AIM: To study the toxicity of bicyclol to animals. METHODS: Acute toxicity test was performed in Kunming strain mice that were orally given bicyclol at the doses of 3 and 5 g/kg body weight, respectively. Wistar rats ...AIM: To study the toxicity of bicyclol to animals. METHODS: Acute toxicity test was performed in Kunming strain mice that were orally given bicyclol at the doses of 3 and 5 g/kg body weight, respectively. Wistar rats were orally administered bicyclol at a dose of 5 g/kg body weight. Death and clinical symptoms of animals were recorded within 7 d. Sub-acute toxicity test was carried out in rats that were treated with various doses of bicyclol (150, 300, 600 mg/kg) once daily for 14 d. Animal behaviors, blood biochemical markers, blood and urine pictures were examined. Chronic toxicity test was conducted in 80 Wistar rats of both sexes. The animals were orally administered with various doses of bicyclol [150, 300, 600 mg/kg, 100-400 folds corresponding to the proposed therapeutic dose (1.5 mg/(kg·d)) of bicyclol for patients] once daily for 6 mo except for Sunday. The control group was given the same volume of 0.2% sodium carboxyl methylcellulose (Na-CMC). Twenty-one beagle dogs received bicyclol (25, 75, 225 mg/kg, 16.6, 50, 150 folds corresponding to the proposed therapeutic dose of bicyclol for patients) once a day for 6 mo except for Sunday. The body weight, food intake, urine and feces, blood picture, blood biochemical markers, and pathological examination of main organs were determined. Mutagenicity and teratogenicity were determined. Mutagenicity assay included Ames's test, chromosome aberration test in CHL cells and micronucleus test in mice. For the teratogenicity assay, pregnant Wistar rats weighing 200-250 g were treated with 0.2,1.0 g/kg bicyclol once daily from the 7th d of gestation for 10 d. RESULTS: The oral LD50 of bicyclol was over 5 g/kg in mice and rats. No noticeable alterations in subacute and chronic toxicity of rats and dogs were demonstrated. No mutagenicity and teratogenicity of bicyclol were found. CONCLUSION: Bicyclol has no detectable chronic toxicity as well as mutagenicity and teratogenicity in animals.展开更多
A polypyrrole-modified glassy carbon electrode （PPy/GC electrode） was prepared and its electrocatalytic behavior towards naphthoquinone in the presence of acid was characterized by linear sweep voltammetry （LSV）. ...A polypyrrole-modified glassy carbon electrode （PPy/GC electrode） was prepared and its electrocatalytic behavior towards naphthoquinone in the presence of acid was characterized by linear sweep voltammetry （LSV）. A well-defined new reduction peak appeared at a more positive potential than the original reduction peak. The new reduction peak current was linearly related to the acid value （AV） of oil. Based on it, a rapid electrochemical method for determining AV of transformer oil was developed using PPy/GC electrode. A working curve was obtained in the AV range of 0.01 to 0.40 mg（KOH）.g^-1, with a sensitivity of 39.42 μA0.5/（mg（KOH）.g-l） and the detection limit of 0.0014 mg（KOH）.g^-1 （signal-to-noise ratio is 3, standard deviation is 2.247%）. Moreover, the proposed method has been successfully applied to AV determination of several transformer oil samples with advantages of rapidness, high sensitivity and accuracy compared to the conventional method.展开更多
The design of variants to enhance conformational stability of proteins is an important aspect of protein engineering. Oligomeric proteins are often stabilized by aromatic clusters located within the subunit interfaces...The design of variants to enhance conformational stability of proteins is an important aspect of protein engineering. Oligomeric proteins are often stabilized by aromatic clusters located within the subunit interfaces. In the present study, the authors constructed five variants of Ps3aHSD （Pseudomonas sp. B-0831 3a-hydroxysteroid dehydrogenase） in which one or two residues at the dimer interface were replaced with aromatic residues, and examined the effects of introducing aromatic residues in this region on protein thermostability. Under their experimental conditions, all variants formed dimers, similar to wild-type Ps3aHSD. Thermal denaturation experiments indicated that Tm of all variants was 0.2-16.2 °C lower than that of wild-type protein, indicating less stable thanwild-type protein. The results collectively suggest that aromatic residues of natural oligomeric proteins are strictly posted in the interface to facilitate optimal interactions and avoid conformational strain.展开更多
