AIM： To examine the effect of alisol B acetate on the growth of human gastric cancer cell line SGC7901 and its possible mechanism of action.METHODS： The cytotoxic effect of alisol B acetate on SGC7901 cells was meas...AIM： To examine the effect of alisol B acetate on the growth of human gastric cancer cell line SGC7901 and its possible mechanism of action.METHODS： The cytotoxic effect of alisol B acetate on SGC7901 cells was measured by 3-（4,5-dimethylthiazol- 2-yl）-2,5-diphenyltetrazolium bromide （MI-I-） assay. Phase-contrast and electron microscopy were used to observe the morphological changes. Cell cycle and mitochondrial transmembrane potential （A^Pm） were determined by flow cytometry. Western blotting was used to detect the expression of apoptosis-regulated gene Bcl-2, Bax, Apaf-1, caspase-3, caspase-9, Akt, P-Akt and phosphatidylinositol 3-kinases （PI3K）.RESULTS： Alisol B acetate inhibited the proliferation of SGC7901 cell line in a time- and dose-dependent manner. PI staining showed that alisol B acetate can change the cell cycle distribution of SGC7901, increase the proportion of cells in G0-G1 phase and decrease the proportion of S phase cells and G2-M phase cells. Alisol B acetate at a concentration of 30 pmol/L induced apoptosis after 24, 48 and 72 h incubation, with occurrence rates of apoptotic cells of 4.36%, 14.42% and 21.16%, respectively. Phase-contrast and electron microscopy revealed that the nuclear fragmentation and chromosomal condensed, cells shrank and attachment loss appeared in the SGC7901 treated with alisol B acetate. Apoptosis of SGC7901 cells was associated with cell cycle arrest, caspase-3 and caspase-9 activation, loss of mitochondrial membrane potential and up-regulation of the ratio of Bax/Bcl-2 and inhibition of the PI3K/Akt.CONCLUSION： Alisol B acetate exhibits an antiproliferative effect in SGC7901 cells by inducing apoptosis. Apoptosis of SGC7901 cells involves mitochondria-caspase and PI3K/Akt dependent pathways.展开更多
Tributyl phosphate （TBP） solvent was used for impregnation into Amberlite XAD-16 nonionic polymeric resin beads using the wet method to prepare solvent impregnated resin （SIR）. Undiluted TBP in a ratio to the resi...Tributyl phosphate （TBP） solvent was used for impregnation into Amberlite XAD-16 nonionic polymeric resin beads using the wet method to prepare solvent impregnated resin （SIR）. Undiluted TBP in a ratio to the resin support （volume to mass） of 6.0 at room temperature （RT） in 24 h was impregnated the resin with a mass ratio of 1.944, while the prepared gross sample of SIR at the ratio of solvent to resin of 3.0 was impregnated with a mass ratio of 1.88. Cerium（Ⅳ） oxide concentrate, prepared from crude Egyptian monazite sand, containing 37% cerium, 1.6% thorium and about 40% the other trivalent rare earth oxides, was used to prepare cerium（Ⅳ） nitrate solution for extraction using the prepared SIR. The impregnated resin was satisfactory for Ce（Ⅳ） extraction from nitric acid medium at room temperature. Cerium loading capacity of the impregnated resin reached 95.6% of the calculated theoretical capacity （173 g/kg （Ce/SIR）） under the conditions of 51.57 g/L cerium and 2.48 g/L thorium, 5.0 mol/L free nitric acid, solution to resin ratio of 10.0 and contacting the phases for 5.0 min. The loading capacity reached 98.75% when cerium concentration was increased to 91.43 g/L under the same conditions.展开更多
Adsorption of gold on TBP extracting resin from HCI solution was researched. All the effects of factors, such as solution acidity, TBP content,tempo)uture, etc. , on adsorption equilibrium were discussed and the equil...Adsorption of gold on TBP extracting resin from HCI solution was researched. All the effects of factors, such as solution acidity, TBP content,tempo)uture, etc. , on adsorption equilibrium were discussed and the equilibrium equation was formulated. The breakthough time of adsorption process withfixed bed uns studied through experiment.展开更多
