1-脫氧野尻霉素是一種多羥基生物堿，可競爭性地與α-葡萄糖苷酶結合，除降血糖的研究外，在抗腫瘤、抗病毒、抗氧化方面的研究也逐漸增加。研究者采用多種方法對1-脫氧野尻霉素進行結構修飾，不只在環(huán)內N原子上進行結構改造，在骨架其他部位的修飾也逐漸增多，取代基的種類多種多樣，烷基鏈的某些碳原子可以被雜原子或官能團取代，也可以在末端連接其他基團。取代基的不同對活性有一定的影響，同一取代基也可能有不止一種活性，碳原子用雜原子取代對活性提高有幫助，化合物的旋光性也是影響活性的因素。綜述了不同種類官能團取代的1-脫氧野尻霉素衍生物及其活性的研究進展，為1-脫氧野尻霉素的結構修飾研究提供參考。

1-Deoxynojirimycin is a polyhydroxy alkaloid that can competitively bind to the α-glucosidase. In addition to hypoglycemic activity, research of 1-deoxynojirimycin on anti-tumor, antiviral, and antioxidant activities is also gradually increasing. Researchers have used various methods to modify the structure of 1-deoxynojirimycin. People not only carry out structural modifications on the N atoms in the ring, but also gradually increase the modification of other parts of the skeleton. There are various types of substituents. Some carbon atoms in the alkyl chain can be substituted by heteroatoms or functional groups, and other groups can also be connected at the end. Different substituents have a certain impact on the activity. The same substituent may also have more than one activity. Substitution of carbon atoms with heteroatoms can help improve the activity. The optical activity of compounds is also a factor that affects the activity. This article reviews the research progress of 1-deoxynojirimycin derivatives with different functional groups and their activities, providing a reference for the structural modification of 1-deoxynojirimycin.

R914

國家重點研發(fā)計劃項目（2019YFC1710504）；國家自然科學基金資助項目（82173710）；北京市自然科學基金資助項目（7192129）；中國醫(yī)學科學院醫(yī)學與健康科技創(chuàng)新工程項目（2021-I2M-1-028，2022-I2M-2-002）