The solubility of D-xylose in formic acid and binary solvents of formic acid with formic acid and acetic acid, propionic acid, n-butyric acid or isobutyric acid was measured in the temperature range from 300.35 to 325...The solubility of D-xylose in formic acid and binary solvents of formic acid with formic acid and acetic acid, propionic acid, n-butyric acid or isobutyric acid was measured in the temperature range from 300.35 to 325.05 K using the synthetic method by a laser monitoring technique at atmospheric pressure. The solid-liquid equilibrium data will provide essential support for industrial design and further theoretical study. The experimental data show that the solubility of D-xylose in formic acid and in the mixtures of formic acid + acetic acid(1︰1), formic acid + propionic acid(1︰1), formic acid + n-butyric acid(1︰1), and formic acid + isobutyric acid(1︰1) increases with temperature. The Apelblat equation, the λh model, and the ideal solution equation correlate the solubility data well.展开更多
AIM: To study glutamine synthetase (GS) activity and glutamate uptake in the hippocampus and frontal cortex (FC) from rats with prehepatic portal vein hypertension. METHODS: Male Wistar rats were divided into shamoper...AIM: To study glutamine synthetase (GS) activity and glutamate uptake in the hippocampus and frontal cortex (FC) from rats with prehepatic portal vein hypertension. METHODS: Male Wistar rats were divided into shamoperated group and a portal hypertension (PH) group with a regulated stricture of the portal vein. Animals were sacrificed by decapitation 14 d after portal vein stricture. GS activity was determined in the hippocampus and FC. Specific uptake of radiolabeled L-glutamate was studied using synaptosome-enriched fractions that were freshly prepared from both brain areas. RESULTS: We observed that the activity of GS increased in the hippocampus of PH rats, as compared to control animals, and decreased in the FC. A significant decrease in glutamate uptake was found in both brain areas, and was more marked in the hippocampus. The decrease in glutamate uptake might have been caused by a deficient transport function, signif icantly and persistent increase in this excitatory neurotransmitter activity. CONCLUSION: The presence of moderate ammonia blood levels may add to the toxicity of excitotoxic glutamate in the brain, which causes alterations in brain function. Portal vein stricture that causes portal hypertension modif ies the normal function in some brain regions.展开更多
Nitro and halogen substituted derivatives of the juglone naphthoquinone were synthesized and assayed for their antibacterial activity. 8-Nitrojuglone was obtained as the exclusive product from the direct nitration of ...Nitro and halogen substituted derivatives of the juglone naphthoquinone were synthesized and assayed for their antibacterial activity. 8-Nitrojuglone was obtained as the exclusive product from the direct nitration of juglone with nickel （Ⅱ） nitrate and p-toluenesulphonic acid. In addition, a series of five 8-halojuglone derivatives were synthesized via a solvent-free Friedel-Crafts acylation reaction. One of the acylation reactions afforded an anthraquinone-type derivative as the minor product. The 8-nitrojuglone derivative displayed the most notable activity against S. aureus. However, all of the 8-halojuglone derivatives were found to be less active than juglone against the bacteria assayed.展开更多
