科研综述

俞飚研究员在实验室

俞飚以糖的“化学结构决定其生物活性和功能”为主线，在糖苷键的构建、复杂糖链和糖缀合物的全合成及其生物功能研究方面，做出了具有重要国际影响的系统性成果，推动了糖化学领域的发展。主要贡献包括互相关联的三个方面：

（1）发明的两个糖苷化方法提升了对于聚糖和糖缀合物的获取能力。其中以糖基三氟乙酰亚胺酯为给体的方法已成为复杂聚糖和糖缀合物合成的通用方法，被全球100多家实验室成功应用，被称为催化糖苷化的三个里程碑之一；以糖基邻炔基苯甲酸酯为给体的金催化糖苷化反应则实现了其它方法不能实现的特殊糖苷键的构建，被称为俞氏糖苷化反应 (Yu Glycosylation)。

（2）率先实现了一系列复杂天然糖缀合物的全合成，完成肠道菌O-抗原128聚鼠李甘露聚糖的合成。

（3）深入开展了聚糖和糖苷分子的构效关系和作用机理研究和药物研发。合作阐明Hoodia皂苷通过激活GPR119受体来控制食欲和治疗糖尿病的机理、研发了糖基化雷公藤内酯作为抗肿瘤药物先导化合物等 。

学术论著

截至2021年11月，俞飚先后发表论文近300篇 。代表论著如下 ：

1. Gold (I)-Catalyzed glycosylation with glycosyl o-alkynylbenzoates as donors. B. Yu,* Acc. Chem. Res. 2018, 51, 507-516.

2. Inhibition of cancer stem cell like cells by a synthetic retinoid. J. Chen, X. Cao, Q. An, Y. Zhang, K. Li, W. Yao, F. Shi, Y. Pan, Q. Jia, W. Zhou, F. Yang, F. Wei, N. Wang,* B. Yu,* Nature Commun. 2018, 9:1406.

3 .Amipurimycin, total synthesis of the proposed structures and diastereoisomers. S. Wang, J. Sun, Q. Zhang, X. Cao, Y. Zhao, G. Tang, B. Yu,* Angew. Chem. Int. Ed. 2018, 57, 2884-2888.

4. Gold-catalyzed glycosylation on the synthesis of complex carbohydrate-containing natural products. W, Li, B. Yu,* Chem. Soc. Rev. 2018, 47, 7954–7984.

5. Total synthesis of echinoside A, a representative triterpene glycoside of sea cucumbers. X. Chen, X. Shao, W. Li, X. Zhang, B. Yu,* Angew. Chem. Int. Ed. 2017, 56, 7648-7652.

6. Synthesis of bradyrhizose oligosaccharides relevant to the Bradyrhizobium O-antigen. W. Li, A. Silipo, L. B. A. Gersby, M.-A. Newman, A. Molinaro,* B. Yu,* Angew. Chem. Int. Ed. 2017, 56, 2092-2096.

7. Total synthesis of periploside A, a unique pregnane hexasaccharide with potent immunosuppressive effects. X. Zhang, Y. Zhou, J. Zuo, B. Yu,* Nat. Commun. 2015, 6, 5879.

8. Total Synthesis of Linckosides A and B, the Representative Starfish Polyhydroxysteroid Glycosides with Neuritogenic Activities. D. Zhu, B. Yu,* J. Am. Chem. Soc. 2015, 137, 15098-15101.

9. A Modular Approach to the Total Synthesis of Tunicamycins. J. Li, B. Yu,* Angew. Chem. Int. Ed. 2015, 54, 6618–6621.

10.O-Glycosylation methods in the total synthesis of complex natural glycosides. Y. Yang,* X. Zhang, B. Yu,* Nat. Prod. Rep. 2015, 32, 1331-1355.

11.Molecular matchmaking between the popular ‘weight loss’ herb Hoodia gordonii and GPR119, a potential drug target for metabolic disorder. S. Zhang, Y. Ma, J. Li, J. Ma, B. Yu,* X. Xie,* Proc. Natl. Acad. Sci. USA 2014, 111, 14571-14576.

12.Total synthesis of nucleoside antibiotic A201A. S. Nie, W. Li, B. Yu,* J. Am. Chem. Soc. 2014, 136, 4157-4160.

13.Mechanistic insights into the gold(I)-catalyzed activation of glycosyl ortho-alkynylbenzoates for glycosidation. Y. Tang, J. Li, Y. Zhu, Y. Li, B. Yu,* J. Am. Chem. Soc. 2013, 135, 18396-18405.

14.Assembly of naturally occurring glycosides, evolved tactics and glycosylation methods. B. Yu,* J. Sun, X. Yang, Acc. Chem. Res. 2012, 45, 1227-1236.

15.Total synthesis of landomycin A, a potent antitumor angucycline antibiotic. X. Yang, B. Fu, B. Yu,* J. Am. Chem. Soc. 2011, 133, 12433-12435.

16.An efficient approach to the synthesis of nucleosides, gold(I)-catalyzed N-glycosylation of pyrimidines and purines with glycosyl ortho-alkynylbenzoates. Q. Zhang, J. Sun, Y. Zhu, F. Zhang, B. Yu,* Angew. Chem. Int. Ed. 2011, 50, 4933–4936.

17.Characterization of the isochromen-4-yl-gold(I) intermediate in the gold(I)-catalyzed glycosidation of glycosyl o-alkynylbenzoates and enhancement of the catalytic efficiency thereof. Y. Zhu, B. Yu,* Angew. Chem. Int. Ed. 2011, 50, 8329–8332.

18.Total synthesis and structural revision of TMG-chitotriomycin, a specific inhibitor of insect and fungal ?-N-acetylglucosaminidases Y. Yang, Y. Li, B. Yu,* J. Am. Chem. Soc. 2009, 131, 12076-12077.

19.Total synthesis of Lobatoside E, a potent antitumor cyclic triterpene saponin. C. Zhu, P. Tang, B. Yu,* J. Am. Chem. Soc. 2008, 130, 5872-5873

20.Total synthesis of Candicanoside A, a potent antitumor saponin bearing a rearranged steroid side chain. P. Tang, B. Yu,* Angew. Chem. Int. Ed. 2007, 46, 2527-2530.

学术交流

科研项目

科研成果奖励

截至2021年11月，俞飚先后获得上海市青年科技杰出贡献奖和自然科学牡丹奖、国家自然科学奖二等奖；获得授权专利24件，实施专利7件 。

人才培养

教授课程

俞飚在中国科学院上海有机化学研究所讲授《天然产物合成的战略与战术》《化学小分子全合成与化学生物学》《现代有机合成与设计》等课程 。

指导学生

截至2021年11月，俞飚先后培养（合作培养）博士生60人、硕士生23人、出站博士后14人；其中已有16位成为教授（研究员） 。

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