α-Glucosidase inhibitors are effective in controlling postprandial hyperglycemia,which play crucial roles in the management of type 2 diabetes.Protocatechuic acid(PCA)is one of phenolic acids existing not only in var...α-Glucosidase inhibitors are effective in controlling postprandial hyperglycemia,which play crucial roles in the management of type 2 diabetes.Protocatechuic acid(PCA)is one of phenolic acids existing not only in various plant foods but also as a major microbial metabolite of dietary anthocyanins in the large colon.The present study investigated the inhibitory mechanism of PCA on a-glucosidase in vitro and examined its effect on postprandial blood glucose levels in vivo.Results from in vitro experiments demonstrated that PCA was a mix-type inhibitor of a-glucosidase.Driven by hydrogen bonds and van der Waals interactions,PCA reversibly bound withα-glucosidase to form a stable a-glucosidase-PCA complex in a spontaneous manner.The computational simulation found that PCA could insert into the active cavity of a-glucosidase and establish hydrogen bonds with catalytic amino acid residues.PCA binding aroused the steric hindrance for substrates to enter active sites and caused the structural changes of interacted catalytic amino acid residues.PCA also exhibited postprandial hypoglycemic capacity in diabetic mice.This study may provide the theoretical basis for the application of PCA as an active ingredient of functional foods in dietary management of diabetes.展开更多
Four polysaccharides(MCPa,MCPb,MCPc,MCPd)were obtained from Lepidium meyenii Walp.Their structures were characterized by chemical and instrumental methods including total sugar,uronic acid and protein content determi-...Four polysaccharides(MCPa,MCPb,MCPc,MCPd)were obtained from Lepidium meyenii Walp.Their structures were characterized by chemical and instrumental methods including total sugar,uronic acid and protein content determi-nation,UV,IR and NMR spectroscopy,as well as monosaccharide composition determination and methylation analy-ses.Four polysaccharides were a group of glucans with different molecular weights ranging from 3.12 to 14.4 kDa,and shared a similar backbone chain consisting of(1→4)-glucose linkages with branches attached to C-3 and C-6.Furthermore,bioactivity assay showed that MCPs had concentration-dependent inhibitory activity onα-glucosidase.MCPb(Mw=10.1 kDa)and MCPc(Mw=5.62 kDa)with moderate molecular weights exhibited higher inhibitory activ-ity compared with MCPa and MCPd.展开更多
Objective The Morus alba root bark is a well-known Chinese herbal medicine called Sang-Bai-Pi and has often been used to relieve the hyperglycemic symptom of diabetes patients.The current work aims to further explore ...Objective The Morus alba root bark is a well-known Chinese herbal medicine called Sang-Bai-Pi and has often been used to relieve the hyperglycemic symptom of diabetes patients.The current work aims to further explore its bioactive constituents with α-glucosidase inhibitory activity for the potential treatment of diabetes.Methods A combination of different separating techniques including routine column chromatograph and HPLC especially on chiral columns were applied for the isolation of target molecules,while comprehensive spectroscopic experiments comprising MS,NMR,ECD,etc.were carried out to complete the structural assignment.The anti-hyperglycemic property of the isolates was evaluated by an in vitro α-glucosidase inhibitory bioassay.Results Two pairs of new flavanone-monoterpene hybrid enantiomers were isolated and identified,and an interesting phenomenon of mutual transformation between these cometabolites were detected,which resulted in their regio-isomerization and enantiomerization.The bioassay results revealed remarkable α-glucosidase inhibitory activity for these fascinating molecules.Conclusions The Morus alba root bark is a rich source of bioactive flavonoid derivatives and deserves further investigations to develop new potential chemotherapies for diabetes control and treatment.展开更多
