Theranostics 2021; 11(3):1513-1526. doi:10.7150/thno.53459


Recent advances in supramolecular antidotes

Hang Yin1*, Xiangjun Zhang1*, Jianwen Wei1*, Siyu Lu2, David Bardelang3✉, Ruibing Wang1✉

1. State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Taipa, Macau, China.
2. Green Catalysis Center, College of Chemistry, Zhengzhou University, 100 Kexue Road, Zhengzhou 450001, China.
3. Aix Marseille Univ, CNRS, ICR, Marseille, France.
*These authors contributed equally to this work.

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Yin H, Zhang X, Wei J, Lu S, Bardelang D, Wang R. Recent advances in supramolecular antidotes. Theranostics 2021; 11(3):1513-1526. doi:10.7150/thno.53459. Available from

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Poisons always have fascinated humankind. Initially considered as deleterious or hazardous substances, the modern era has witnessed the controlled utilization of dangerous poisons in medicine and cosmetics. Simultaneously, antidotes have become crucial as reversal agents to counteract the effects of a poison, and they are also used today to positively cancel the benefits of a poison after use. Currently, the majority of poisons are composed of small molecules. This review focuses on recent developments to reverse or prevent toxic effects of poisons by encapsulation in host molecules. Cyclodextrins, cucurbiturils, acyclic cucurbituril derivatives, calixarenes, and pillararenes, have been reported to largely impact the effects of toxic compounds, thus extending the current paradigm of small molecule antidotes by adding a new family of macrocyclic compounds to the current arsenal of antidotes. Along this line of research, endogenous "harmful" species are also sequestered by one or more of these supramolecular host molecules, expanding the potential of supramolecular antidotes to diverse therapeutic areas.

Keywords: Poisons, Macrocycles, Supramolecular Chemistry, Antidotes, Host-guest