In weak acidic medium the alkaline cationic Safranine T interacts with acidic biological rnacromolecule heparin intensively causing the change of the molecular conformation, the maximum absorption wavelength and the a...In weak acidic medium the alkaline cationic Safranine T interacts with acidic biological rnacromolecule heparin intensively causing the change of the molecular conformation, the maximum absorption wavelength and the absorption value. The optimum experimental condition was given and a new method to determine the heparin was established. The linear range was 0.05-2.0 mg/L and the correlation coefficient was 0.9974. The method has been applied to analyze the samples and the results are satisfactory. Furthermore, the interaction mechanism was indicated.展开更多
A series of triethylammonium-based chlorogallate（Ⅲ） ionic liquids with varied Lewis acidity was synthesized, characterized, and firstly applied to isobutane alkylation. The [Et3NHC1]-GaCl3 with XGaCl3 =0.65 display...A series of triethylammonium-based chlorogallate（Ⅲ） ionic liquids with varied Lewis acidity was synthesized, characterized, and firstly applied to isobutane alkylation. The [Et3NHC1]-GaCl3 with XGaCl3 =0.65 displayed a potential catalytic activity for the alkylation. The addition of copper halide into the chlorogallate（Ⅲ） ionic liquids dramatically enhanced the alkylation reac- tion. Up to 70.1% Cs selectivity and 91.3 RON were achieved with the [Et3NHC1]-GaC13-CuC1 （XGaCl3 = 0.65, CuCI = 5% tool） under 0.5 MPa, 900 r/min, 15 min, 288 K using the industrial C4 cut （isobutane/butene = 10）. These results indicate that the chlorogallate（Ⅲ） system may be used as a promising catalyst for the C4 alkylation.展开更多
Frozen soils or those with permafrost cover large areas of the earth's surface and support unique vegetative ecosystems. Plants growing in such harsh conditions have adapted to small niches, which allow them to su...Frozen soils or those with permafrost cover large areas of the earth's surface and support unique vegetative ecosystems. Plants growing in such harsh conditions have adapted to small niches, which allow them to survive. In northern Alaska, USA, both moist acidic and non-acidic tundra occur, yet determination of frozen soil p Hs currently requires thawing of the soil so that electrometric pH methods can be utilized. Contrariwise, a portable X-ray fluorescence(PXRF) spectrometer was used in this study to assess elemental abundances and relate those characteristics to soil pH through predictive multiple linear regressions. Two operational modes, Soil Mode and Geochem Mode, were utilized to scan frozen soils in-situ and under laboratory conditions, respectively, after soil samples were dried and ground. Results showed that lab scanning produced optimal results with adjusted coefficient of determination(R^2) of 0.88 and 0.33 and root mean squared errors(RMSEs) of 0.87 and 0.34 between elemental data and lab-determined pH for Soil Mode and Geochem Mode, respectively. Even though the presence of ice attenuated fluoresced radiation under field conditions, adjusted R^2 and RMSEs between the datasets still provided reasonable model generalization(e.g., 0.73 and 0.49 for field Geochem Mode). Principal component analysis qualitatively separated multiple sampling sites based on elemental data provided by PXRF, reflecting differences in the chemical composition of the soils studied. Summarily, PXRF can be used for in-situ determination of soil pH in arctic environments without the need for sample modification and thawing. Furthermore, use of PXRF for determination of soil pH may provide higher sample throughput than traditional eletrometric-based methods, while generating elemental data useful for the prediction of multiple soil parameters.展开更多
OBJECTIVE: To evaluate the influence of the Tibetan medicine Ru Peng15 powder(RPP15) on uric acid levels, and explore its possible mechanisms of action in hyperuricemic animal models.METHODS: Hyperuricemic mice were g...OBJECTIVE: To evaluate the influence of the Tibetan medicine Ru Peng15 powder(RPP15) on uric acid levels, and explore its possible mechanisms of action in hyperuricemic animal models.METHODS: Hyperuricemic mice were generated by orally administering yeast extract paste twice daily(30 g/kg) for 8 days, to mimic human hyperuricemia induced by high-protein diets. Hyperuricemic rats were generated by intraperitoneal injection of 250 mg/kg potassium oxonate to