Yuanhuacin and Related Anti-Inflammatory and Anticancer Daphnane Diterpenes from Genkwa Flos-An Overview

The dried flower buds of the plant Daphne genkwa Sieb. et Zucc. have been largely used in traditional Chinese medicine for the treatment of inflammatory diseases. Numerous diterpenoids have been isolated from the Genkwa Flos (yuanhua in Chinese), including a series of daphnane-type diterpene designated as yuanhuacin (YC, often improperly designated as yuanhuacine) and analogues with a patronymic name. The series includes ten daphnane-type diterpenes: yuanhuacin, yuanhuadin (YD), yuanhuafin (YF), yuanhuagin (YG), yuanhuahin (YH), yuanhuajin (YJ), yuanhualin (YL), yuanhuamin (YM), yuanhuapin (YP), and yuanhuatin (YT). They are distinct from the rare flavonoid yuanhuanin. The series comprises several anticancer agents, such as the lead compound YC, which has revealed potent activity in vitro and in vivo against models of lung and breast cancers. The main signaling pathways implicated in the antitumor effects have been delineated. Protein kinase C is a key factor of activity for YC, but in general the molecular targets at the origin of the activity of these compounds remain little defined. Promising anticancer effects have been reported with analogues YD and YT, whereas compounds YF and YP are considered more toxic. The pharmacological activity of each compound is presented, as well as the properties of Genkwa Flos extracts. The potential toxic effects associated with the use of these compounds are also underlined.

Automated summary

The dried flower buds of Daphne genkwa Sieb. et Zucc. have long been used in traditional Chinese medicine to treat inflammatory diseases. Various diterpenoids, including the yuanhuacin (YC) series and analogues, have been isolated from Genkwa Flos. These compounds have shown potential as anticancer agents, with YC being particularly effective against lung and breast cancers. Although protein kinase C has been identified as a key factor in YC's activity, the exact molecular targets of these compounds remain unclear. The pharmacological activity of each compound and the properties of Genkwa Flos extracts are discussed, along with the potential toxic effects associated with their use.