Recently, the team of Professor Liu Jikai from the School of Pharmaceutical Sciences of SCUN cooperated with the team of Zeng Ying, a researcher from Kunming Institute of Botany of Chinese Academy of Sciences, and discovered a new cyclase which can catalyze the formation of a unique fused bicyclic β-Lactone in Vibralactone. The research results were published in the authoritative academic journal “Angew. Chem. Int. Ed.” (2020, 59, 7209-7213；https://www.onlinelibrary.wiley.com/doi/10.1002/anie.202000710) with the title of A Hydrolase-Catalyzed Cyclization Forms the Fused Bicyclic β-Lactone in Vibralactone”.
The research results of Professor Liu Jikai's team of School of Pharmaceutical Sciences were published in the authoritative academic journal Angew. Chem. Int. Ed.
Photo by School of Pharmaceutical Sciences
In this research, Professor Liu Jikai's team analyzed the crystal structure of the new cyclase and discussed its special catalytic mechanism. The discovery of the new cyclases will lay the foundation for developing new chemical reactions, synthesizing these kinds of compounds and producing vibralactone in large quantities by biotechnology.
It is known that vibralactone is a kind of lipase selective inhibitor with strong activity discovered by Professor Liu Jikai's team in 2006. In the early period of the research, the research team clarified the biosynthetic pathway of vibralactone. Vibralactone derivatives have been studied as a candidate drug for weight loss for many years, but it cannot be mass produced through fermentation and total synthesis, so how to obtain a large quantity of vibralactone has cause a bottleneck for new drug R&D. It is for the first time in the world that the cyclization reaction catalyzed by the new cyclase has been discovered. The results of this study will eliminate the bottleneck and create favorable conditions for the R&D Class-I new drugs.
The research has been funded by the National Natural Science Foundation of China and the national key research and development plan.