Atglistatin targets the triacylglycerol (TG) hydrolase activity of adipose triglyceride lipase (ATGL) in white adipose tissue (WAT), inhibiting it in a dose-dependent manner and achieving up to a 78% reduction at the highest tested concentration. In WAT lysates from ATGL knockout (ko) animals, where TG hydrolase activity is already diminished by about 70%, Atglistatin exerts a moderate effect on the remaining activity. This suggests that the majority of the non-ATGL related TG hydrolase activity can be attributed to hormone-sensitive lipase (HSL), especially since the combined inhibition with Atglistatin and an HSL inhibitor nearly abolishes TG hydrolase activity in WAT (-95%)[1].
Atglistatin 动物研究
Animal study
Administered orally in olive oil, Atglistatin influences plasma and tissue TG levels, among other metabolic parameters, in animals. Lipolytic indicators such as fatty acids (FA) and glycerol show reductions 4 and 8 hours post-administration, with levels returning to baseline after 12 hours. A dose-dependent decrease in FA and glycerol, up to 50% and 62% respectively, is observed 8 hours following treatment. Additionally, Atglistatin significantly lowers plasma TG levels by 43% without affecting blood glucose, total cholesterol, ketone bodies, and insulin levels. These effects are also seen when Atglistatin is administered via intraperitoneal injection, highlighting its potential as an anti-lipolytic agent[1].
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