Aim To establish a LC-MS method for determining the concentration of nifedipine in human plasma and to evaluate the pharmacokinetic characteristics of nifedipine sustained-release tablets. Methods A XB-C18 (5 μm, 4....Aim To establish a LC-MS method for determining the concentration of nifedipine in human plasma and to evaluate the pharmacokinetic characteristics of nifedipine sustained-release tablets. Methods A XB-C18 (5 μm, 4.6 mm ×150 mm) column and a mobile phase of methanol: 0.01 mol·L^-1ammonium acetate (60:40, V/V) were used to separate nifedipine, the detections was accuracy under atmosperic pressure electronic spray ionization (AP-ESI) mode and ion mass spectrum (m/z) of 314.9 [M+H]^+ for nifedipine, and 320.8 [M+H]^+ for lorazepam (Internal Standard, IS). Results The linear range of nifedipine was 0.3 - 80 ng·mL^-1 ( r = 0.9997), and the limit of quantitation (LOQ) was 0.3 ng·mL^-1. The nifedipine pharmacokinetic parameters after a single dose of 20 mg nifedipine sustained-release tablets test (T) or reference (R) were as the followings, t1/2 (6.73 ± 2.00) h and (7.04 ± 2.18) h, Tmax (4.28 ± 0.70) h and (4.48 ± 0.70) h, Cmax(39.66 ± 10.58) ng·mL^-1 and (40.19 ± 10.97) ng·mL^-1, AUC0-36 (391.63 ± 108.55) ng·mL^-1·h and (387.57 ± 121.51) ng·mL^-1·h, and AUC0-∞ (408.28 ± 121.16) ng·mL^-1·h and (406.15 ± 133.13) ng·mL^-1·h. The relative bioavailability of nifedipine sustained-release tablets (test) was (103.02 ± 13.93) %. Conclusion LC-MS method for the determination of concentrations of nifedipine in human plasma was sensitive and accurate, and could be used in nifedipine bioavailability and pharmacokinetic studies.展开更多
Modified classical Boltzmann entropy as generalized entropy, then proposed Maximum Generalized Entropy Principle fusing physics and biology, and established a new model for biological origin and evolutions based on th...Modified classical Boltzmann entropy as generalized entropy, then proposed Maximum Generalized Entropy Principle fusing physics and biology, and established a new model for biological origin and evolutions based on this principle, finally took protein evolution for an example to analyze. The model provided some reference for biological complexity research.展开更多
A new HPLC MS method to determine loratadine in human plasma was established. The method involved extracting drug with organic solvent under basic conditions. The samples were seperated by ODS column and determined ...A new HPLC MS method to determine loratadine in human plasma was established. The method involved extracting drug with organic solvent under basic conditions. The samples were seperated by ODS column and determined by mass detector. The calibration curve of loratadine was linear within the range of 0.4~100 ng·mL -1 with r=0.9995 . The recovery of this method was within 95%~104%, within day and between day RSD were less than 12%. To study the pharmacokinetics and relative bioavailability of loratadine tablets, two formulations of loratadine tablets were given to 18 healthy male volunteers according to a randomized 2 way cross over design. The C max , AUC 0 t and T max values of the two formulations were 51.89±20.18 ng·mL -1 and 52.48±22.35 ng·mL -1 ; 140.75±88.42 ng·h·mL -1 and 147.24±92.33 ng·h·mL -1 ; 0.81±0.35 h and 0.81±0.27 h respectively. Results from statistic analysis showed that there were no significant difference between the C max , AUC 0-t and T max values of the two formulations. The relative bioavailability of tablets I with respect to tablets II was 97%±13% from the AUC 0 t measurement. Bioequivalance was observed between the two tablets.展开更多
Middle-sized chambers (40cmx40cmx20 cm) and an infrared gas analyzer (IRGA) were used for the measurement of net photosynthesis of the grass layer and soil CO2 evolution, in Quercus liaotungensis Koidz. forest, which ...Middle-sized chambers (40cmx40cmx20 cm) and an infrared gas analyzer (IRGA) were used for the measurement of net photosynthesis of the grass layer and soil CO2 evolution, in Quercus liaotungensis Koidz. forest, which is a typical temperate forest ecosystem in the mountainous areas of Beijing. Changes of CO2 concentrations in both the atmosphere (2m above canopy) and the forest canopy (2m below the top of the canopy) together with those of net photosynthesis and soil CO2 evolution were also examined, in order to find the characteristics of CO2 exchange between the different components of the temperate forest ecosystem and the atmosphere. Atmospheric CO2 averaged (323+10) and (330+1) mol mol-1 respectively in summer and autumn. During the 24-hour measurements, large differences as much as -46 and -61 mol mol-1 respectively in the atmosphere and forest were found. Net photosynthesis of the grass layer in summer was (2. 59 9+ 1.05) mol CO2 m-2 S-1, two times of that in autumn, (1.31+0.39) mol CO2 s-1 In summer, there was much more CO2 evolved from soil than in autumn, averaging (5.18+0.75) mol CO2 m-2 s-1 and (1.96 + 0.57) (mol CO2 m-2 s-1, respectively. A significant correlation was found between soil CO2 evolution and ground temperature, with F =-0.864 2+0.310 1X,r=0.7164, P<0.001 (n=117). Both the minimal atmospheric CO2 level and the maximum net photosynthesis occurred around 14:00; and an increase in atmospheric CO2 and of soil CO2 evolution during night times were also found to be remarkable.展开更多
Aim Investigation of alkaloids from the leaves of Brazilian medicinal plantCroton hemiargyerius var. gymnodiscus. Methods Silica gel column chromatography was used repeatedlyfor the isolation and purification, and the...Aim Investigation of alkaloids from the leaves of Brazilian medicinal plantCroton hemiargyerius var. gymnodiscus. Methods Silica gel column chromatography was used repeatedlyfor the isolation and purification, and their structures were identified by extensive spectroscopyand comparison of the chemical and physical data with those of authentic samples reported inliterature. Results Twelve alkaloids were isolated and their structures were identified. ConclusionFour new alkaloids named hemiargines A (1), B (5), C (6) and D (7), together with eight knownalkaloids namely isoc-orydine (2), corydine (3), norcorydine (4), salutaridine (8), glaucine (9),tetrahydropalmatrubine (10), xylopinoine (11), and norlaudanosine (12) were isolated.展开更多
