苦参碱来源于豆科植物苦参Sophora flavescens、苦豆子Sophora alopecuroides等中药，具有多种药理作用，资源丰富。槐果碱是苦参碱D环C-13，14位脱氢的结构类似物，由于其结构的高度相似性，槐果碱同样表现出广泛的药理活性。但苦参碱和槐果碱的药理活性不强，对此开展了大量的结构改造工作。以修饰位点分类，就苦参碱及槐果碱的结构改造及衍生物活性研究进展进行综述，并对其今后发展趋势进行展望。

Matrine is pyrrolizidine alkaloid derived from Chinese materia medica such as Sophora flavescens and Sophora alopecuroides. It has a wide range of pharmacological effects and abundant resources. Sophocarpine is a D ring 13,14-position dehydrogenation analogue of matrine. Due to the high similarity in structure, sophocarpine also exhibits a wide range of pharmacological activities. However, the pharmacological activities of matrine and sophocarpine are not strong, so a great scale of structural modification were carried out. In this paper, the structural modification and derivative activity of matrine and sophoridine were reviewed according to the modification sites classification, and the future development trend was prospected.

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国家自然科学基金资助项目（81502929）；中国医学科学院医学与健康科技创新工程经费资助（2016-I2M-3-015）