In the current study, (-) pseudosemiglabrin effectively suppressed TLR-4, NF-κB, IL-1β, and TNF-α mRNA expressions, which were induced by pilocarpine injection, implying that it has the potential to prevent the development of epilepsy by suppressing astrocyte activation, inflammatory cytokine production, and their upstream transcription factors, TLR-4 and NF-κB, and was involved in neuroinflammation control. The gene discussed is TLR4; the disease is epilepsy.