Matrine-family alkaloids as tetracycloquinolizindine analogues from Traditional Chinese Medicine Sophora flavescens Ait, Sophora subprostrata and Sophora alopecuroides L possess various pharmacological activities and have aroused great interests over the past decades. Especially, a lot of matrine derivatives have been designed and synthesized and their biological activities investigated, and encouraging results have continuously been achieved in recent several years. These studies are helpful to develop more potent candidates or therapeutic agents and disclose their molecular targets and mechanisms. This paper reviews recent advances in the bioactive modifications of matrine-family alkaloids from derivatization of the C-13, C-14 or C-15 position, opening D ring, fusing D ring and structural simplification.

苦参碱类生物碱作为中药四环喹啉嗪类似物，具有苦参的药理活性，在过去的几十年中引起了极大的兴趣。特别是，已经设计并合成了许多苦参碱衍生物，并对其生物学活性进行了研究，并且在最近几年中不断取得令人鼓舞的结果。这些研究有助于开发更有效的候选物或治疗剂，并揭示其分子靶标和机制。本文综述了苦参碱家族生物碱的生物活性修饰的最新进展，这些生物碱是从C-13，C-14或C-15位置衍生化，打开D环，融合D环和结构简化而来。