The title compounds 1-(4,5-dihydro-3-phenyl pyridine-1-yl)-2-(1H-1,2,4-triazole-1-yl) ethyl ketones were studied as a corrosion inhibitor in a mild steel in 1 mol /L hydrochloric acid solution using weight loss me...The title compounds 1-(4,5-dihydro-3-phenyl pyridine-1-yl)-2-(1H-1,2,4-triazole-1-yl) ethyl ketones were studied as a corrosion inhibitor in a mild steel in 1 mol /L hydrochloric acid solution using weight loss measurement, potentiodynamic polarization, and electrochemical impedance spectroscopy (EIS). Results indicated that these compounds had excellent inhibition properties. Polarization curves indicated that the inhibitor behaved mainly as mixed-type inhibitor. The EIS results showed that the charge transfer controlled the corrosion process in the uninhibited and inhibited solutions. Adsorption of the inhibitor on the mild steel surface followed Langmuir's adsorption isotherm with negative value of the free energy of adsorption ΔGads^o. The thermodynamic parameters of adsorption were determined and discussed.展开更多
The ethanolic extract of Kleinia grandiflora leaves was characterized and tested for its potential anticorrosion properties on mild steel in 1 M H2SO4 medium using mass-loss analysis, potentiodynamic polarization meas...The ethanolic extract of Kleinia grandiflora leaves was characterized and tested for its potential anticorrosion properties on mild steel in 1 M H2SO4 medium using mass-loss analysis, potentiodynamic polarization measurements, electrochemical impedance spectroscopy, Fourier-transform infrared spectroscopy, scanning electron microscopy, UV–visible spectroscopy, and X-ray diffraction analysis. The effect of temperature on the corrosion behavior of mild steel was studied in the range of 308 to 328 K. The inhibition efficiency was observed to increase with increasing concentration of the extract. Polarization curves revealed that the Kleinia grandiflora leaf extract is a mixed inhibitor. Impedance diagrams revealed that an increase of Kleinia grandiflora leaf extract concentration increased the charge transfer resistance and decreased the double-layer capacitance. The adsorption process obeys Langmuir's model, with a standard free energy of adsorption(ΔGads) of-18.62 k J/mol. The obtained results indicate that the Kleinia grandiflora leaf extract can serve as an effective inhibitor for the corrosion of mild steel in a sulfuric acid medium.展开更多
The corrosion inhibition of a green scale inhibitor, polyepoxysuccinic acid (PESA) was studied based on dynamic tests. It is found that when PESA is used alone, it had good corrosion inhibition. So, PESA should be inc...The corrosion inhibition of a green scale inhibitor, polyepoxysuccinic acid (PESA) was studied based on dynamic tests. It is found that when PESA is used alone, it had good corrosion inhibition. So, PESA should be included in the category of corrosion inhibitors. It is not only a kind of green scale inhibitor, but also a green corrosion inhibitor. The synergistic effect between PESA and Zn2+ or sodium gluconate is poor. However, the synergistic effect among PESA, Zn2+ and sodium gluconate is excellent, and the corrosion inhibition efficiency for carbon steel is higher than 99%. Further study of corrosion inhibition mechanism reveals that corrosion inhibition of PESA is not affected by carboxyl group, but by the oxygen atom inserted. The existence of oxygen atom in PESA molecular structure makes it easy to form stable chelate with pentacyclic structure.展开更多
AIM To study the molecular mechanisms ofretinoic acid(RA)on proliferation andexpression of cyclin-dependent kinase inhibitors(CKI),i.e.p16,p21 and p27 in cultured rathepatic stellate cells(HSC)stimulated withtransform...AIM To study the molecular mechanisms ofretinoic acid(RA)on proliferation andexpression of cyclin-dependent kinase inhibitors(CKI),i.e.p16,p21 and p27 in cultured rathepatic stellate cells(HSC)stimulated withtransforming growth factor beta 1(TGF-β1).METHODS HSC were isolated from healthy ratlivers and cultured.After stimulated with1 mg/L TGF-β1,subcultured HSC were treatedwith or without 1 nmol/L RA.MTT assay,immunocytochemistry(ICC)for p16,p21,p27and α-smooth muscle actin(α-SMA)protein,insitu hybridization(ISH)for retinoic acidreceptor beta 2(RAR-β2)and p16,p21 and p27mRNA and quantitative image analysis(partially)were performed.RESULTS RA inhibited HSC proliferation(41.50%,P【0.05),decreased the protein levelof α-SMA(55.09%,P【0.05),and induced HSCto express RAR-β2 mRNA.In addition,RAincreased the protein level of p16(218.75%,P【0.05)and induced p21 protein expression;meanwhile,p27 was undetectable by ICC in bothcontrol and RA-treated HSC.However,RA hadno influence on the mRNA levels of p16,p21 orp27 as determined by ISH.CONCLISION Up-regulation of p16 and p21 on post-transcriptional level may contribule, in part to RA inhibition of TGF-β1-initiated rat HSC activation in vitro.展开更多
