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1.
Braz. j. microbiol ; 49(2): 258-268, Apr.-June 2018. graf
Article in English | LILACS | ID: biblio-889233

ABSTRACT

Abstract Cellulosimicrobium cellulans CWS2, a novel strain capable of utilizing benzo(a)pyrene (BaP) as the sole carbon and energy source under nitrate-reducing conditions, was isolated from PAH-contaminated soil. Temperature and pH significantly affected BaP biodegradation, and the strain exhibited enhanced biodegradation ability at temperatures above 30 °C and between pH 7 and 10. The highest BaP removal rate (78.8%) was observed in 13 days when the initial BaP concentration was 10 mg/L, and the strain degraded BaP at constant rate even at a higher concentration (50 mg/L). Metal exposure experimental results illustrated that Cd(II) was the only metal ion that significantly inhibited biodegradation of BaP. The addition of 0.5 and 1.0 g/L glucose enhanced BaP biodegradation, while the addition of low-molecular-weight organic acids with stronger acidity reduced BaP removal rates during co-metabolic biodegradation. The addition of phenanthrene and pyrene, which were degraded to some extent by the strain, showed no distinct effect on BaP biodegradation. Gas chromatography-mass spectrometry (GC-MS) analysis revealed that the five rings of BaP opened, producing compounds with one to four rings which were more bioavailable. Thus, the strain exhibited strong BaP degradation capability and has great potential in the remediation of BaP-/PAH-contaminated environments.


Subject(s)
Soil Microbiology , Soil Pollutants/metabolism , Benzo(a)pyrene/metabolism , Actinobacteria/isolation & purification , Actinobacteria/metabolism , Temperature , Cadmium/metabolism , Carbon/metabolism , Carboxylic Acids/metabolism , Biotransformation , Actinobacteria/classification , Culture Media/chemistry , Enzyme Inhibitors/metabolism , Glucose/metabolism , Hydrogen-Ion Concentration , Anaerobiosis , Gas Chromatography-Mass Spectrometry
2.
Braz. j. microbiol ; 46(2): 367-375, Apr-Jun/2015. tab, graf
Article in English | LILACS | ID: lil-749711

ABSTRACT

The pH of the culture medium directly influences the growth of microorganisms and the chemical processes that they perform. The aim of this study was to assess the influence of the initial pH of the culture medium on the production of 11 low-molecular-weight organic acids and on the solubilization of calcium phosphate by bacteria in growth medium (NBRIP). The following strains isolated from cowpea nodules were studied: UFLA03-08 (Rhizobium tropici), UFLA03-09 (Acinetobacter sp.), UFLA03-10 (Paenibacillus kribbensis), UFLA03-106 (Paenibacillus kribbensis) and UFLA03-116 (Paenibacillus sp.). The strains UFLA03-08, UFLA03-09, UFLA03-10 and UFLA03-106 solubilized Ca3(PO4)2 in liquid medium regardless of the initial pH, although without a significant difference between the treatments. The production of organic acids by these strains was assessed for all of the initial pH values investigated, and differences between the treatments were observed. Strains UFLA03-09 and UFLA03-10 produced the same acids at different initial pH values in the culture medium. There was no correlation between phosphorus solubilized from Ca3(PO4)2 in NBRIP liquid medium and the concentration of total organic acids at the different initial pH values. Therefore, the initial pH of the culture medium influences the production of organic acids by the strains UFLA03-08, UFLA03-09, UFLA03-10 and UFLA03-106 but it does not affect calcium phosphate solubilization.


Subject(s)
Acinetobacter/metabolism , Carboxylic Acids/metabolism , Culture Media/chemistry , Paenibacillus/metabolism , Phosphates/metabolism , Rhizobium tropici/metabolism , Acinetobacter/growth & development , Acinetobacter/isolation & purification , Fabaceae/microbiology , Hydrogen-Ion Concentration , Paenibacillus/growth & development , Paenibacillus/isolation & purification , Rhizobium tropici/growth & development , Rhizobium tropici/isolation & purification , Root Nodules, Plant/microbiology
3.
Acta Pharmaceutica Sinica ; (12): 332-336, 2015.
Article in Chinese | WPRIM | ID: wpr-251775

