Synthesis and anti-oxidation activity of schisandrone derivatives / 药学实践杂志

Objective To design and synthesize schisandrone derivatives for the therapy of disease like AD,and to meas-ure their anti-oxidation activity.Methods Ten compounds were synthesized,and seven of them were first reported.The influ-ence all the compounds on SOD from the mouse serum were measured to evaluate anti-oxidation activity.Structure-activity rela-tionship(SARs)were also discussed.Results Compounds 2,3,5 and 8 could increase the activity of SOD in mouse serum.Fur-thermore,Compounds 2,3 and 5 showed better activities than schisandrone.Conclusion Synthesized schisandrone derivatives showed anti-oxidation activity.The SARs demonstrated the carbonyl of C-1 position and the methyls of C-2 and 3 had no influ-ences to the anti-oxidant activity.

Schisandrone improves learning and memory abilities of Alzheimer-like rats and influences expression of NF-κB, iNOS in rat hippocampus / 第二军医大学学报

Objective: To investigate the influence of Schisandrone on the learning and memory abilities of rats with Alzheimer-like disease and on the expression of NF-κB, iNOS in rat hippocampus, so as to study the prevention effect of Schisandrone on Alzheimer disease (AD). Methods: Totally 30 male SD rats were evenly randomized into 3 groups: blank control group, AD model group and Schisandrone intervention group. The AD animal model was established by stereotactic injection of Aβ25-35 into lateral cerebral ventricle of rats; the rats in Schisandrone intervention group were administrated with Schisandrone. The learning and memory abilities of animals were determined by Morris water maze; the expression of NF-κB, iNOS in the hippocampus was detected by immunohistochemistry. Results: The learning and memory abilities of rats in the Schisandrone intervention group were significantly improved compared with those in the AD model group (P<0.05). The expression of NF-κB and iNOS in the hippocampus was significantly decreased in the Schisandrone group than in the AD model group(P<0.05). The expression of NF-κB and iNOS in the hippocampus was positively correlated with each other. The correlation coefficients for the blank control,AD model and Schisandrone intervention groups were 0.639,0.656 and 0.682, respectively(all P<0.05). Conclusion: Schisandrone can suppress the Aβ-induced oxidative stress and inflammatory reaction through influencing NF-κB signaling pathway, exerting its protective effect on AD.

Influence of schisandrone on levels of IL-1? and iNOS mRNA in hippocampus of rats with Alzheimer-like disease / 第二军医大学学报

Objective:To observe the influence of schisandrone on the levels of IL-1? and iNOS mRNA in the hippocampus of rats with Alzheimer-like disease(AD) and to investigate the probable prevention and therapy effect of schisandrone on AD. Methods: Totally 30 male SD rats, 8-12 weeks old, weighing 250-300 g, were randomly divided into 3 groups: blank control group,AD model group and schisandrone intervention group(n=10). The animal model of AD was established by 10 mmol/L amyloid-beta protein(A? 25-35 ) 5 ?l stereotactic injection into lateral cerebral ventricle of rats and the rats of schisandrone intervention group were administrated with corn oil with 1 mmol/L schisandrone. And then the levels of IL-1? and iNOS mRNA in the hippocampus were detected by RT-PCR. Results: The levels of IL-1? and iNOS mRNA in the hippocampus of rats with Alzheimer-like disease (0.333 7?0.122 3, 0.266 6?0.088 5) decreased obviously after administration of schisandrone (0.969 3?0.153 9, 0.666 0?0.121 1)(P