Parietochloris incisa is an arachidonic acid rich snow green alga. The main physiological profiles, such as ash free dry weight (AFDW), chlorophyll, carotenoid, protein and total fatty acids (TFA), in this alga expose...Parietochloris incisa is an arachidonic acid rich snow green alga. The main physiological profiles, such as ash free dry weight (AFDW), chlorophyll, carotenoid, protein and total fatty acids (TFA), in this alga exposed to old culture supernatant (OCS) at the decline phase or its crude ethyl acetate extracts (CEAE) were investigated by using tubular photobioreactors of different diameters. Results showed that both OCS and CEAE had strong inhibitory effect on the above physiological parameters. The longer the culture was exposed to OCS and the more CEAE were added into the algal culture, the more the above physiological properties were inhibited. Arachidonic acid (AA), the dominant component of fatty acids in this alga, was also seriously inhibited with respect to total TFA, AFDW of cell mass, or culture volume, due to a probable reduction of enzymes activities catalyzing chain elongation from C18:1ω9 to AA. These results incontestably evidenced that some CEAE dissolving substances existing in OCS, like auto inhibitors, inhibited P. incisa growth through feedback. Hence, any efficient removal of auto inhibitors from algal culture to decrease their bioactivity could be good for maximal production of desired products like AA.展开更多
The effects of kojic acid on phenoloxidase (PO) of Plutella xylostella were investigated, when it had been partially purified by 40% saturated [(NH4)2SO4] and Sephadex G-100 gel filtration. Kojic acid showed inhibit...The effects of kojic acid on phenoloxidase (PO) of Plutella xylostella were investigated, when it had been partially purified by 40% saturated [(NH4)2SO4] and Sephadex G-100 gel filtration. Kojic acid showed inhibitory effects on both monophenolase and o-diphenolase activity of the PO. The inhibitor concentrations leading to 50% (IC50) activity lost were estimated to be 0.07 mmol L-1 for monophenolase and 1 mmol L-1 for diphenolase, respectively. Kojic acid can also prolong the lag time of PO for oxidation of L-tyrosine. The inhibition kinetics were analyzed by Lineweaver-Burk plots and kojic acid was found to be a reversible competitive inhibitor with the Ki of 0.47 mmol L-1. The ability of kojic acid to inhibit the enzyme activity may be associated with its ability to chelate copper at the active site. In addition, the iron ion was found to shorten the lag time obviously, but have no important effect on the monophenolase activity.展开更多
Corrosion inhibition of Al and Al-3.5Mg alloy by organic compounds, namely chalcones in hydrochloric acid solutions has been investigated by rapid polarization technique and weight loss method. Polarization measuremen...Corrosion inhibition of Al and Al-3.5Mg alloy by organic compounds, namely chalcones in hydrochloric acid solutions has been investigated by rapid polarization technique and weight loss method. Polarization measurements show that, the inhibitors act cathodically both in case of Al and Al-3.5Mg alloy. It was found from the weight loss measurements that, the inhibition efficiency depends on the substituent in the chalcone compound. The relative inhibitive efficiency of these compounds has been explained on the basis of structure dependent electron donor properties of the inhibitors and the metal inhibitor interaction on the surface. The inhibition efficiency ranges from 16 to 64% for Al and from 30% to 91% for Al-3.5Mg alloy展开更多
The ability of Cocos nucifera L.water(CW) as non-toxic corrosion inhibitor for acid corrosion of aluminium in 0.5 mol/L HCl has been studied using chemical technique.CW shows significant inhibition as corrosion inhi...The ability of Cocos nucifera L.water(CW) as non-toxic corrosion inhibitor for acid corrosion of aluminium in 0.5 mol/L HCl has been studied using chemical technique.CW shows significant inhibition as corrosion inhibitor,with 93%efficiency at the highest concentration of the inhibitor.The inhibitive action is attributed to the adsorption of the inhibitor molecules on metal surface following Langmuir adsorption isotherm.展开更多
A new method for the synthesis of 4, 4-diaryl/diheteroaryl-3-butenyl derivatives of nipecotic acid as GABA transporter inhibitors is described. The key intermediates 4-tosyl-1, 1-diaryl/diheteroaryl-1-butene 10a-d wer...A new method for the synthesis of 4, 4-diaryl/diheteroaryl-3-butenyl derivatives of nipecotic acid as GABA transporter inhibitors is described. The key intermediates 4-tosyl-1, 1-diaryl/diheteroaryl-1-butene 10a-d were synthesized by Wittig reaction, and followed by alkylation with (R)-3-piperidinecarboxylate. The resulting N-cycloalkylated amino acid esters 11a-d were saponified and then acidified to get the target compounds 1a-d. The preliminary bioassays showed that la-d exhibited excellent inhibition of [3H]-GABA uptake in vitro of culture cells.展开更多