ABSTRACT

To discover novel fluoroquinolone lead compounds as possible anti-infective or/and antitumor chemotherapies, combination principle of pharmacophore-based drug design, a series of novel tricyclic fluoroquinolone title compounds, [1,2,4]triazino[3,4-h][1,8]naphthyridine-8-one-7-carboxylic acid derivatives ( 5a-5p), were designed and synthesized with a fused [1,2,4]-triazine ring unit. Their structures were characterized by spectral data and elemental analysis and the in vitro antibacterial and anti-cell proliferation activities were also evaluated. The results showed that the titled compounds exhibited more significant inhibitory activities against drug-resistant bacteria (Methicillin-resistant Staphylococcus aureus and multi drug-resistant Escherichia coli strains) and three tested cancer cell lines (human hepatoma SMMC-7721, murine leukemia L1210 and human murine leukemia HL60 cells). Interestingly, SAR showed that compounds with electron-donating groups attached to benzene ring had stronger antibacterial activity than antitumor activity, but electron-withdrawing compounds displayed more potential antitumor activity than antibacterial activity, especially antitumor activity of nitro compounds was comparable to comparison doxorubicin. Thus, novel triazine-fused tricyclic fluoroquinolones as potent anti-infective or/and antitumor lead compounds are valuable to pay attention and for further development.


Subject(s)
Animals , Anti-Bacterial Agents , Chemistry , Antineoplastic Agents , Chemistry , Carboxylic Acids , Carcinoma, Hepatocellular , Cell Line , Cell Proliferation , Drug Design , Escherichia coli , Fluoroquinolones , Chemistry , HL-60 Cells , Humans , Leukemia L1210 , Liver Neoplasms , Methicillin-Resistant Staphylococcus aureus , Mice , Naphthyridines , Triazines
4.
Biol. Res ; 48: 1-8, 2015. ilus, graf, tab
Article in English | LILACS | ID: biblio-950788

ABSTRACT

BACKGROUND: The development of clean or novel alternative energy has become a global trend that will shape the future of energy. In the present study, 3 microbial strains with different oxygen requirements, including Clostridium acetobutylicum ATCC 824, Enterobacter cloacae ATCC 13047 and Kluyveromyces marxianus 15D, were used to construct a hydrogen production system that was composed of a mixed aerobic-facultative anaerobic-anaerobic consortium. The effects of metal ions, organic acids and carbohydrate substrates on this system were analyzed and compared using electrochemical and kinetic assays. It was then tested using small-scale experiments to evaluate its ability to convert starch in 5 L of organic wastewater into hydrogen. For the one-step biohydrogen production experiment, H1 medium (nutrient broth and potato dextrose broth) was mixed directly with GAM broth to generate H2 medium (H1 medium and GAM broth). Finally, Clostridium acetobutylicum ATCC 824, Enterobacter cloacae ATCC 13047 and Kluyveromyces marxianus 15D of three species microbial co-culture to produce hydrogen under anaerobic conditions. For the two-step biohydrogen production experiment, the H1 medium, after cultured the microbial strains Enterobacter cloacae ATCC 13047 and Kluyveromyces marxianus 15D, was centrifuged to remove the microbial cells and then mixed with GAM broth (H2 medium). Afterward, the bacterial strain Clostridium acetobutylicum ATCC 824 was inoculated into the H2 medium to produce hydrogen by anaerobic fermentation. RESULTS: The experimental results demonstrated that the optimum conditions for the small-scale fermentative hydrogen production system were at pH 7.0, 35°C, a mixed medium, including H1 medium and H2 medium with 0.50 mol/L ferrous chloride, 0.50 mol/L magnesium sulfate, 0.50 mol/L potassium chloride, 1% w/v citric acid, 5% w/v fructose and 5% w/v glucose. The overall hydrogen production efficiency in the shake flask fermentation group was 33.7 mL/h-1.L-1, and those the two-step and the one-step processes of the small-scale fermentative hydrogen production system were 41.2 mLVh-1.L-1 and 35.1 mL/h-1.L-1, respectively. CONCLUSION: Therefore, the results indicate that the hydrogen production efficiency of the two-step process is higher than that of the one-step process.


Subject(s)
Fermentation/physiology , Microbial Consortia/physiology , Hydrogen/metabolism , Industrial Waste , Starch/metabolism , Time Factors , Kluyveromyces/metabolism , Carboxylic Acids/metabolism , Feasibility Studies , Enterobacter cloacae/metabolism , Coculture Techniques , Clostridium acetobutylicum/metabolism , Electric Conductivity , Microbial Interactions/physiology , Renewable Energy , Waste Water/analysis , Hydrogen/analysis , Ions/metabolism , Metals/metabolism
5.
Article in Chinese | WPRIM | ID: wpr-815220

