Synthesis and biological evaluation of phosphorylated flavonoids as potent and selective inhibitors of cholesterol esterase.

A series of phosphorylated flavonoids were synthesized and investigated in vitro as inhibitors of pancreatic cholesterol esterase (CEase) and acetylcholinesterase (AChE). The results showed that most of the synthesized compounds exhibited nanomolar potency against CEase, much better than the parent flavonoids. Furthermore, these phosphorylated flavonoids demonstrated good to high selectivity for CEase over AChE, which only showed micromolar potency inhibition of AChE.

A new synthesis of fully phosphorylated flavones as potent pancreatic cholesterol esterase inhibitors.

Five flavones possessing one to four phenolic groups were fully phosphorylated efficiently and the obtained compounds showed excellent pancreatic cholesterol esterase (CEase) inhibitory activities with IC(50) in the nanomolar range, which were much more potent than their parent compounds. The inhibition mechanism and kinetic characterization studies indicate that they are irreversible competitive inhibitors.

Effect of asiaticoside on hypertrophic scar in the rabbit ear model.

Background: Previous observations suggested that asiaticoside had a possible antiscaring effect. However, the precise pathological mechanism still remain unknown. We questioned whether asiaticoside might alleviate the formation of hypertrophic scar by affecting the expression of Transform growth factor beta (TGF-beta)/Smad signaling.

Effects of basic fibroblast growth factors on hypertrophic scarring in a rabbit ear model.

Background: Basic fibroblast growth factor (bFGF) was clinically proven to accelerate acute and chronic wound healing. Accelerated wound healing may lead to improved scarring. These studies suggested a possible antiscarring effect of bFGF during wound healing.

[Synthetic evaluation on stand quality of protection forests in the Three Gorges Reservoir Region in western Hubei Province].

Stand qualities of 19 kinds of protection forests in the Three Gorges Reservoir Region in Western Hubei Province were evaluated synthetically by using 12 indexes, and could be classified into four different grades. The relationships between stand quality and some major factors such as crown density, elevation, and origin were also discussed in this paper. The results showed that elevation was a very important factor that influenced the stand quality, and the stand quality of natural forest was higher than other forests.