Abstract: OBJECTIVE To synthesize five new traditional Chinese medicines of hesperetin calcium, iron, selenium, zinc, and chromium complexes, and to study their antibacterial and anti-tumor activities and the ability to scavenge free radicals. METHODS The complexes of hesperetin with calcium, iron, selenium, zinc and chromium were synthesized under alkaline conditions. The inhibitory activity of hesperetin and its complexes on 8 kinds of bacteria was determined by multiple dilution method, and the effect of hesperetin and its complexes on the proliferation of 6 kinds of tumor cells, such as Tca-8113, was determined by MTT method, superoxide anion radical scavenging method was used to determine the scavenging ability of hesperetin and its complexes to superoxide anion radicals. RESULTS The coordination ratio of the five complexes was 2:1(hesperetin:microelements), and the yield was over 70%. The acute toxicity experiment of mice showed that the five complexes had no obvious toxicity. The minimal inhibit concentration of the five complexes was lower than that of hesperetin, and the antibacterial activity was increased to 1-4 times at least. The IC₅₀ of the five complexes was lower than that of hesperetin, and the antitumor activity was increased to 1.19-2.41 times at least. Hesperetin and its complexes had a certain scavenging effect on superoxide anion radicals, and both of them were concentration dependent. The scavenging rate of complexes to superoxide anion radicals was higher than hesperetin. CONCLUSION The anti-bacterial and anti-tumor activities and free radical scavenging ability of five kinds of hesperetin microelement complexes were better than that of hesperetin.