We have extracted and purified flavonoids as active ingredients from Ceylon green tea (Dilmah). In this project, an in vitro hypoxic model using human brain epithelial cells (HBEC) was studied with treatment of th...We have extracted and purified flavonoids as active ingredients from Ceylon green tea (Dilmah). In this project, an in vitro hypoxic model using human brain epithelial cells (HBEC) was studied with treatment of the tea extract before inducing hypoxia. We have tested the hypothesis that flavonoids extracted from Ceylon green tea act as potential therapeutic ingredient (s) to reduce oxidative stress in hypoxic cells through its antioxidant properties and its ability to reduce cerebral cellular death. The biochemical antioxidant tests show that the Ceylon green tea has 68% ± 2.8% inhibition property of scavenging of ABTS. The inhibition of pyrogallol red bleaching by HOCI from Ceylon tea was 79% ± 4.5%. After exposing to hypoxia, the cell viability was 29% ± 2.3% in the hypoxia control group but 41% ± 4.7% for flavonoids extract treated group. In LDH assay, flavonoids extract treated group had 75% ± 3.7% reducing of LDH release. The flavonoids extract treated groups significantly increased in antioxidant enzyme activity assays: the activity level of SOD [(1.5 ± 0.6) μmol/min/mg protein], CAT [(0.61 ± 0.06) μmol/min/mg protein], GPx [(2.6 ± 0.41) μmol/min/mg protein] and GST [(6.0 ± 2.4) μmol/min/mg protein] are significantly increased as compared with hypoxic control [(0.5 ± 0.52, 0.51 ± 0.04, 1.2 ± 0.35 and 3.1 ± 1.6) μmol/min/mg protein, respectively]. The study demonstrated a great clinical potential and opened a new avenue to prevent stroke by drinking Ceylon tea.展开更多
[Objectives]To study the effect of total flavonoids extracted from Polygonum perfoliatum L.(TFP)on immune-mediated liver injury induced by bacillus Calmette-Guerin plus lipopolysaccharide(BCG+LPS)in mice,and to explor...[Objectives]To study the effect of total flavonoids extracted from Polygonum perfoliatum L.(TFP)on immune-mediated liver injury induced by bacillus Calmette-Guerin plus lipopolysaccharide(BCG+LPS)in mice,and to explore its action mechanism.[Methods]60 Kunming mice were divided into normal group,model group,control group(bifendate)and TFP low,medium and high dose groups according to random number table method,with 10 mice in each group.On the first day of modeling,mice were injected with 0.2 mL of BCG solution(12.5 mg/mL)through the tail vein,and on the eleventh day,0.2 mL of LPS(37.5μg/mL)were injected into the tail vein to prepare a mouse model of immune-mediated liver injury;from the first day of modeling,the normal group and the model group were administered intragastrically with the corresponding volume of distilled water,and the bifendate group and the TFP high,medium,and low dose groups were administered intragastrically with the corresponding doses once a day for 11 d.After the last time administration,fasting but giving water for 16 h,took blood from eyes,then collected the liver tissue.The levels of alanine transaminase(ALT)and aspartate transaminase(AST)in serum were detected by biochemical method;transforming growth factor-β1(TGF-β1),intercellular adhesion molecule-1(ICAM-1),interleukin-6(IL-6)and interleukin-1β(IL-1β)expression levels in liver tissue were detected by enzyme-linked immunosorbent assay(ELISA);phosphorylated protein tyrosine kinase JAK-2(p-JAK2),phosphorylated signal transducer and activator of transcription 3(p-STAT3)protein expression levels were detected by Western Blot method;the degree of liver tissue lesions was detected by HE staining.