AIM:To investigate the mechanism by which galangin,a polyphenolic compound derived from medicinal herbs,induces apoptosis of hepatocellular carcinoma(HCC) cells.METHODS:The 3-(4,5-Dimethyl-thiazol-2-yl)-2,5-diphenyl-t...AIM:To investigate the mechanism by which galangin,a polyphenolic compound derived from medicinal herbs,induces apoptosis of hepatocellular carcinoma(HCC) cells.METHODS:The 3-(4,5-Dimethyl-thiazol-2-yl)-2,5-diphenyl-tetrazolium bromide assay was used to measure cell viability.Apoptosis was evaluated by in situ uptake of propidium iodide and Hoechst 33258 and was then detected by fluorescence microscopy.Protein expressions were detected by Western blotting.To confirm the apoptotic pathway mediated by galangin,cells were transfected by bcl-2 gene to overexpress Bcl-2 or siRNA to down-regulate Bcl-2 expression.RESULTS:Galangin(46.25-370.0 μmol/L) exerted an anti-proliferative effect,induced apoptosis,and decreased mitochondrial membrane potential in a dose and time-dependent manner.Treatment with galangin induced apoptosis by translocating the pro-apoptotic protein Bax to the mitochondria,which released apoptosis-inducing factor and cytochrome c into the cytosol.Overexpression of Bcl-2 attenuated galangin-induced HepG2 cell apoptosis,while decreasing Bcl-2 expression enhanced galangin-induced cell apoptosis.CONCLUSION:Our data suggests that galangin mediates apoptosis through a mitochondrial pathway,and may be a potential chemotherapeutic drug for the treatment of HCC.展开更多
A high sensitive flow-injection chemiluminescence （FI-CL） method for the determination of tryptophan has been developed. The method is based on the chemiluminescence reaction of galangin-potassium permanganate-trypt...A high sensitive flow-injection chemiluminescence （FI-CL） method for the determination of tryptophan has been developed. The method is based on the chemiluminescence reaction of galangin-potassium permanganate-tryptophan in polyphosphoric acid （PPA） media. Under the optimized conditions, tryptophan was determined in the range 0.05-10 μg/mL with the detection limit （3tr） of 5.0 × 10^-3 μg/mL. The relative standard deviation （RSD） was 1.0% for 11 replicate determinations of 1.0 μg/mL tryptophan. Three synthetic samples were determined selectively with recoveries in the range from 99.6% to 102.0% in the presence of other amino acids.展开更多
OBJECTIVE Galangin,apotent scavenger of free radicals,is used as herbal medicine for various ailments for centuries in Asia.With complex pathophysiology,ischemic stroke is one of the most frequent causes of death and ...OBJECTIVE Galangin,apotent scavenger of free radicals,is used as herbal medicine for various ailments for centuries in Asia.With complex pathophysiology,ischemic stroke is one of the most frequent causes of death and disability worldwide.We have reported that galangin provides a direct protection against ischemic injury as a potential neuroprotective agent and has potential therapeutic effects on the changes of serum amino acids for ischemic stroke;however,its mechanism on changes of amino acids in the ischemic brain tissue has not yet been clarified.METHODS In this paper,we explored the amino acid biomarkers of brain tissue in the acute phase of cerebral ischemia and the effect of galangin on those potential biomarkers with a rapid,sensitive and accurate methodology of simultaneous quantification of 12 AAs in rat brain tissue by the RRLC/QQQ.RESULTS we identified that glutamic acid,alanine and aspartic acid all showed significant change in galangin-treated groups compared to vehicle-treated rats and four pathway-related enzymes were identified by multiplex interactions with the three amino acids.With metabolite-protein network analysis and molecule docking,six of 28 proteins were identified and may become the potential biomarkers of galangin for acute ischemic stroke.CONCLUSION All data in our study provide thought for exploring the mechanism of disease,discovering new targets for drug candidates and elucidating the related regulatory signal network.展开更多
Objective: To assess the protective effect of galangin on membrane bound enzymes in rats with streptozotocin-induced diabetes. Methods: A single low dose of streptozotocin was injected to adult male albino rats to ind...Objective: To assess the protective effect of galangin on membrane bound enzymes in rats with streptozotocin-induced diabetes. Methods: A single low dose of streptozotocin was injected to adult male albino rats to induce hyperglycemia. Galangin(8 mg/kg) or glibenclamide 600 μg/kg as a standard drug was given orally once daily for 45 days by gavage. Membrane-bound adenosine triphosphatases were determined including total ATPase, sodium-potassium-ATPase, calcium-ATPase and magnesium-ATPase in erythrocytes and tissues(kidney, liver, and heart). Results: The levels of total ATPases, sodium-potassium-ATPase, calcium-ATPase and magnesium-ATPase in erythrocytes and tissues were significantly altered in diabetic rats as compared to that in normal rats. After 45 days of treatment with galangin or glibenclamide, the levels of these enzymes were similar to that of normal control rats. Conclusions: Oral administration of galangin or glibenclamide can improve activities of these membrane-bound ATPases towards normal levels. Mechanism of galangin needs to be further explored in future.展开更多
