Synthesis of chrysin derivatives and screening of antitumor activity.

A series of aromatic or long-chain chrysin derivatives (1-10) were synthesized by esterification of chrysin and acyl chloride. The chemical structures of these compounds were determined by mass spectrum (MS), 1H NMR, and 13C NMR spectra. Though aromatic chrysin derivatives (1-9) with a rigid structure were hard to dissolve in common organic solvents, the long-chain chrysin derivative (10) with a flexible structure had better solubility, and its anticancer activity (IC50 = 14.79 µmol/L) against liver cancer cell lines was 5.4 times better than chrysin (IC50 = 74.97 µmol/L), which showed superposition of pharmacological activity.

[Effect of ethanolic extract of Polygonum cuspidatum on acute gouty arthritis in mice through NLRP3/ASC/caspase-1 axis].

The aim of this paper was to study the effect and mechanism of alcohol extract from Polygonum cuspidatum(PCE) on acute gouty arthritis in C57 BL/6 mice through NLRP3/ASC/caspase-1 axis. The model mice which injected with ankle joint injection of sodium urate crystals(MSU) were orally administrated with three different concentration of PCE, with colchicine as positive control. HE staining was used for observing the morphological changes of synovial tissue; concentration of IL-1ß, IL-6 and TNF-α secreted by synovial tissue of the ankle joint were detected by ELISA; mRNA and protein expression of NLRP3, ASC and caspase-1 in synovial tissue were detected by RT-PCR and Western blot respectively. The results showed that the swelling degree of ankle joint in model mice were significantly elevated; expression of IL-1ß, IL-6 and TNF-α were significantly increased; mRNA and protein expression of NLRP3, ASC and caspase-1 also significant increase, compared with normal control group. The swelling degree of ankle joint significantly relief; expression of IL-1ß, IL-6 and TNF-α in joint synovium significantly decrease; mRNA and protein expression of NLRP3, ASC and caspase-1 were significantly decrease in PCE treatment group compared with model group. Our research implied that alcohol extract from P. cuspidatum had positive effect on acute gouty arthritis in mice, and the regulation of NLRP3/ASC/caspase-1 axis may be its mechanism.