[Results]Compared with the model group,the levels of ALT and AST in the serum of mice in each dose group of TFP(high dose 600 mg/kg,medium dose 400 mg/kg,and low dose 200 mg/kg)were reduced,and the activities of T-SOD and GSH-Px were increased;the content or expression ofβ1,ICAM-1,IL-6,IL-1βdecreased,and the expression of p-JAK2 and p-STAT3 protein decreased;pathological sections showed that the degree of inflammatory necrosis and the degree of lesions in the liver tissues of each dose group of TFP were reduced by varying degrees.[Conclusions]TFP has a protective effect on BCG+LPS-induced immune-mediated liver injury in mice.The mechanism may be related to regulating the phosphorylation level of JAK2 and inhibiting the inflammatory reaction,thereby regulating the TGF-β1/STAT3 signaling pathway and improving the immune-mediated liver injury.展开更多
Parkinson’s disease(PD) is a common degenerative disease of the central nervous system, and the pathologic features are mainly degeneration of substantianigra and dopamine neurons. Studies have shown that safflower f...Parkinson’s disease(PD) is a common degenerative disease of the central nervous system, and the pathologic features are mainly degeneration of substantianigra and dopamine neurons. Studies have shown that safflower flavonoid extract(SAFE) exhibits the neuroprotective effect. In this study, the safflower flavonoid extract drop pills(SAFE-DPs) for anti-PD were prepared by the heating and melting method using SAFE and matrix PEG6000. The performances of the pills were evaluated with powder X-ray diffraction(PXRD), differential scanning calorimetry(DSC), Fourier transform infrared spectroscopy(FT-IR), scanning electron microscopy(SEM) and dissolution testing. The analysis results demonstrated an amorphous state for SAFE dispersion in the matrix PEG6000 without any chemical reaction. The SAFE-DPs demonstrated acceptable chemical and physical stability irrespective of the manufacturing process and the storage period. Dissolution testing in three dissolution media(pH 1.0, pH 6.8 and pH 7.5) indicated that SAFE-DPs had excellent dissolution property. The transport of Kaempferol-3-rutinoside(K3 R) on the Caco-2 monolayer and the absorption of K3 R in situ intestinal perfusion revealed that the principal component of SAFE had a good transport and absorption capacity. Therefore, the drop pills had better release and absorption in the gastrointestinal tract, corresponding with the pharmacological and pharmacodynamic results for PD in vivo.展开更多
文摘We have extracted and purified flavonoids as active ingredients from Ceylon green tea (Dilmah). In this project, an in vitro hypoxic model using human brain epithelial cells (HBEC) was studied with treatment of the tea extract before inducing hypoxia. We have tested the hypothesis that flavonoids extracted from Ceylon green tea act as potential therapeutic ingredient (s) to reduce oxidative stress in hypoxic cells through its antioxidant properties and its ability to reduce cerebral cellular death. The biochemical antioxidant tests show that the Ceylon green tea has 68% ± 2.8% inhibition property of scavenging of ABTS. The inhibition of pyrogallol red bleaching by HOCI from Ceylon tea was 79% ± 4.5%. After exposing to hypoxia, the cell viability was 29% ± 2.3% in the hypoxia control group but 41% ± 4.7% for flavonoids extract treated group. In LDH assay, flavonoids extract treated group had 75% ± 3.7% reducing of LDH release. The flavonoids extract treated groups significantly increased in antioxidant enzyme activity assays: the activity level of SOD [(1.5 ± 0.6) μmol/min/mg protein], CAT [(0.61 ± 0.06) μmol/min/mg protein], GPx [(2.6 ± 0.41) μmol/min/mg protein] and GST [(6.0 ± 2.4) μmol/min/mg protein] are significantly increased as compared with hypoxic control [(0.5 ± 0.52, 0.51 ± 0.04, 1.2 ± 0.35 and 3.1 ± 1.6) μmol/min/mg protein, respectively]. The study demonstrated a great clinical potential and opened a new avenue to prevent stroke by drinking Ceylon tea.
