镓元素在医疗卫生领域的应用:以抗癌与抗菌为例

Gallium’s Application in Medicine and Hygiene:Examples of Antineoplastic and Anti-Microbial

镓(Ga)位于元素周期表第四周期第ⅢA族,在临床疾病诊断和治疗中有重要应用。在体内,氧化还原惰性的三价镓(Ga(Ⅲ))通常作为Fe(Ⅲ)的竞争性抑制剂,破坏病变(肿瘤或感染)部位的铁稳态,从而实现抗肿瘤或抗菌的作用。在癌症诊疗方面,Ga(Ⅲ)可以通过与转铁蛋白结合或独立运输的方式进入细胞:其放射性同位素(^(67)Ga或^(68)Ga)在癌组织中富集,实现肿瘤的放射影像学诊断;而非放射性Ga则通过抑制核糖核苷酸还原酶(RR)的正常功能、引起线粒体氧化应激等途径杀灭癌细胞。在抗菌方面,Ga与Fe在生化反应中形成竞争关系,从而破坏细菌生物被膜的结构和功能,实现抗菌作用。本文从化学原理出发,介绍了Ga在癌症的诊疗和抗菌领域的应用,并对Ga基药物的发展进行了展望。

Gallium is located at the fourth period and theⅢA 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(^(67)Ga or ^(68)Ga)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.