ABSTRACT

OBJECTIVE@#To investigate correlation between the change in metabolic components of serum and the abnormal balgam syndrome by using a rat model of abnormal balgam syndrome.@*METHODS@#Male Wistar rats were randomly divided into a control group and a test group. According to Uyghur medicine theory, the test group of rats were given wet cold diet (seeds of spinach and parsley, 24 hours) in a cold (6 °C) and humid (85%-95%, 10 hours) environment for 40 days to establish the rat model of abnormal balgam syndrome. 1H MR based metabonomic analysis of serum was performed. Data was analyzed using Orthogonal Partial Least Squares-Discriminant Analysis (OPLS-DA) software.@*RESULTS@#Compared with the control group, the serum components including glutamate, phenylalanine, tyrosine, citric acid, β-hydrocxy butyrate, acetoacetate, pyruvic acid and creatine were decreased, while the glucose, lactic acid, low density lipoprotein and very low density lipoprotein were increased in the test group (P<0.05).@*CONCLUSION@#The low energy production and consumption in the rat model of abnormal balgam syndrome suggests that the dysfunctional metabolisms of three major nutrients might be the molecular basis for the abnormal balgam syndrome.


Subject(s)
Animals , Blood Glucose , Carboxylic Acids , Blood , Creatine , Blood , Disease Models, Animal , Lipoproteins, LDL , Blood , Male , Medicine, Chinese Traditional , Metabolomics , Rats , Rats, Wistar , Syndrome
6.
Braz. j. microbiol ; 45(3): 937-943, July-Sept. 2014. graf, tab
Article in English | LILACS | ID: lil-727024

ABSTRACT

Strain P17 was a bacterial strain identified as Bacillus megaterium isolated from ground accumulating phosphate rock powder. The fermentation broth of strain P17 and the yellow-brown soil from Nanjing Agricultural University garden were collected to conduct this study. The simulation of fixed insoluble phosphorous forms after applying calcium superphosphate into yellow-brown soil was performed in pots, while available P and total P of soil were extremely positive correlative with those of groundwater. Then the dissolving effect of strain P17 on insoluble P of yellow-brown soil was studied. Results showed that Bacillus megaterium strain P17 had notable solubilizing effect on insoluble phosphates formed when too much water-soluble phosphorous fertilizer used. During 100 days after inoculation, strain P17 was dominant. Until the 120th day, compared with water addition, available P of strain P17 inoculation treated soil increased by 3 times with calcium superphosphate addition. Besides available P, pH, activity of acid and alkaline phosphatase and population of P-solubilizing microbes were detected respectively. P-solubilizing mechanism of P-solubilizing bacteria strain P17 seems to be a synergetic effect of pH decrease, organic acids, phosphatase, etc.


Subject(s)
Bacillus megaterium/metabolism , Calcium Phosphates/metabolism , Phosphorus/metabolism , Soil/chemistry , Bacillus megaterium/isolation & purification , Carboxylic Acids/metabolism , Hydrogen-Ion Concentration , Phosphoric Monoester Hydrolases/metabolism , Soil Microbiology
7.
Asia Oceania Journal of Nuclear Medicine and Biology. 2014; 2 (2): 87-94
in English | IMEMR | ID: emr-167751

ABSTRACT

We performed a phase IIa clinical trial of trans-1-amino-3-[18]Ffluoro-cyclobutane carboxylic acid [anti-[18]F-FACBC], a synthetic amino acid analog for PET, in patients with metastatic prostate cancer. The study subjects consisted of 10 untreated prostate cancer patients having lymph node and/or bone metastasis. Five patients underwent whole-body PET 5 and 30 min after intravenous injection of anti-[18]F-FACBC. The other five patients underwent 60 min dynamic PET of the pelvis. Safety assessment was performed before and 24 h after injection. PET/CT images were assessed visually, and time courses of anti-[18]F-FACBC uptake were evaluated from dynamic imaging. Two mild adverse events were observed and resolved without treatment. All 10 patients showed increased accumulation of anti-[18]F-FACBC in the primary prostate lesion. CT revealed five enlarged lymph nodes indicating metastasis, and all showed increased uptake. Additionally, anti-[18]F-FACBC PET delineated unenlarged lymph nodes as hot spots. Anti-[18]F-FACBC PET demonstrated metastatic bone lesions, similar to conventional imaging. In one of two patients with lung metastasis, some lesions showed increased uptake. Regarding the time course, increased uptake of anti-[18]F-FACBC in the lesion was demonstrated immediately after injection, followed by gradual washout. The results of this phase IIa clinical trial indicated the safety of anti-[18]F-FACBC in patients with prostate cancer and the potential of anti-[18]F-FACBC PET to delineate primary prostate lesions and metastatic lesions. This clinical trial was registered as JapicCTI-101326


Subject(s)
Humans , Male , Prostatic Neoplasms/secondary , Carboxylic Acids , Neoplasm Metastasis , Positron-Emission Tomography , Cyclobutanes
8.
Article in English | WPRIM | ID: wpr-812298