The intrinsic growth ability of all the neurons declines during development although some may grow better than others. Numerous intracellular signaling proteins and transcription factors have been shown to regulate th...The intrinsic growth ability of all the neurons declines during development although some may grow better than others. Numerous intracellular signaling proteins and transcription factors have been shown to regulate the intrinsic growth capacity in mature neurons. Among them, PI3 kinase/Akt pathway is important for controlling axon elongation. As a negative regulator of this pathway, the tumor suppressor phosphatase and tensin homolog （PTEN） appears critical to con- trol the regenerative ability of young and adult neurons. This review will focus on recent research progress in axon regeneration and neural repair by PTEN inhibition and therapeutic potential of blocking this phosphatase for neurological disorders. Inhibition of PTEN by deletion in con- ditional knockout mice, knockdown by short-hairpin RNA, or blockade by pharmacological approaches, including administration of selective PTEN antagonist peptides, stimulates various degrees of axon regrowth in juvenile or adult rodents with central nervous system injuries. Im- portantly, post-injury PTEN suppression could enhance axonal growth and functional recovery in adult central nervous system after injury.展开更多
Soil acidification is a major threat to agricultural sustainability in tropical and subtropical regions.Biodegradable and environmentally friendly materials,such as calcium lignosulfonate(CaLS),calcium poly(aspartic a...Soil acidification is a major threat to agricultural sustainability in tropical and subtropical regions.Biodegradable and environmentally friendly materials,such as calcium lignosulfonate(CaLS),calcium poly(aspartic acid)(PASP-Ca),and calcium polyγ-glutamic acid(γ-PGA-Ca),are known to effectively ameliorate soil acidity.However,their effectiveness in inhibiting soil acidification has not been studied.This study aimed to evaluate the effect of CaLS,PASP-Ca,andγ-PGA-Ca on the resistance of soil toward acidification as directly and indirectly(i.e.,via nitrification)caused by the application of HNO_(3)and urea,respectively.For comparison,Ca(OH)_(2)and lignin were used as the inorganic and organic controls,respectively.Among the materials,γ-PGA-Ca drove the substantial improvements in the pH buffering capacity(pHBC)of the soil and exhibited the greatest potential in inhibiting HNO_(3)-induced soil acidification via protonation of carboxyl,complexing with Al~(3+),and cation exchange processes.Under acidification induced by urea,CaLS was the optimal one in inhibiting acidification and increasing exchangeable acidity during incubation.Furthermore,the sharp reduction in the population sizes of ammonia-oxidizing bacteria(AOB)and ammonia-oxidizing archaea(AOA)confirmed the inhibition of nitrification via CaLS application.Therefore,compared to improving soil pHBC,CaLS may play a more important role in suppressing indirect acidification.Overall,γ-PGA-Ca was superior to PASP-Ca and CaLS in enhancing the soil pHBC and the its resistance to acidification induced by HNO_(3) addition,whereas CaLS was the best at suppressing urea-driven soil acidification by inhibiting nitrification.In conclusion,these results provide a reference for inhibiting soil re-acidification in intensive agricultural systems.展开更多
Objective:To investigate the in vivo and in vitro antidiabetic potential of Chrysophyllum albidum.Methods:The effects of oral treatment with hydro-ethanolic extract(125,250 and 500 mg/kg)of the stem bark of Chrysophyl...Objective:To investigate the in vivo and in vitro antidiabetic potential of Chrysophyllum albidum.Methods:The effects of oral treatment with hydro-ethanolic extract(125,250 and 500 mg/kg)of the stem bark of Chrysophyllum albidum and glibenclamide for 21 d on glucose level,serum enzyme markers for liver function,lipid profile,total protein,serum urea,serum creatinine,and body weight were evaluated in experimental diabetic rats administered with 45 mg/kg of streptozotocin.In vitro assays including glucose uptake in C2 C12 cells and 3 T3-L1 adipose tissues,α-glucosidase andα-amylase inhibition were employed to evaluate the possible mechanism of hypoglycemic action of the extract.DPPH and nitric oxide radical antioxidant activity of the extract was also measured.Results:The increased levels of blood glucose,triglycerides,lowdensity lipoprotein,total cholesterol,serum aspartate,and alanine transaminases,creatinine,and urea in the diabetic animals were reduced significantly(P<0.01)after treatment with Chrysophyllum albidum extract.The decreased total protein and high-density lipoprotein concentrations were normalized after treatment.In addition,the extract significantly(P<0.01)increased the transport of glucose in 3 T3-L1 cells and C2 C12 myotubes and exhibited considerable potential to inhibitα-amylase andα-glucosidase.It also demonstrated potent antioxidant action by scavenging considerably DPPH and nitric oxide radicals.Conclusions:Chrysophyllum albidum stem bark extract exhibits considerable antidiabetic effect by stimulating glucose uptake and utilization in C2 C12 myotubes and 3 T3-L1 adipocytes as well as inhibiting the activities ofα-amylase andα-glucosidase.展开更多