Aim To establish a sensitive and specific liquid chromatography-mass spectrometry (HPLC-MS) method for measuring lovastatin level in human plasma and the relative bioavailability. Methods Lovastatin in the plasma was ...Aim To establish a sensitive and specific liquid chromatography-mass spectrometry (HPLC-MS) method for measuring lovastatin level in human plasma and the relative bioavailability. Methods Lovastatin in the plasma was extracted with acetoacetate. Simvastatin was added as internal standard (IS). Samples were separated on a C_ 18 column with a mobile phase consisting of methanol and 50 mmol·L~ -1 sodium acetate (88 ∶ 12). The flow rate was 1 mL·min~ -1 . Sample was detected using an electrospray ionization (ES...展开更多
Ahn To develop a high resolution HPLC method for the determination of ondansetron in human plasma and to study the pharmacokinetics of ondansetron in orally disintegrating tablets. Methods HPLC determination involved ...Ahn To develop a high resolution HPLC method for the determination of ondansetron in human plasma and to study the pharmacokinetics of ondansetron in orally disintegrating tablets. Methods HPLC determination involved liquid-liquid extraction, separation on a CN column and ultraviolet detection at 310 ran with granisetron as an internal standard. Pharmacokinetics and bioequivalence of ondansetron in orally disintegrating tablets by direct compression and conventional 8 mg tablets were evaluated and compared in 20 healthy human male volunteers after a single oral dose in a randomized cross-over study. Results The limit of quantification was 0.25 ng· mL^-1. The recovery was about 85 % or over for ondan setron and about 90% for internal standard. Linearity was good within the concentration range of 0.5 - 50 ng·mL^-1 with r^2 ranging from 0.997 1 to 0.999 9. Intra- and inter-assay coefficients of variation ranged from 1.78% to 2.38% and 3.88% -5.19%, respectively. Accuracies for spiked concentrations of 2.0, 10.0, and 30.0 ng·mL^-1 were 104.7% ±4.4%, 102.2% ± 1.1%, and99.51% ±2.34%, respectively. Pharmacokinetic parameters of AUCo-t, AUCo-∞ , Cmax, Tmax, and T1/2 were 230.2 ± 78.0 ng·h·L^-1 , 265.2± 101.5 ng·h·mL^-1, 35.67 ± 8.94 ng·mL^-l, 1.51 ±0.79 h, and 5.00± 1.41 h for orally disintegrating tablets, respectively. The analysis of variance did not show any significant difference between orally disintegrating tablets and conventional tablets, and 90% confidence intervals fell within the acceptable range for bioequivalence. Conclusion High resolution HPLC method has been set up and applied in pharmacokinetic evaluation of ondansetron in orally disintegrating tablets.展开更多
Three separate 5'-flanking regions (1.1 kb, 1.9 kb and 2.2 kb) of crtO were cloned through walking upstream. Results of sequence analysis show that three 5'-flanking regions of crtO might have some similar putati...Three separate 5'-flanking regions (1.1 kb, 1.9 kb and 2.2 kb) of crtO were cloned through walking upstream. Results of sequence analysis show that three 5'-flanking regions of crtO might have some similar putative cis-acting elements such as ABA (abscisic acid)-responsive element (ABRE), C-repeat/dehydration responsive element (C-repeat/DRE), light-responsive element (G-box, GAG-motif, I-box and ATC-motif), wound-responsive element (WUN-motif), auxin-responsive element (TGA-element), MeJA-responsive element (TGACG-element) and MYB binding site (MBS), except for typical TATA box or CCAAT box. These findings might mean diversiform regulatory patterns of crtO being in astaxanthin biosynthesis of Haematococcus pluvialis.展开更多
The unicellular green alga Haematococcus pluvia/is uniquely accumulates carotenoids in the cytoplasm and in late developmental stages turns deep-red in color because of accumulation of astaxanthin in the cytosol. The ...The unicellular green alga Haematococcus pluvia/is uniquely accumulates carotenoids in the cytoplasm and in late developmental stages turns deep-red in color because of accumulation of astaxanthin in the cytosol. The enzyme, isopentenyl pyrophosphate (IPP) isomerase, plays a key role in astaxanthin biosynthesis of H. pluvialis. In this paper, two separate 5'-flanking regions (1.8 kb and 2.5 kb) of IPP isomerase gene was cloned through walking upstream firstly. Results of sequence analysis =showed that two separate 5'-flanking regions of IPP isomerase gene might have similar putative cis-acting elements such as ABA (abscisic acid)-responsive element (ABRE), drought-responsive element (DRE/C-repeat), light-responsive element (G-box, GAG-motif, I-box and ATC-motif), heat-shock element (HSE), wound-responsive element (WUN-motif), SA (salicylic acid)-responsive element (TCA-element), auxin-responsive element (TGA-element), MeJA (methyl jasmonate)-responsive element (TGACG-element), enhancer-like element involved in anoxic specific inducibility (GC-motif) and MYB binding sites (MBS and MRE), except for typical TATA box or CCAAT box, which exhibit diversiform transcriptional patterns of IPP isomerase gene in astaxanthin biosynthesis of Haematococcus pluvialis.展开更多
Recent studies have uncovered two signaling pathways that activate the host innate immunity against viral infection. One of the pathways utilizes members of the Toll-like receptor (TLR) family to detect viruses that...Recent studies have uncovered two signaling pathways that activate the host innate immunity against viral infection. One of the pathways utilizes members of the Toll-like receptor (TLR) family to detect viruses that enter the endosome through endocytosis. The TLR pathway induces interferon production through several signaling proteins that ultimately lead to the activation of the transcription factors NF-kB, IRF3 and IRFT. The other antiviral pathway uses the RNA helicase RIG-Ⅰ as the receptor for intracellular viral double-stranded RNA. RIG-Ⅰ activates NF-kB and IRFs through the recently identified adaptor protein MAVS, a CARD domain containing protein that resides in the mitochondrial membrane. MAVS is essential for antiviral innate immunity, but it also serves as a target of Hepatitis C virus (HCV), which employs a viral protease to cleave MAVS off the mitochondria, thereby allowing HCV to escape the host immune system.展开更多
