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.

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. The most selective and potent inhibitor of CEase (3e) had IC50 value of 0.72 nM and 11800-fold selectivity for CEase over AChE. The structure-activity relationships revealed that the free hydroxyl group at position 5 and phosphate group at position 7 of the phosphorylated flavonoids are favorable to the inhibition of CEase. The inhibition mechanism and kinetic characterization studies indicated that they are irreversible competitive inhibitors of CEase.

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. Little was known about the precise pathologic mechanisms of bFGF on scarring formation. AIMS: The aim of this study was to investigate the effect of bFGF on hypertrophic scarring in a rabbit ear model and clarify the mechanism of bFGF on scar treatment. METHODS: The rabbit model of hypertrophic scarring was created and received of a low- or high-dose topical treatment three times daily for 1, 2, or 3 months. Then we examined the changes in the macroscopic and histopathologic characteristics of the scars. The expression of collagen, alpha(1)beta(2) integrin, and matrix metalloproteinase 1 (MMP-1) was studied by applying reverse transcriptase-polymerase chain reaction, enzyme-linked immunosorbent assay, and Western blotting. RESULT: High-dose bFGF remarkably alleviated the scar in the rabbit ear model and decreased collagen type I expression. Further study revealed that bFGF remarkably enhanced MMP-1 and decreased alpha(1)beta(2) integrin expression. CONCLUSION: This study supports the hypothesis that bFGF exerted a net negative effect on collagen remodeling, therefore suggesting a potential antiscarring role.

[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. Moreover, some strategies on protection forest construction and stand quality optimization were put forward.