Objective To determine the effect of the phosphodiesterase-5 inhibitor sildenafil compared with placebo on exercise capacity and clinical status in HFPEF. Design Multicenter, double-blind, placebo-controlled, paralle...Objective To determine the effect of the phosphodiesterase-5 inhibitor sildenafil compared with placebo on exercise capacity and clinical status in HFPEF. Design Multicenter, double-blind, placebo-controlled, parallel-group, randomized clinical trial of 216 sta- ble outpatients with HF, ejection fraction ≥ 50%, elevated N-terminal brain-type natriuretic peptide or elevat- ed invasively measured filling pressures, and reduced exercise capacity. Participants were randomized from October 2008 through February 2012 at 26 centers in North America. Follow-up was through August 30, 2012.展开更多
The incidence of diabetes has increased considerably, and become the third serious chronic disease following cancer and cardiovascular diseases. Though acarbose, metformin, and 1-deoxynojirimycin have good efficacy fo...The incidence of diabetes has increased considerably, and become the third serious chronic disease following cancer and cardiovascular diseases. Though acarbose, metformin, and 1-deoxynojirimycin have good efficacy for clinical application as hypoglycemic drugs, their expensive costs and some degree of side effects have limited their clinical application. Recently, increasing attention has concentrated on the polysaccharides from natural plant and animal sources for diabetes. In order to illustrate the pharmaceutical activity of polysaccharides as natural hypoglycemic agents, polysaccharides isolated from Astragalus, oyster mushroom, and Yacon were evaluated for their inhibitory effects on α-glucosidase. Polysaccharides were extracted and purified from Astragalus, Oyster mushroom, and Yacon with hot water at 90 °C for 3 h, respectively. The total sugar content of the polysaccharide was determined by the phenol-sulfuric acid method. The α-glucosidase inhibitory activity was measured by the glucose oxidase method. The results exhibited that the inhibitory effects on α-glucosidase were in decreasing order, Astragalus > oyster mushroom > Yacon. The α-glucosidase inhibition percentage of Astragalus polysaccharide and oyster mushroom polysaccharide were over 40% at the polysaccharide concentration of 0.4 mg·mL-1. The IC50 of Astragalus polysaccharide and oyster mushroom polysaccharide were 0.28 and 0.424 mg·mL-1, respectively. The information obtained from this work is beneficial for the use polysaccharides as a dietary supplement for health foods and therapeutics for diabetes.展开更多
The present study was designed to investigate the bioactive constituents ofXanthoceras sorbifolia in terms of amounts and their antioxidant, DNA scissiou protection, and ct-glucosidase inhibitory activities. Simultane...The present study was designed to investigate the bioactive constituents ofXanthoceras sorbifolia in terms of amounts and their antioxidant, DNA scissiou protection, and ct-glucosidase inhibitory activities. Simultaneous quantification of 10 X. sorbifolia constituents was carried out by a newly established ultra-high performance liquid chromatography-quadrupole mass spectrometry method （UHPLC-MS）, The antioxidant activities were evaluated by measuring DPPH radical scavenging and DNA scission protective activities. The a-glucosidase inhibitory activities were investigated by using an assay with a-glucosidase from Bacillus Stearothermophilus and disaccharidases from mouse intestine. We found that the wood ofX. sorbifolia was rich in phenolic compounds with the contents of catechin, epicatechin, myricetin, and dihydromyricetin being 0.12-0.19, 1.94-2.16, 0.77-0.91, and 6.76-7.89 mg.g-1, respectively. The four constituents strongly scavenged DPPH radicals （with ECs0 being 4.2, 3.8 and 5.7 μg-mL-1, respectively） and remarkably protected peroxyl radical-induced DNA strand scission （92.10%, 94.66%, 75.44% and 89.95% of protection, respectively, at a concentration of 10 μmol.L-1）. A dimeric flavan 3-ol, epigallocatechin-（4β→8, 2β→O-7）-epicatechin potently inhibited a-glucosidase with an IC50 value being as low as 1.2 μg.mL1. The established UHPLC-MS method could serve as a quality control tool for X. sorbifolia. In conclusion, the high contents of antioxidant and α-glucosidase inhibitory constituents in X. sorbifolia support its use as complementation of other therapeutic agents for metabolic disorders, such as diabetes and hypertension.展开更多
