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Pristimerin

CAS No. : 1258-84-0

MCE 国际站：Pristimerin

产品活性：Pristimerin是高效可逆的单酰基甘油脂肪酶(MGL)抑制剂，IC₅₀值为93 nM。

研究领域：Anti-infection

作用靶点：Bacterial

结构分类：萜类  |  三萜

来源：植物  |  卫矛科  |  雷公藤

In Vitro: Pristimerin inhibits the activity of purified MGL with an IC₅₀ of 93±8 nM and that of non-purified MGL (cell lysates of MGL-transfected HeLa cells) with an IC₅₀ of 398±68 nM. Pristimerin inhibits MGL through a mechanism that is rapid, reversible and non-competitive. The binding of pristimerin to MGL might be strengthened by formation of a polar interaction with a regulatory cysteine, possibly Cys²⁰⁸. Pristimerin inhibits HFLS-RA and HUVEC cell viability in a dose- and time-dependent manner. Pristimerin decreases VEGF-induced autophosphorylation of VEGFR2 and attenuates the activation of the VEGF-induced VEGFR2-mediated signaling pathway .

In Vivo: Pristimerin inhibits inflammation and tumor angiogenesis. Pristimerin significantly reduces vessel density in synovial membrane tissues of inflamed joints and reduces the expression of pro-angiogenic factors in sera, including TNF-α, Ang-1, and MMP-9.

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