Neuroprotective activity of two active chemical constituents from Tinospora hainanensis

Objective:To determine the chemical structure of the new compound and investigate the protective effects of Tinosporaic acid A and B towards in-vitro neuro.Methods:The structures of two new compounds were established by analyzing its 1D and 2D NMR spectra as well as HRESIMS.Their neuroprotective effects with respect to the antioxidant properties were evaluated by radical scavenging tests and hydrogen peroxide-injured oxidative stress model in PC12 cell lines.Cell morphology of treated PC12 cells was observed by phase contrast microscopy.In-vitro MTT assay,lactate dehydrogenase activity assay and oxidative stress markers(intracellular ROS production,MDA level,and caspase-3 activity) were used to evaluate the protective effects against hydrogen peroxide induced cytotoxicity in PC12 cells.Results:The two new compounds,named Tinosporaic acid A and B,were isolated and identified from the stem bark of Tinospora hainanensis.Cell viability studies identified a representative concentration for each extract that was subsequently used to measure oxidative stress markers.Both extracts were able to reverse the oxidative damage caused by hydrogen peroxide,thus promoting PC12 cells survival.The concentration of Tinosporaic acid A and B were 86.34 μg/mL and 22.06 μg/mL respectively,which is neuroprotective for EC_(50).The results indicated that both of them significantly attenuated hydrogen peroxide-induced neurotoxicity.Conclusion:The two new compounds isolated from ethanol extracts of Tinospora hainanensis are the promising natural ones with neuroprotective activity and needed for further research.

Effect of Tetrahydroberberine on improving vascular endothelial cell injury

Objective:To investigate the effects and mechanisms of tetrahydroberberine(THB)on vascular endothelial cell injury induced by oxygen glucose deprivation(OGD)and LPS-induced cell injury model.Methods:MTT assay was used to detect the effects of THB final concentration on the survival rate of EA.hy926 cells,which were 0μg/mL,2.5μg/mL,5μg/mL,10μg/mL,20μg/mL and 40μg/mL,respectively.Group I of the experiment:normal control group,OGD group,OGD+THB-10μg/mL group,OGD+THB-20μg/mL group,OGD+THB-40μg/mL group;Experimental group II group:normal Control group,LPS group,OGD+LPS group and OGD+LPS+THB-20μg/mL group.The relative expression of inflammation-related factors such as Caspase-1,ASC,IL-1βand IL-6 was detected by fluorescence quantitative PCR,and the expression of IL-1βand HO-1 was detected by Western Blot analysis.Results:The results of MTT assay showed that THB had no effect on the survival of EA.hy926 cells.The qPCR results of the experimental group I and II showed that the OGD model could play an anti-inflammatory protective role by down-regulating the expression of Caspase-1,ASC,IL-1βand IL-6 genes.The anti-inflammatory effect of THB on the OGD model was general,but it was found that THB also exerted an anti-inflammatory effect by down-regulating the expression of inflammatory genes by OGD+LPS group compared with OGD+LPS+THB-20μg/mL group.Western Blot analysis showed that the expression of IL-1βprotein was consistent with the results of qPCR.The expression of HO-1 protein as a protective factor was contrary to that of inflammatory factor fluorescence quantitative analysis.Conclusion:OGD model can improve the protective effect of cell stress.THB plays an anti-inflammatory role by down-regulating the expression of Caspase-1,ASC,IL-1βand IL-6 genes,up-regulating the expression of HO-1 protein and inhibiting the activation of NLRP3 inflammatory bodies.

Evaluation of the quality of olanzapine orally disintegrated tablets by multiple dissolution curves

Objective: To investigate the dissolution behavior similarity between Self-made praeparatum and reference praeparatum in different pH menstruum,using the Olanzapine Orally Disintegrating Tablets listed in abroad as the reference praeparatum. Methods: The dissolution curve of olanzapine in Self-made praeparatum and reference praeparatum was measured,the similarity of the dissolution curve was evalued by F2 similar factor. Results: The single-point dissolution of both Self-made praeparatum and reference praeparatum within 15 min was more than 85%. Conclusion: Self-made praeparatum and reference praeparatum were similar in dissolution behavior.