Quantitative structure activity relationship (QSAR) studies were performed on 45 anthranilic acid derivatives for their potent allosteric inhibition activities of HCV NSSB polymerase. Genetic algorithm based genetic...Quantitative structure activity relationship (QSAR) studies were performed on 45 anthranilic acid derivatives for their potent allosteric inhibition activities of HCV NSSB polymerase. Genetic algorithm based genetic function approximation (GFA) method of variable selection was used to generate the model. Highly statistically significant model with r^2 = 0.966 and r^2cv = 0.951 was obtained when the number of descriptors in the equation was set to 5. High r^2pred value of 0.884 indicates the good predictive power of the best model. Spatial descriptors of radius of gyration (RadOfGration), molecular volume (Vm), length of molecule in the z dimension (Shadow-Zlength), thermodynamic descriptors of the octanol/water partition coefficient (LogP) and molecular refractivity index (MR) showed enormous contributions to HCV NS5B polymerase inhibition. The validation of the model was done by leave-one-out (LOO) test, randomization tests and external test set prediction. The model gives insight on indispensable structural requirements for the activity and can be used to design more potent analogs against HCV NSSB polymerase.展开更多
A study of Eruca vesicaria, Bromelia hemisphaerica and Erythrina americana as eco-friendly corrosion inhibitors for 1018 carbon steel in 0.5 M H<sub>2</sub>SO<sub>4</sub> has been carried out b...A study of Eruca vesicaria, Bromelia hemisphaerica and Erythrina americana as eco-friendly corrosion inhibitors for 1018 carbon steel in 0.5 M H<sub>2</sub>SO<sub>4</sub> has been carried out by using weight loss tests, potentiodynamic polarization curves and electrochemical impedance spectroscopy measuremnts. Results have shown that the three extracts performed as good corrosion inhibitors, but the Eruca vesicaria exhibited the best performance followed by Erythrina americana. The three inhibitors formed a protective, passive film which protected the steel from corrosion. This was because they contain antioxidants present in their molecular structure with heteroatoms such as N, C and O like phenols, amino acids, etc., which react with metal and environment to form the protective film.展开更多
The modern lifestyle caters to an increase in the incidence of peptic ulcer disease,gastroesophageal reflux disease and several other acid-related conditions of the gut. The drugs to prevent these conditions work eith...The modern lifestyle caters to an increase in the incidence of peptic ulcer disease,gastroesophageal reflux disease and several other acid-related conditions of the gut. The drugs to prevent these conditions work either through H2 receptor blockade or inhibition of the H^+, K^+ ATPase enzyme. Although proton pump inhibitors have been proven to be efficacious, they have a slow onset of action with limited resolution of symptoms in most patients. Potassium-competitive acid blockers(P-CABs) are novel drugs that bind reversibly to K^+ ions and block the H^+, K^+ ATPase enzyme, thus preventing acid production. P-CABs have a fast onset of action and have dose-dependent effects on acid production. Animal studies exist that differentiate the better results of P-CABs from proton pump inhibitors; further human trials will give a comprehensive picture of the results and will help to elucidate the therapeutic benefits of this new group of drugs.展开更多
In this work, we conducted a QSAR study on 18 molecules using descriptors from the Density Functional Theory (DFT) in order to predict the inhibitory activity of hydroxamic acids on histone deacetylase 7. This study i...In this work, we conducted a QSAR study on 18 molecules using descriptors from the Density Functional Theory (DFT) in order to predict the inhibitory activity of hydroxamic acids on histone deacetylase 7. This study is performed using the principal component analysis (PCA) method, the Ascendant Hierarchical Classification (AHC), the linear multiple regression method (LMR) and the nonlinear multiple regression (NLMR). DFT calculations were performed to obtain information on the structure and information on the properties on a series of hydroxamic acids compounds studied. Multivariate statistical analysis yielded two quantitative models (model MLR and model MNLR) with the quantum descriptors: electronic affinity (AE), vibration frequency of the OH bond (ν(OH)) and that of the NH bond (ν(NH)). The LMR model gives statistically significant results and shows a good predictability R2 = 0.9659, S = 0.488, F = 85 and p-value . Electronic affinity is the priority descriptor in predicting the activity of HDAC7 inhibitors in this study. The results obtained suggest that the descriptors derived from the DFT could be useful to predict the activity of histone deacetylase 7 inhibitors. These models were evaluated according to the criteria of Tropsha et al.展开更多