基金Natural Science Foundation Project of Guangxi(2017GXNSFAA 198326)。
文摘[Objectives]To study the effect of total flavonoids extracted from Polygonum perfoliatum L.(TFP)on immune-mediated liver injury induced by bacillus Calmette-Guerin plus lipopolysaccharide(BCG+LPS)in mice,and to explore its action mechanism.[Methods]60 Kunming mice were divided into normal group,model group,control group(bifendate)and TFP low,medium and high dose groups according to random number table method,with 10 mice in each group.On the first day of modeling,mice were injected with 0.2 mL of BCG solution(12.5 mg/mL)through the tail vein,and on the eleventh day,0.2 mL of LPS(37.5μg/mL)were injected into the tail vein to prepare a mouse model of immune-mediated liver injury;from the first day of modeling,the normal group and the model group were administered intragastrically with the corresponding volume of distilled water,and the bifendate group and the TFP high,medium,and low dose groups were administered intragastrically with the corresponding doses once a day for 11 d.After the last time administration,fasting but giving water for 16 h,took blood from eyes,then collected the liver tissue.The levels of alanine transaminase(ALT)and aspartate transaminase(AST)in serum were detected by biochemical method;transforming growth factor-β1(TGF-β1),intercellular adhesion molecule-1(ICAM-1),interleukin-6(IL-6)and interleukin-1β(IL-1β)expression levels in liver tissue were detected by enzyme-linked immunosorbent assay(ELISA);phosphorylated protein tyrosine kinase JAK-2(p-JAK2),phosphorylated signal transducer and activator of transcription 3(p-STAT3)protein expression levels were detected by Western Blot method;the degree of liver tissue lesions was detected by HE staining.[Results]Compared with the model group,the levels of ALT and AST in the serum of mice in each dose group of TFP(high dose 600 mg/kg,medium dose 400 mg/kg,and low dose 200 mg/kg)were reduced,and the activities of T-SOD and GSH-Px were increased;the content or expression ofβ1,ICAM-1,IL-6,IL-1βdecreased,and the expression of p-JAK2 and p-STAT3 protein decreased;pathological sections showed that the degree of inflammatory necrosis and the degree of lesions in the liver tissues of each dose group of TFP were reduced by varying degrees.[Conclusions]TFP has a protective effect on BCG+LPS-induced immune-mediated liver injury in mice.The mechanism may be related to regulating the phosphorylation level of JAK2 and inhibiting the inflammatory reaction,thereby regulating the TGF-β1/STAT3 signaling pathway and improving the immune-mediated liver injury.
基金Science and Technology Major Projects:Significant New-Drugs Creation(Grant No.2012ZX09103201-042)
文摘Parkinson’s disease(PD) is a common degenerative disease of the central nervous system, and the pathologic features are mainly degeneration of substantianigra and dopamine neurons. Studies have shown that safflower flavonoid extract(SAFE) exhibits the neuroprotective effect. In this study, the safflower flavonoid extract drop pills(SAFE-DPs) for anti-PD were prepared by the heating and melting method using SAFE and matrix PEG6000. The performances of the pills were evaluated with powder X-ray diffraction(PXRD), differential scanning calorimetry(DSC), Fourier transform infrared spectroscopy(FT-IR), scanning electron microscopy(SEM) and dissolution testing. The analysis results demonstrated an amorphous state for SAFE dispersion in the matrix PEG6000 without any chemical reaction. The SAFE-DPs demonstrated acceptable chemical and physical stability irrespective of the manufacturing process and the storage period. Dissolution testing in three dissolution media(pH 1.0, pH 6.8 and pH 7.5) indicated that SAFE-DPs had excellent dissolution property. The transport of Kaempferol-3-rutinoside(K3 R) on the Caco-2 monolayer and the absorption of K3 R in situ intestinal perfusion revealed that the principal component of SAFE had a good transport and absorption capacity. Therefore, the drop pills had better release and absorption in the gastrointestinal tract, corresponding with the pharmacological and pharmacodynamic results for PD in vivo.