Syzygium aromaticum ethanol extract reduces AlCl_3-induced neurotoxicity in mice brain through regulation of amyloid precursor protein and oxidative stress gene expression

Objective: To investigate the neuroprotective effects of Syzygium aromaticum(S.aromaticum)extract(500 mg/kg) on AlCl_3(300 mg/kg)-induced mouse model of oxidative stress and neurotoxicity.Methods: An ethanolic extract of S.aromaticum seeds was prepared and the active compounds were identified using nuclear magnetic resonance spectroscopy.BALB/c mice were divided into five groups(negative control, AlCl_3-treated, self-recovery, AlCl_3 + S.aromaticum, S.aromaticum only; n=10) and treated with AlCl_3 and S.aromaticum extract.Expression of oxidative markers [Superoxide dismutase 1(SOD1) and peroxiredoxin 6(Prdx6)] and amyloid precursor protein(APP) in the hippocampus and cortex was evaluated via PCR.Histopathological assessment was performed to investigate the extent of neurodegeneration.Results: It was observed that AlCl_3 exposure increased the expression of APP770 while simultaneously down regulated the expression of APP695.AlCl_3 also induced a significant decrease(P<0.05) and an increase(P<0.05) in the expression level of SOD1 and Prdx6, respectively.A substantial decrease substantial(P<0.05) in the density of Nissl substance was also observed in cortex of the mice treated with AlCl_3.Interestingly, treatment with S.aromaticum extract normalized the alterations in the expression level of SOD1, Prdx6 and APPisoforms and improved the neuronal structural damage.Conclusions: The results showed that S.aromaticum is a promising antioxidant and a neuroprotective agent.

Morpholine hydrazone scaffold： Synthesis, anticancer activity and docking studies

In this paper, synthesis and anticancer activities of morpholine hydrazones scaffold（1-17） thoroughly studied. Small series of morpholine hydrazones synthesized by treating 5-morpholinothiophene-2-carbaldehyde with different aryl hydrazides to form morpholine hydrazones scaffold（1-17）. The in vitro anticancer potential of all these compounds was checked against human cancer cell lines like Hep G2（human hepatocellular liver carcinoma） and MCF-7（human breast adenocarcinoma）. Analogs 13 had similar substantial cytotoxic effects towards Hep G2 with IC_（50） value 6.31±1.03μmmol/L when compared with the standard Doxorubicin（IC_（50）value 6.00±0.80μmmol/L）; while compounds 5,8 and 9 showed potent cytotoxicity against MCF-7 with IC_（50） value 7.08±0.42μmmol/L, 1.26±0.34μmmol/L and11.22±0.22μmmol/L respectively when compared with the standard Tamoxifen（IC_（50）= 11.00±0.40μmol/L）. Molecular docking studies also performed to understand the binding interaction.