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

• Published in: Molecules (Basel, Switzerland) Vol. 26; no. 17; p. 5401
• Main Authors: Kang, Fenghua, Zhang, Sha, Chen, Dekun, Tan, Jianbing, Kuang, Min, Zhang, Jinlin, Zeng, Guangyuan, Xu, Kangping, Zou, Zhenxing, Tan, Guishan
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 05.09.2021; MDPI
• Subjects: A549 Cells; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; antiproliferative activity; Apoptosis; Apoptosis - drug effects; biflavonoid; Biflavonoids - chemistry; Biflavonoids - pharmacology; Carcinoma, Non-Small-Cell Lung - metabolism; Caspase-3; Cell cycle; Cell Cycle - drug effects; Cell proliferation; Cotton; Flavones; Flow cytometry; Humans; Investigations; Lung cancer; Lung Neoplasms - metabolism; Metabolites; Morphology; NMR; Non-small cell lung carcinoma; Nuclear magnetic resonance; Selaginella; Selaginella doederleinii; Selaginellaceae - chemistry; Survivin; Toxicity; XIAP protein; apoptosis; Selaginella doederleinii; cell cycle; antiproliferative activity; biflavonoid
• ISSN: 1420-3049; 1420-3049
• DOI: 10.3390/molecules26175401

Four new biflavonoids ( - ) were isolated from together with a known biflavonoid derivative ( ). 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 (IC = 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 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 may be worth studying further for intervention of NSCLC.