Parthenolide(PTL)is a sesquiterpene lactone derived from medicinal plant feverfew(Tanacetum parthenium).Recent studies have demonstrated that it has multiple pharmacological activities,especially in the treatment of v...Parthenolide(PTL)is a sesquiterpene lactone derived from medicinal plant feverfew(Tanacetum parthenium).Recent studies have demonstrated that it has multiple pharmacological activities,especially in the treatment of various hematological and solid cancers.The superior anticancer activity of PTL suggests that it has the potential to be a first-line drug.However,due to the limited physical and chemical properties,as well as bioavailability,structural modification strategies are strongly recommended to improve the anticancer activity.This review describes representative PTL derivatives obtained by different modification strategies,which are reported to exert antiproliferative activities superior to the parent compound PTL.Furthermore,we also summarize their basic mechanisms on cancer-related signaling pathways,so as to explain the potential and characteristics of PTL and its derivatives in cancer therapy.展开更多
基金supported by the Natural Science Foundation of Jiangsu Province(No.BK20201332)the“Double First-Class”University Project(No.CPU2018GF03)+1 种基金the Six Talent Peaks Project of Jiangsu Province(No.SWYY-107)Jiangsu Province‘333’Project,111 Center from Ministry of Education of China and the State Administration of Foreign Experts Affairs of China(No.B18056).
文摘Parthenolide(PTL)is a sesquiterpene lactone derived from medicinal plant feverfew(Tanacetum parthenium).Recent studies have demonstrated that it has multiple pharmacological activities,especially in the treatment of various hematological and solid cancers.The superior anticancer activity of PTL suggests that it has the potential to be a first-line drug.However,due to the limited physical and chemical properties,as well as bioavailability,structural modification strategies are strongly recommended to improve the anticancer activity.This review describes representative PTL derivatives obtained by different modification strategies,which are reported to exert antiproliferative activities superior to the parent compound PTL.Furthermore,we also summarize their basic mechanisms on cancer-related signaling pathways,so as to explain the potential and characteristics of PTL and its derivatives in cancer therapy.