大学化学 >> 2022, Vol. 37 >> Issue (3): 2203050.doi: 10.3866/PKU.DXHX202203050

所属专题: 生物无机与大健康

今日化学 上一篇    

镓元素在医疗卫生领域的应用:以抗癌与抗菌为例

彭信心1,*(), 许李智2, 张佳仪2, 景彦博2, 田松林2, 吴颖涵2, 曹润禹2, 张俊龙1,*()   

  1. 1 北京分子科学国家研究中心, 北京大学化学与分子工程学院,北京 100871
    2 北京大学医学部药学院,北京 100191
  • 收稿日期:2022-03-19 录用日期:2022-03-22 发布日期:2022-03-23
  • 通讯作者: 彭信心,张俊龙 E-mail:1901110330@pku.edu.cn;zhangjunlong@pku.edu.cn
  • 作者简介:Email: zhangjunlong@pku.edu.cn (张俊龙)
    Email: 1901110330@pku.edu.cn (彭信心)
    第一联系人:

    共同第一作者,对本文工作同等贡献

  • 基金资助:
    国家自然科学基金(21571007);国家自然科学基金(21621061);国家自然科学基金(21778002);国家自然科学基金(21861162008)

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

Xinxin Peng1,*(), Lizhi Xu2, Jiayi Zhang2, Yanbo Jing2, Songlin Tian2, Yinghan Wu2, Runyu Cao2, JunLong Zhang1,*()   

  1. 1 College of Chemistry and Molecular Engineering, Beijing National Laboratory for Molecular Sciences, Peking University, Beijing 100871, China
    2 School of Pharmaceutical Sciences, Peking University, Beijing 100191, China
  • Received:2022-03-19 Accepted:2022-03-22 Published:2022-03-23
  • Contact: Xinxin Peng,JunLong Zhang E-mail:1901110330@pku.edu.cn;zhangjunlong@pku.edu.cn

摘要:

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(67Ga或68Ga)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。

关键词: 镓, 金属药物, 抗肿瘤, 抗菌

Abstract:

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.

Key words: Gallium, Metallodrugs, Antineoplastic, Anti-microbial

MSC2000: 

  • G64