Gallium is located at the fourth period and the IIIA group. It plays a significant role in clinical diagnosis and treatment of various diseases. Ga(Ⅲ) usually acts as a competitive inhibitor of Fe(Ⅲ) in organisms, as it shares most chemical characteristics except redox activity with Fe(Ⅲ). It can disrupt iron homeostasis in tumor or in microorganisms, thereby achieving antineoplastic or anti-microbial effects. In the aspect of cancer diagnosis and treatment, Ga(Ⅲ) can be taken up by cells through transferrin or independent transportation. On the one hand, its radioactive isotope (67Ga or 68Ga) concentrates in cancer tissues, realizing radiographic diagnosis of tumors. On the other hand, non-radioactive gallium kills cancer cells by inhibiting the normal function of ribonucleotide reductase (RR) and causing mitochondrial oxidative stress. In terms of antibacterial activity, Ga competes with Fe in biochemical reactions which enables it to destroy biofilms of bacteria and cause their death. In this review, we introduce the application of gallium in antineoplastic and antibacterial fields with the chemical mechanism revealed. And the development of Ga-based drugs will also be expected.

Keywords： Gallium ; Metallodrugs ; Antineoplastic ; Anti-microbial