BACKGROUND: Nitric oxide synthase (NOS) inhibrtors have been widely used to investigate the role of NO on cerebral ischemic injury, but the results are controversial. Moreover, it has been considered to aggravate t...BACKGROUND: Nitric oxide synthase (NOS) inhibrtors have been widely used to investigate the role of NO on cerebral ischemic injury, but the results are controversial. Moreover, it has been considered to aggravate the ischemic neuronal damage with the release of excessively excitatory amino acids (EAA) during cerebral ischemia. On the other hand, some inhibitory amino acid is suggested to be important for the neuronal protection against ischemic brain damage. Our study has recently showed that treatment with the NOS inhibitor NG-nitro-L-arginine (L-NA) reduced focal cerebral ischemic damage. The effect of L-NA on the contents of excitatory and inhibitory amino acid in the rat brain following cerebral ischemia is still unclear. OBJECTIVE: By evaluating the effect of NOS inhibitor, L-NA on the contents of aspartate, glutamate, glycine and γ-aminobutyric acid (GABA) in striatum, hippocampus and cortex in the rat brain following cerebral ischemia respectively, to investigate the beneficial effect of L-NA on cerebral ischemic injury and the possible mechanism. DESIGN: A randomized and controlled experiment SETTING : Department of Pharmacology, Hebei Academy of Medical Sciences MATERIALS: A total of 42 male healthy SD rats (grade Ⅱ, weighting 250-300 g) were provided by the Experimental Animal Center of Hebei Province (Certification: 04036). Aspartate, glutamate, glycine, GABA, L-NA and 2,3,5-triphenyltetrazolium chloride (TTC) were obtained from Sigma Chemicals Co, St Louis, MO, USA. HPLC-ultraviolet detector system consisted of Agilent 1100 HPLC. METHODS: The experiment was carried out in Department of Pharmrcology, Hebei Academy of Medical Sciences from June 2005 to June 2006. Rats were randomly divided into three groups: sham-operated group (n = 6), ischemic group (n = 18), L-NA group (n = 18). The model of focal cerebral ischemia in rat was prepared with intraluminal line occlusion methods. In sham-operated rats, the external carotid artery was surgically prepared, but the filament was not inserted. Each group was further divided into 3 subgroups (n = 6 for each): drugs were administrated at 2, 6 and 12 hours after the middle cerebral artery occlusion (MCAO) respectively. L-NA (20 mg/kg, ip) was administrated, twice a day, for 3 consecutive days. Same volume of normal saline was administrated in ischemic and sham operation groups. The changes of infarcted volume and the contents of amino acids were respectively assayed. Image analysis software was used for the measurement of the infarcted area. The results were expressed as a percentage of the infarcted volume of cerebral/volume of whole brain (IV%) in order to control for edema formation. The contents of aspartate, glutamate, glycine and GABA in striatum, hippocampus and cortex in the rat brain following cerebral ischemia were respectively measured by HPLC method. All data were analyzed with one-way ANOVA and Dunnett's test. MAIN OUTCOME MEASURES: (1) The volume of cerebral infarction; (2) The contents of aspartate, glutamate glycine and GABA in brain tissue after cerebral ischemia. RESULTS : All 42 rats were involved in the final analysis. (1) Infarcted volume: Volume was 0 in sham-operated group. When L-NA was administrated at 2 and 6 hours after MCAO, the infarcted volume was (20.13±3.59)% and (23.12±5.84)% in L-NA group, which was not similar to that in ischemic group [(22.10±3.98)%, (25.38± 5.37)%, P〉 0.05]. However, the infarcted volume was markedly decreased compared with that of ischemic group when L-NA was administrated at 12 hours after MCAO [(26.11±3.55)% and (37.15±3.58)%, P 〈 0.01]. Changes of amino acid content: At 2 and 6 hours after ischemia, the contents of aspartate, glutamate, glycine and GABA in striatum, hippocampus and cortex in ischemic group were significantly increased compared with those in sham-operated group ( P〈 0.05-0.01). However, contents in L-NA group were similar to those in ischemic group (P 〉 0.05). At 12 hours after ischemia, the contents of aspartate [(0.21 ±0.06), (0.36±0.05), (0.29±0.12) mg/g] and glutamate [(0.55±0.06), (0.78±0.10), (0.52±0.10) mg/g] in striatum, hippocampus and cortex in L-NA group were significantly decreased compared with those in ischemic group [(0.49±0.17), (0.63± 0.03), (0.51±0.15) mg/g; (0.98±0.30), (1.15±0.15), (0.93±0.15) mg/g, P〈 0.05-0.01]. Glycine in hippocampus was (0.40±0.07) mg/g, which was higher than that in ischemic group [(0.21±0.07) mg/g, P 〈 0.05]. GABA in striatum, hippocampus and cortex was (0.93±0.10), (0.62±0.12) and (0.81 ±0.10) mg/g, respectively, which was higher than that in ischemic group [(0.60±0.08), (0.37±0.17), (0.59±0.10) mg/g, P 〈 0.05-0.01]. CONCLUSION : It may be concluded that L-NA have beneficial effect on ischemic cerebral injury in ischemic later stage in rats. The possible mechanism is that L-NA can decrease the contents of aspartate and glutamate, increase the contents of glycine and GABA.展开更多