[ Objective] To identify a novel snoRNA gene in Arabidopsis thalianan. [ Method ] Genome sequence of Arabidopsis thalianan was screened by using bioinformatics methods, and the sequence structure, organization form an...[ Objective] To identify a novel snoRNA gene in Arabidopsis thalianan. [ Method ] Genome sequence of Arabidopsis thalianan was screened by using bioinformatics methods, and the sequence structure, organization form and function of typical candidate gene were analyzed. [ Result] The identified snR95 box H/ACA snoRNA had conservative component and structural features of box C/D snoRNA family, possessed two more than 10 nt long rRNA antisense elements. The result revealed that the novel snoRNA is a partial counterpart of the rice Z270, named box C/D snoRNA -AthZ270. [ Conclusion ] Z270 snoRNA in Arabidopsis thalianan has different function with common snoRNA.展开更多
Objective: To study the biological activity of Myco-plasma penetrans 35kDa lipoprotein(P35) in vitro, prokaryotic expression vector pQE31//p35 was constructed and recombinant fusion protein P35 (rP35) was expressed in...Objective: To study the biological activity of Myco-plasma penetrans 35kDa lipoprotein(P35) in vitro, prokaryotic expression vector pQE31//p35 was constructed and recombinant fusion protein P35 (rP35) was expressed in E.coli. Methods: The p35 gene was amplified by polymerase chain reaction(PCR), cloned to pQE31, and a positive clone was screened. PCR-mediated mutagenesis was used to change the two "TGA" triplets to "TGG" triplets within the p35 gene. Production of the recombinant protein was induced by the addition of IPTG to the E.coli culture. rP35 was purified with a Ni-NTA Spin Kit and rP35 purification was analyzed by Western blot. Results: About 1Kb PCR amplification was cloned into pQE31. The two "TGA" triplets within the p35 gene were successfully changed to "TGG" triplets. The pQE31/p35 vector expressed a protein with a calculated molecular mass of 37.4kDa in E.coli. Western blot indicated the 37.4kDa protein was rP35 . Conclusion: PQE31/p35, a prokaryotic expression vector containing p35 gene, was successfully constructed and expressed in E.coli.展开更多
Cyanobacteria are oxygenic photosynthetic Gram-negative bacteria that can form potentially toxic blooms in eutrophic and slow flowing aquatic ecosystems. Bloom toxicity varies spatially and temporally, but understandi...Cyanobacteria are oxygenic photosynthetic Gram-negative bacteria that can form potentially toxic blooms in eutrophic and slow flowing aquatic ecosystems. Bloom toxicity varies spatially and temporally, but understanding the mechanisms that drive these changes remains largely a mystery. Changes in bloom toxicity may result from changes in intracellular toxin pool sizes of cyanotoxins with differing molecular toxicities, and/or from changes in the cell concentrations of toxic and non-toxic cyanobacterial species or strains within bloom populations. We show here how first-order rate kinetics at the cellular level can be used to explain how environmental conditions drive changes in bloom toxicity at the ecological level. First order rate constants can be calculated for changes in cell concentration( μ_c : specific cell division rate) or the volumetric biomass concentration( μ_g : specific growth rate) between short time intervals throughout the cell cycle. Similar first order rate constants can be calculated for changes in nett volumetric cyanotoxin concentration( μ_(tox) : specific cyanotoxin production rate) over similar time intervals. How μ_c(or μ_g) covaries with μ tox over the cell cycle shows conclusively when cyanotoxins are being produced and metabolised, and how the toxicity of cells change in response to environment stressors. When μ_(tox)/μ_c >1, cyanotoxin cell quotas increase and individual cells become more toxic because the nett cyanotoxin production rate is higher than the cell division rate. When μ_(tox)/μ_c =1, cell cyanotoxin quotas remains fixed because the nett cyanotoxin production rate matches the cell division rate. When μ_(tox)/μ_c <1, the cyanotoxin cell quota decreases because either the nett cyanotoxin production rate is lower than the cell division rate, or metabolic breakdown and/or secretion of cyanotoxins is occurring. These fundamental equations describe cyanotoxin metabolism dynamics at the cellular level and provide the necessary physiological background to understand how environmental stressors drive changes in bloom toxicity.展开更多
AIM: To study the action of hepatitis virus infectionassociated genes at transcription level during liver regeneration (LR). METHODS: Hepatitis virus infection-associated genes were obtained by collecting the data...AIM: To study the action of hepatitis virus infectionassociated genes at transcription level during liver regeneration (LR). METHODS: Hepatitis virus infection-associated genes were obtained by collecting the data from databases and retrieving the correlated articles, and their expression changes in the regenerating rat liver were detected with the rat genome 230 2.0 array. RESULTS: Eighty-eight genes were found to be associated with liver regeneration. The number of genes initially and totally expressed during initial LR [0.5-4 h affer partial hepatectomy (PH)], transition from (30 to G1 (4-6 h affer PH), cell proliferation (6-66 h after PH), cell differentiation and reorganization of structurefunction (66-168 h after PH) was 37, 8, 48, 3 and 37, 26, 80, 57, respectively, indicating that the genes were mainly triggered at the early stage of LR (0.5-4 h after PH), and worked at different phases. These genes were classified into 5 types according to their expression similarity, namely 37 up-regulated, 9 predominantly upregulated, 34 down-regulated, 6 predominantly downregulated and 2 up/down-regulated genes. Their total up- and down-regulation frequencies were 359 and 149 during LR, indicating that the expression of most genes was enhanced, while the expression of a small number of genes was attenuated during LR. According to time relevance, they were classified into 12 groups (0.5 and 1h, 2 and 4h, 6h, 8 and 12h, 16 and 96h, 18 and 24 h, 30 and 42 h, 36 and 48 h, 54 and 60 h, 66 and 72 h, 120 and 144 h, 168 h), demonstrating that the cellular physiological and biochemical activities during LR were fluctuated. According to expression changes of the genes, their expression patterns were classified into 23 types, suggesting that the cellular physiological and biochemical activities during LR were diverse and complicated. CONCLUSION: The anti-virus infection capacity of regenerating liver can be enhanced and 88 genes play an important role in LR.展开更多
