45-6.0mM. Amongst the derivatives of colchicine, colchiceyltaurine proved to be a non-competitive inhibitor of acid phosphatase (Ki=3.0mM); desacetylcolchiceine behaved like colchiceine. The inhbitory actions of colchiceine and desacetylcholchiceine could be completely reversed by the addition of Mg2, Ca2, or Zn2, respectively. This interaction with divalent cations demonstrates a novel type of action of the metabolite colchiceine when compared with its mother alkaloid and is possibly of major biological significance.
研究了秋水仙碱及其一些代谢产物和衍生物对大肠杆菌和小牛肠碱性磷酸酶以及马铃薯酸性磷酸酶的抑制作用。秋水仙碱本身基本上没有效果，其代谢产物O2 - 去甲基秋水仙碱和O3 - 去甲基秋水仙碱也是如此。发现代谢产物O10 - 去甲基秋水仙碱（=秋水仙酰胺）是所有三种磷酸酶的强效非竞争性抑制剂，其抑制常数（Ki）在0.45 - 6.0mM范围内。在秋水仙碱的衍生物中，秋水仙酰牛磺酸被证明是酸性磷酸酶的非竞争性抑制剂（Ki = 3.0mM）；去乙酰秋水仙酰胺的表现与秋水仙酰胺相似。分别加入Mg2、Ca2或Zn2可完全逆转秋水仙酰胺和去乙酰秋水仙酰胺的抑制作用。与母体生物碱相比，这种与二价阳离子的相互作用证明了代谢产物秋水仙酰胺的一种新型作用，并且可能具有重要的生物学意义。