Several derivatives have been synthesized from chrysin, diosmetin, apigenin, and luteolin, which were isolated from diverse natural plants. The α-glucosidase inhibitory activity of these compounds was evaluated. The ...Several derivatives have been synthesized from chrysin, diosmetin, apigenin, and luteolin, which were isolated from diverse natural plants. The α-glucosidase inhibitory activity of these compounds was evaluated. The glucosidase inhibitory activity of all derivatives （IC50 〈 24.396 μmol]L） was higher compared with that of the reference drug, acarbose （IC50=563.601 ±40.492μmol/L）, and 1- deoxynojirimycin （IC50 = 226.912± 12.573 μmol/L）. O3＇,O7-Hexyl diosmetin （IC50 = 2.406 ± 0.101μmol/L） was the most potent inhibitor identified. These compounds showed a higher inhibitory ability compared with their precursors except the luteolin derivatives. In general, the inhibitory activity of the synthetic derivatives was enhanced with long alkyl chains at positions 3＇, 4＇ and 7 of the flavonoid.展开更多
The conditions for extracting polysaccharides from tea （Camellia sinensis L.） fruit peel （TFPPs） were studied. Three parameters （temperature, time, and liquid/solid ratio） affecting the extraction of TFPP were o...The conditions for extracting polysaccharides from tea （Camellia sinensis L.） fruit peel （TFPPs） were studied. Three parameters （temperature, time, and liquid/solid ratio） affecting the extraction of TFPP were optimized using response surface methodology （RSM）. Under the optimized conditions, the yield of TFPP was predicted to be 4.98%. The physicochemical properties, in vitro antioxidant activities, and inhibitory effects on α-glucosidase of frac- tionated TFPPs （TFPP-0, TFPP-20, TFPP-40, and TFPP-60） were investigated. We found that the TFPPs were all acid protein-bound heteropolysaccharides, although with different chemical compositions. They had not only re- markable scavenging activity on 2,2＇-azinobis（3-ethylbenzothiazoline-6-sulfonic acid） diammonium salt （ABTS） and reducing activity, but also excellent inhibitory potential against α-glucosidase in vitro. Our results suggest that tea fruit peel could be treated as a potential bioresource for the development of polysaccharide antioxidants.展开更多
基金supported by the General Research Fund of Hong Kong (14105820)。
文摘α-Glucosidase inhibitors are effective in controlling postprandial hyperglycemia,which play crucial roles in the management of type 2 diabetes.Protocatechuic acid(PCA)is one of phenolic acids existing not only in various plant foods but also as a major microbial metabolite of dietary anthocyanins in the large colon.The present study investigated the inhibitory mechanism of PCA on a-glucosidase in vitro and examined its effect on postprandial blood glucose levels in vivo.Results from in vitro experiments demonstrated that PCA was a mix-type inhibitor of a-glucosidase.Driven by hydrogen bonds and van der Waals interactions,PCA reversibly bound withα-glucosidase to form a stable a-glucosidase-PCA complex in a spontaneous manner.The computational simulation found that PCA could insert into the active cavity of a-glucosidase and establish hydrogen bonds with catalytic amino acid residues.PCA binding aroused the steric hindrance for substrates to enter active sites and caused the structural changes of interacted catalytic amino acid residues.PCA also exhibited postprandial hypoglycemic capacity in diabetic mice.This study may provide the theoretical basis for the application of PCA as an active ingredient of functional foods in dietary management of diabetes.
基金the National Natural Science Foundation of China(No.31872675)the Cooperation Project with DR PLANT Company(2023).
文摘Four polysaccharides(MCPa,MCPb,MCPc,MCPd)were obtained from Lepidium meyenii Walp.Their structures were characterized by chemical and instrumental methods including total sugar,uronic acid and protein content determi-nation,UV,IR and NMR spectroscopy,as well as monosaccharide composition determination and methylation analy-ses.Four polysaccharides were a group of glucans with different molecular weights ranging from 3.12 to 14.4 kDa,and shared a similar backbone chain consisting of(1→4)-glucose linkages with branches attached to C-3 and C-6.Furthermore,bioactivity assay showed that MCPs had concentration-dependent inhibitory activity onα-glucosidase.MCPb(Mw=10.1 kDa)and MCPc(Mw=5.62 kDa)with moderate molecular weights exhibited higher inhibitory activ-ity compared with MCPa and MCPd.