Aim To explore the reason that the antiarrhythmic effect of the extract oftraditional Chinese medicinal herb, matrine, is weaker than quinidine and verapamil by comparison ofthe effect and efficacy of matrine on vario...Aim To explore the reason that the antiarrhythmic effect of the extract oftraditional Chinese medicinal herb, matrine, is weaker than quinidine and verapamil by comparison ofthe effect and efficacy of matrine on various kinds of transmembrane ionic currents with those ofquinidine and verapamil; and to demonstrate the best targets for antiarrhythmic drugs. MethodsWhole-cell patch-clamp techniques were used to record the action potential and ionic currents insingle cells of rat ventricular myocytes. Aconitine was used to induce the changes of ioniccurrents, then study the effects of matrine and quinidine, verapamil on aconitine-induced unbalancedchannel currents and action potential. Results Aconitine 1 μmol·L^(-1) induced significantchanges in transmembrane currents and action potential in single cells of rat ventricular myocytes.APD was significantly prolonged by aconitine. Simultaneously, aconitine increased sodium, L-typecalcium and inward rectifier potassium currents. Matrine 100 μmol· L^(-1) reversed theaconitine-induced changes of sodium current (I_(Na)) from (-70.2+- 10.5) pA/pF to ( - 39.6+-4.0)pA/pF(n = 5, P < 0.05 vs aconitine); L-type calcium current (I_(Ca-L)) from (20.4+- 3.8) pA/pF to (- 12.9+- 2.9) pA/pF ( n = 6, P < 0.01); the inward rectifier potassium current (I_(k1) ) from (-32.2+- 1.08) pA/pF to ( -24.0+-3.4) pA/pF (n = 6, P < 0.01), and action potential duration. Thereversal effects of quinidine and verapamil on aconitine-induced changes of APD and ionic currentswere more marked than matrine. Conclusion Aco-nitine significantly disturbs the normal equilibriumof ion channels in ventricular myocytes. It induces changes of I_(Na), I_(Ca-L), I_(K1) andprolongation of action potential duration. Matrine at concentration 50 or 100 μmol·L^(-1)statistically significantly suppresses aconitine-induced changes of APD and ionic currents. Thepotency and efficacy of inhibitory effect of matrine are markedly weaker than those of commonly usedverapamil and quinidine.展开更多
The evaluation of sustainable land use is the key issue in the field of studying the sustainable land utilization. In general analysis, the sustainable land use is evaluated respectively from its ecological sustainabi...The evaluation of sustainable land use is the key issue in the field of studying the sustainable land utilization. In general analysis, the sustainable land use is evaluated respectively from its ecological sustainability, economic sustainability and social sustainability in China and other countries in recent years. Although this evaluation is an important work, it seems insufficient and hard to comprehensively reflect the whole degree of land use sustainability. Thus, to make up this deficiency, this paper brings forward the evaluation indexes, which make it possible to quantitatively reflect the whole degree of land use sustainability, namely, the concept of "degrees of overall land use sustainability" (Dos), and research and measurement development of the method of and calculation in Dos. Taking the evaluation of the degree of land use sustainability in county regions of Yunnan Province as the actual example for analysis, results are basically as follows: 1) The degree of land use sustainability (Dos) is the ration index to organically and systematically integrate the degree of ecological friendliness (DeF), the degree of economic viability (Dev) and the degree of social acceptability (Dsa), able to comprehensively reflect the whole sustainability degree of regional land use 2) Based on the value of Dos, the grading system and standard for the sustainability of land use may be established and totally divided into five grades, namely, the high-degree sustainability, middle-degree sustainability, low-degree sustainability, conditional sustainability and non-sustainability. Meanwhile, the standard for distinguishing sustainability grades has also been confirmed so as to determine the nature of sustainability degrees in different grades. This makes the possibility for the combination of nature determination with ration in research result and provides with the scientific guideline and decision-making gist for better implementation of sustainable land use strategy. 3) The practice in evaluation of sustainability degree in county regional land use in Yunnan shows that the value of the degree of land use sustainability (Dos) of whole Yunnan Province is only 58.39, belonging to the grade of low-degree sustainability. Two thirds of counties in the whole province represent the grade of "conditional sustainability" and "non-sustainability" in the sustainability of land use. Among these counties, 11.11 % shows "non- sustainability'. The lowest degree of land use sustainability appears especially in the middle plateau mountain region of Northeast Yunnan, where the value of Dos in most counties (districts) is below 40 %, belonging to the grade of "non-sustainability". The sustainability degree in the karst mountainous region in lower-middle plateau mountain region in Southeast Yunnan is generally low and the value of sustainability degree (Dos) in most of the counties (cities and districts) is below 55. The value of sustainability degree (Dos) in most of the counties (cities and districts) in the north, west, northwest and southwest parts of Yunnan is below 55. This article also analyzes the reasons of low degree of sustainability in land use in Yunnan and puts forward the countermeasures to increase the degree of sustainability in land use in the whole province.展开更多