ABSTRACT

A significant number of organic carboxylic acids have been shown to influence the absorption and distribution of drugs mediated by organic anion transporters (OATs). In this study, uptake experiments were performed to assess the inhibitory effects of cinnamic acid, ferulic acid, oleanolic acid, deoxycholic acid, and cynarin on hOAT1, hOAT3, hOATP1B1, and hOATP2B1. After a drug-drug interaction (DDI) investigation, cinnamic acid, ferulic acid, deoxycholic acid, and cynarin were found and validated to inhibit hOAT1 in a competitive manner, and deoxycholic acid was found to be an inhibitor of all four transporters. The apparent 50% inhibitory concentrations of cinnamic acid, ferulic acid, deoxycholic acid, and cynarin were estimated to be 133.87, 3.69, 90.03 and 6.03 μmol·L(-1) for hOAT1, respectively. The apparent 50% inhibitory concentrations of deoxycholic acid were estimated to be 9.57 μmol·L(-1) for hOAT3, 70.54 μmol·L(-1) for hOATP1B1, and 168.27 μmol·L(-1) for hOATP2B1. Because cinnamic acid, ferulic acid, and cynarin are ingredients of food or food additives, the present study suggests there are new food-drug interactions to be disclosed. In addition, deoxycholic acid may be used as a probe for studying the correlation of OATs and OATPs.


Subject(s)
Carboxylic Acids , Pharmacology , Cinnamates , Pharmacology , Coumaric Acids , Pharmacology , Deoxycholic Acid , Pharmacology , Diet , Drug Interactions , HEK293 Cells , Humans , Organic Anion Transport Protein 1 , Organic Anion Transporters , Plant Extracts , Pharmacology , Plants, Medicinal , Chemistry
9.
Article in Chinese | WPRIM | ID: wpr-300214

ABSTRACT

To investigate formation mechanism of secologanic acid sulfonates in sulfur-fumigated buds of Lonicera japonica, secologanic acid was enriched and purified from the sun-dried buds of L. japonica by various column chromatography on macroporus resin HPD-100, silica gel and ODS. The stimulation experiments of sulfur-fumigation process were carried out using secologanic acid reacted with SO2 in the aqueous solution. The reaction mechanism could be involved in the esterification or addition reaction. The present investigation provides substantial evidences for interpreting formation pathway of secologanic acid sulfonates in sulfur-fumigated buds of L. japonica.


Subject(s)
Alkanesulfonates , Chemistry , Carboxylic Acids , Chemistry , Chromatography, High Pressure Liquid , Flowers , Chemistry , Lonicera , Chemistry , Models, Chemical , Molecular Structure , Sulfur , Chemistry , Pharmacology , Sulfur Dioxide , Chemistry , Water , Chemistry
10.
Braz. j. microbiol ; 44(4): 1121-1131, Oct.-Dec. 2013. ilus, graf, tab
Article in English | LILACS | ID: lil-705292

ABSTRACT

Among the native yeasts found in alcoholic fermentation, rough colonies associated with pseudohyphal morphology belonging to the species Saccharomyces cerevisiae are very common and undesirable during the process. The aim of this work was to perform morphological and physiological characterisations of S. cerevisiae strains that exhibited rough and smooth colonies in an attempt to identify alternatives that could contribute to the management of rough colony yeasts in alcoholic fermentation. Characterisation tests for invasiveness in Agar medium, killer activity, flocculation and fermentative capacity were performed on 22 strains (11 rough and 11 smooth colonies). The effects of acid treatment at different pH values on the growth of two strains ("52" -rough and "PE-02" smooth) as well as batch fermentation tests with cell recycling and acid treatment of the cells were also evaluated. Invasiveness in YPD Agar medium occurred at low frequency; ten of eleven rough yeasts exhibited flocculation; none of the strains showed killer activity; and the rough strains presented lower and slower fermentative capacities compared to the smooth strains in a 48-h cycle in a batch system with sugar cane juice. The growth of the rough strain was severely affected by the acid treatment at pH values of 1.0 and 1.5; however, the growth of the smooth strain was not affected. The fermentative efficiency in mixed fermentation (smooth and rough strains in the same cell mass proportion) did not differ from the efficiency obtained with the smooth strain alone, most likely because the acid treatment was conducted at pH 1.5 in a batch cell-recycle test. A fermentative efficiency as low as 60% was observed with the rough colony alone.