AIM: To investigate the growth effects of 4-phenyl butyric acid (PBA) on human gastric carcinoma cells and their mechanisms. METHODS: Moderately-differentiated human gastric carcinoma SGC-7901 and lowly-differentiated...AIM: To investigate the growth effects of 4-phenyl butyric acid (PBA) on human gastric carcinoma cells and their mechanisms. METHODS: Moderately-differentiated human gastric carcinoma SGC-7901 and lowly-differentiated MGC-803 cells were treated with 5, 10, 20, 40, and 60 μmol/L PBA for 1-4 d. Cell proliferation was detected using the MTT colorimetric assay. Cell cycle distributions were examined using flow cytometry.RESULTS: The proliferation of gastric carcinoma cells was inhibited by PBA in a doseand time-dependent fashion. Flow cytometry showed that SGC-7901 cells treated with low concentrations of PBA were arrested at the G0/G1 phase, whereas cells treated with high concentrations of PBA were arrested at the G2/M phase. Although MGC-803 cells treated with low concentrations of PBA were also arrested at the G0/G1 phase, cells treated with high concentrations of PBA were arrested at the S phase. CONCLUSION: The growth inhibitory effect of PBA on gastric cancer cells is associated with alteration of the cell cycle. For moderately-differentiated gastric cancer cells, the cell cycle was arrested at the G0/G1 and G2/M phases. For lowly-differentiated gastric cancer cells, the cell cycle was arrested at the G0/G1 and S phases.展开更多
基金the financial of the Knowledge Innovation Program of the Chinese Academy of Sciences as a major guiding project(KZCX2-YW-210)as well as "Eleventh Five-Year" National Scientific and Technological Support Project(2007BAB27B00)
文摘The title compounds 1-(4,5-dihydro-3-phenyl pyridine-1-yl)-2-(1H-1,2,4-triazole-1-yl) ethyl ketones were studied as a corrosion inhibitor in a mild steel in 1 mol /L hydrochloric acid solution using weight loss measurement, potentiodynamic polarization, and electrochemical impedance spectroscopy (EIS). Results indicated that these compounds had excellent inhibition properties. Polarization curves indicated that the inhibitor behaved mainly as mixed-type inhibitor. The EIS results showed that the charge transfer controlled the corrosion process in the uninhibited and inhibited solutions. Adsorption of the inhibitor on the mild steel surface followed Langmuir's adsorption isotherm with negative value of the free energy of adsorption ΔGads^o. The thermodynamic parameters of adsorption were determined and discussed.
文摘The ethanolic extract of Kleinia grandiflora leaves was characterized and tested for its potential anticorrosion properties on mild steel in 1 M H2SO4 medium using mass-loss analysis, potentiodynamic polarization measurements, electrochemical impedance spectroscopy, Fourier-transform infrared spectroscopy, scanning electron microscopy, UV–visible spectroscopy, and X-ray diffraction analysis. The effect of temperature on the corrosion behavior of mild steel was studied in the range of 308 to 328 K. The inhibition efficiency was observed to increase with increasing concentration of the extract. Polarization curves revealed that the Kleinia grandiflora leaf extract is a mixed inhibitor. Impedance diagrams revealed that an increase of Kleinia grandiflora leaf extract concentration increased the charge transfer resistance and decreased the double-layer capacitance. The adsorption process obeys Langmuir's model, with a standard free energy of adsorption(ΔGads) of-18.62 k J/mol. The obtained results indicate that the Kleinia grandiflora leaf extract can serve as an effective inhibitor for the corrosion of mild steel in a sulfuric acid medium.
文摘The corrosion inhibition of a green scale inhibitor, polyepoxysuccinic acid (PESA) was studied based on dynamic tests. It is found that when PESA is used alone, it had good corrosion inhibition. So, PESA should be included in the category of corrosion inhibitors. It is not only a kind of green scale inhibitor, but also a green corrosion inhibitor. The synergistic effect between PESA and Zn2+ or sodium gluconate is poor. However, the synergistic effect among PESA, Zn2+ and sodium gluconate is excellent, and the corrosion inhibition efficiency for carbon steel is higher than 99%. Further study of corrosion inhibition mechanism reveals that corrosion inhibition of PESA is not affected by carboxyl group, but by the oxygen atom inserted. The existence of oxygen atom in PESA molecular structure makes it easy to form stable chelate with pentacyclic structure.
基金the National Natural Science Foundation of China,No.39670287the Scientific Research Foundation for Doctorate Education,State Education Commission.No.96026530
文摘AIM To study the molecular mechanisms ofretinoic acid(RA)on proliferation andexpression of cyclin-dependent kinase inhibitors(CKI),i.e.p16,p21 and p27 in cultured rathepatic stellate cells(HSC)stimulated withtransforming growth factor beta 1(TGF-β1).METHODS HSC were isolated from healthy ratlivers and cultured.After stimulated with1 mg/L TGF-β1,subcultured HSC were treatedwith or without 1 nmol/L RA.MTT assay,immunocytochemistry(ICC)for p16,p21,p27and α-smooth muscle actin(α-SMA)protein,insitu hybridization(ISH)for retinoic acidreceptor beta 2(RAR-β2)and p16,p21 and p27mRNA and quantitative image analysis(partially)were performed.RESULTS RA inhibited HSC proliferation(41.50%,P【0.05),decreased the protein levelof α-SMA(55.09%,P【0.05),and induced HSCto express RAR-β2 mRNA.In addition,RAincreased the protein level of p16(218.75%,P【0.05)and induced p21 protein expression;meanwhile,p27 was undetectable by ICC in bothcontrol and RA-treated HSC.However,RA hadno influence on the mRNA levels of p16,p21 orp27 as determined by ISH.CONCLISION Up-regulation of p16 and p21 on post-transcriptional level may contribule, in part to RA inhibition of TGF-β1-initiated rat HSC activation in vitro.