Comprehensive study on land-use change of spatial pattern and temporal process is the key component in LUCC study nowadays. Based on the theories and methods of Geo-information Tupu (Carto-methodology in Geo-informati...Comprehensive study on land-use change of spatial pattern and temporal process is the key component in LUCC study nowadays. Based on the theories and methods of Geo-information Tupu (Carto-methodology in Geo-information, CMGI), integration of spatial pattern and temporal processes of land-use change in the Yellow River Delta (YRD) are studied in the paper, which is supported by ERDAS and ARC/INFO software. The main contents include: (1) concept models of Tupu by spatial-temporal integration on land-use change, whose Tupu unit is synthesized by "Spatial·Attribute·Process" features and composed of relatively homogeneous geographical unit and temporal unit; (2) data sources and handling process, where four stages of spatial features in 1956, 1984, 1991, and 1996 are acquired; (3) integration of series of temporal-spatial Tupu, reconstruction series of "Arising" Tupu, spatial-temporal Process Tupu and the spatial temporal Pattern Tupu on land-use change by remap tables; (4) Pattern Tupu analysis on land-use change in YRD during 1956-1996; and (5) spatial difference of the Pattern Tupu analysis by dynamic Tupu units. The various landform units and seven sub-deltas generated by the Yellow River since 1855 are different. The Tupu analysis on land-use in the paper is a promising try on the comprehensive research of "spatial pattern of dynamic process" and "temporal process of spatial pattern" in LUCC research. The Tupu methodology would be a powerful and efficient tool on integrated studies of spatial pattern and temporal process in Geo-science.展开更多
文摘Aim To establish a LC-MS method for determining the concentration of nifedipine in human plasma and to evaluate the pharmacokinetic characteristics of nifedipine sustained-release tablets. Methods A XB-C18 (5 μm, 4.6 mm ×150 mm) column and a mobile phase of methanol: 0.01 mol·L^-1ammonium acetate (60:40, V/V) were used to separate nifedipine, the detections was accuracy under atmosperic pressure electronic spray ionization (AP-ESI) mode and ion mass spectrum (m/z) of 314.9 [M+H]^+ for nifedipine, and 320.8 [M+H]^+ for lorazepam (Internal Standard, IS). Results The linear range of nifedipine was 0.3 - 80 ng·mL^-1 ( r = 0.9997), and the limit of quantitation (LOQ) was 0.3 ng·mL^-1. The nifedipine pharmacokinetic parameters after a single dose of 20 mg nifedipine sustained-release tablets test (T) or reference (R) were as the followings, t1/2 (6.73 ± 2.00) h and (7.04 ± 2.18) h, Tmax (4.28 ± 0.70) h and (4.48 ± 0.70) h, Cmax(39.66 ± 10.58) ng·mL^-1 and (40.19 ± 10.97) ng·mL^-1, AUC0-36 (391.63 ± 108.55) ng·mL^-1·h and (387.57 ± 121.51) ng·mL^-1·h, and AUC0-∞ (408.28 ± 121.16) ng·mL^-1·h and (406.15 ± 133.13) ng·mL^-1·h. The relative bioavailability of nifedipine sustained-release tablets (test) was (103.02 ± 13.93) %. Conclusion LC-MS method for the determination of concentrations of nifedipine in human plasma was sensitive and accurate, and could be used in nifedipine bioavailability and pharmacokinetic studies.
基金Supported by National Basic Research Program of China (973 Program) (Grant No. 2007CB714101)~~
文摘Modified classical Boltzmann entropy as generalized entropy, then proposed Maximum Generalized Entropy Principle fusing physics and biology, and established a new model for biological origin and evolutions based on this principle, finally took protein evolution for an example to analyze. The model provided some reference for biological complexity research.
文摘A new HPLC MS method to determine loratadine in human plasma was established. The method involved extracting drug with organic solvent under basic conditions. The samples were seperated by ODS column and determined by mass detector. The calibration curve of loratadine was linear within the range of 0.4~100 ng·mL -1 with r=0.9995 . The recovery of this method was within 95%~104%, within day and between day RSD were less than 12%. To study the pharmacokinetics and relative bioavailability of loratadine tablets, two formulations of loratadine tablets were given to 18 healthy male volunteers according to a randomized 2 way cross over design. The C max , AUC 0 t and T max values of the two formulations were 51.89±20.18 ng·mL -1 and 52.48±22.35 ng·mL -1 ; 140.75±88.42 ng·h·mL -1 and 147.24±92.33 ng·h·mL -1 ; 0.81±0.35 h and 0.81±0.27 h respectively. Results from statistic analysis showed that there were no significant difference between the C max , AUC 0-t and T max values of the two formulations. The relative bioavailability of tablets I with respect to tablets II was 97%±13% from the AUC 0 t measurement. Bioequivalance was observed between the two tablets.
基金This is a key project of National Natural Science Foundation of China.
文摘Middle-sized chambers (40cmx40cmx20 cm) and an infrared gas analyzer (IRGA) were used for the measurement of net photosynthesis of the grass layer and soil CO2 evolution, in Quercus liaotungensis Koidz. forest, which is a typical temperate forest ecosystem in the mountainous areas of Beijing. Changes of CO2 concentrations in both the atmosphere (2m above canopy) and the forest canopy (2m below the top of the canopy) together with those of net photosynthesis and soil CO2 evolution were also examined, in order to find the characteristics of CO2 exchange between the different components of the temperate forest ecosystem and the atmosphere. Atmospheric CO2 averaged (323+10) and (330+1) mol mol-1 respectively in summer and autumn. During the 24-hour measurements, large differences as much as -46 and -61 mol mol-1 respectively in the atmosphere and forest were found. Net photosynthesis of the grass layer in summer was (2. 59 9+ 1.05) mol CO2 m-2 S-1, two times of that in autumn, (1.31+0.39) mol CO2 s-1 In summer, there was much more CO2 evolved from soil than in autumn, averaging (5.18+0.75) mol CO2 m-2 s-1 and (1.96 + 0.57) (mol CO2 m-2 s-1, respectively. A significant correlation was found between soil CO2 evolution and ground temperature, with F =-0.864 2+0.310 1X,r=0.7164, P<0.001 (n=117). Both the minimal atmospheric CO2 level and the maximum net photosynthesis occurred around 14:00; and an increase in atmospheric CO2 and of soil CO2 evolution during night times were also found to be remarkable.
