Study of the Constituents of Amaryllidaceae Plants as Antiviral Agents

从石蒜科植物Leucojum asetivum L.中分离得到5种新的生物碱，分别为无色胺、0-去甲基无色胺、3-0-乙酰基ungiminorine、去甲基maritidine和（-）-N-去甲基石蒜胺。和Hymenocallis rotata。从文殊兰中分离得到的拉替芬的结构由其光谱数据和外消旋体的合成确定。酸A和酸B的结构由它们的光谱数据和酸A的合成确定，酸A和酸B是力可拉敏的氧化产物。阿朴加兰他敏类似物由卤代-N-苄基-苯乙胺衍生物的光化学反应制备<beta>。4-苯基-1，2，3，用0价镍与非那酰胺衍生物环合，合成了4-四氢-4-异喹啉醇类化合物，并对石蒜科生物碱（由去甲颠茄碱&lt;C_（15）&gt; &lt;H_（17）&gt; N生物合成<O_3>）进行了抗单纯疱疹病毒/ Vero细胞系统的抗病毒活性试验，结果表明：（1）在7个化合物中，有3组化合物有一定的抗病毒活性，即石蒜碱、他泽汀和石蒜氨酸。（2）化学治疗指数为0.2或更小的化合物具有六氢吲哚环作为共同结构。（3）生物碱的活性与抑制病毒增殖有关。（4）抑制DNA聚合酶活性可能是其作用机制。

Novel alkaloids, leucotamine, 0-demethylleucotamine, 3-0-acetylungiminorine, demethylmaritidine and (-)-N-demethyllycoramine, were isolated from Amaryllidaceae plants, namely Leucojum asetivum L. and Hymenocallis rotata. The structure of latifine isolated from Crinum latifolium was determined by its spectral data and by the synthesis of its racemate.The structures of acid A and acid B, oxidation products of lycoramine, were confirmed by their spectral data and by the synthesis of acid A.The apogalanthamine analogs were prepared by photochemical reaction of halo-N-benzyl- <beta> -phenethylamine derivatives.A novel synthesis of 4-phenyl-1,2,3,4-tetrahydro-4-isoquinolinols was carried out by cyclization of phenacylamine derivatives with zerovalent nickel.With regard to Amaryllidaceae alkaloids(biosynthesized from norbelladine <C_(15)> <H_(17)> N <O_3> ), tests for antiviral activity in a system of herpes simplex virus/ Vero cells gave the following results:(1)some activity was found in 3 groups of compounds, out of seven, namely Lycorine, Tazettine and Lycorenine. (2)Compounds with a 0.2 or less, chemotherapeutic index had as a common structure a hexahydroindole ring. (3)The activity of those alkaloids was due to their capacity to inhibit the viral multiplication. (4)The mechanism could be explained by the inhibition of DNA polymerase activity.