Subject(s)
Alcohols/metabolism , Saccharomyces cerevisiae/growth & development , Saccharomyces cerevisiae/metabolism , Carboxylic Acids/metabolism , Culture Media/chemistry , Fermentation , Hydrogen-Ion Concentration , Saccharomyces cerevisiae/drug effects
11.
Article in English | IMSEAR | ID: sea-163307

ABSTRACT

The matrix metalloproteinase-13 (MMP-13) inhibitory activities of carboxylic acid based compounds, in presence and absence of bovine serum albumin (BSA), have been analyzed quantitatively in terms of chemometric descriptors. The statistically validated quantitative structure-activity relationship (QSAR) models obtained through combinatorial protocol in multiple linear regression (CP-MLR) analysis and the participated descriptors in these models provided rationales to explain the inhibitory activities of these congeners. For MMP-13 inhibition activity, the identified descriptors (BEHm1, BELm1 and BEHm8) have highlighted the role of the atomic mass in terms of the highest and lowest eigenvalues derived from Burden matrix. The positive correlation with activity suggested that their higher values are desirable in improving the activity of a compound. Additionally, the descriptor C-027 representing R-CH-X type fragment in a molecular structure advocates the absence of such type of fragment for the improved activity. On the other hand presence of RCO-N< or >N-X=X type fragment (descriptor N-072) would be beneficiary to the MMP-13 inhibitory activity. The structural features, rationalized by the descriptors MSD (Balaban’s mean square distance index), nCrHR (number of ring tertiary C (sp3), H-047 (H attached to C1(sp3)/C0(sp2)) and H-050 (H attached to heteroatom) have imparted positive impact on the MMP-13 w/BSA inhibition activity. The atomic properties such as atomic polarizability and atomic Sanderson’s electronegativity have shown their positive impact on the activity via descriptors BELp4 and GATS3e in respective eigenvalues or lag. The other descriptors, MATS1m and MATS3e, have revealed the negative influence of atomic mass and electronegativity on the of MMP-13 w/BSA inhibition activity. The results obtained from CP-MLR analysis have been supported further through partial least-squares (PLS) study.


Subject(s)
Carboxylic Acids/analogs & derivatives , Carboxylic Acids/analysis , Carboxylic Acids/metabolism , Enzyme Inhibitors/chemistry , Linear Models , Matrix Metalloproteinase Inhibitors/analysis , Matrix Metalloproteinase Inhibitors/chemistry , Models, Chemical , Molecular Structure , Quantitative Structure-Activity Relationship
12.
Acta Pharmaceutica Sinica ; (12): 149-154, 2013.
Article in Chinese | WPRIM | ID: wpr-235689

ABSTRACT

The purpose of this study is to investigate the intracellular transporters effect and the cytotoxicity of carboxyl nanodiamond (CND) - podophyllotoxin (PPT). Nanodiamond (ND) was treated with mixed carboxylic acid and finally got 64 nm CND by centrifugation, and then it was reacted with PPT to form CND-PPT. UV spectrophotometry was used to calculate the content of PPT in CND-PPT, the particle size distribution and zeta potential were measured by Dynamic laser scattering instrument. CND, PPT, CND-PPT and CND + PPT (physical mixture of CND and PPT) were characterized by Fourier transform infrared spectroscopy, at the same time, thermal analysis and element analysis were used to estimate the content of the PPT in CND-PPT. The affect of CND, PPT, CND-PPT on HeLa cell was measured with MTT assay. The results showed that content of PPT combined with CND accounted for about 10%. MTT assay showed that CND has low cytotoxicity and CND-PPT can increase the water soluble of PPT. As a conclusion, CND as a hydrophilic pharmaceutical carrier combined with PPT is able to increase the water solubility of PPT, at low concentration, CND-PPT can enhance the antitumor activity in comparison with PPT, so CND can be used as a potential anticancer drug carrier.


Subject(s)
Antineoplastic Agents, Phytogenic , Chemistry , Pharmacology , Carboxylic Acids , Chemistry , Drug Carriers , HeLa Cells , Humans , Nanodiamonds , Chemistry , Particle Size , Podophyllotoxin , Chemistry , Pharmacology , Solubility , Spectrophotometry, Ultraviolet , Spectroscopy, Fourier Transform Infrared
13.
Braz. j. microbiol ; 44(2): 629-637, 2013. ilus, tab
Article in English | LILACS | ID: lil-688594

