Biflavonoids from Selaginella doederleinii as Potential Antitumor Agents for Intervention of Non-Small Cell Lung Cancer

  • Molecules. 2021 Sep 5;26(17):5401. doi: 10.3390/molecules26175401.
Fenghua Kang  1  2  3 ,  Sha Zhang  1  2  3 ,  Dekun Chen  1  2  3 ,  Jianbing Tan  1  2  3 ,  Min Kuang  1  2  3 ,  Jinlin Zhang  1  2  3 ,  Guangyuan Zeng  1  2  3 ,  Kangping Xu  1  2  3 ,  Zhenxing Zou  1  2  3 ,  Guishan Tan  1  2  3
Affiliations
  • 1. Xiangya School of Pharmaceutical Sciences, Central South University, Changsha 410013, China.
  • 2. Xiangya Hospital of Central South University, Changsha 410008, China.
  • 3. Hunan Key laboratory of Diagnostic and Therapeutic Drug Research for Chronic Diseases, Central South University, Changsha 410013, China.
PMID: 34500834 DOI: 10.3390/molecules26175401
Abstract

Four new biflavonoids (1-4) were isolated from Selaginella doederleinii together with a known biflavonoid derivative (5). Their structures contained a rare linker of individual Flavones to each Other by direct C-3-O-C-4''' bonds, and were elucidated by extensive spectroscopic data, including HRESIMS, NMR and ECD data. All isolates significantly inhibited the proliferation of NSCLC cells (IC50 = 2.3-8.4 μM) with low toxicity to non-cancer MRC-5 cells, superior to the clinically used drug DDP. Furthermore, the most active compound 3 suppressed XIAP and Survivin expression, promoted upregulation of Caspase-3/cleaved-caspase-3, as well as induced cell Apoptosis and cycle arrest in A549 cells. Together, our findings suggest that 3 may be worth studying further for intervention of NSCLC.

Keywords
Selaginella doederleinii; antiproliferative activity; apoptosis; biflavonoid; cell cycle.
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