Abstract: Hesperidin and hesperitin are mainly found in citrus fruits of Rutaceae and belong to dihydroflavones. A variety of biological activities of hesperidin have been approved, drawing increasing scientific attention. With established biological activities and a wide range of pharmacological effects, hesperidin has been widely used in medicine and shows broad prospects for development and utilization. However, the bioavailability of hesperidin is low due to its poor solubility and absorption. Moreover, hesperitin is easy to be metabolized, so it's hard to maintain a high blood concentration.Therefore, the chemical modification of hesperidin and hesperitin becomes a hot spot of new drug design and development. In order to optimize the development and utilization of hesperidin and hesperitin, previous researches were summarized and knowledge gaps were explored based on studies at home and abroad, the latest progress in the synthesis of hesperitin and hesperidin derivatives and their pharmacological activities were also reviewed, so as to provide reference for structural modification and innovative drug research of hesperidin and hesperetin.