Objective:To review the anticancer effects of Radix astragali(RA),one of the most commonly used herbs to manage cancer in East Asia,and its constituents and to provide evidence of clinical usage through previously performed clinical studies.Methods:Preclinical and clinical studies related to the anticancer effects of RA were searched from inception to November 2013 in electronic databases.Two reviewers independently investigated 92 eligible studies,extracted all the data of studies and appraised methodological quality of clinical trials.The studies were categorized into in vitro and in vivo experimental studies and clinical studies,and analyzed by saponins,polysaccharides,and flavonoids of RA constituents,RA fraction,and whole extract.Results:In preclinical studies,RA was reported to have tumor growth inhibitory effects,immunomodulatory effects,and attenuating adverse effects by cytotoxic agents as well as chemopreventive effects.Saponins seemed to be the main constituents,which directly contributed to suppression of tumor growth through the activation of both intrinsic and extrinsic apoptotic pathway,modulation of intracellular signaling pathway,and inhibition of invasion and angiogenesis.Flavonoids suppressed tumor growth through the similar mechanisms with saponins.Polysaccharides showed immunomodulatory effects,contributing tumor shrinkages in animal models,despite the low cytotoxicity to cancer cells.Most of the clinical studies were performed with low evidence level of study designs because of various limitations.RA whole extracts and polysaccharides of RA were reported to improve the quality of life and ameliorate myelosuppression and other adverse events induced by cytotoxic therapies.Conclusion:The polysaccharides,saponins,and flavonoids of RA,and the whole extract of RA have been widely reported with their anticancer effects in preclinical studies and showed a potential application as a adjunctive cancer therapeutics with the activities of immunomodulation,anti-proliferation and attenuation of adverse effects induced by cytotoxic therapy. Objective: To review the anticancer effects of Radix astragali (RA), one of the most commonly used herbs to manage cancer in East Asia, and its constituents and to provide evidence of clinical usage through previously performed clinical studies. Methods: Preclinical and clinical studies related to the anticancer effects of RA were searched from inception to November 2013 in electronic databases. Two reviewers were investigated 92 eligible studies, extracted all the data of studies and appraised methodological quality of clinical trials. The studies were categorized into in vitro and in vivo experimental studies and clinical studies, and analyzed by saponins, polysaccharides, and flavonoids of RA constituents, RA fractions, and whole extract. Results: In preclinical studies, RA was reported to have tumor growth inhibitory effects, immunomodulatory effects, and attenuating adverse effects by cytotoxic agents as well as chemopreventive effects. saponins seemed to be the main constituents, which direct ly contributed to suppression of tumor growth through the activation of both intrinsic and extrinsic apoptotic pathway, modulation of intracellular signaling pathway, and inhibition of invasion and angiogenesis. Flavonoids suppressed tumor growth through the similar mechanisms with saponins. Population analysis of immunomodulatory effects, contributing tumor shrinkages in animal models, the low cytotoxicity to cancer cells. Host of the clinical studies were performed with low evidence level of study designs due to various limitations. RA Whole extracts and polysaccharides of RA were reported to improve the quality of life and ameliorate myelosuppression and other adverse events induced by cytotoxic therapies. Conlusion: The polysaccharides, saponins, and flavonoids of RA, and the whole extract of RA have been widely reported with their anticancer effects in preclinical studies and showed a potential application as a adjunctive cancer therapeutics with the activities of immunomodulation, anti-proliferation and attenuation of adverse effects induced by cytotoxic therapy.