Advances in Structural Modification and Pharmacological Activity of Catalpol and its Derivatives

Abstract Catalpol and its derivatives were found in a variety of Chinese medicinal plants and possess various biological activities, such as anti‐inflammatory, anti‐oxidant, neuroprotective, cardiovascular protective, anti‐tumor and hypoglycemic and so on. The extensive pharmacological activities of catalpol have been attracted much attention to researchers, but the clinical applications are limited by poor lipid solubility, low bioavailability and short half‐life, so pharmacologists have made various structural modifications to catalpol, such as increasing lipid solubility to enhance its biological activities in the hope that it can be widely used in clinical applications. In this paper, using “Catalpol” and “Catalpol derivatives” as the keywords, more than 200 articles from 1965 to 2021 were obtained from databases, such as CNKI, PubMed, Scifinder and so on. Finally, 93 articles were selected to systematically analyze the structure and efficacy of catalpol and its derivatives according to pharmacological activity, which will provide ideas for the development of new catalpol drugs in the future.