Naturally Occurring Cytotoxic [3'→8″]-Biflavonoids from Podocarpus nakaii

  • J Tradit Complement Med. 2012 Jul;2(3):220-6. doi: 10.1016/s2225-4110(16)30103-1.
Pen-Ho Yeh  1 ,  Yun-Dar Shieh  2 ,  Li-Chun Hsu  3 ,  Li-Ming Yang Kuo  4 ,  Jhih-Hu Lin  5 ,  Chia-Ching Liaw  5 ,  Yao-Haur Kuo  6
Affiliations
  • 1. Institute of Pharmacology, National Yang-Ming University, Taipei 112, Taiwan.
  • 2. Institute of Pharmacology, National Yang-Ming University, Taipei 112, Taiwan ; National Research Institute of Chinese Medicine, Taipei 112, Taiwan.
  • 3. National Research Institute of Chinese Medicine, Taipei 112, Taiwan ; Department of Biochemical Science and Technology, National Taiwan University, Taipei 106, Taiwan.
  • 4. National Research Institute of Chinese Medicine, Taipei 112, Taiwan ; School of Pharmacy, Taipei Medical University, Taipei 110, Taiwan.
  • 5. National Research Institute of Chinese Medicine, Taipei 112, Taiwan.
  • 6. National Research Institute of Chinese Medicine, Taipei 112, Taiwan ; Graduate Institute of Integrated Medicine, China Medical University, Taichung 404, Taiwan.
PMID: 24716136 DOI: 10.1016/s2225-4110(16)30103-1
Abstract

Bioassay-guided fractionation of the EtOH extract of the dried twigs of Podocarpus nakaii Hayata (Podocarpaceae), endemic plant in Taiwan has resulted in isolation of four [3'→8″]-biflavonoid derivatives, amenotoflavone (AF), podocarpusflavone-A (PF), II-4″,I-7-dimethoxyamentoflavone (DAF), and heveaflavone (HF). Their structures were determined by physical and extensive spectroscopic analyses such as (1)H, (13)C, (1)H-(1)H COSY, HMQC, and HMBC, as well as comparison with literature values. Compounds PF and DAF showed significant inhibitions against DLD, KB, MCF-7, HEp-2 tumor cell lines (ED50 CA. 4.56-16.24 μg/mL) and induced cell Apoptosis in MCF-7 via mainly sub-G1/S phase arrest. Furthermore, these compounds exhibited moderate Topoisomerase I inhibitory activity.

Keywords
Apoptosis; Cytotoxicity; Podocarpus nakaii; Topoisomerase I; [3′→8″]-Biflavonoids.
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