Phytochemical analysis of a methanol–dichloromethane
(1:1)
extract of the aerial parts of Tephrosialinearis led
to the isolation of 18 compounds. Seven of these, namely, lineaflavones
A–D (1–4), 6-methoxygeraldone
(5), 8″-acetylobovatin (6), and 5-hydroxy-7-methoxysaniculamin
A (7) are new compounds. The compounds were characterized
based on their NMR and HRMSn data. The anti-inflammatory
effects of the crude extract and isolated compounds were evaluated
by measuring the levels of interleukins (IL-1β, IL-2, and IL-6),
granulocyte-macrophage colony-stimulating factor (GM-CSF), and tumor
necrosis factor-α (TNF-α) in lipopolysaccharide (LPS)-stimulated
peripheral blood mononuclear cells (PBMCs). The crude extract inhibited
the release of all cytokines except IL-1β, which slightly increased
in comparison to the LPS control. All the tested compounds suppressed
the production of IL-2, GM-CSF, and TNF-α. Whereas compounds 1, 2, 4–8, 10–15, 17, and 18 decreased production of IL-6, compounds 1, 2, 4, 7, 10, 13–15, and 17 inhibited the release
of IL-1β. It is worth noting that most of the compounds tested
showed a superior reduction in cytokines release compared to the reference
drug ibuprofen.