ABSTRACT

The endophytic strain Zong1 isolated from root nodules of the legume Sophora alopecuroides was characterized by conducting physiological and biochemical tests employing gfp-marking, observing their plant growth promoting characteristics (PGPC) and detecting plant growth parameters of inoculation assays under greenhouse conditions. Results showed that strain Zong1 had an effective growth at 28 ºC after placed at 4-60 ºC for 15 min, had a wide range pH tolerance of 6.0-11.0 and salt tolerance up to 5% of NaCl. Zong1 was resistant to the following antibiotics (µg/mL): Phosphonomycin (100), Penicillin (100) and Ampicillin (100). It could grow in the medium supplemented with 1.2 mmol/L Cu, 0.1% (w/v) methylene blue and 0.1-0.2% (w/v) methyl red, respectively. Zong1 is closely related to Pseudomonas chlororaphis based on analysis the sequence of 16S rRNA gene. Its expression of the gfp gene indicated that strain Zong1 may colonize in root or root nodules and verified by microscopic observation. Furthermore, co-inoculation with Zong1 and SQ1 (Mesorhizobium sp.) showed significant effects compared to single inoculation for the following PGPC parameters: siderophore production, phosphate solubilization, organic acid production, IAA production and antifungal activity in vitro. These results suggest strains P. chlororaphi Zong1 and Mesorhizobium sp. SQ1 have better synergistic or addictive effect. It was noteworthy that each growth index of co-inoculated Zong1+SQ1 in growth assays under greenhouse conditions is higher than those of single inoculation, and showed a significant difference (p < 0.05) when compared to a negative control. Therefore, as an endophyte P. chlororaphis Zong1 may play important roles as a potential plantgrowth promoting agent.


Subject(s)
Endophytes/isolation & purification , Endophytes/metabolism , Pseudomonas/isolation & purification , Pseudomonas/metabolism , Sophora/microbiology , Antibiosis , Anti-Bacterial Agents/pharmacology , Cluster Analysis , Carboxylic Acids/metabolism , DNA, Bacterial/chemistry , DNA, Bacterial/genetics , DNA, Ribosomal/chemistry , DNA, Ribosomal/genetics , Endophytes/classification , Endophytes/genetics , Fungi/growth & development , Hydrogen-Ion Concentration , Indoleacetic Acids/metabolism , Molecular Sequence Data , Phylogeny , Plant Development , Phosphates/metabolism , Plant Roots/microbiology , Pseudomonas/classification , Pseudomonas/genetics , /genetics , Sequence Analysis, DNA , Siderophores/metabolism , Sodium Chloride/metabolism , Sophora/growth & development , Temperature
14.
Acta Pharmaceutica Sinica ; (12): 1710-1715, 2013.
Article in Chinese | WPRIM | ID: wpr-298021

ABSTRACT

In this study, the adsorption behavior of epirubicin hydrochloride (EPI) on carboxylated single-walled carbon nanotubes (c-SWNTs) obtained by mixture acid treatment was investigated. The results indicated that the dispersion of c-SWNTs in water was obviously improved. The absorption of EPI on c-SWNTs came to equilibrium after 240 min and could be explained by pseudo-second-order model. Moreover, there were heterogeneous distribution of active sites onto c-SWNTs surface and the Freundlich isotherm model was better fit to describe the absorption precess of EPI on c-SWNTs. The absorption capacity of EPI on c-SWNTs increased obviously with the increasing pH and decreasing temperature. Compared with multi-walled carbon nanotubes, carboxylated multi-walled carbon nanotubes, SWNTs, c-SWNTs possessed higher absorption capacity for EPI. The controlled, targeted and sustained release of EPI from c-SWNTs-EPI could be instructive for the development of nano-carrier.


Subject(s)
Adsorption , Antibiotics, Antineoplastic , Chemistry , Carboxylic Acids , Chemistry , Drug Carriers , Epirubicin , Chemistry , Nanotubes, Carbon , Chemistry
15.
Arch. latinoam. nutr ; 62(4): 389-390, dic. 2012. ilus, tab
Article in Spanish | LILACS | ID: lil-714894

ABSTRACT

Volatiles from aqueous extract of peppermint commercial sachets were investigated through gas chromatography/flame ionization detection (GC/FID) and GC/mass spectrometry (MS). Samples were prepared under similar conditions as in homemade tea. Volatiles were isolated using solid phase extraction method (SPE) with Porapak Q trap followed by desorption with acetone. Estimated mean values for short and medium chain carboxylic acids (C2- C12) and ketones lay in the range of 50-64 μg kg-1 whilst aliphatic alcohols and acyclic hydrocarbons had values lower than 6 μg kg-1. The major volatiles were terpenes (275-382 μg kg-1) that reached 89 % of the total composition. A total of 16 compounds, among them dodecane, acetoin, acetol, citral, geraniol and octanoic acid have been described by the first time in peppermint tea. These findings could be attributed to the different analytical approach employed, mainly to the use of different extraction/pre-concentration techniques. Given the apparently lower proportion of terpenes in the aqueous extract it may be that the chemical properties of the peppermint essential oil are not entirely reproduced with homemade tea.