基金Financial support is from the Natural Science Foundation of Shandong Province for Distinguished Young Scholars(No.JQ201721).
文摘Objective The Morus alba root bark is a well-known Chinese herbal medicine called Sang-Bai-Pi and has often been used to relieve the hyperglycemic symptom of diabetes patients.The current work aims to further explore its bioactive constituents with α-glucosidase inhibitory activity for the potential treatment of diabetes.Methods A combination of different separating techniques including routine column chromatograph and HPLC especially on chiral columns were applied for the isolation of target molecules,while comprehensive spectroscopic experiments comprising MS,NMR,ECD,etc.were carried out to complete the structural assignment.The anti-hyperglycemic property of the isolates was evaluated by an in vitro α-glucosidase inhibitory bioassay.Results Two pairs of new flavanone-monoterpene hybrid enantiomers were isolated and identified,and an interesting phenomenon of mutual transformation between these cometabolites were detected,which resulted in their regio-isomerization and enantiomerization.The bioassay results revealed remarkable α-glucosidase inhibitory activity for these fascinating molecules.Conclusions The Morus alba root bark is a rich source of bioactive flavonoid derivatives and deserves further investigations to develop new potential chemotherapies for diabetes control and treatment.
基金supported by research grants to SL from NIH(1R21NS066114,1R01NS079432 and 1R01EY024575)Christopher&Dana Reeve Foundation(LA1-1002-2)Shriners Research Foundation(86300)
文摘The intrinsic growth ability of all the neurons declines during development although some may grow better than others. Numerous intracellular signaling proteins and transcription factors have been shown to regulate the intrinsic growth capacity in mature neurons. Among them, PI3 kinase/Akt pathway is important for controlling axon elongation. As a negative regulator of this pathway, the tumor suppressor phosphatase and tensin homolog （PTEN） appears critical to con- trol the regenerative ability of young and adult neurons. This review will focus on recent research progress in axon regeneration and neural repair by PTEN inhibition and therapeutic potential of blocking this phosphatase for neurological disorders. Inhibition of PTEN by deletion in con- ditional knockout mice, knockdown by short-hairpin RNA, or blockade by pharmacological approaches, including administration of selective PTEN antagonist peptides, stimulates various degrees of axon regrowth in juvenile or adult rodents with central nervous system injuries. Im- portantly, post-injury PTEN suppression could enhance axonal growth and functional recovery in adult central nervous system after injury.
基金supported by the Major project of Ministry of Agriculture and Rural Affairs of the People’s Republic of China(No.NK2022180401)the major project of Ministry of Agriculture and Rural Affairs of the People’s Republic of China(No.NK2022180404)。
文摘Soil acidification is a major threat to agricultural sustainability in tropical and subtropical regions.Biodegradable and environmentally friendly materials,such as calcium lignosulfonate(CaLS),calcium poly(aspartic acid)(PASP-Ca),and calcium polyγ-glutamic acid(γ-PGA-Ca),are known to effectively ameliorate soil acidity.However,their effectiveness in inhibiting soil acidification has not been studied.This study aimed to evaluate the effect of CaLS,PASP-Ca,andγ-PGA-Ca on the resistance of soil toward acidification as directly and indirectly(i.e.,via nitrification)caused by the application of HNO_(3)and urea,respectively.For comparison,Ca(OH)_(2)and lignin were used as the inorganic and organic controls,respectively.Among the materials,γ-PGA-Ca drove the substantial improvements in the pH buffering capacity(pHBC)of the soil and exhibited the greatest potential in inhibiting HNO_(3)-induced soil acidification via protonation of carboxyl,complexing with Al~(3+),and cation exchange processes.Under acidification induced by urea,CaLS was the optimal one in inhibiting acidification and increasing exchangeable acidity during incubation.Furthermore,the sharp reduction in the population sizes of ammonia-oxidizing bacteria(AOB)and ammonia-oxidizing archaea(AOA)confirmed the inhibition of nitrification via CaLS application.Therefore,compared to improving soil pHBC,CaLS may play a more important role in suppressing indirect acidification.Overall,γ-PGA-Ca was superior to PASP-Ca and CaLS in enhancing the soil pHBC and the its resistance to acidification induced by HNO_(3) addition,whereas CaLS was the best at suppressing urea-driven soil acidification by inhibiting nitrification.In conclusion,these results provide a reference for inhibiting soil re-acidification in intensive agricultural systems.