文摘Aim Investigation of alkaloids from the leaves of Brazilian medicinal plantCroton hemiargyerius var. gymnodiscus. Methods Silica gel column chromatography was used repeatedlyfor the isolation and purification, and their structures were identified by extensive spectroscopyand comparison of the chemical and physical data with those of authentic samples reported inliterature. Results Twelve alkaloids were isolated and their structures were identified. ConclusionFour new alkaloids named hemiargines A (1), B (5), C (6) and D (7), together with eight knownalkaloids namely isoc-orydine (2), corydine (3), norcorydine (4), salutaridine (8), glaucine (9),tetrahydropalmatrubine (10), xylopinoine (11), and norlaudanosine (12) were isolated.
文摘Aim To establish a sensitive and specific liquid chromatography-mass spectrometry (HPLC-MS) method for measuring lovastatin level in human plasma and the relative bioavailability. Methods Lovastatin in the plasma was extracted with acetoacetate. Simvastatin was added as internal standard (IS). Samples were separated on a C_ 18 column with a mobile phase consisting of methanol and 50 mmol·L~ -1 sodium acetate (88 ∶ 12). The flow rate was 1 mL·min~ -1 . Sample was detected using an electrospray ionization (ES...
文摘Ahn To develop a high resolution HPLC method for the determination of ondansetron in human plasma and to study the pharmacokinetics of ondansetron in orally disintegrating tablets. Methods HPLC determination involved liquid-liquid extraction, separation on a CN column and ultraviolet detection at 310 ran with granisetron as an internal standard. Pharmacokinetics and bioequivalence of ondansetron in orally disintegrating tablets by direct compression and conventional 8 mg tablets were evaluated and compared in 20 healthy human male volunteers after a single oral dose in a randomized cross-over study. Results The limit of quantification was 0.25 ng· mL^-1. The recovery was about 85 % or over for ondan setron and about 90% for internal standard. Linearity was good within the concentration range of 0.5 - 50 ng·mL^-1 with r^2 ranging from 0.997 1 to 0.999 9. Intra- and inter-assay coefficients of variation ranged from 1.78% to 2.38% and 3.88% -5.19%, respectively. Accuracies for spiked concentrations of 2.0, 10.0, and 30.0 ng·mL^-1 were 104.7% ±4.4%, 102.2% ± 1.1%, and99.51% ±2.34%, respectively. Pharmacokinetic parameters of AUCo-t, AUCo-∞ , Cmax, Tmax, and T1/2 were 230.2 ± 78.0 ng·h·L^-1 , 265.2± 101.5 ng·h·mL^-1, 35.67 ± 8.94 ng·mL^-l, 1.51 ±0.79 h, and 5.00± 1.41 h for orally disintegrating tablets, respectively. The analysis of variance did not show any significant difference between orally disintegrating tablets and conventional tablets, and 90% confidence intervals fell within the acceptable range for bioequivalence. Conclusion High resolution HPLC method has been set up and applied in pharmacokinetic evaluation of ondansetron in orally disintegrating tablets.
基金supported by the National Natural Science Foundation (40706050 40706048)+4 种基金Natural Science Foundation of Shandong University of Technology (4040306017)Start-up Foundation for Ph.D of Shandong University of Technology (4041-4050174041-405016)National Key Technology R&D program(11200602)Foundation of State Commonweal Institute (2060402/2)
文摘Three separate 5'-flanking regions (1.1 kb, 1.9 kb and 2.2 kb) of crtO were cloned through walking upstream. Results of sequence analysis show that three 5'-flanking regions of crtO might have some similar putative cis-acting elements such as ABA (abscisic acid)-responsive element (ABRE), C-repeat/dehydration responsive element (C-repeat/DRE), light-responsive element (G-box, GAG-motif, I-box and ATC-motif), wound-responsive element (WUN-motif), auxin-responsive element (TGA-element), MeJA-responsive element (TGACG-element) and MYB binding site (MBS), except for typical TATA box or CCAAT box. These findings might mean diversiform regulatory patterns of crtO being in astaxanthin biosynthesis of Haematococcus pluvialis.
基金supported by the National Natural Science Foundation in China (NO. 30671126 40706050 and 40706048)+3 种基金National Key Technology R&D Program (No. 11200602)The Special Foundation of State-level and Public Interest Research Institute (No. 2060402/2)Natural Science Foundation in Shandong University of Technology (No. 4040306017) Start-up Foundation for Ph.D in Shandong University of Technology (No. 4041-405017 and 4041-405016)
文摘The unicellular green alga Haematococcus pluvia/is uniquely accumulates carotenoids in the cytoplasm and in late developmental stages turns deep-red in color because of accumulation of astaxanthin in the cytosol. The enzyme, isopentenyl pyrophosphate (IPP) isomerase, plays a key role in astaxanthin biosynthesis of H. pluvialis. In this paper, two separate 5'-flanking regions (1.8 kb and 2.5 kb) of IPP isomerase gene was cloned through walking upstream firstly. Results of sequence analysis =showed that two separate 5'-flanking regions of IPP isomerase gene might have similar putative cis-acting elements such as ABA (abscisic acid)-responsive element (ABRE), drought-responsive element (DRE/C-repeat), light-responsive element (G-box, GAG-motif, I-box and ATC-motif), heat-shock element (HSE), wound-responsive element (WUN-motif), SA (salicylic acid)-responsive element (TCA-element), auxin-responsive element (TGA-element), MeJA (methyl jasmonate)-responsive element (TGACG-element), enhancer-like element involved in anoxic specific inducibility (GC-motif) and MYB binding sites (MBS and MRE), except for typical TATA box or CCAAT box, which exhibit diversiform transcriptional patterns of IPP isomerase gene in astaxanthin biosynthesis of Haematococcus pluvialis.
