Glycoalkaloids are natural products widely found in Solanaceae plants,which have been valued by people for their important biological activities.The different combinations of aglycone and sugar moieties in glycoalkaloids give them different chemical structures which determine their biological activities.The most studied at present is their remarkable antitumor activity.However,the exact antitumor pharmacological mechanism and structure-activity relationship of these compounds have not been elucidated yet up to now.Therefore,we review the chemical structure,antitumor activity and structure-activity relationship of glycoalkaloids in this paper to provide a scientific basis for their antitumor clinical application.