文摘Parietochloris incisa is an arachidonic acid rich snow green alga. The main physiological profiles, such as ash free dry weight (AFDW), chlorophyll, carotenoid, protein and total fatty acids (TFA), in this alga exposed to old culture supernatant (OCS) at the decline phase or its crude ethyl acetate extracts (CEAE) were investigated by using tubular photobioreactors of different diameters. Results showed that both OCS and CEAE had strong inhibitory effect on the above physiological parameters. The longer the culture was exposed to OCS and the more CEAE were added into the algal culture, the more the above physiological properties were inhibited. Arachidonic acid (AA), the dominant component of fatty acids in this alga, was also seriously inhibited with respect to total TFA, AFDW of cell mass, or culture volume, due to a probable reduction of enzymes activities catalyzing chain elongation from C18:1ω9 to AA. These results incontestably evidenced that some CEAE dissolving substances existing in OCS, like auto inhibitors, inhibited P. incisa growth through feedback. Hence, any efficient removal of auto inhibitors from algal culture to decrease their bioactivity could be good for maximal production of desired products like AA.
基金The study was supperted by the State Science and Technology Commission of China(30270887).
文摘The effects of kojic acid on phenoloxidase (PO) of Plutella xylostella were investigated, when it had been partially purified by 40% saturated [(NH4)2SO4] and Sephadex G-100 gel filtration. Kojic acid showed inhibitory effects on both monophenolase and o-diphenolase activity of the PO. The inhibitor concentrations leading to 50% (IC50) activity lost were estimated to be 0.07 mmol L-1 for monophenolase and 1 mmol L-1 for diphenolase, respectively. Kojic acid can also prolong the lag time of PO for oxidation of L-tyrosine. The inhibition kinetics were analyzed by Lineweaver-Burk plots and kojic acid was found to be a reversible competitive inhibitor with the Ki of 0.47 mmol L-1. The ability of kojic acid to inhibit the enzyme activity may be associated with its ability to chelate copper at the active site. In addition, the iron ion was found to shorten the lag time obviously, but have no important effect on the monophenolase activity.
文摘Corrosion inhibition of Al and Al-3.5Mg alloy by organic compounds, namely chalcones in hydrochloric acid solutions has been investigated by rapid polarization technique and weight loss method. Polarization measurements show that, the inhibitors act cathodically both in case of Al and Al-3.5Mg alloy. It was found from the weight loss measurements that, the inhibition efficiency depends on the substituent in the chalcone compound. The relative inhibitive efficiency of these compounds has been explained on the basis of structure dependent electron donor properties of the inhibitors and the metal inhibitor interaction on the surface. The inhibition efficiency ranges from 16 to 64% for Al and from 30% to 91% for Al-3.5Mg alloy
文摘The ability of Cocos nucifera L.water(CW) as non-toxic corrosion inhibitor for acid corrosion of aluminium in 0.5 mol/L HCl has been studied using chemical technique.CW shows significant inhibition as corrosion inhibitor,with 93%efficiency at the highest concentration of the inhibitor.The inhibitive action is attributed to the adsorption of the inhibitor molecules on metal surface following Langmuir adsorption isotherm.
文摘A new method for the synthesis of 4, 4-diaryl/diheteroaryl-3-butenyl derivatives of nipecotic acid as GABA transporter inhibitors is described. The key intermediates 4-tosyl-1, 1-diaryl/diheteroaryl-1-butene 10a-d were synthesized by Wittig reaction, and followed by alkylation with (R)-3-piperidinecarboxylate. The resulting N-cycloalkylated amino acid esters 11a-d were saponified and then acidified to get the target compounds 1a-d. The preliminary bioassays showed that la-d exhibited excellent inhibition of [3H]-GABA uptake in vitro of culture cells.
基金supported by the National Natural Science Foundation of China (No. 30500339)Natural Science Foundation of Zhejiang Province (NO.Y407308)the Sprout Talented Project Program of Zhejiang Province (No. 2008R40G2020019)
文摘Quantitative structure activity relationship (QSAR) studies were performed on 45 anthranilic acid derivatives for their potent allosteric inhibition activities of HCV NSSB polymerase. Genetic algorithm based genetic function approximation (GFA) method of variable selection was used to generate the model. Highly statistically significant model with r^2 = 0.966 and r^2cv = 0.951 was obtained when the number of descriptors in the equation was set to 5. High r^2pred value of 0.884 indicates the good predictive power of the best model. Spatial descriptors of radius of gyration (RadOfGration), molecular volume (Vm), length of molecule in the z dimension (Shadow-Zlength), thermodynamic descriptors of the octanol/water partition coefficient (LogP) and molecular refractivity index (MR) showed enormous contributions to HCV NS5B polymerase inhibition. The validation of the model was done by leave-one-out (LOO) test, randomization tests and external test set prediction. The model gives insight on indispensable structural requirements for the activity and can be used to design more potent analogs against HCV NSSB polymerase.