文摘Recent studies have uncovered two signaling pathways that activate the host innate immunity against viral infection. One of the pathways utilizes members of the Toll-like receptor (TLR) family to detect viruses that enter the endosome through endocytosis. The TLR pathway induces interferon production through several signaling proteins that ultimately lead to the activation of the transcription factors NF-kB, IRF3 and IRFT. The other antiviral pathway uses the RNA helicase RIG-Ⅰ as the receptor for intracellular viral double-stranded RNA. RIG-Ⅰ activates NF-kB and IRFs through the recently identified adaptor protein MAVS, a CARD domain containing protein that resides in the mitochondrial membrane. MAVS is essential for antiviral innate immunity, but it also serves as a target of Hepatitis C virus (HCV), which employs a viral protease to cleave MAVS off the mitochondria, thereby allowing HCV to escape the host immune system.
基金Supported by Natural Science Project Establishment Subject of Jiangxi Science & Technology Normal University(KY2008ZY03 )Teaching Research Provincial Project Establishment Subject of Higher Education of Jiangxi Province (JXJG-13-29)~~
文摘[ Objective] To identify a novel snoRNA gene in Arabidopsis thalianan. [ Method ] Genome sequence of Arabidopsis thalianan was screened by using bioinformatics methods, and the sequence structure, organization form and function of typical candidate gene were analyzed. [ Result] The identified snR95 box H/ACA snoRNA had conservative component and structural features of box C/D snoRNA family, possessed two more than 10 nt long rRNA antisense elements. The result revealed that the novel snoRNA is a partial counterpart of the rice Z270, named box C/D snoRNA -AthZ270. [ Conclusion ] Z270 snoRNA in Arabidopsis thalianan has different function with common snoRNA.
基金Supported by the Nature Science Fund of Hunan Province(02JJY2025) Health Office of Hunun Province(Y02-066).
文摘Objective: To study the biological activity of Myco-plasma penetrans 35kDa lipoprotein(P35) in vitro, prokaryotic expression vector pQE31//p35 was constructed and recombinant fusion protein P35 (rP35) was expressed in E.coli. Methods: The p35 gene was amplified by polymerase chain reaction(PCR), cloned to pQE31, and a positive clone was screened. PCR-mediated mutagenesis was used to change the two "TGA" triplets to "TGG" triplets within the p35 gene. Production of the recombinant protein was induced by the addition of IPTG to the E.coli culture. rP35 was purified with a Ni-NTA Spin Kit and rP35 purification was analyzed by Western blot. Results: About 1Kb PCR amplification was cloned into pQE31. The two "TGA" triplets within the p35 gene were successfully changed to "TGG" triplets. The pQE31/p35 vector expressed a protein with a calculated molecular mass of 37.4kDa in E.coli. Western blot indicated the 37.4kDa protein was rP35 . Conclusion: PQE31/p35, a prokaryotic expression vector containing p35 gene, was successfully constructed and expressed in E.coli.
文摘Cyanobacteria are oxygenic photosynthetic Gram-negative bacteria that can form potentially toxic blooms in eutrophic and slow flowing aquatic ecosystems. Bloom toxicity varies spatially and temporally, but understanding the mechanisms that drive these changes remains largely a mystery. Changes in bloom toxicity may result from changes in intracellular toxin pool sizes of cyanotoxins with differing molecular toxicities, and/or from changes in the cell concentrations of toxic and non-toxic cyanobacterial species or strains within bloom populations. We show here how first-order rate kinetics at the cellular level can be used to explain how environmental conditions drive changes in bloom toxicity at the ecological level. First order rate constants can be calculated for changes in cell concentration( μ_c : specific cell division rate) or the volumetric biomass concentration( μ_g : specific growth rate) between short time intervals throughout the cell cycle. Similar first order rate constants can be calculated for changes in nett volumetric cyanotoxin concentration( μ_(tox) : specific cyanotoxin production rate) over similar time intervals. How μ_c(or μ_g) covaries with μ tox over the cell cycle shows conclusively when cyanotoxins are being produced and metabolised, and how the toxicity of cells change in response to environment stressors. When μ_(tox)/μ_c >1, cyanotoxin cell quotas increase and individual cells become more toxic because the nett cyanotoxin production rate is higher than the cell division rate. When μ_(tox)/μ_c =1, cell cyanotoxin quotas remains fixed because the nett cyanotoxin production rate matches the cell division rate. When μ_(tox)/μ_c <1, the cyanotoxin cell quota decreases because either the nett cyanotoxin production rate is lower than the cell division rate, or metabolic breakdown and/or secretion of cyanotoxins is occurring. These fundamental equations describe cyanotoxin metabolism dynamics at the cellular level and provide the necessary physiological background to understand how environmental stressors drive changes in bloom toxicity.
基金Supported by the National Natural Science Foundation of China, No. 30270673
文摘AIM: To study the action of hepatitis virus infectionassociated genes at transcription level during liver regeneration (LR). METHODS: Hepatitis virus infection-associated genes were obtained by collecting the data from databases and retrieving the correlated articles, and their expression changes in the regenerating rat liver were detected with the rat genome 230 2.0 array. RESULTS: Eighty-eight genes were found to be associated with liver regeneration. The number of genes initially and totally expressed during initial LR [0.5-4 h affer partial hepatectomy (PH)], transition from (30 to G1 (4-6 h affer PH), cell proliferation (6-66 h after PH), cell differentiation and reorganization of structurefunction (66-168 h after PH) was 37, 8, 48, 3 and 37, 26, 80, 57, respectively, indicating that the genes were mainly triggered at the early stage of LR (0.5-4 h after PH), and worked at different phases. These genes were classified into 5 types according to their expression similarity, namely 37 up-regulated, 9 predominantly upregulated, 34 down-regulated, 6 predominantly downregulated and 2 up/down-regulated genes. Their total up- and down-regulation frequencies were 359 and 149 during LR, indicating that the expression of most genes was enhanced, while the expression of a small number of genes was attenuated during LR. According to time relevance, they were classified into 12 groups (0.5 and 1h, 2 and 4h, 6h, 8 and 12h, 16 and 96h, 18 and 24 h, 30 and 42 h, 36 and 48 h, 54 and 60 h, 66 and 72 h, 120 and 144 h, 168 h), demonstrating that the cellular physiological and biochemical activities during LR were fluctuated. According to expression changes of the genes, their expression patterns were classified into 23 types, suggesting that the cellular physiological and biochemical activities during LR were diverse and complicated. CONCLUSION: The anti-virus infection capacity of regenerating liver can be enhanced and 88 genes play an important role in LR.
