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.
Highlights
Non-small cell lung cancer (NSCLC) accounts for 85% of all lung cancer cases, and remains the principal cause for cancer-related death worldwide [1,2]
During our continuous effort to discover active ingredients of the air-dried whole herbs of S. doederleinii, a series of dimeric flavones, including four previously undescribed biflavonoids, were isolated. These compounds represented one of a rare biflavonoids family bearing a linker of individual flavones to each other by direct C-3-O-C-4 bonds, which was isolated for the first time from Selaginella doederleinii
It is pertinent to evaluate the effect of biflavones on different proteins or mechanisms that lead to cell apoptosis in cancer cells
Summary
Non-small cell lung cancer (NSCLC) accounts for 85% of all lung cancer cases, and remains the principal cause for cancer-related death worldwide [1,2]. Novel therapeutic agents including safe and effective anti-NSCLC compounds are urgently needed. Comparisons to naringeninyl-(4 ,O,3)-kaempferol [21], previously isolated from the Selaginella chrysocaulos, revealed that the two compounds share same planar structure, when reported in racemic mixture form in the literature, no absolute configuration was elaborated. 120.0 130.4 116.3 155.8 162.6 104.4 181.7 158.8 107.8 165.4 93.8 157.6 103.3 8.0 125.5 128.7 116.1 160.0 a Measured at 125 MHz; b Measured at 200 MHz. chrysocaulos, revealed that the two compounds share same planar structure, when reported in racemic mixture form in the literature, no absolute configuration was elaborated. The 1D and 2D NMR data (Tables 1 and 2) were almost identical to 1 except for an additional methyl at C-6 in 4, which can be proved via the key HMBC correlations of 6 -CH3 (δH 1.88) with C-5. Compound 4 was characterized as (2 S)-6 -methyl-2 ,3 -dihydrodelicaflavone
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