Systematic Studies on Chemical Constituents from Daphne genkwa

Daphne genkwa Sieb. et Zucc. belongs to the family of Thymelaeaceae and is mainly distributed among the provinces along both the Yangtze river and the Yellow river of China. It is used as a folk medicine in China mainly for diuretic, pesticide, antitussive, expectorant, antifertility and anticancer purposes. The chemical constituents of Daphne genkwa have been demonstrated to be diterpenes and flavones. The structure-activity relationship and anticancer activities of diterpenes in Daphne genkwa have received the most attention and deserve special emphasis [1,2]. In order to clarify the constituents of Daphne genkwa, a systematic study on the chemical constituents was carried out. A total of 54 compounds were isolated from the flower bud of Daphne genkwa, including 29 diterpenes, 12 flavones, 7 lignans and 6 sterols. Among them, 10 new compounds were named as yuanhuanine A-J(1–10). The anticancer activities of 22 daphnane-type diterpenes against four tumor cell lines HL-60, A-549, Hep3B and U87 were tested. Most of daphne-type diterpenes were found to possess potent anticancer activities. The structure-activity relationship of daphne-type diterpenes was investigated. The results showed that the presence of acyl groups at C-3, C-20 or C-14 in the molecule might have an important role in cytotoxic activity. Acknowledgements: Support for this research from the National Natural Science Foundation of China (Grant No. 30973868) is gratefully acknowledged. References: [1] Li LZ, Gao PY, et al. (2007) Shenyang Yaoke Daxue Xuebao 24: 587–592. [2] Liao SG, Chen HD, et al. (2009) Chem Rev 109: 1092–1140.