Abstract
Pharmacological experiments confirmed that Puerarin could not only expand the arterial vessels, increase the local blood flow, but also could protect the myocardium, improve the blood supply of ischemic tissue, which was used to treat the cerebrovascular dementia disease in clinical practice. Its own structure particularity caused the lower bioavailability and poorer solubility. In order to improve the deficiency, the related pharmacological experiments of the newly synthesized puerarin derivative (P), so as to expect the better curative effect than puerarin in the process of treating vascular dementia. The vascular dementia model was established by permanently ligating the common carotid artery in mice. The effects of puerarin derivative (P) on learning and memory in mice by water maze, Y maze and new object discrimination methods; The myeloperoxidase activity in the ischemic cerebral cortex was evaluated in mice by biochemical method. The experimental results showed that the mice spontaneous alternation response accuracy in Y maze could be obviously improved in 100mg/kg puerarin derivative group; In water maze, the swimming time to the safe platform would be significantly decreased in puerarin derivative group. Meanwhile, the MPO activity in the cerebral cortex of dementia mice was significantly decreased in 100mg/kg puerarin derivative group by permanently ligating the unilateral common carotid artery.
Highlights
The white blood cells do not exist in the brain tissue
The Puerarin structure was modified aiming to its defects in the paper and the novel puerarin derivative P was designed and synthesized.Its lipophilicity was increased.The effects of the new compound on learning memory functions and MPO activity were investigated preliminarily in vascular dementia mice, so as to improve the permeability of blood brain barrier, enhance its pharmacological activity, which could provide the reference for further developing and utilizingpuerarin and its derivatives in the treatment of vascular dementia
After stirring for 90min, ethyl bromoacetate (35.8g, 216mmol) was added and the mixture was stirred at room temperature for an additional 4h.The mixture was filtered to remove insoluble solids and solvents were removed using a rotovapor until the mixturewas in anoily state; the oily solute was solubilized with anhydrous ether.After again rotovappingtheether solution,the remains werespin-dried dissolved in anhydrous methanol and isolated by silica gel column chromatography
Summary
MS spectra were obtained with an Agilent G6300 Series (HPLC-MS) LC-MS analyzer. 1H NMR spectra were obtainedwith aBruker DMX600MHz / 300MHz. MS spectra were obtained with an Agilent G6300 Series (HPLC-MS) LC-MS analyzer. 1H NMR spectra were obtainedwith aBruker DMX600MHz / 300MHz. NMR spectrometer(DMSO-d6 as solvent-, tetramethylsilaneas internal standard-). Puerarin pharmaceutical raw materials (≥98%) were purchased from Xi'an Frierson Biotechnology Co., Ltd.All reagents and solvents were of analytical grade. The silica gel used for column chromatography (reagent grade, 200 to 300 mesh)was purchased from Qingdao HaiyangChemical Co., Ltd
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