each animal 1 h before the last oral administration of test compounds, which raised the serum uric acid level by inhibiting the decomposition of uric acid. Levels of uric acid and creatinine in serum and urine were detected by the phosphotungstic acid and picric acid methods respectively, and the activity of xanthine oxidase(XOD) was assayed using a commercial test kit.RESULTS: RPP15(0.4, 0.8, 1.2 g/kg) significantly decreased the level of serum uric acid in healthy rats(P < 0.05). Furthermore, hyperuricemic rats treated with RPP15(0.4, 0.8, 1.2 g/kg) had lower serum uric acid levels(P < 0.05), accompanied by lower urine uric acid(P < 0.05). For the hyperuricemic mice, the levels of uric acid in the serum decreased significantly(P < 0.05) and the activity of XOD in the liver was restored to normal levels after treatment with RPP15(P < 0.05).CONCLUSION: RPP15(0.4, 0.8, 1.2 g/kg) demonstrated an anti-hyperuricemic effect on both healthy and hyperuricemic animals, and the mechanism is most likely associated with inhibiting the activity of XOD.展开更多
基金Supported by the Grant From Ministry of Sciences and Technology of China, No.96-901-01 -45
文摘AIM: To study the toxicity of bicyclol to animals. METHODS: Acute toxicity test was performed in Kunming strain mice that were orally given bicyclol at the doses of 3 and 5 g/kg body weight, respectively. Wistar rats were orally administered bicyclol at a dose of 5 g/kg body weight. Death and clinical symptoms of animals were recorded within 7 d. Sub-acute toxicity test was carried out in rats that were treated with various doses of bicyclol (150, 300, 600 mg/kg) once daily for 14 d. Animal behaviors, blood biochemical markers, blood and urine pictures were examined. Chronic toxicity test was conducted in 80 Wistar rats of both sexes. The animals were orally administered with various doses of bicyclol [150, 300, 600 mg/kg, 100-400 folds corresponding to the proposed therapeutic dose (1.5 mg/(kg·d)) of bicyclol for patients] once daily for 6 mo except for Sunday. The control group was given the same volume of 0.2% sodium carboxyl methylcellulose (Na-CMC). Twenty-one beagle dogs received bicyclol (25, 75, 225 mg/kg, 16.6, 50, 150 folds corresponding to the proposed therapeutic dose of bicyclol for patients) once a day for 6 mo except for Sunday. The body weight, food intake, urine and feces, blood picture, blood biochemical markers, and pathological examination of main organs were determined. Mutagenicity and teratogenicity were determined. Mutagenicity assay included Ames's test, chromosome aberration test in CHL cells and micronucleus test in mice. For the teratogenicity assay, pregnant Wistar rats weighing 200-250 g were treated with 0.2,1.0 g/kg bicyclol once daily from the 7th d of gestation for 10 d. RESULTS: The oral LD50 of bicyclol was over 5 g/kg in mice and rats. No noticeable alterations in subacute and chronic toxicity of rats and dogs were demonstrated. No mutagenicity and teratogenicity of bicyclol were found. CONCLUSION: Bicyclol has no detectable chronic toxicity as well as mutagenicity and teratogenicity in animals.
基金Project(11JJ3015)supported by the Natural Science Foundation of Hunan Province,China
文摘A polypyrrole-modified glassy carbon electrode （PPy/GC electrode） was prepared and its electrocatalytic behavior towards naphthoquinone in the presence of acid was characterized by linear sweep voltammetry （LSV）. A well-defined new reduction peak appeared at a more positive potential than the original reduction peak. The new reduction peak current was linearly related to the acid value （AV） of oil. Based on it, a rapid electrochemical method for determining AV of transformer oil was developed using PPy/GC electrode. A working curve was obtained in the AV range of 0.01 to 0.40 mg（KOH）.g^-1, with a sensitivity of 39.42 μA0.5/（mg（KOH）.g-l） and the detection limit of 0.0014 mg（KOH）.g^-1 （signal-to-noise ratio is 3, standard deviation is 2.247%）. Moreover, the proposed method has been successfully applied to AV determination of several transformer oil samples with advantages of rapidness, high sensitivity and accuracy compared to the conventional method.