Estudo da composição da fração volátil do extrato aquoso de sachês de hortelã pimenta (Mentha piperita L.) através da extração em fase sólida. O princípio desse trabalho foi investigar a fração volátil do extrato aquoso de sachês comerciais de hortelã pimenta usando cromatografia gasosa com detectores de ionização em chama e de massas. As amostras foram preparadas em condições similares às usadas para o preparo do chá caseiro. Os compostos voláteis foram isolados via método de extração em fase sólida com adsorvente Porapak Q e eluídos com acetona. Uma estimativa dos valores médios dos ácidos carboxílicos de cadeias média e curta ficou na faixa de 50-64 μg kg-1, enquanto alcoóis alifáticos e hidrocarbonetos acíclicos tiveram valores menores do que 6 μg kg-1. Os terpenos (275-382 μg kg-1) foram os compostos majoritários alcançando 89 % dos sólidos totais. Um total de 16 compostos voláteis, entre eles, dodecano, acetoína, acetol, citral, geraniol e ácido octanóico foram descritos pela primeira vez no chá de hortelã pimenta. Esses resultados poderiam ser atribuídos aos diferentes métodos analíticos empregados, principalmente devido ao uso de diferentes técnicas de extração e pré-concentração. Em função da proporção menor de terpenos no extrato aquoso é razoável especular que as propriedades químicas do óleo essencial da hortelã pimenta não sejam totalmente reproduzidas com o consumo do chá caseiro.


Subject(s)
Mentha piperita/chemistry , Oils, Volatile/analysis , Plant Extracts/analysis , Solid Phase Extraction/standards , Tea/chemistry , Volatile Organic Compounds/analysis , Carboxylic Acids/analysis , Flame Ionization , Gas Chromatography-Mass Spectrometry , Ketones/analysis , Mass Spectrometry/standards , Plant Leaves/chemistry , Terpenes/analysis
16.
Article in English | WPRIM | ID: wpr-146184

ABSTRACT

Carboxylic acids play an important role in both aerobic and anaerobic metabolic pathways of both the snail and the parasite. Monitoring the effects of infection by schistosome on Biomphalaria alexandrina carboxylic acids metabolic profiles represents a promising additional source of information about the state of metabolic system. We separated and quantified pyruvic, fumaric, malic, oxalic, and acetic acids using ion-suppression reversed-phase high performance liquid chromatography (HPLC) to detect correlations between these acids in both hemolymph and digestive gland gonad complex (DGG's) samples in a total of 300 B. alexandrina snails (150 infected and 150 controls) at different stages of infection. The results showed that the majority of metabolite pairs did not show significant correlations. However, some high correlations were found between the studied acids within the control group but not in other groups. More striking was the existence of reversed correlations between the same acids at different stages of infection. Some possible explanations of the underlying mechanisms were discussed. Ultimately, however, further data are required for resolving the responsible regulatory events. These findings highlight the potential of metabolomics as a novel approach for fundamental investigations of host-pathogen interactions as well as disease surveillance and control.


Subject(s)
Animals , Biomphalaria/chemistry , Carboxylic Acids/analysis , Chromatography, High Pressure Liquid , Gastrointestinal Tract/chemistry , Hemolymph/chemistry , Schistosoma mansoni/chemistry
17.
Article in Chinese | WPRIM | ID: wpr-246573

ABSTRACT

<p><b>OBJECTIVE</b>To compare the production of organic acid of different genotype Streptococcus mutans (S. mutans) isolated from children with different caries experience.</p><p><b>METHODS</b>66 strains of S.mutans isolated from dental plaques of children aged from 3 to 5 with different caries experience were chosen as test bacteria. The quantities of organic acid include formic acid, acetic acid and lactic acid which produced by different genotype of S. mutans, were measured by gas chromatograph.</p><p><b>RESULTS</b>There were significant difference in production of organic acid among the different genotypes of S. mutans isolated from children with different caries susceptibility, and so were the strains isolated from children within the same caries susceptibility (P < 0.05). The more genotypes the strain had, the more organic acid it produced (P < 0.05). Among all the organic acid, the quantity of lactic acid was much more than that of formic acid and acetic acid.</p><p><b>CONCLUSIONS</b>There were significant difference in the ability of the strains with different genotypes to produce organic acid, and the more genotypes it has, the more organic acid it produced.</p>


Subject(s)
Carboxylic Acids , Metabolism , Child, Preschool , Dental Caries , Microbiology , Dental Plaque , Microbiology , Genotype , Humans , Streptococcus mutans , Genetics , Metabolism
18.
Acta Pharmaceutica Sinica ; (12): 1017-1024, 2010.
Article in Chinese | WPRIM | ID: wpr-353392