基金supported by some funds from KNUST Research Fund(KReF)
文摘Objective:To investigate the in vivo and in vitro antidiabetic potential of Chrysophyllum albidum.Methods:The effects of oral treatment with hydro-ethanolic extract(125,250 and 500 mg/kg)of the stem bark of Chrysophyllum albidum and glibenclamide for 21 d on glucose level,serum enzyme markers for liver function,lipid profile,total protein,serum urea,serum creatinine,and body weight were evaluated in experimental diabetic rats administered with 45 mg/kg of streptozotocin.In vitro assays including glucose uptake in C2 C12 cells and 3 T3-L1 adipose tissues,α-glucosidase andα-amylase inhibition were employed to evaluate the possible mechanism of hypoglycemic action of the extract.DPPH and nitric oxide radical antioxidant activity of the extract was also measured.Results:The increased levels of blood glucose,triglycerides,lowdensity lipoprotein,total cholesterol,serum aspartate,and alanine transaminases,creatinine,and urea in the diabetic animals were reduced significantly(P<0.01)after treatment with Chrysophyllum albidum extract.The decreased total protein and high-density lipoprotein concentrations were normalized after treatment.In addition,the extract significantly(P<0.01)increased the transport of glucose in 3 T3-L1 cells and C2 C12 myotubes and exhibited considerable potential to inhibitα-amylase andα-glucosidase.It also demonstrated potent antioxidant action by scavenging considerably DPPH and nitric oxide radicals.Conclusions:Chrysophyllum albidum stem bark extract exhibits considerable antidiabetic effect by stimulating glucose uptake and utilization in C2 C12 myotubes and 3 T3-L1 adipocytes as well as inhibiting the activities ofα-amylase andα-glucosidase.
文摘Objective To determine the effect of the phosphodiesterase-5 inhibitor sildenafil compared with placebo on exercise capacity and clinical status in HFPEF. Design Multicenter, double-blind, placebo-controlled, parallel-group, randomized clinical trial of 216 sta- ble outpatients with HF, ejection fraction ≥ 50%, elevated N-terminal brain-type natriuretic peptide or elevat- ed invasively measured filling pressures, and reduced exercise capacity. Participants were randomized from October 2008 through February 2012 at 26 centers in North America. Follow-up was through August 30, 2012.
基金supported by the Foundation of Tianjin University of Science and Technology(No.20120106)The International Science&Technology Cooperation Program of China(No.2013DFA31160)the Foundation of Tianjin Educational Committee(No.20090604)
文摘The incidence of diabetes has increased considerably, and become the third serious chronic disease following cancer and cardiovascular diseases. Though acarbose, metformin, and 1-deoxynojirimycin have good efficacy for clinical application as hypoglycemic drugs, their expensive costs and some degree of side effects have limited their clinical application. Recently, increasing attention has concentrated on the polysaccharides from natural plant and animal sources for diabetes. In order to illustrate the pharmaceutical activity of polysaccharides as natural hypoglycemic agents, polysaccharides isolated from Astragalus, oyster mushroom, and Yacon were evaluated for their inhibitory effects on α-glucosidase. Polysaccharides were extracted and purified from Astragalus, Oyster mushroom, and Yacon with hot water at 90 °C for 3 h, respectively. The total sugar content of the polysaccharide was determined by the phenol-sulfuric acid method. The α-glucosidase inhibitory activity was measured by the glucose oxidase method. The results exhibited that the inhibitory effects on α-glucosidase were in decreasing order, Astragalus > oyster mushroom > Yacon. The α-glucosidase inhibition percentage of Astragalus polysaccharide and oyster mushroom polysaccharide were over 40% at the polysaccharide concentration of 0.4 mg·mL-1. The IC50 of Astragalus polysaccharide and oyster mushroom polysaccharide were 0.28 and 0.424 mg·mL-1, respectively. The information obtained from this work is beneficial for the use polysaccharides as a dietary supplement for health foods and therapeutics for diabetes.