Objective:To make Galangin-PLGA nanoparticles(GL-PLGA NPs)were prepared using the biodegradable material polylactic-coglycolic acid(PLGA)as the carrier material,and the formulation was optimized.Methods:Nanoparticles ...Objective:To make Galangin-PLGA nanoparticles(GL-PLGA NPs)were prepared using the biodegradable material polylactic-coglycolic acid(PLGA)as the carrier material,and the formulation was optimized.Methods:Nanoparticles were prepared by modified emulsification-solvent evaporation method and the content of galangin was determined by HPLC.With particle size and entrapment efficiency as the indexes,single factor and orthogonal test were used to optimize the formulation,and the quality of the optimized GL-PLGA NPs was evaluated from the surface configuration,particle size distribution,Zeta potential and entrapment efficiency.Results:The optimal prescription conditions of GL-PLGA NPs were:the volume ratio of organic phase to aqueous phase was 1:8,the concentration of PVA was 1.5%,the concentration of PLGA was 1.0%,and the drug concentration was 0.2%.Under these conditions,the average particle size of GL-PLGA NPs was 249±1.32nm,polydispersity index(PDI)was 0.059,Zeta potential was-4.86mV,and the entrapment efficiency was 75.3%.The results of electron microscopy showed that the nanoparticles were spherical,uniform particle size and good dispersion.Conclusion:The preparation method is simple and stable,and GL-PLGA NPs with suitable particle size and high entrapment efficiency can be obtained.展开更多
Urate acid transporter 1(URAT1)is the main transporter of uric acid reabsorption,which closely related to the pathogenesis of hyperuricemia.Screening URAT1 inhibitors and studying their possible metabolic processes is...Urate acid transporter 1(URAT1)is the main transporter of uric acid reabsorption,which closely related to the pathogenesis of hyperuricemia.Screening URAT1 inhibitors and studying their possible metabolic processes is a hot spot in the development of uric acid-lowering drugs.Studies have shown that many food-borne plant polyphenols have uric acid lowering activity with non-toxic side eff ects,and can be used to improve and alleviate hyperuricemia.In this study,we take galangin(GAL)as an example to explore the mechanism of plant polyphenols aff ecting hyperuricemia by inhibiting URAT1.Homology modeling was used to construct a three-dimensional model of URAT1 protein,and the structure was optimized.Ramachandran diagram was used to verify the rationality of model protein structure.A known URAT1 inhibitor,benzbromarone(BBR),was used to dock with URAT1 to determine the docking site and show the key amino acids.GAL and model protein were docked by molecular docking method to analyze their interaction.Meanwhile,comparing the interaction of BBR and GAL with the key amino acids of model proteins,the binding of GAL was more stable,suggesting that GAL could aff ects hyperuricemia by inhibiting URAT1.This paper aims to provide theoretical guidance for the development of new functional food ingredients for lowering uric acid.展开更多
基金Supported by The administration of traditional Chinese medicine of Guangdong province,China,No.1050047
文摘AIM:To investigate the mechanism by which galangin,a polyphenolic compound derived from medicinal herbs,induces apoptosis of hepatocellular carcinoma(HCC) cells.METHODS:The 3-(4,5-Dimethyl-thiazol-2-yl)-2,5-diphenyl-tetrazolium bromide assay was used to measure cell viability.Apoptosis was evaluated by in situ uptake of propidium iodide and Hoechst 33258 and was then detected by fluorescence microscopy.Protein expressions were detected by Western blotting.To confirm the apoptotic pathway mediated by galangin,cells were transfected by bcl-2 gene to overexpress Bcl-2 or siRNA to down-regulate Bcl-2 expression.RESULTS:Galangin(46.25-370.0 μmol/L) exerted an anti-proliferative effect,induced apoptosis,and decreased mitochondrial membrane potential in a dose and time-dependent manner.Treatment with galangin induced apoptosis by translocating the pro-apoptotic protein Bax to the mitochondria,which released apoptosis-inducing factor and cytochrome c into the cytosol.Overexpression of Bcl-2 attenuated galangin-induced HepG2 cell apoptosis,while decreasing Bcl-2 expression enhanced galangin-induced cell apoptosis.CONCLUSION:Our data suggests that galangin mediates apoptosis through a mitochondrial pathway,and may be a potential chemotherapeutic drug for the treatment of HCC.
文摘A high sensitive flow-injection chemiluminescence （FI-CL） method for the determination of tryptophan has been developed. The method is based on the chemiluminescence reaction of galangin-potassium permanganate-tryptophan in polyphosphoric acid （PPA） media. Under the optimized conditions, tryptophan was determined in the range 0.05-10 μg/mL with the detection limit （3tr） of 5.0 × 10^-3 μg/mL. The relative standard deviation （RSD） was 1.0% for 11 replicate determinations of 1.0 μg/mL tryptophan. Three synthetic samples were determined selectively with recoveries in the range from 99.6% to 102.0% in the presence of other amino acids.
