雪峰虫草是新的虫草类药用资源，课题组前期研究表明雪峰虫草提取物对NB4细胞的生长抑制作用优于冬虫夏草；对U937细胞的生长抑制作用与冬虫夏草相当，优于顺铂，但活性成分群不明确，阻碍了其以新资源或药品身份进入国内外主流医药市场。鉴于此，本项目首先以中药整体观为指导，使用肿瘤细胞靶向垂钓雪峰虫草活性成分群，并结合多模式、多维色谱及联用技术，建立生物指纹图谱并鉴定活性成分组成；接着设计构建新型HSCCC分离制备体系并结合活性成分敲除/敲入理念，实现有效成分群的精准迭代组合，建立“整合—拆分—精准整合”研究模式；最后，通过体内外抗肿瘤药理研究，分析其与血中移行成分的相关性，阐明不同活性成分之间的协同、叠加作用及在体内发挥作用的机制，揭示雪峰虫草的抗肿瘤物质基础。研究成果为中药抗肿瘤活性成分群的快速筛选、迭代组合和协同作用机制研究提供了有效的思路和方法。

Ophiocordyceps xuefengensis, a new medicinal fungi resource, demonstrates significant cytotoxic activities against NB4 and U937 tumor cell lines, which are superior or sometimes equivalent to cordyceps sinensis and positive control cisplatin. However, the bioactive components remain unclear, which has significantly hampered its wide application in clinical trials. Here, we, at first, proposed a strategy based on tumor cell ligand fishing combination with multidimensional chromatographic and hyphenated techniques for holistic evaluation of the bioactive components in O. xuefengensis. Then, we develop novel HSCCC separation system to efficiently separate each peak, and accurate combination is conveniently achieved by knockout/knockin any interested peaks for screening bioactive multi-components that represents the efficacy of O. xuefengensis. After that, we estimate the anti-tutor bioactivity contribution of each component and its corresponding in vivo metabolites to elucidate the interactions of anti-tumor multi-components. The proposed approach is useful for holistic screening of bioactive multi-components, accurate combination and elucidation of the multi-component interactions in tradition Chinese medicine.