口腔鳞癌是我国高发致死性恶性肿瘤，中晚期患者缺乏有效治疗药物，是口腔鳞癌临床治疗亟待解决的。研究发现Aurora B激酶的高表达与口腔鳞癌的发生发展密切相关，前期工作中我们借助超级计算机模拟筛选为平台，从传统抗肿瘤中药库中筛选出Aurora B激酶潜在抑制剂丹参酮IIA，能有效缓解口腔癌前病变，但作用机制不明。本项目拟以计算机模拟对接为指导，从分子、细胞水平阐明丹参酮IIA抑制Aurora B激酶活性的分子机制，并借助裸鼠移植瘤和病人肿瘤组织来源的移植瘤模型体内验证丹参酮IIA抗口腔鳞癌的药理作用。本研究将阐明丹参酮IIA的抗肿瘤机制，拓宽我们对中药抗肿瘤机制的认识，为建立抗肿瘤中药库，筛选其他激酶抑制剂提供新思路。

Oral squamous cell carcinoma (OSCC) is one of the leading causes of cancer-related death in China. Insufficiency of the efficient therapeutic agents in patients with advanced OSCC is a major obstacle for clinical treatment. Previous studies suggested that high expression of Aurora B kinase is involved in the tumorigenesis of OSCC. Here, using the virtual computational screening of the Traditional Chinese Medicine Database, we identified that Tanshinone IIA as an Aurora B kinase inhibitor. We will focus on the molecular mechanism of Tanshinone IIA-mediated Aurora B suppression via performing of a series of in vitro and ex vivo assays. Additionally, we will construct the xenograft mouse model and patient-derived xenograft mouse model to investigate the in vivo anti-OSCC efficacy of Tanshinone IIA. Overall, this study will help us to understand the novel antitumor mechanism of Traditional Chinese Medicine, and provide an instructive framework for subsequent discovery of novel kinase inhibitors.