Background: Sanguinarine, a kind of benzophenanthridine alkaloid, is a natural compound with potential development value for its anticancer activity. Hundreds of studies have been carried out in vivo or in vitro, trying to make it feasible for the anticancer clinic medication of sanguinarine. However, sanguinarine was branded as a toxicant or even a carcinogen according to some toxicological experiments and cancer investigations.

Objective: Aiming at safety and effectiveness of sanguinarine, this article reviews the extant information on present studies of sanguinarine, and both anticancer carcinogenesis mechanism details are summarized. The future potential research directions of this valued compound are also discussed to provide reference for future drugs development.

Methods: PubMed, Web of Science, CNKI and WanFang databases were used to search current studies and experimental researches about anticancer effect or carcinogenic information of sanguinarine.

Results: Our results indicated that sanguinarine exhibited anticancer effect through anti-proliferation, anti-invasion, anti-angiogenesis and apoptosis within cancer lesion. Also, many clinical investigations indicated that sanguinarine and its related products might be associated to pre-carcinoma within oral or skin potentially.

Conclusion: Sanguinarine is a natural compound with good development value for its potent anticancer activity; however, its carcinogenesis effect should also be taken seriously. Studies on structural modification and analogue design should be carried out to improve its safety and efficiency in the future.

背景：血根碱是一种苯并菲啶生物碱，是一种具有抗癌活性的具有潜在开发价值的天然化合物。已在体内或体外进行了数百项研究，试图使血根碱抗癌临床用药成为可能。然而，根据一些毒理学实验和癌症调查，血根碱被标记为毒物甚至致癌物。

目的：针对血根碱的安全性和有效性，文章回顾了现有的血根碱研究资料，总结了两者的抗癌致癌机制细节。并对这一有价值的化合物未来潜在的研究方向进行了探讨，为未来的药物开发提供参考。

方法：利用PubMed、Web of Science、CNKI和万方数据库检索血根碱抗癌作用或致癌信息的最新研究和实验研究。

结果：我们的研究结果表明，血根碱通过抗癌病灶内的抗增殖、抗侵袭、抗血管生成和凋亡而发挥抗癌作用。此外，许多临床研究表明，血根碱及其相关产品可能与口腔或皮肤内的癌前病变有关。

结论：血根碱具有较强的抗癌活性，是一种具有良好开发价值的天然化合物；但是，它的致癌作用也应引起重视。未来应进行结构修改和模拟设计研究，以提高其安全性和效率。