The ethyl acetate-soluble fraction from the ethanolic extract of Angelica keiskei showed potent inhibitory activity against the production of nitric oxide (NO) in lipopolysaccharide (LPS)-activated RAW 264.7 cells. We identified seven chalcones (1-7) from EtOAc-soluble fractions through the activity-guided separation. Four active principles, identified as 4-hydroxyderrcine (1), xanthoangelol E (2), xanthokeismin A (4), and xanthoangelol B (5), inhibited the production of NO and the expression of proinflammatory cytokines, interleukin (IL)-1β and IL-6, in LPS-activated macrophages. Western blotting and reverse transcription-polymerase chain reaction analysis demonstrated that these chalcones attenuated protein and mRNA levels of inflammatory enzymes such as inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2). Moreover, these active compounds suppressed the degradation of inhibitory-κBα (I-κBα) and the translocation of nuclear factor κB (NF-κB) into nuclei of LPS-activated macrophages. These data demonstrate that four chalcones (1, 2, 4, and 5) from A. keiskei can suppress the LPS-induced production of NO and the expression of iNOS/COX-2 genes by inhibiting the degradation of I-κBα and nuclear translocation of NF-κB. Taken together, four chalcones from A. keiskei may have efficacy as anti-inflammatory agents.

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Activation of microglia has been associated with pathological hallmarks of several neurodegenerative diseases. The regulation of microglial activation by inhibiting the production of pro‐inflammatory molecules can be useful therapeutic approach against neurodegenerative disorders.Anemarrhena asphodeloides Bunge (Liliaceae) has been used as an anti‐pyretic, anti‐inflammatory and anti‐diabetic agent in traditional medicine in Korea, China and Japan. (−)‐Nyasol, a norlignan isolated from Anemarrhena asphodeloides, showed anti‐inflammatory potential in LPS‐activated BV‐2 microglial cells. (−)‐Nyasol suppressed the mRNA levels of tumor necrosis factor α (TNF‐α) and Interleukin 1β (IL‐1β) in activated microglial cells. It also inhibited the production of nitric oxide (NO) and prostaglandin E2 (PGE2) by down‐regulation of inducible nitric oxide synthase (i‐NOS) and cyclooxygenase‐2 (COX‐2), respectively. These inhibitory effects were correlated with the suppression of LPS‐induced nuclear factor κB (NF‐κB) nuclear translocation through the inactivation of p38 mitogen‐activated protein kinase (MAPK). These results suggest that (−)‐nyasol can be a modulator in neuro‐inflammatory conditions induced by microglial activation.