This study was aimed to summarize main-bone structure of cantharidin-based small molecules and facts about three typical candidates including its origin, physical-chemical properties and general synthetic approaches. Basic chemical and pharmacological information as well as development of anti-cancer activities, which were related to cantharidin, norcantharidin and their analogues were reviewed, especially the relationship between the structures and their inhibitory activity and selectivity of serine-threonine protein phosphatases PP1, PP2A and PP2B in cancer treatment. The designs and developments of new biological cantharidin-based small molecules were also reviewed.

This study was aimed to verify the chemical component cantharidin from Chinese blister beetle by LC-MS/MS. Components were first processed by HPLC to choose the appropriate separation conditions before LC/MS/MS analysis. Through the positive and negative ions pre-scan, positive ions scanning way was selected in the scanning of each separate component. The scanned maps were obtained and the relative molecular mass was deduced. The results showed that 8 types of cantharidin compounds were identified, including three isomers. It was concluded that LC-MS/MS was able to determine the chemical component cantharidin from Chinese blister beetle rapidly and accurately, which was existed in the body by the form of combined amino acid.