Four new diphenyl ether derivatives from a mangrove endophytic fungus Epicoccum sorghinum / 中国天然药物

Four new diphenyl ethers, named epicoccethers K-N (1-4), were purified from the fermentation medium of a fungus Epicoccum sorghinum derived from Myoporum bontioides, and identified through HR-ESI-MS and NMR spectral analysis. Except that compound 1 showed moderate antifungal activity against Penicillium italicum and Fusarium graminearum, the other three compounds showed stronger activity against them than triadimefon. All of them showed moderate or weak antibacterial activity towards Staphylococcus aureus and Escherichia coli with O6 and O78 serotypes except that 3 was inactive to E. coli O6.

Intervention effects of Jiaotai pills on PCPA-induced insomnia in rats / 中国中药杂志

To elucidate the intervention effects of Jiaotai pills(JTP) on p-chlorophenylalanine (PCPA)-induced insomnia in rats and its underlying mechanism, the insomnia model was established by single intraperitoneal injection with PCPA in rats. The locomotor activity of rats was observed, and the levels of nerve growth factor(NGF) in hypothalamus, hippocampus, prefrontal cortex and serum of rats were determined by using ELISA. Moreover, a proton nuclear magnetic resonance(¹H-NMR)-based metabonomic approach was developed to profile insomnia-related metabolites in rat serum and hippocampus and analyze the intervention effects of JTP on changes in underlying biomarkers related to locomotor activity, NGF and insomnia. According to the results, JTP could significantly suppress the locomotor activity of insomnia rats, and increase the NGF levels in hypothalamus, hippocampus, prefrontal cortex and serum of rats with insomnia. The disturbed metabolic state associated with PCPA-induced insomnia in rat serum and hippocampus could be intervened by JTP. Meanwhile, six and five potential biomarkers related to insomnia in rat serum and hippocampus were reversed by administration of JTP. In conclusion, the current study demonstrated that JTP had protective effects against PCPA-induced insomnia in rats, which was probably correlated with regulation of NGF level and metabolism of amino acids, lipids and choline.

Modulation of proton-gated current by substance P in trigeminal ganglion neurons of rat / 中华神经医学杂志

Objective To investigate the modulatory effect of substance P (SP) on proton-gated current in the membrane of rat trgeminal ganglion (TG) neurons and its underlying mechanism. Methods Neurons were isolated mechanically and enzymatically from TG of rat. Whole-cell patch clamp technique was used for recording the proton-gated current in freshly isolated neurons. Results Proton-gated currents recorded from rat TG neurons could be classified into 4 distinct types: T-type, S-type, B-type and O-type in the present study. Co-application of SP and proton potentiated S-type proton-gated currents in a concentration-dependent manner, and the potentiation was not blocked by SP receptor antagonist, GR82334; co-application of SP and proton potentiated B-type proton-gated currents, and GR82334 and intracellular dialysis of GDP-β-S blocked the potentiation of SP. Pre-application of SP inhibited B-type proton-gated current, especially the transient component. The inhibition could not be reversed by pretreatment wit-h GR82334. Conclusions The mechanisms of modulation of proton-gated current by SP is associated with the difference of their makeup of subunits of acid-sensing ion channels (ASICs), and there may be an allosteric position of SP in the outside framework of ASICs in neuronal membrane.