Medicinal plants are well-known in affording clinically useful agents, with rich medicinal values by combining with disease targets through various mechanisms. Plant secondary metabolites as lead compounds lay the foundation for the discovery and development of new drugs in disease treatment. Genus Uncaria from Rubiaceae family is a significant plant source of active alkaloids, with anti-hypertensive, sedative, anti-Alzheimer’s disease, anti-drug addiction and anti-inflammatory effects. This review summarizes and discuss the research progress of Uncaria based on alkaloids in the past 15 years, mainly in the past 5 years, including biosynthesis, phytochemistry, pharmacology and structural chemistry. Among, focusing on representative compounds rhynchophylline and isorhynchophylline, the pharmacological activities surrounding the central nervous system and cardiovascular system are described in detail. On the basis of case studies, this article provides a brief overview of the synthesis and analogues of representative compounds types. In summary, this review provides an early basis for further searching for new targets and activities, discussing the mechanisms of pharmacological activity and studying the structure-activity relationships of active molecules.

药用植物通过提供通过各种机制与疾病靶标结合而提供具有丰富医学价值的临床有用药剂而众所周知。植物的次生代谢产物作为先导化合物为疾病治疗新药的发现和开发奠定了基础。茜草科的Uncaria属是活性生物碱的重要植物来源，具有抗高血压，镇静，抗阿尔茨海默氏病，抗药物成瘾和抗炎作用。这篇综述总结并讨论了钩藤的研究进展在过去的15年中以生物碱为基础，主要是在过去的5年中，包括生物合成，植物化学，药理学和结构化学。其中，针对代表性的化合物儿茶碱和异儿茶碱，详细描述了围绕中枢神经系统和心血管系统的药理活性。在个案研究的基础上，本文简要概述了代表性化合物的合成及其类似物。总之，本综述为进一步寻找新的靶标和活性，讨论药理活性的机理以及研究活性分子的构效关系提供了早期基础。