文摘A study of Eruca vesicaria, Bromelia hemisphaerica and Erythrina americana as eco-friendly corrosion inhibitors for 1018 carbon steel in 0.5 M H<sub>2</sub>SO<sub>4</sub> has been carried out by using weight loss tests, potentiodynamic polarization curves and electrochemical impedance spectroscopy measuremnts. Results have shown that the three extracts performed as good corrosion inhibitors, but the Eruca vesicaria exhibited the best performance followed by Erythrina americana. The three inhibitors formed a protective, passive film which protected the steel from corrosion. This was because they contain antioxidants present in their molecular structure with heteroatoms such as N, C and O like phenols, amino acids, etc., which react with metal and environment to form the protective film.
文摘The modern lifestyle caters to an increase in the incidence of peptic ulcer disease,gastroesophageal reflux disease and several other acid-related conditions of the gut. The drugs to prevent these conditions work either through H2 receptor blockade or inhibition of the H^+, K^+ ATPase enzyme. Although proton pump inhibitors have been proven to be efficacious, they have a slow onset of action with limited resolution of symptoms in most patients. Potassium-competitive acid blockers(P-CABs) are novel drugs that bind reversibly to K^+ ions and block the H^+, K^+ ATPase enzyme, thus preventing acid production. P-CABs have a fast onset of action and have dose-dependent effects on acid production. Animal studies exist that differentiate the better results of P-CABs from proton pump inhibitors; further human trials will give a comprehensive picture of the results and will help to elucidate the therapeutic benefits of this new group of drugs.
文摘In this work, we conducted a QSAR study on 18 molecules using descriptors from the Density Functional Theory (DFT) in order to predict the inhibitory activity of hydroxamic acids on histone deacetylase 7. This study is performed using the principal component analysis (PCA) method, the Ascendant Hierarchical Classification (AHC), the linear multiple regression method (LMR) and the nonlinear multiple regression (NLMR). DFT calculations were performed to obtain information on the structure and information on the properties on a series of hydroxamic acids compounds studied. Multivariate statistical analysis yielded two quantitative models (model MLR and model MNLR) with the quantum descriptors: electronic affinity (AE), vibration frequency of the OH bond (ν(OH)) and that of the NH bond (ν(NH)). The LMR model gives statistically significant results and shows a good predictability R2 = 0.9659, S = 0.488, F = 85 and p-value . Electronic affinity is the priority descriptor in predicting the activity of HDAC7 inhibitors in this study. The results obtained suggest that the descriptors derived from the DFT could be useful to predict the activity of histone deacetylase 7 inhibitors. These models were evaluated according to the criteria of Tropsha et al.
基金the Natural Sci-ence Foundation of HebeiProvince, No. C2005000840
文摘BACKGROUND: Nitric oxide synthase (NOS) inhibrtors have been widely used to investigate the role of NO on cerebral ischemic injury, but the results are controversial. Moreover, it has been considered to aggravate the ischemic neuronal damage with the release of excessively excitatory amino acids (EAA) during cerebral ischemia. On the other hand, some inhibitory amino acid is suggested to be important for the neuronal protection against ischemic brain damage. Our study has recently showed that treatment with the NOS inhibitor NG-nitro-L-arginine (L-NA) reduced focal cerebral ischemic damage. The effect of L-NA on the contents of excitatory and inhibitory amino acid in the rat brain following cerebral ischemia is still unclear. OBJECTIVE: By evaluating the effect of NOS inhibitor, L-NA on the contents of aspartate, glutamate, glycine and γ-aminobutyric acid (GABA) in striatum, hippocampus and cortex in the rat brain following cerebral ischemia respectively, to investigate the beneficial effect of L-NA on cerebral ischemic injury and the possible mechanism. DESIGN: A randomized and controlled experiment SETTING : Department of Pharmacology, Hebei Academy of Medical Sciences MATERIALS: A total of 42 male healthy SD rats (grade Ⅱ, weighting 250-300 g) were provided by the Experimental Animal Center of Hebei Province (Certification: 04036). Aspartate, glutamate, glycine, GABA, L-NA and 2,3,5-triphenyltetrazolium chloride (TTC) were obtained from Sigma Chemicals Co, St Louis, MO, USA. HPLC-ultraviolet detector system consisted of Agilent 1100 HPLC. METHODS: The experiment was carried out in Department of Pharmrcology, Hebei Academy of Medical Sciences from June 2005 to June 2006. Rats were randomly divided into three