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Biflavonoids from Selaginella doederleinii as Potential Antitumor Agents for Intervention of Non-Small Cell Lung Cancer
Authors:Fenghua Kang  Sha Zhang  Dekun Chen  Jianbing Tan  Min Kuang  Jinlin Zhang  Guangyuan Zeng  Kangping Xu  Zhenxing Zou  Guishan Tan
Institution:1.Xiangya School of Pharmaceutical Sciences, Central South University, Changsha 410013, China; (F.K.); (S.Z.); (D.C.); (J.T.); (M.K.); (J.Z.); (G.Z.); (K.X.);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
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  biflavonoid  antiproliferative activity  apoptosis  cell cycle
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