Total Synthesis of Euphopia B and Discovery of a Selective Inhibitor of Potassium Efflux-Independent NLRP3 Inflammasome Activation
-mediated cyclization as key steps. This synthesis enables single-batch preparation of euphopia B on a > 100 mg scale and provides a solid foundation for biological studies. Systematic bioactivity screening subsequently revealed that euphopia B selectively inhibits NLRP3 inflammasome activation induced by potassium efflux-independent activators, thereby providing a critical chemical probe for elucidating the complex activation mechanism of NLRP3.
Authors
- R W Liu
- Yong Qin (ORCID: https://orcid.org/0000-0003-3434-5747)
- Fenglin Wang (ORCID: https://orcid.org/0000-0002-5872-2693)
- Guobin Xie
- T. T. Wang
- Chaoyun Xue
- Ze Zhang (ORCID: https://orcid.org/0000-0001-7196-6839)
- Jing Yu (ORCID: https://orcid.org/0000-0003-2836-6373)
- Hao Song (ORCID: https://orcid.org/0000-0002-2106-5810)
- Qifeng Chen
- Zhongpeng Ding
Institutions
- National Medical Products Administration (CN)
- Sichuan University (CN)
- National Institute of Biological Sciences, Beijing (CN)
- Tsinghua University (CN)
Publication Details
- Journal
- Journal of the American Chemical Society
- Published
- 2026-04-13
- DOI
- https://doi.org/10.1021/jacs.6c02838
- Primary Topic
- Inflammasome and immune disorders
- Type
- article
- Field-Weighted Citation Impact
- 0.00
Funders
- National Natural Science Foundation of China
- Natural Science Foundation of Sichuan Province