基金The project supported by National Natural Science Foundation of China(81303261,81274133)the Major Scientific and Technological Special Project for″Significant New Drugs Creation″(2012ZX09103-201-055)the Fundamental Research Funds for the Central public welfare research institutes of China(ZZ2014005,ZZ2014060)
文摘OBJECTIVE Galangin,apotent scavenger of free radicals,is used as herbal medicine for various ailments for centuries in Asia.With complex pathophysiology,ischemic stroke is one of the most frequent causes of death and disability worldwide.We have reported that galangin provides a direct protection against ischemic injury as a potential neuroprotective agent and has potential therapeutic effects on the changes of serum amino acids for ischemic stroke;however,its mechanism on changes of amino acids in the ischemic brain tissue has not yet been clarified.METHODS In this paper,we explored the amino acid biomarkers of brain tissue in the acute phase of cerebral ischemia and the effect of galangin on those potential biomarkers with a rapid,sensitive and accurate methodology of simultaneous quantification of 12 AAs in rat brain tissue by the RRLC/QQQ.RESULTS we identified that glutamic acid,alanine and aspartic acid all showed significant change in galangin-treated groups compared to vehicle-treated rats and four pathway-related enzymes were identified by multiplex interactions with the three amino acids.With metabolite-protein network analysis and molecule docking,six of 28 proteins were identified and may become the potential biomarkers of galangin for acute ischemic stroke.CONCLUSION All data in our study provide thought for exploring the mechanism of disease,discovering new targets for drug candidates and elucidating the related regulatory signal network.
文摘Objective: To assess the protective effect of galangin on membrane bound enzymes in rats with streptozotocin-induced diabetes. Methods: A single low dose of streptozotocin was injected to adult male albino rats to induce hyperglycemia. Galangin(8 mg/kg) or glibenclamide 600 μg/kg as a standard drug was given orally once daily for 45 days by gavage. Membrane-bound adenosine triphosphatases were determined including total ATPase, sodium-potassium-ATPase, calcium-ATPase and magnesium-ATPase in erythrocytes and tissues(kidney, liver, and heart). Results: The levels of total ATPases, sodium-potassium-ATPase, calcium-ATPase and magnesium-ATPase in erythrocytes and tissues were significantly altered in diabetic rats as compared to that in normal rats. After 45 days of treatment with galangin or glibenclamide, the levels of these enzymes were similar to that of normal control rats. Conclusions: Oral administration of galangin or glibenclamide can improve activities of these membrane-bound ATPases towards normal levels. Mechanism of galangin needs to be further explored in future.
基金National natural science foundation of China(No.81660649)Innovation and entrepreneurship training program for undergraduates of Hainan medical university in 2019(No.X201911810073)。
文摘Objective:To make Galangin-PLGA nanoparticles(GL-PLGA NPs)were prepared using the biodegradable material polylactic-coglycolic acid(PLGA)as the carrier material,and the formulation was optimized.Methods:Nanoparticles were prepared by modified emulsification-solvent evaporation method and the content of galangin was determined by HPLC.With particle size and entrapment efficiency as the indexes,single factor and orthogonal test were used to optimize the formulation,and the quality of the optimized GL-PLGA NPs was evaluated from the surface configuration,particle size distribution,Zeta potential and entrapment efficiency.Results:The optimal prescription conditions of GL-PLGA NPs were:the volume ratio of organic phase to aqueous phase was 1:8,the concentration of PVA was 1.5%,the concentration of PLGA was 1.0%,and the drug concentration was 0.2%.Under these conditions,the average particle size of GL-PLGA NPs was 249±1.32nm,polydispersity index(PDI)was 0.059,Zeta potential was-4.86mV,and the entrapment efficiency was 75.3%.The results of electron microscopy showed that the nanoparticles were spherical,uniform particle size and good dispersion.Conclusion:The preparation method is simple and stable,and GL-PLGA NPs with suitable particle size and high entrapment efficiency can be obtained.
基金This work was supported by Young and Middle Aged Teachers’Career Development Support Project of Shenyang Pharmaceutical University(ZQN2019005).
文摘Urate acid transporter 1(URAT1)is the main transporter of uric acid reabsorption,which closely related to the pathogenesis of hyperuricemia.Screening URAT1 inhibitors and studying their possible metabolic processes is a hot spot in the development of uric acid-lowering drugs.Studies have shown that many food-borne plant polyphenols have uric acid lowering activity with non-toxic side eff ects,and can be used to improve and alleviate hyperuricemia.In this study,we take galangin(GAL)as an example to explore the mechanism of plant polyphenols aff ecting hyperuricemia by inhibiting URAT1.Homology modeling was used to construct a three-dimensional model of URAT1 protein,and the structure was optimized.Ramachandran diagram was used to verify the rationality of model protein structure.A known URAT1 inhibitor,benzbromarone(BBR),was used to dock with URAT1 to determine the docking site and show the key amino acids.GAL and model protein were docked by molecular docking method to analyze their interaction.Meanwhile,comparing the interaction of BBR and GAL with the key amino acids of model proteins,the binding of GAL was more stable,suggesting that GAL could aff ects hyperuricemia by inhibiting URAT1.This paper aims to provide theoretical guidance for the development of new functional food ingredients for lowering uric acid.
