Chinese Journal of Organic Chemistry ›› 2021, Vol. 41 ›› Issue (7): 2601-2609.DOI: 10.6023/cjoc202101008 Previous Articles     Next Articles



许亚文a, 王健鲲b, 甄乐b,*(), 王广基a,b,*()   

  1. a 广东药科大学药学院 广州 510006
    b 中国药科大学药物代谢动力学重点实验室 南京 210009
  • 收稿日期:2021-01-05 修回日期:2021-03-18 发布日期:2021-04-16
  • 通讯作者: 甄乐, 王广基
  • 基金资助:
    国家自然科学基金(81973186); 国家自然科学基金(81903707); 国家科技重大新药创制专项(2019ZX09301-151); 江苏省优青(BK20200081)

Research Progress of Small-Molecular Hydropersulfide Donors

Yawen Xua, Jiankun Wangb, Le Zhenb(), Guangji Wanga,b()   

  1. a College of Pharmacy, Guangdong Pharmaceutical University, Guangzhou 51000
    b Key Laboratory of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing 210009
  • Received:2021-01-05 Revised:2021-03-18 Published:2021-04-16
  • Contact: Le Zhen, Guangji Wang
  • Supported by:
    National Natural Science Foundation of China(81973186); National Natural Science Foundation of China(81903707); National Major Scientific & Technological Special Project for “Significant New Drugs Development”(2019ZX09301-151); Jiangsu Provincial Funds for Excellent Young Scientists(BK20200081)

The unique chemical structure endowed small-molecular hydropersulfides (RSSH) with unclear but fascinating biological activities, which have been attracted much attention. The donors that could release RSSH smoothlyin situ under physiological or pathological conditions will become powerful chemical tools for exploring the physiological functions, mechanism of action, and potential therapeutic benefit of RSSH. Over the past five years, a substantial breakthrough had been achieved in the design and development of RSSH donors, which is summarized in this perspective. According to the activation patterns, the existing donors are divided into five categories, namely esterase-activated donor, ROS (reactive oxygen species)-activated donor, pH-dependent donor, light-activated donor, and nitroreductase-activated donor. All kinds of donors played ideal roles in improving the oxidative stress at the cellular level, part of which also show a positive therapeutic effect in the context of myocardial ischemia-reperfusion injury. Besides, the related release mechanisms and the proof of concept of the donors are briefly introduced. In the next five years, waves of novel donors are emerging. On one hand, diverse donors, with stable and controllable release rate, clear release process, and identified release components, will be designed. On the other hand, the indispensable toolbox of donors will be fully assembled for more in-depth and comprehensive biological activity researches.

Key words: hydropersulfides, donor, oxidative stress, esterase, sulfane sulfur