Anti-inflammatory effects of Scutellaria baicalensis water extract in LPS-induced THP-1 Macrophages through metabolomics study

(1) Background: Scutellaria baicalensis (Huang Qin) is a traditional Chinese Medicine possess beneficial effects of anti-inflammation in various diseases. In this study, we aimed to use untargeted metabolomics approach to investigate the possible underlying metabolic mechanisms of anti-inflammation effects of Scutellaria baicalensis in LPS-induced macrophages.; (2) Methods: Scutellaria baicalensis water extract (SBE) were applied to the THP-1 cells which were induced by phorbol 12-myristate 13-acetate (PMA) into macrophages under the LPS treated conditions. The cell lysate were collected and metabolites were extracted before characterizing by ultra-performance liquid chromatography (UPLC) combined with Q-Exactive mass/mass spectrometry (LC-MS/MS). The differential accumulated metabolites and related metabolism pathways affected by SBE in LPS-induced macrophages were identified. Further investigation of the secretion and expression of inflammatory cytokines IL-1β, TNF-ɑ and VEGFR were tested by real-time polymerase chain reaction (RT-PCR). (3) Results: The metabolome profile have indicated that retinol metabolism, arachidonic acid metabolism and linoleic acid metaoblism pathways were the most significantly enriched pathways response to SBE in LPS induced inflammatory model. Besides, SBE could inhibit the expression of the pro-inflammatory cytokines IL-1β and TNF-ɑ, and downregulation of the macrophage migration accelerator VEGFR1 in a dose dependent manner; (4) Conclusions: These findings indicated that SBE may exerted anti-inflammatory ability by regulating multiple fatty acids metabolism pathways as well as inhibiting the secretion of pro-inflammatory cytokines and VEGFR. This study provides evidences for Scutellaria baicalensis as the material for developing natural, effective anti-inflammatory products.