β-咔啉生物碱是一类广泛存在于自然界中的生物碱，具有结构简单且易于合成和结构修饰的特点。β-咔啉生物碱及其衍生物呈现广泛的生物活性，如抗肿瘤、抗疟疾、治疗阳痿、降血糖、抗病毒、抗真菌等。β-咔啉生物碱的结构特点和良好活性得到了制药企业和研究机构的持续关注，目前已经成为有机合成和药物化学研究的热点，尤其是通过高通量筛选和计算机辅助药物设计技术设计合成了不少活性很好的药物先导物。对近20年来从海洋生物、陆生植物和高等真菌中提取分离的β-咔啉生物碱及其生物活性进行了综述。

β-carboline alkaloids are widely distributed in nature. Their structures are usually simple and thus are easy to synthesized or modified. β-carboline alkaloids exhibit a wide range of biological activities, such as antitumor, antimalarial, cure impotence, treatment for type 2 diabetes, antiviral, antifungal, etc. Since its structural features and good biological activities, pharmaceutical corporations and research institutes have focused on it in a long time, which results in β-carboline alkaloids become a research hotspot in organic synthesis and medicinal chemistry areas, especially some pharmaceutical corporations designed and synthesized many β-carboline alkaloids derivatives with excellent biological activities by high throughput screening and computer aided drug design technologies. This review summarizes the recent progress on β-carboline alkaloids extracted from marine organism, terrestrial plant, and fungi together with their biological activities over the past 20 years.

重庆市自然科学基金重点项目（cstc2013jjB0011）；重庆市应用开发计划项目（cstc2013yykfB10013）；重庆市农发资金项目（17412）