2. Academic Validation
  3. Cytotoxic prenylated flavones from the stem and root bark of Daphne giraldii

Cytotoxic prenylated flavones from the stem and root bark of Daphne giraldii

  • Bioorg Med Chem Lett. 2016 Aug 15;26(16):3968-72. doi: 10.1016/j.bmcl.2016.07.002.
Qian Sun 1,  Di Wang 1,  Fei-Fei Li 2,  Guo-Dong Yao 3,  Xue Li 4,  Ling-Zhi Li 1,  Xiao-Xiao Huang 5,  Shao-Jiang Song 6
Affiliations

Affiliations

  • 1 School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China; Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China.
  • 2 School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China; Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China; Yangtze River Pharmaceutical (Group) Co., Ltd, Taizhou 225300, People's Republic of China.
  • 3 China-Japan Research Institute of Medical Pharmaceutical Sciences, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China.
  • 4 School of Life Sciences and Biopharmaceutics, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China.
  • 5 School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China; Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China. Electronic address: xiaoxiao270@163.com.
  • 6 School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China; Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China. Electronic address: songsj99@163.com.
PMID: 27400887 DOI: 10.1016/j.bmcl.2016.07.002
Abstract

Three new prenylated Flavones (1-3), along with three known analogues (4-6), were isolated from the stem and root bark of Daphne giraldii. Their structures were determined by comprehensive NMR and HRESIMS spectroscopic data analyses. The absolute configurations of compounds 2 and 3 were assigned by optical rotation comparison, CD and [Rh2(OCOCF3)4]-induced CD spectral methods. The in vitro cytotoxicity experiments carried out involving five Cancer cell lines (U251, A549, HepG2, MCF-7 and Bcap37) showed that 2 markedly inhibited the proliferation of all tested cells with IC50 values ranging from 4.26 to 20.82μM. The preliminary structure-activity relationships of these Flavones are discussed. In addition, compound 2 was found to effectively induce Apoptosis in HepG2 cells according to a flow cytometry analysis.

Keywords

Apoptosis; Cytotoxicity; Daphne giraldii; Flavone.

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