The aim of this work was to increase the efficacy of erythromycin ethyl succinate by encapsulation in beeswax lipid matrix using Myrj 52 as emulsifier. Different batches of SLM＇s （solid-lipid microparticles） were f...The aim of this work was to increase the efficacy of erythromycin ethyl succinate by encapsulation in beeswax lipid matrix using Myrj 52 as emulsifier. Different batches of SLM＇s （solid-lipid microparticles） were formulated and stable ones were selected. The encapsulation efficiency and loading capacities were calculated. The batch with the highest loading capacity was used for further assays. The particle size was determined by light microscopy. The sensitivity of different clinical bacterial isolates to erythromycin was tested using in vitro cultures and E. coli was selected for efficacy tests. The activity of the formulated drug was tested in the in vitro culture and compared to that of the unformulated drug. White albino mice were infected with E. coli and left for one day to develop significant bacteremia. They were then divided into 4 groups （n = 4） and treated with the formulation and unformulated drug at a dose of 7.14 mg/kg 8 hourly for 56 hours. A third group was given SLM＇s that do not contain drug, while another group was left untreated. The selected batch has an encapsulation efficiency of 94.83% with a loading capacity of 3.88%. The particle size was 17 ± 4 μm. At the end of the three day period of treatment, the group treated with unformulated erythromycin had much stooling anti weakness in the mice, and some deaths were recorded, while that treated with the formulation had 33.8% bacteremia and the clinical signs had largely subsided. The other two groups recorded deaths the following day after bacteremia induction. The results show marked improvement in efficacy of erythromycin ethyl succinate by formulation in SLMs with beeswax and lecithin as lipid matrix.展开更多
Background：Paraoxonase 1（PON1） is an antioxidant enzyme that protects high-density lipoprotein（HDL） and low-density lipoprotein against oxidation.Limited studies have addressed the influenc of exercise on PON1 ac...Background：Paraoxonase 1（PON1） is an antioxidant enzyme that protects high-density lipoprotein（HDL） and low-density lipoprotein against oxidation.Limited studies have addressed the influenc of exercise on PON1 activity and its relationship with PON1 phenotypes.We investigated relationships between PON1-192 phenotypes,PON1 activity,aerobic exercise,and blood lipid and lipoprotein concentrations in middle-aged women.Methods：An exercise group（n=50） engaging in regular aerobic exercise and a control group（n=41） were selected from a subset of 300 Caucasian women that met the inclusion criteria.Serum PON1,salt-stimulated PON1（SSPON1）,and arylesterase（ARE） activities;cholesterol levels and ARE activities of total HDL and HDL subgroups（HDLs）（supernatants obtained by polyethylene glycol）;and blood lipid and lipoprotein concentrations were determined by standardized enzymatic methods.PON1-192 QQ（low activity）,QR（moderate activity）,and RR（high activity） phenotype groups were define using serum SSPON1/ARE activity ratios.The R-carries（RC） phenotype group consisted of the QR and RR groups combined.Results：All lipid and lipoprotein concentrations were greater in the exercise group than in the control group.Regardless of phenotype,no significan differences were observed between the exercise and control groups in terms of serum PON1,SSPON1,or ARE activity associated with HDLs（p〉 0.05）,whereas PON1 activities in QQ-phenotyped women in the exercise group were significant y higher than those in the control group（p〈0.01）,but not the RC group.A statistically significan interaction between PON1 phenotypes（QQ and RC groups） and exercise（exercise and control groups） on PON1 activity was found.Conclusion：These results showed that a regular aerobic exercise program can improve PON1 activity depending on PON1-192 phenotype,but not on lipid and lipoprotein levels,in middle-aged Turkish women.展开更多
Hesperetin,an abundant bioactive component of citrus fruits,is poorly water-soluble,resulting in low oral bioavailability.We developed new formulations to improve the water solubility,antioxidant activity,and oral abs...Hesperetin,an abundant bioactive component of citrus fruits,is poorly water-soluble,resulting in low oral bioavailability.We developed new formulations to improve the water solubility,antioxidant activity,and oral absorption of hesperetin.Two nano-based formulations were developed,namely hesperetin-TPGS(D-α-tocopheryl polyethylene glycol 1000 succinate)micelles and hesperetin-phosphatidylcholine(PC)complexes.These two formulations were prepared by a simple technique called solvent dispersion,using US Food and Drug Administration(FDA)-approved excipients for drugs.Differential scanning calorimetry(DSC)and dynamic light scattering(DLS)were used to characterize the formulations’physical properties.Cytotoxicity analysis,cellular antioxidant activity assay,and a pharmacokinetic