开心散始载于唐代孙思邈的《备急千金要方》，由人参、茯苓、远志、石菖蒲4味药按3：3：2：2的比例组成。开心散发挥药理作用的物质基础主要涉及人参皂苷、远志皂苷、远志糖酯和远志酮，而茯苓、石菖蒲的活性成分是否为开心散的药效成分的研究较少，研究范围较局限；开心散药理作用的研究主要集中在抗抑郁作用、抗老年痴呆、改善学习记忆能力、抗疲劳和镇静安神等方面，涉及机制包括神经系统、免疫系统和内分泌系统。对开心散的药效物质基础、药理作用及其机制进行较为系统的阐述，以期为日后开心散的临床应用提供一定的思路。

Kai-Xin-San (KXS) is a well-known formula that was first recorded in an ancient Chinese book "Important Prescriptions Worth a Thousand Gold for Emergency" by Si-miao Sun from the Tang Dynasty. KXS is composed of Panax ginseng, Poria cocos, Polygala tenuifolia, and Acorus tatarinowii at a ratio of 3:3:2:2. The material basis of the pharmacological action of KXS is mainly related to ginsenosides, polygala saponins, polygala oligosaccharide esters, and polygalactone. However, the active components of P. tenuifolia and A. tatarinowii are less studied, and the research scope is limited. The pharmacological researches of KXS are mainly focused on antidepressant effect, antisenile dementia, improving learning and memory ability, antifatigue, and sedation. The mechanisms involved include nervous system, immune system and endocrine system. The material basis, pharmacological effects and known mechanisms of KXS are systematically described in this paper in order to provide some ideas for the clinical application of KXS in the future.

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国家杰出青年科学基金资助项目（81302909）；国家自然科学基金面上项目（81373996，81673877，81674082）