Scutellarein, the main metabolite of scutellarin in vivo, has relatively better solubility, bioavailability and bio-activity than scutellarin. However, compared with scutellarin, it is very difficult to obtain scutellarein from Nature. Therefore, the present study focused on establishing an efficient route for the synthesis of scutellarein by hydrolyzing scutellarin. Neurological deficit score and cerebral infarction volume with the administration of scutellarein were then used to compare its neuroprotective effects on focal cerebral ischemia/reperfusion in rats induced by middle cerebral artery occlusion (MCAO) with those of scutellarin. The results showed that scutellarein had better protective effect on focal cerebral ischemia/reperfusion than scutellarin, which laid the foundation for further research and development of scutellarein as a promising candidate for ischemic cerebro-vascular disease.
For more than thirty years, scutellarin (Scu) has been used in China to clinically treat acute cerebral infarction and paralysis. Scutellarein (Scue), the major Scu metabolite in vivo, exhibits heightened neuroprotective effects when compared to Scu. To explore the neuroprotective role of these compounds, we performed ultra-high-performance liquid chromatography-quadrupole/time-of-flight mass spectrometry (UHPLC-QTOF/MS) coupled with a pattern recognition approach to investigate metabolomic differences in a rat model of ischemia after treatment with each compound. We examined metabolites in urine, hippocampal tissue, and plasma, and we tentatively identified 23 endogenous metabolites whose levels differed significantly between sham-operated and model groups. Upon pathway analysis, we found an additional 11 metabolic pathways in urine, 14 metabolic pathways in the hippocampal tissue, and 3 metabolic pathways in plasma. These endogenous metabolites were mainly involved in sphingolipid metabolism, lysine biosynthesis, and alanine, aspartate, and glutamate metabolism. We found that metabolic changes after ischemic injury returned to near-normal levels after Scue intervention, unlike Scu treatment, further validating the heightened protective effects exerted by Scue compared to Scu. These results demonstrate that Scue is a potential drug for treatment of ischemic insult.
The crystal structure of 2,5-dimethyl-2,5-hexanediol tetrahydrate, C8H18O2 · 4H2O, has been determined at room temperature from diffractometer data with MoKα radiation. The structure is monoclinic, P21/c with two formula units in a cell of dimensions a=6.158(2), b=6.169(2), c=17.854(5) Å, β=101.8(2)°. The parameters were refined anisotropically by least squares to R=0.057 for 1015 reflections. The structure consists of layers of hydrogen bonded hydroxyl and water molecules alternating with layers of hydrocarbon chains. The water hydroxyl layers consist of puckered sheets of edge-sharing pentagons analogous to the water structure found in the pinacol and piperazine hexahydrates. The hydrocarbon chains of the glycol molecules are aligned parallel, analogous to the long-chain hydrocarbons and fatty acids, but spaced further apart. There are no hydrogen bonds between the puckered sheets of pentagons, and therefore the three-dimensional hydrogen bond framework which characterizes the hexahydrates as ``semiclathrates'' does not occur in this tetrahydrate.
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