基金supported by National Natural Science Foundation of China(No.81360474)
文摘The present study was designed to investigate the bioactive constituents ofXanthoceras sorbifolia in terms of amounts and their antioxidant, DNA scissiou protection, and ct-glucosidase inhibitory activities. Simultaneous quantification of 10 X. sorbifolia constituents was carried out by a newly established ultra-high performance liquid chromatography-quadrupole mass spectrometry method （UHPLC-MS）, The antioxidant activities were evaluated by measuring DPPH radical scavenging and DNA scission protective activities. The a-glucosidase inhibitory activities were investigated by using an assay with a-glucosidase from Bacillus Stearothermophilus and disaccharidases from mouse intestine. We found that the wood ofX. sorbifolia was rich in phenolic compounds with the contents of catechin, epicatechin, myricetin, and dihydromyricetin being 0.12-0.19, 1.94-2.16, 0.77-0.91, and 6.76-7.89 mg.g-1, respectively. The four constituents strongly scavenged DPPH radicals （with ECs0 being 4.2, 3.8 and 5.7 μg-mL-1, respectively） and remarkably protected peroxyl radical-induced DNA strand scission （92.10%, 94.66%, 75.44% and 89.95% of protection, respectively, at a concentration of 10 μmol.L-1）. A dimeric flavan 3-ol, epigallocatechin-（4β→8, 2β→O-7）-epicatechin potently inhibited a-glucosidase with an IC50 value being as low as 1.2 μg.mL1. The established UHPLC-MS method could serve as a quality control tool for X. sorbifolia. In conclusion, the high contents of antioxidant and α-glucosidase inhibitory constituents in X. sorbifolia support its use as complementation of other therapeutic agents for metabolic disorders, such as diabetes and hypertension.
基金supported by the Research Fund for the Doctoral Program of Higher Education of China(No.20114301120004)Hunan Provincial Natural Science Foundation of China(No.12JJ6081)+1 种基金Dr.’s Start-up Foundation of Xiangtan University(No.06KZjKZ08035)Natural Science Foundation of Xiangtan University(No.2011XZX09)
文摘Several derivatives have been synthesized from chrysin, diosmetin, apigenin, and luteolin, which were isolated from diverse natural plants. The α-glucosidase inhibitory activity of these compounds was evaluated. The glucosidase inhibitory activity of all derivatives （IC50 〈 24.396 μmol]L） was higher compared with that of the reference drug, acarbose （IC50=563.601 ±40.492μmol/L）, and 1- deoxynojirimycin （IC50 = 226.912± 12.573 μmol/L）. O3＇,O7-Hexyl diosmetin （IC50 = 2.406 ± 0.101μmol/L） was the most potent inhibitor identified. These compounds showed a higher inhibitory ability compared with their precursors except the luteolin derivatives. In general, the inhibitory activity of the synthetic derivatives was enhanced with long alkyl chains at positions 3＇, 4＇ and 7 of the flavonoid.
基金supported by the Ministry of Science and Technology of China(No.2012BAD36B06-5)
文摘The conditions for extracting polysaccharides from tea （Camellia sinensis L.） fruit peel （TFPPs） were studied. Three parameters （temperature, time, and liquid/solid ratio） affecting the extraction of TFPP were optimized using response surface methodology （RSM）. Under the optimized conditions, the yield of TFPP was predicted to be 4.98%. The physicochemical properties, in vitro antioxidant activities, and inhibitory effects on α-glucosidase of frac- tionated TFPPs （TFPP-0, TFPP-20, TFPP-40, and TFPP-60） were investigated. We found that the TFPPs were all acid protein-bound heteropolysaccharides, although with different chemical compositions. They had not only re- markable scavenging activity on 2,2＇-azinobis（3-ethylbenzothiazoline-6-sulfonic acid） diammonium salt （ABTS） and reducing activity, but also excellent inhibitory potential against α-glucosidase in vitro. Our results suggest that tea fruit peel could be treated as a potential bioresource for the development of polysaccharide antioxidants.
