1-脫氧野尻霉素是一種多羥基生物堿，可競(jìng)爭(zhēng)性地與α-葡萄糖苷酶結(jié)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(duì)1-脫氧野尻霉素進(jìn)行結(jié)構(gòu)修飾，不只在環(huán)內(nèi)N原子上進(jìn)行結(jié)構(gòu)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(tuán)取代，也可以在末端連接其他基團(tuán)。取代基的不同對(duì)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(duì)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(tuán)取代的1-脫氧野尻霉素衍生物及其活性的研究進(jìn)展，為1-脫氧野尻霉素的結(jié)構(gòu)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(guó)家重點(diǎn)研發(fā)計(jì)劃項(xiàng)目（2019YFC1710504）；國(guó)家自然科學(xué)基金資助項(xiàng)目（82173710）；北京市自然科學(xué)基金資助項(xiàng)目（7192129）；中國(guó)醫(yī)學(xué)科學(xué)院醫(yī)學(xué)與健康科技創(chuàng)新工程項(xiàng)目（2021-I2M-1-028，2022-I2M-2-002）