Gentianine is an effective Swertiamarin derivative, which has anti-diabetic, antipsychotic, anti-inflammatory, hypotensive, diuretic and other effects, and has the potential to be developed into a safe antihypertensive drug.

Gentianine significantly decreased TLR4, MyD88 and NF-κB expression, as well as NO production and inflammatory cytokines release. Gentianine co-treatment with TLR4 inhibitor, further decreased TLR4, MyD88 and NF-κB expression, NO production, as well as the inflammatory cytokines. Taken together, Gentianine could be used as a potential anti-ischemic stroke agent by suppressing inflammatory responses via TLR4/NF-κB signaling pathway.[2]
Treatment with Gentianine significantly increased adipogenesis, which was associated with a significant increase in the mRNA expression of PPAR-γ, GLUT-4 and adiponectin[1]

Effect of Gentianine on tMCAO mouse demonstrated that Gentianine significantly ameliorated tMCAO induced ischemic injury by decreasing brain infarct volume and increasing the neurological score and upper limb muscle strength. Meanwhile, Gentianine significantly decreased the release of serum inflammatory cytokines. Machine learning enables that Gentianine might had anti-ischemic stroke effect through the TLR4/NF-κB signaling pathway. [2]