study were performed to evaluate the biological properties of these two formulations.The final weight ratios of both hesperetin to TPGS and hesperetin to PC were 1:12 based on their water solubility,which increased to 21.5-and 20.7-fold,respectively.The hesperetin-TPGS micelles had a small particle size of 26.19 nm,whereas the hesperetin-PC complexes exhibited a larger particle size of 219.15 nm.In addition,the cellular antioxidant activity assay indicated that both hesperetin-TPGS micelles and hesperetin-PC complexes increased the antioxidant activity of hesperetin to 4.2-and 3.9-fold,respectively.Importantly,the in vivo oral absorption study on rats indicated that the micelles and complexes significantly increased the peak plasma concentration(Cmax)from 2.64μg/mL to 20.67 and 33.09μg/mL and also increased the area under the concentration–time curve of hesperetin after oral administration to 16.2-and 18.0-fold,respectively.The micelles and complexes increased the solubility and remarkably improved the in vitro antioxidant activity and in vivo oral absorption of hesperetin,indicating these formulations’potential applications in drugs and healthcare products.展开更多
文摘AIM： To examine the effect of alisol B acetate on the growth of human gastric cancer cell line SGC7901 and its possible mechanism of action.METHODS： The cytotoxic effect of alisol B acetate on SGC7901 cells was measured by 3-（4,5-dimethylthiazol- 2-yl）-2,5-diphenyltetrazolium bromide （MI-I-） assay. Phase-contrast and electron microscopy were used to observe the morphological changes. Cell cycle and mitochondrial transmembrane potential （A^Pm） were determined by flow cytometry. Western blotting was used to detect the expression of apoptosis-regulated gene Bcl-2, Bax, Apaf-1, caspase-3, caspase-9, Akt, P-Akt and phosphatidylinositol 3-kinases （PI3K）.RESULTS： Alisol B acetate inhibited the proliferation of SGC7901 cell line in a time- and dose-dependent manner. PI staining showed that alisol B acetate can change the cell cycle distribution of SGC7901, increase the proportion of cells in G0-G1 phase and decrease the proportion of S phase cells and G2-M phase cells. Alisol B acetate at a concentration of 30 pmol/L induced apoptosis after 24, 48 and 72 h incubation, with occurrence rates of apoptotic cells of 4.36%, 14.42% and 21.16%, respectively. Phase-contrast and electron microscopy revealed that the nuclear fragmentation and chromosomal condensed, cells shrank and attachment loss appeared in the SGC7901 treated with alisol B acetate. Apoptosis of SGC7901 cells was associated with cell cycle arrest, caspase-3 and caspase-9 activation, loss of mitochondrial membrane potential and up-regulation of the ratio of Bax/Bcl-2 and inhibition of the PI3K/Akt.CONCLUSION： Alisol B acetate exhibits an antiproliferative effect in SGC7901 cells by inducing apoptosis. Apoptosis of SGC7901 cells involves mitochondria-caspase and PI3K/Akt dependent pathways.
文摘Tributyl phosphate （TBP） solvent was used for impregnation into Amberlite XAD-16 nonionic polymeric resin beads using the wet method to prepare solvent impregnated resin （SIR）. Undiluted TBP in a ratio to the resin support （volume to mass） of 6.0 at room temperature （RT） in 24 h was impregnated the resin with a mass ratio of 1.944, while the prepared gross sample of SIR at the ratio of solvent to resin of 3.0 was impregnated with a mass ratio of 1.88. Cerium（Ⅳ） oxide concentrate, prepared from crude Egyptian monazite sand, containing 37% cerium, 1.6% thorium and about 40% the other trivalent rare earth oxides, was used to prepare cerium（Ⅳ） nitrate solution for extraction using the prepared SIR. The impregnated resin was satisfactory for Ce（Ⅳ） extraction from nitric acid medium at room temperature. Cerium loading capacity of the impregnated resin reached 95.6% of the calculated theoretical capacity （173 g/kg （Ce/SIR）） under the conditions of 51.57 g/L cerium and 2.48 g/L thorium, 5.0 mol/L free nitric acid, solution to resin ratio of 10.0 and contacting the phases for 5.0 min. The loading capacity reached 98.75% when cerium concentration was increased to 91.43 g/L under the same conditions.
文摘Adsorption of gold on TBP extracting resin from HCI solution was researched. All the effects of factors, such as solution acidity, TBP content,tempo)uture, etc. , on adsorption equilibrium were discussed and the equilibrium equation was formulated. The breakthough time of adsorption process withfixed bed uns studied through experiment.
