稀有人參皂苷是人參皂苷中一類重要的活性成分，該類化合物具有極強的抗腫瘤活性。其主要通過糖苷化的方法來實現(xiàn)，現(xiàn)有的糖苷化方法主要包括化學合成法、酶解法和微生物轉(zhuǎn)化法。研究表明糖苷化能改變化合物的生物活性、穩(wěn)定性、水溶性、以及與受體分子的相互識別和結(jié)合特性，另外還能降低或除去內(nèi)源和外源有毒物質(zhì)的毒性。綜述了3類糖苷化方法，并對比總結(jié)各個方法的優(yōu)劣之處，有利于選擇出最佳的合成稀有人參皂苷的糖苷化方法，以滿足臨床和科研等方面的需求。對人參皂苷的糖苷化最新研究進展進行綜述，并對糖苷化人參皂苷的發(fā)展趨勢作了簡要的討論。

Rare ginsenosides, as a class of important active components of ginsenosides, have strongly potent antitumor effects. Glycosylation is the mainly method to synthesis them. There are three methods for glycosylation, namely chemical synthesis, enzymolysis, and microbial transformation. At the same time, studies have shown that glycosylation could change the biological activity, stability, water solubility, and the mutual recognition and binding property with receptor molecules. It can also reduce or eliminate the toxicity of endogenous and exogenous toxic substances. Three types of glycosylation methods have been summarized, and the pros and cons of each method have been compared and concluded, which help us choose the best glycosylation method for the synthesis of rare ginsenosides in order to meet the needs of clinical and scientific research. In this paper, the new progress on the glycosylation of rare ginsenosides are summarized, and the trends in the development of glycosylation of ginsenosides in the future are also briefly discussed.

國家自然科學基金資助項目（81273389）