ABSTRACT

A series of adefovir mono-L-amino acid esters, mono non-steroidal anti-inflammatory drugs carboxylic ester prodrugs with more potent anti-HBV activity and lower nephrotoxicity were designed and synthesized. Adefovir bis (L-amino acid) ester was used as lead compound, according to pathological and pharmacological findings that non-steroidal anti-inflammatory drugs can effectively inhibit the organic anion transporter 1 (hOAT1)-mediated adefovir phosphonic acid pairs of anion transport across tubular basement membrane thereby reducing the nephrotoxicity of adefovir. Flatten design principle was used to introducing non-steroidal anti-inflammatory drugs structural fragments to design and synthesize target adefovir mixture ester prodrugs. HepG2 2.2.15 cell line was used as in vitro anti-HBV activity evaluation model. Five compounds exhibited antiviral activity, and compound 18 showed the most potent anti-HBV activity and relatively high selective index (EC50 3.92 micromol L(-1), SI 9.97). HK-2 cell line was used as in vitro model to evaluate nephrotoxicity. Results suggested the target compounds have lower cytotoxicity than the positive control. Moreover, by analyzing the primary structure and activity relationship of these compounds, it could suggest that mono-L-amino acid ester, mono non-steroidal anti-inflammatory drugs carboxylic ester prodrugs strategy has significant potential in the acyclic nucleoside phosphonates prodrug design.


Subject(s)
Adenine , Chemistry , Pharmacology , Amino Acids , Chemistry , Pharmacology , Anti-Inflammatory Agents, Non-Steroidal , Chemistry , Pharmacology , Antiviral Agents , Chemistry , Pharmacology , Carboxylic Acids , Chemistry , Pharmacology , Cell Survival , Drug Design , Hep G2 Cells , Humans , Kidney Tubules, Proximal , Cell Biology , Metabolism , L-Lactate Dehydrogenase , Metabolism , Molecular Structure , Organophosphonates , Chemistry , Pharmacology , Prodrugs , Chemistry , Pharmacology
19.
Article in Chinese | WPRIM | ID: wpr-328052

ABSTRACT

<p><b>OBJECTIVE</b>To isolate and purify gallic acid and brevifolincarboxylic acid simultaneously by high-speed counter-current chromatography (HSCCC) from a crude extract of Polygonum capitatum.</p><p><b>METHOD</b>The biphasic solvent system composed of ethyl acetate-n-butanol-0.44% acetic acid (3:1:5) was used at a flow rate of 2.0 mL x min(-1), while the aqueous phase was selected as the mobile phase and the apparatus was rotated at 860 r x min(-1). The effluent was detected at 272 nm.</p><p><b>RESULT</b>51.5 mg of gallic acid and 5.9 mg of brevifolincarboxylic acid were separated from 1.07 g of the crude extract with the purities of 99.7% and 97.5%, respectively, while brevifolincarboxylic acid was obtained firstly from the genus Polygonum. The structures of the compounds were identified by ultraviolet spectrometry (UV), infra-red spectrometry (IR), liquid chromatography/mass spectrometry (LC/MS), time-of-flight mass spectrometry( TOF-MS), 1H-nuclear magnetic resonance (NMR) and 13C-NMR.</p><p><b>CONCLUSION</b>This method is feasible and rapid for isolation and purification of gallice acid and brevifolincarboxylil acid.</p>


Subject(s)
Carboxylic Acids , Countercurrent Distribution , Methods , Gallic Acid , Plant Extracts , Polygonum , Chemistry
20.
Chinese Journal of Biotechnology ; (12): 1795-1807, 2009.
Article in Chinese | WPRIM | ID: wpr-336302

ABSTRACT

Nitriles are an important type of synthetic intermediates in the production of fine chemicals because of their easy preparations and versatile transformations. The traditional chemical conversion of nitriles to carboxylic acids and amides is feasible but it requires relatively harsh conditions of heat, acid or alkali. Nitrile converting enzymes (nitrilase, nitrile hydratase and amidase) which are used as biocatalyst for the production of fine chemicals have attracted substantial interest because of their ability to convert readily available nitriles into the corresponding higher value amides or acids under mild conditions with excellent chemo-, regio- and stereo-selectivities. Many nitrile converting enzymes have been explored and widely used for the production of fine chemicals. In this paper, various examples of biocatalytic synthesis of pharmaceuticals and their intermediates, agrochemicals and their intermediates, food and feed additives, and other fine chemicals are presented. In the near future, an increasing number of novel nitrile converting enzymes will be screened and their potential in the production of useful fine chemicals will be further exploited.


Subject(s)
Amides , Metabolism , Amidohydrolases , Metabolism , Aminohydrolases , Metabolism , Carboxylic Acids , Metabolism , Chemical Industry , Methods , Hydro-Lyases , Metabolism , Nitriles , Chemistry
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