文摘The aim of this work was to increase the efficacy of erythromycin ethyl succinate by encapsulation in beeswax lipid matrix using Myrj 52 as emulsifier. Different batches of SLM＇s （solid-lipid microparticles） were formulated and stable ones were selected. The encapsulation efficiency and loading capacities were calculated. The batch with the highest loading capacity was used for further assays. The particle size was determined by light microscopy. The sensitivity of different clinical bacterial isolates to erythromycin was tested using in vitro cultures and E. coli was selected for efficacy tests. The activity of the formulated drug was tested in the in vitro culture and compared to that of the unformulated drug. White albino mice were infected with E. coli and left for one day to develop significant bacteremia. They were then divided into 4 groups （n = 4） and treated with the formulation and unformulated drug at a dose of 7.14 mg/kg 8 hourly for 56 hours. A third group was given SLM＇s that do not contain drug, while another group was left untreated. The selected batch has an encapsulation efficiency of 94.83% with a loading capacity of 3.88%. The particle size was 17 ± 4 μm. At the end of the three day period of treatment, the group treated with unformulated erythromycin had much stooling anti weakness in the mice, and some deaths were recorded, while that treated with the formulation had 33.8% bacteremia and the clinical signs had largely subsided. The other two groups recorded deaths the following day after bacteremia induction. The results show marked improvement in efficacy of erythromycin ethyl succinate by formulation in SLMs with beeswax and lecithin as lipid matrix.
基金supported by the Ege University Scientifi Research Projects Directorate(2006-BESYO-004)
文摘Background：Paraoxonase 1（PON1） is an antioxidant enzyme that protects high-density lipoprotein（HDL） and low-density lipoprotein against oxidation.Limited studies have addressed the influenc of exercise on PON1 activity and its relationship with PON1 phenotypes.We investigated relationships between PON1-192 phenotypes,PON1 activity,aerobic exercise,and blood lipid and lipoprotein concentrations in middle-aged women.Methods：An exercise group（n=50） engaging in regular aerobic exercise and a control group（n=41） were selected from a subset of 300 Caucasian women that met the inclusion criteria.Serum PON1,salt-stimulated PON1（SSPON1）,and arylesterase（ARE） activities;cholesterol levels and ARE activities of total HDL and HDL subgroups（HDLs）（supernatants obtained by polyethylene glycol）;and blood lipid and lipoprotein concentrations were determined by standardized enzymatic methods.PON1-192 QQ（low activity）,QR（moderate activity）,and RR（high activity） phenotype groups were define using serum SSPON1/ARE activity ratios.The R-carries（RC） phenotype group consisted of the QR and RR groups combined.Results：All lipid and lipoprotein concentrations were greater in the exercise group than in the control group.Regardless of phenotype,no significan differences were observed between the exercise and control groups in terms of serum PON1,SSPON1,or ARE activity associated with HDLs（p〉 0.05）,whereas PON1 activities in QQ-phenotyped women in the exercise group were significant y higher than those in the control group（p〈0.01）,but not the RC group.A statistically significan interaction between PON1 phenotypes（QQ and RC groups） and exercise（exercise and control groups） on PON1 activity was found.Conclusion：These results showed that a regular aerobic exercise program can improve PON1 activity depending on PON1-192 phenotype,but not on lipid and lipoprotein levels,in middle-aged Turkish women.
基金Project supported by the National Natural Science Foundation of China(Nos.51773176,51522304,and U1501243)the Natural Science Foundation of Zhejiang Province(No.LY17H300002),China
文摘Hesperetin,an abundant bioactive component of citrus fruits,is poorly water-soluble,resulting in low oral bioavailability.We developed new formulations to improve the water solubility,antioxidant activity,and oral absorption of hesperetin.Two nano-based formulations were developed,namely hesperetin-TPGS(D-α-tocopheryl polyethylene glycol 1000 succinate)micelles and hesperetin-phosphatidylcholine(PC)complexes.These two formulations were prepared by a simple technique called solvent dispersion,using US Food and Drug Administration(FDA)-approved excipients for drugs.Differential scanning calorimetry(DSC)and dynamic light scattering(DLS)were used to characterize the formulations’physical properties.Cytotoxicity analysis,cellular antioxidant activity assay,and a pharmacokinetic study were performed to evaluate the biological properties of these two formulations.The final weight ratios of both hesperetin to TPGS and hesperetin to PC were 1:12 based on their water solubility,which increased to 21.5-and 20.7-fold,respectively.The hesperetin-TPGS micelles had a small particle size of 26.19 nm,whereas the hesperetin-PC complexes exhibited a larger particle size of 219.15 nm.In addition,the cellular antioxidant activity assay indicated that both hesperetin-TPGS micelles and hesperetin-PC complexes increased the antioxidant activity of hesperetin to 4.2-and 3.9-fold,respectively.Importantly,the in vivo oral absorption study on rats indicated that the micelles and complexes significantly increased the peak plasma concentration(Cmax)from 2.64μg/mL to 20.67 and 33.09μg/mL and also increased the area under the concentration–time curve of hesperetin after oral administration to 16.2-and 18.0-fold,respectively.The micelles and complexes increased the solubility and remarkably improved the in vitro antioxidant activity and in vivo oral absorption of hesperetin,indicating these formulations’potential applications in drugs and healthcare products.