文摘The design of variants to enhance conformational stability of proteins is an important aspect of protein engineering. Oligomeric proteins are often stabilized by aromatic clusters located within the subunit interfaces. In the present study, the authors constructed five variants of Ps3aHSD （Pseudomonas sp. B-0831 3a-hydroxysteroid dehydrogenase） in which one or two residues at the dimer interface were replaced with aromatic residues, and examined the effects of introducing aromatic residues in this region on protein thermostability. Under their experimental conditions, all variants formed dimers, similar to wild-type Ps3aHSD. Thermal denaturation experiments indicated that Tm of all variants was 0.2-16.2 °C lower than that of wild-type protein, indicating less stable thanwild-type protein. The results collectively suggest that aromatic residues of natural oligomeric proteins are strictly posted in the interface to facilitate optimal interactions and avoid conformational strain.
基金Supported by Science and Technology Breakthrough Major Project in Henan Province(112101210200)
文摘The solubility of D-xylose in formic acid and binary solvents of formic acid with formic acid and acetic acid, propionic acid, n-butyric acid or isobutyric acid was measured in the temperature range from 300.35 to 325.05 K using the synthetic method by a laser monitoring technique at atmospheric pressure. The solid-liquid equilibrium data will provide essential support for industrial design and further theoretical study. The experimental data show that the solubility of D-xylose in formic acid and in the mixtures of formic acid + acetic acid(1︰1), formic acid + propionic acid(1︰1), formic acid + n-butyric acid(1︰1), and formic acid + isobutyric acid(1︰1) increases with temperature. The Apelblat equation, the λh model, and the ideal solution equation correlate the solubility data well.
基金Supported by Grant B013 from the University of Buenos Aires, Argentina and PIP 5869 from National Research Council of Argentina
文摘AIM: To study glutamine synthetase (GS) activity and glutamate uptake in the hippocampus and frontal cortex (FC) from rats with prehepatic portal vein hypertension. METHODS: Male Wistar rats were divided into shamoperated group and a portal hypertension (PH) group with a regulated stricture of the portal vein. Animals were sacrificed by decapitation 14 d after portal vein stricture. GS activity was determined in the hippocampus and FC. Specific uptake of radiolabeled L-glutamate was studied using synaptosome-enriched fractions that were freshly prepared from both brain areas. RESULTS: We observed that the activity of GS increased in the hippocampus of PH rats, as compared to control animals, and decreased in the FC. A significant decrease in glutamate uptake was found in both brain areas, and was more marked in the hippocampus. The decrease in glutamate uptake might have been caused by a deficient transport function, signif icantly and persistent increase in this excitatory neurotransmitter activity. CONCLUSION: The presence of moderate ammonia blood levels may add to the toxicity of excitotoxic glutamate in the brain, which causes alterations in brain function. Portal vein stricture that causes portal hypertension modif ies the normal function in some brain regions.
文摘Nitro and halogen substituted derivatives of the juglone naphthoquinone were synthesized and assayed for their antibacterial activity. 8-Nitrojuglone was obtained as the exclusive product from the direct nitration of juglone with nickel （Ⅱ） nitrate and p-toluenesulphonic acid. In addition, a series of five 8-halojuglone derivatives were synthesized via a solvent-free Friedel-Crafts acylation reaction. One of the acylation reactions afforded an anthraquinone-type derivative as the minor product. The 8-nitrojuglone derivative displayed the most notable activity against S. aureus. However, all of the 8-halojuglone derivatives were found to be less active than juglone against the bacteria assayed.
文摘In weak acidic medium the alkaline cationic Safranine T interacts with acidic biological rnacromolecule heparin intensively causing the change of the molecular conformation, the maximum absorption wavelength and the absorption value. The optimum experimental condition was given and a new method to determine the heparin was established. The linear range was 0.05-2.0 mg/L and the correlation coefficient was 0.9974. The method has been applied to analyze the samples and the results are satisfactory. Furthermore, the interaction mechanism was indicated.
