The research results of structural modification of dammarane-type saponins and their structure-activity relationships and other aspects were collected in this paper. The structure-activity relationships of dammarane-type saponins and the main structural modification methods including chemical method

biological transformation method and combinatorial chemistry method were introduced by researching the literature over the past two decades in National Knowledge Infrastructure (CNKI) and in the Medline database. By modifying the structure of dammarane-type saponins

the physical and chemical properties are improved

the biological activity and the bioavailability are enhanced

and the side effects are reduced. In this way

not only the clinical application range is expanded

but also a number of new compounds would be got for biological activity screening. This research provides the theory basis for making full use of dammarane-type saponins. And it is believed that dammarane-type saponins and their derivatives will play a more important role in the future science research.