An antagonistic communication exists between adenosinergic and dopaminergic signaling in the basal ganglia,which suggests that the suppression of adenosine A2A receptors-cyclic adenosine monophosphate pathway may be a...An antagonistic communication exists between adenosinergic and dopaminergic signaling in the basal ganglia,which suggests that the suppression of adenosine A2A receptors-cyclic adenosine monophosphate pathway may be able to restore the disrupted dopamine transmission that results in motor symptoms in Parkinson’s disease(PD).Arbutin is a natural glycoside that possesses antioxidant,antiinflammatory,and neuroprotective properties.The purpose of this study was to investigate whether arbutin could ameliorate the symptoms of PD and to examine the underlying mechanism.In this study,Swiss albino mouse models of PD were established by the intraperitoneal injection of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine for 4 successive days,with the concurrent intraperitoneal administration of arbutin(50 and 100 mg/kg)for 7 days.The results showed that arbutin significantly reduced lipid peroxidation,total nitrite levels,and inflammation in the substantia nigra and striatum of PD mouse models.In addition,arbutin decreased the activity of endogenous antioxidants,reduced the levels of dopamine,3,4-dihydroxyphenylacetic acid,homovanillic acid,andγ-aminobutyric acid,and minimized neurodegeneration in the striatum.Arbutin also reduced the abnormal performance of PD mouse models in the open field test,bar test,pole test,and rotarod test.The therapeutic efficacy of arbutin was similar to that of madopar.The intraperitoneal injection of the A2AR agonist CGS21680(0.5 mg/kg)attenuated the therapeutic effects of arbutin,whereas the intraperitoneal injection of forskolin(3 mg/kg)enhanced arbutin-mediated improvements.These findings suggest that arbutin can improve the performance of PD mouse models by inhibiting the function of the A2AR and enhancing the effects of cyclic adenosine monophosphate.This study was approved by the Institutional Animal Ethics Committee(1616/PO/Re/S/12/CPCSEA)on November 17,2019(approval No.IAEC/2019/010).展开更多
Arbutin was synthesized from glucose by two-step reaction below: (a) 2,3,4,6-tetra-O-acetyl-a-D-glucosyl chloride or bromide was prepared by glucose and acetyl halide (chloride or bromide). (b) 2,3,4,6-tetra-O-acetyl-...Arbutin was synthesized from glucose by two-step reaction below: (a) 2,3,4,6-tetra-O-acetyl-a-D-glucosyl chloride or bromide was prepared by glucose and acetyl halide (chloride or bromide). (b) 2,3,4,6-tetra-O-acetyl-a-D-glucosyl halide (Cl, Br) reacted with hydroquinone, methanol as solvent at pH=9.5～10.0.展开更多
The relative molecular mass of Arbutin is small. Both fluorolabeling and radiolabeling may affect its properties and functions. Therefore, the immunoassay of Arbutin was studied. Arbutin was coupled to bovine serum al...The relative molecular mass of Arbutin is small. Both fluorolabeling and radiolabeling may affect its properties and functions. Therefore, the immunoassay of Arbutin was studied. Arbutin was coupled to bovine serum albumin to get the Arbutin\|BSA conjugate with high molar ratio of Arbutin to BSA. Two rabbits were injected with the conjugate to develop the anti\|Arbutin serum. Ammonium sulfate precipitation and affinity chromatography were used to purify the antibody. Double agar diffusion test and enzyme\|linked immunosorbent assay (ELISA) were adopted to identify the antibody titer. The results demonstrated that the purity and activity of the antibody are high. The method proposed is satisfactory for the immunological detection of Arbutin.展开更多
Heliciopsis lobata is a medicinal plant, which is exclusively used to treat tumor in Li folk region. Two new arbutin derivatives, 6'-((E)2-methoxy-5-hydroxycinnamoyl) arbutin(1) and 2'-((E)2, 5-dihydroxycinnam...Heliciopsis lobata is a medicinal plant, which is exclusively used to treat tumor in Li folk region. Two new arbutin derivatives, 6'-((E)2-methoxy-5-hydroxycinnamoyl) arbutin(1) and 2'-((E)2, 5-dihydroxycinnamoyl) arbutin(2) along with five known compounds(3–7), were isolated from the leaves of Heliciopsis lobata. Their structures were elucidated on the basis of extensive spectroscopic interpretations. They were evaluated for their potential anticancer activity. Compounds 6 and 7 exhibited cytotoxicity against MGC-803 cells with IC_(50) values being 44.1 and 11.3 μg·m L^(–1), respectively. Additionally, compounds 1, 2 and 5–7 exhibited a moderate inhibition of MGC-803 cells invasion; compound 2 at 20 μg·m L^(–1) inhibited the invasion of MGC-803 cells by 43.0%, compared with the controls..展开更多