基金the financial support from the Beijing Municipal Natural Science Foundation (2122052)Key Program of National Natural Science Foundation of China (21036007)National Basic Research Program of China (2009CB219904)
文摘A series of triethylammonium-based chlorogallate（Ⅲ） ionic liquids with varied Lewis acidity was synthesized, characterized, and firstly applied to isobutane alkylation. The [Et3NHC1]-GaCl3 with XGaCl3 =0.65 displayed a potential catalytic activity for the alkylation. The addition of copper halide into the chlorogallate（Ⅲ） ionic liquids dramatically enhanced the alkylation reac- tion. Up to 70.1% Cs selectivity and 91.3 RON were achieved with the [Et3NHC1]-GaC13-CuC1 （XGaCl3 = 0.65, CuCI = 5% tool） under 0.5 MPa, 900 r/min, 15 min, 288 K using the industrial C4 cut （isobutane/butene = 10）. These results indicate that the chlorogallate（Ⅲ） system may be used as a promising catalyst for the C4 alkylation.
文摘Frozen soils or those with permafrost cover large areas of the earth's surface and support unique vegetative ecosystems. Plants growing in such harsh conditions have adapted to small niches, which allow them to survive. In northern Alaska, USA, both moist acidic and non-acidic tundra occur, yet determination of frozen soil p Hs currently requires thawing of the soil so that electrometric pH methods can be utilized. Contrariwise, a portable X-ray fluorescence(PXRF) spectrometer was used in this study to assess elemental abundances and relate those characteristics to soil pH through predictive multiple linear regressions. Two operational modes, Soil Mode and Geochem Mode, were utilized to scan frozen soils in-situ and under laboratory conditions, respectively, after soil samples were dried and ground. Results showed that lab scanning produced optimal results with adjusted coefficient of determination(R^2) of 0.88 and 0.33 and root mean squared errors(RMSEs) of 0.87 and 0.34 between elemental data and lab-determined pH for Soil Mode and Geochem Mode, respectively. Even though the presence of ice attenuated fluoresced radiation under field conditions, adjusted R^2 and RMSEs between the datasets still provided reasonable model generalization(e.g., 0.73 and 0.49 for field Geochem Mode). Principal component analysis qualitatively separated multiple sampling sites based on elemental data provided by PXRF, reflecting differences in the chemical composition of the soils studied. Summarily, PXRF can be used for in-situ determination of soil pH in arctic environments without the need for sample modification and thawing. Furthermore, use of PXRF for determination of soil pH may provide higher sample throughput than traditional eletrometric-based methods, while generating elemental data useful for the prediction of multiple soil parameters.
基金Supported by the National Natural Sciences Foundation of China(A Study on the Anti-gout Effects and Related Mechanisms of Tibetan Medicine Rupeng15 Powder,No.81160410)
文摘OBJECTIVE: To evaluate the influence of the Tibetan medicine Ru Peng15 powder(RPP15) on uric acid levels, and explore its possible mechanisms of action in hyperuricemic animal models.METHODS: Hyperuricemic mice were generated by orally administering yeast extract paste twice daily(30 g/kg) for 8 days, to mimic human hyperuricemia induced by high-protein diets. Hyperuricemic rats were generated by intraperitoneal injection of 250 mg/kg potassium oxonate to each animal 1 h before the last oral administration of test compounds, which raised the serum uric acid level by inhibiting the decomposition of uric acid. Levels of uric acid and creatinine in serum and urine were detected by the phosphotungstic acid and picric acid methods respectively, and the activity of xanthine oxidase(XOD) was assayed using a commercial test kit.RESULTS: RPP15(0.4, 0.8, 1.2 g/kg) significantly decreased the level of serum uric acid in healthy rats(P < 0.05). Furthermore, hyperuricemic rats treated with RPP15(0.4, 0.8, 1.2 g/kg) had lower serum uric acid levels(P < 0.05), accompanied by lower urine uric acid(P < 0.05). For the hyperuricemic mice, the levels of uric acid in the serum decreased significantly(P < 0.05) and the activity of XOD in the liver was restored to normal levels after treatment with RPP15(P < 0.05).CONCLUSION: RPP15(0.4, 0.8, 1.2 g/kg) demonstrated an anti-hyperuricemic effect on both healthy and hyperuricemic animals, and the mechanism is most likely associated with inhibiting the activity of XOD.
