The Dr. Li Shen‘s research group of Institute of Marine Biology and Pharmacology (Ocean college, Zhejiang University), successfully made impressive academic progress in the fundamental research of anti-tumor marine drugs.

An original research article entitled “Design, Synthesis and Structure-Activity Relationship Studies of Glycosylated Derivatives of Marine Natural Product Lamellarin D” was published in the prestigious scientific journal European Journal of Medicinal Chemistry （EJMC）on January 28, 2021, which takes master student Liuliu Zheng as the first-author.

Lamellarin D, an alkaloid marine natural product, acts as a potent anticancer lead compound. But its druggability and further progression were limited due to its poor aqueous solubility, which is caused by its unique pentacyclic skeleton.

A major research focus in Li Shen’s research group is to modify the derivatives of lamellarins for the drug candidates based on the medicinal chemistry. In the article, regioselective glycosylation strategy was applied in the total synthesis of novel glycosylated derivatives of lamellarin D for both improving the aqueous solubility and anticancer activity.

The results indicated that the modification of glycosylation effectively enhanced the proliferation inhibitory activity. Some glycosylated derivatives exhibited 500-fold higher in the aqueous solubility than the parent compound lamellarin D. This work also laid the foundation for further R&D of novel marine medicine with independent intellectual property rights in China.

The research project was sponsored by National Natural Science Foundation of China for General Program (No.82073694), National Natural Science Foundation of China for Young Scholars (No.81402845), Natural Science Foundation of Zhejiang Province (No. LY21H300002,) and the Science and Technology Project of Zhoushan (No. 2018 C81035).

Source：Institute of Marine Biology and Pharmacology