Study of the Constituents of Amaryllidaceae Plants as Antiviral Agents

从石蒜科植物中分离得到新的生物碱，分别为亮亮胺、0-去甲基亮胺、3-0-乙酰钨亚胺、去甲基马利替丁和(-)-N-去甲基利可拉明，分别为石蒜科植物亮亮胺、0-去甲亮胺和3-0-乙酰钨亚胺。通过光谱数据和外消旋体的合成，确证了从宽叶金鸡儿中分离得到的乳糖的结构。石蒜胺的氧化产物酸A和酸B的结构通过其光谱数据和酸A的合成得到了确证。通过卤代-N-苄基-β和苯乙胺衍生物的光化学反应合成了阿佛兰胺类似物。以去甲花碱生物碱为原料合成了4-苯基-1，2，3，4-四氢-4-异喹啉。以去甲肾上腺素生物碱为原料合成了4-苯基-1，2，3，4-四氢-4-异喹啉。H_(17)&gt；N&lt；O_3&gt；在单纯疱疹病毒/Vero细胞系统中的抗病毒活性试验结果如下：(1)在7组化合物中，有3组化合物具有一定的抗病毒活性，即石蒜碱、塔泽汀和石蒜碱。(2)化学治疗指数小于或等于0.2的化合物的共同结构为六氢吲哚环。(3)生物碱的活性与其抑制病毒增殖能力有关。(4)其作用机制可能与抑制DNA聚合酶活性有关。

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.