pristimerin

Описание

Monoacylglycerol lipase (MAGL) hydrolyzes the endogenous cannabinoid 2-arachidonoyl glycerol (2-AG), terminating its capacity to activate cannabinoid receptors. Pristimerin is a naturally occurring terpenoid that potently inhibits MAGL (IC₅₀ = 93 nM). Its actions are rapid, reversible, and noncompetitive. Pristimerin (1 μM) significantly increases 2-AG levels in isolated rat neurons, indicating that it inhibits endogenous MAGL in cultured cells. Moreover, it does not increase levels of palmitoyl ethanolamide, suggesting that pristimerin does not affect the activity of fatty acid amide hydrolase (FAAH).

Использование

Pristimerin is a triterpenoid that inhibits tumor angiogenesis by targeting VEGFR2 activation and is known to exhibit anti-inflammatory properties.

Общее описание

A cell-permeable plant dienone-phenolic triterpenoid, naturally isolated from tripterygium wilfordii, whose inhibitory activities against proteasome chymotrypsin subunit (IC₅₀ = 2.2 and 3.0 μM against purified rabbit 20S and human 26S proteasome, respectively) and cellular NF-κB pathway/IKK activation most likely account for its reported anticancer efficacy both in vitro (IC₅₀ ≤610 nM in A549, K562, KBM5, MCF-7, MDA-MB-231, HepG2, and primary human leukemia cell cultures) and in mice in vivo (1 to 2.5 mg/kg/day, s.c.), including imatinib/STI571-resistant cancer cells harboring Bcr-Abl T315I mutation. Also reported to inhibit the activity of monoacylglycerol lipase (MGL), the enzyme that hydrolyzes and deactivates the cannabionoid receptor ligand 2-Arachidonoyl-sn-glycerol (2-AG), in a reversible manner with high potency (IC₅₀ = 93 nM).

Биологическая активность

Potent and reversible inhibitor of monoacylglycerol lipase (MGL) (IC 50 = 93 nM). Also suppresses NF- κ B activation via inhibition of proteasome chymotrypsin-like activity and IKK α / β . Displays antitumor, anti-inflammatory and antimicrobial activities.