文摘An antagonistic communication exists between adenosinergic and dopaminergic signaling in the basal ganglia,which suggests that the suppression of adenosine A2A receptors-cyclic adenosine monophosphate pathway may be able to restore the disrupted dopamine transmission that results in motor symptoms in Parkinson’s disease(PD).Arbutin is a natural glycoside that possesses antioxidant,antiinflammatory,and neuroprotective properties.The purpose of this study was to investigate whether arbutin could ameliorate the symptoms of PD and to examine the underlying mechanism.In this study,Swiss albino mouse models of PD were established by the intraperitoneal injection of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine for 4 successive days,with the concurrent intraperitoneal administration of arbutin(50 and 100 mg/kg)for 7 days.The results showed that arbutin significantly reduced lipid peroxidation,total nitrite levels,and inflammation in the substantia nigra and striatum of PD mouse models.In addition,arbutin decreased the activity of endogenous antioxidants,reduced the levels of dopamine,3,4-dihydroxyphenylacetic acid,homovanillic acid,andγ-aminobutyric acid,and minimized neurodegeneration in the striatum.Arbutin also reduced the abnormal performance of PD mouse models in the open field test,bar test,pole test,and rotarod test.The therapeutic efficacy of arbutin was similar to that of madopar.The intraperitoneal injection of the A2AR agonist CGS21680(0.5 mg/kg)attenuated the therapeutic effects of arbutin,whereas the intraperitoneal injection of forskolin(3 mg/kg)enhanced arbutin-mediated improvements.These findings suggest that arbutin can improve the performance of PD mouse models by inhibiting the function of the A2AR and enhancing the effects of cyclic adenosine monophosphate.This study was approved by the Institutional Animal Ethics Committee(1616/PO/Re/S/12/CPCSEA)on November 17,2019(approval No.IAEC/2019/010).
文摘Arbutin was synthesized from glucose by two-step reaction below: (a) 2,3,4,6-tetra-O-acetyl-a-D-glucosyl chloride or bromide was prepared by glucose and acetyl halide (chloride or bromide). (b) 2,3,4,6-tetra-O-acetyl-a-D-glucosyl halide (Cl, Br) reacted with hydroquinone, methanol as solvent at pH=9.5～10.0.
文摘The relative molecular mass of Arbutin is small. Both fluorolabeling and radiolabeling may affect its properties and functions. Therefore, the immunoassay of Arbutin was studied. Arbutin was coupled to bovine serum albumin to get the Arbutin\|BSA conjugate with high molar ratio of Arbutin to BSA. Two rabbits were injected with the conjugate to develop the anti\|Arbutin serum. Ammonium sulfate precipitation and affinity chromatography were used to purify the antibody. Double agar diffusion test and enzyme\|linked immunosorbent assay (ELISA) were adopted to identify the antibody titer. The results demonstrated that the purity and activity of the antibody are high. The method proposed is satisfactory for the immunological detection of Arbutin.
基金supported by Hainan Province modernization of Chinese medicine program,China(No.24201326)the Priority Academic Program Development of Jiangsu Higher Education Institutions
文摘Heliciopsis lobata is a medicinal plant, which is exclusively used to treat tumor in Li folk region. Two new arbutin derivatives, 6'-((E)2-methoxy-5-hydroxycinnamoyl) arbutin(1) and 2'-((E)2, 5-dihydroxycinnamoyl) arbutin(2) along with five known compounds(3–7), were isolated from the leaves of Heliciopsis lobata. Their structures were elucidated on the basis of extensive spectroscopic interpretations. They were evaluated for their potential anticancer activity. Compounds 6 and 7 exhibited cytotoxicity against MGC-803 cells with IC_(50) values being 44.1 and 11.3 μg·m L^(–1), respectively. Additionally, compounds 1, 2 and 5–7 exhibited a moderate inhibition of MGC-803 cells invasion; compound 2 at 20 μg·m L^(–1) inhibited the invasion of MGC-803 cells by 43.0%, compared with the controls..