groups: sham-operated group (n = 6), ischemic group (n = 18), L-NA group (n = 18). The model of focal cerebral ischemia in rat was prepared with intraluminal line occlusion methods. In sham-operated rats, the external carotid artery was surgically prepared, but the filament was not inserted. Each group was further divided into 3 subgroups (n = 6 for each): drugs were administrated at 2, 6 and 12 hours after the middle cerebral artery occlusion (MCAO) respectively. L-NA (20 mg/kg, ip) was administrated, twice a day, for 3 consecutive days. Same volume of normal saline was administrated in ischemic and sham operation groups. The changes of infarcted volume and the contents of amino acids were respectively assayed. Image analysis software was used for the measurement of the infarcted area. The results were expressed as a percentage of the infarcted volume of cerebral/volume of whole brain (IV%) in order to control for edema formation. The contents of aspartate, glutamate, glycine and GABA in striatum, hippocampus and cortex in the rat brain following cerebral ischemia were respectively measured by HPLC method. All data were analyzed with one-way ANOVA and Dunnett's test. MAIN OUTCOME MEASURES: (1) The volume of cerebral infarction; (2) The contents of aspartate, glutamate glycine and GABA in brain tissue after cerebral ischemia. RESULTS : All 42 rats were involved in the final analysis. (1) Infarcted volume: Volume was 0 in sham-operated group. When L-NA was administrated at 2 and 6 hours after MCAO, the infarcted volume was (20.13±3.59)% and (23.12±5.84)% in L-NA group, which was not similar to that in ischemic group [(22.10±3.98)%, (25.38± 5.37)%, P〉 0.05]. However, the infarcted volume was markedly decreased compared with that of ischemic group when L-NA was administrated at 12 hours after MCAO [(26.11±3.55)% and (37.15±3.58)%, P 〈 0.01]. Changes of amino acid content: At 2 and 6 hours after ischemia, the contents of aspartate, glutamate, glycine and GABA in striatum, hippocampus and cortex in ischemic group were significantly increased compared with those in sham-operated group ( P〈 0.05-0.01). However, contents in L-NA group were similar to those in ischemic group (P 〉 0.05). At 12 hours after ischemia, the contents of aspartate [(0.21 ±0.06), (0.36±0.05), (0.29±0.12) mg/g] and glutamate [(0.55±0.06), (0.78±0.10), (0.52±0.10) mg/g] in striatum, hippocampus and cortex in L-NA group were significantly decreased compared with those in ischemic group [(0.49±0.17), (0.63± 0.03), (0.51±0.15) mg/g; (0.98±0.30), (1.15±0.15), (0.93±0.15) mg/g, P〈 0.05-0.01]. Glycine in hippocampus was (0.40±0.07) mg/g, which was higher than that in ischemic group [(0.21±0.07) mg/g, P 〈 0.05]. GABA in striatum, hippocampus and cortex was (0.93±0.10), (0.62±0.12) and (0.81 ±0.10) mg/g, respectively, which was higher than that in ischemic group [(0.60±0.08), (0.37±0.17), (0.59±0.10) mg/g, P 〈 0.05-0.01]. CONCLUSION : It may be concluded that L-NA have beneficial effect on ischemic cerebral injury in ischemic later stage in rats. The possible mechanism is that L-NA can decrease the contents of aspartate and glutamate, increase the contents of glycine and GABA.
基金Supported by Natural Science Foundation of Ningbo, No. 2009A610134Natural Sciences Foundation of Zhejiang, No. Y207244+3 种基金College Students’ Science-Technology Innovation Program of Zhejiang Province, No. 200959the Excellent Disser-tation Foundation of Ningbo University, No. 201014KC Wong Magna Fund of Ningbo Universitythe Scientific Innovation Team Project of Ningbo, No.2011B82014
文摘AIM: To investigate the growth effects of 4-phenyl butyric acid (PBA) on human gastric carcinoma cells and their mechanisms. METHODS: Moderately-differentiated human gastric carcinoma SGC-7901 and lowly-differentiated MGC-803 cells were treated with 5, 10, 20, 40, and 60 μmol/L PBA for 1-4 d. Cell proliferation was detected using the MTT colorimetric assay. Cell cycle distributions were examined using flow cytometry.RESULTS: The proliferation of gastric carcinoma cells was inhibited by PBA in a doseand time-dependent fashion. Flow cytometry showed that SGC-7901 cells treated with low concentrations of PBA were arrested at the G0/G1 phase, whereas cells treated with high concentrations of PBA were arrested at the G2/M phase. Although MGC-803 cells treated with low concentrations of PBA were also arrested at the G0/G1 phase, cells treated with high concentrations of PBA were arrested at the S phase. CONCLUSION: The growth inhibitory effect of PBA on gastric cancer cells is associated with alteration of the cell cycle. For moderately-differentiated gastric cancer cells, the cell cycle was arrested at the G0/G1 and G2/M phases. For lowly-differentiated gastric cancer cells, the cell cycle was arrested at the G0/G1 and S phases.