Pristimerin is a potent and reversible monoacylglycerol lipase (MGL) inhibitor with an IC50 of 93 nM. It inhibits MGL rapidly, reversibly, and non-competitively, possibly through a polar interaction with Cys208. Pristimerin also inhibits HFLS-RA and HUVEC cell viability in a dose- and time-dependent manner, and decreases VEGF-induced autophosphorylation of VEGFR2, attenuating the VEGFR2-mediated signaling pathway. Furthermore, Pristimerin inhibits inflammation and tumor angiogenesis, reducing vessel density in synovial membrane tissues of inflamed joints and lowering the expression of pro-angiogenic factors like TNF-α, Ang-1, and MMP-9 in sera.
- Potent and reversible monoacylglycerol lipase (MGL) inhibitor.
- Inhibits HFLS-RA and HUVEC cell viability.
- Attenuates VEGFR2-mediated signaling pathway.
- Inhibits inflammation and tumor angiogenesis.