Amaryllidaceae alkaloids: Absolute configuration and biological activity
Amaryllidaceae alkaloids: Absolute configuration and biological activity
复制标题
DOI：
10.1002/chir.22719
复制
发表时间：
2017-09-01
期刊：
影响因子：
2
通讯作者：
Evidente, Antonio
中科院分区：
文献类型：
--
作者：
Cimmino, Alessio;Masi, Marco;Evidente, Antonio
石蒜科植物因其观赏和药用而闻名。这一组的植物成员分布在世界的热带和亚热带地区，主要分布在南美洲安第斯山脉，地中海盆地和南部非洲。石蒜科植物已被证明是具有广谱生物活性的生物碱的良好来源，后者与生物碱骨架的绝对立体化学密切相关。其中，加兰他敏在医学上的实际应用非常重要，它已经成为阿尔茨海默氏症的处方药，作为乙酰胆碱酯酶的有效和选择性抑制剂。此外，石蒜碱及其相关的异卡巴苯乙烯类似物那环拉西和潘司他汀在体外对不同的恶性预后实体瘤显示出较强的抗癌活性。本文综述了石蒜科生物碱的绝对构型及其与生物活性的关系。
Plants belonging to the Amaryllidaceae family are well known for their ornamental and medicinal use. Plant members of this group are distributed through both tropical and subtropical regions of the world and are dominant in Andean South America, the Mediterranean basin, and southern Africa. Amaryllidaceae plants have been demonstrated to be a good source of alkaloids with a large spectrum of biological activities, the latter being strictly related to the absolute stereochemistry of the alkaloid scaffold. Among them, great importance for practical applications in medicine has galanthamine, which has already spawned an Alzheimer's prescription drug as a potent and selective inhibitor of the enzyme acetylcholinesterase. Furthermore, lycorine as well as its related isocarbostyryl analogs narciclasine and pancratistatine have shown a strong anticancer activity in vitro against different solid tumors with malignant prognosis. This review addresses the assignment of the absolute configuration of several Amaryllidaceae alkaloids and its relationship with their biological activities.