文摘Aim To explore the reason that the antiarrhythmic effect of the extract oftraditional Chinese medicinal herb, matrine, is weaker than quinidine and verapamil by comparison ofthe effect and efficacy of matrine on various kinds of transmembrane ionic currents with those ofquinidine and verapamil; and to demonstrate the best targets for antiarrhythmic drugs. MethodsWhole-cell patch-clamp techniques were used to record the action potential and ionic currents insingle cells of rat ventricular myocytes. Aconitine was used to induce the changes of ioniccurrents, then study the effects of matrine and quinidine, verapamil on aconitine-induced unbalancedchannel currents and action potential. Results Aconitine 1 μmol·L^(-1) induced significantchanges in transmembrane currents and action potential in single cells of rat ventricular myocytes.APD was significantly prolonged by aconitine. Simultaneously, aconitine increased sodium, L-typecalcium and inward rectifier potassium currents. Matrine 100 μmol· L^(-1) reversed theaconitine-induced changes of sodium current (I_(Na)) from (-70.2+- 10.5) pA/pF to ( - 39.6+-4.0)pA/pF(n = 5, P < 0.05 vs aconitine); L-type calcium current (I_(Ca-L)) from (20.4+- 3.8) pA/pF to (- 12.9+- 2.9) pA/pF ( n = 6, P < 0.01); the inward rectifier potassium current (I_(k1) ) from (-32.2+- 1.08) pA/pF to ( -24.0+-3.4) pA/pF (n = 6, P < 0.01), and action potential duration. Thereversal effects of quinidine and verapamil on aconitine-induced changes of APD and ionic currentswere more marked than matrine. Conclusion Aco-nitine significantly disturbs the normal equilibriumof ion channels in ventricular myocytes. It induces changes of I_(Na), I_(Ca-L), I_(K1) andprolongation of action potential duration. Matrine at concentration 50 or 100 μmol·L^(-1)statistically significantly suppresses aconitine-induced changes of APD and ionic currents. Thepotency and efficacy of inhibitory effect of matrine are markedly weaker than those of commonly usedverapamil and quinidine.
文摘The evaluation of sustainable land use is the key issue in the field of studying the sustainable land utilization. In general analysis, the sustainable land use is evaluated respectively from its ecological sustainability, economic sustainability and social sustainability in China and other countries in recent years. Although this evaluation is an important work, it seems insufficient and hard to comprehensively reflect the whole degree of land use sustainability. Thus, to make up this deficiency, this paper brings forward the evaluation indexes, which make it possible to quantitatively reflect the whole degree of land use sustainability, namely, the concept of "degrees of overall land use sustainability" (Dos), and research and measurement development of the method of and calculation in Dos. Taking the evaluation of the degree of land use sustainability in county regions of Yunnan Province as the actual example for analysis, results are basically as follows: 1) The degree of land use sustainability (Dos) is the ration index to organically and systematically integrate the degree of ecological friendliness (DeF), the degree of economic viability (Dev) and the degree of social acceptability (Dsa), able to comprehensively reflect the whole sustainability degree of regional land use 2) Based on the value of Dos, the grading system and standard for the sustainability of land use may be established and totally divided into five grades, namely, the high-degree sustainability, middle-degree sustainability, low-degree sustainability, conditional sustainability and non-sustainability. Meanwhile, the standard for distinguishing sustainability grades has also been confirmed so as to determine the nature of sustainability degrees in different grades. This makes the possibility for the combination of nature determination with ration in research result and provides with the scientific guideline and decision-making gist for better implementation of sustainable land use strategy. 3) The practice in evaluation of sustainability degree in county regional land use in Yunnan shows that the value of the degree of land use sustainability (Dos) of whole Yunnan Province is only 58.39, belonging to the grade of low-degree sustainability. Two thirds of counties in the whole province represent the grade of "conditional sustainability" and "non-sustainability" in the sustainability of land use. Among these counties, 11.11 % shows "non- sustainability'. The lowest degree of land use sustainability appears especially in the middle plateau mountain region of Northeast Yunnan, where the value of Dos in most counties (districts) is below 40 %, belonging to the grade of "non-sustainability". The sustainability degree in the karst mountainous region in lower-middle plateau mountain region in Southeast Yunnan is generally low and the value of sustainability degree (Dos) in most of the counties (cities and districts) is below 55. The value of sustainability degree (Dos) in most of the counties (cities and districts) in the north, west, northwest and southwest parts of Yunnan is below 55. This article also analyzes the reasons of low degree of sustainability in land use in Yunnan and puts forward the countermeasures to increase the degree of sustainability in land use in the whole province.
文摘Comprehensive study on land-use change of spatial pattern and temporal process is the key component in LUCC study nowadays. Based on the theories and methods of Geo-information Tupu (Carto-methodology in Geo-information, CMGI), integration of spatial pattern and temporal processes of land-use change in the Yellow River Delta (YRD) are studied in the paper, which is supported by ERDAS and ARC/INFO software. The main contents include: (1) concept models of Tupu by spatial-temporal integration on land-use change, whose Tupu unit is synthesized by "Spatial·Attribute·Process" features and composed of relatively homogeneous geographical unit and temporal unit; (2) data sources and handling process, where four stages of spatial features in 1956, 1984, 1991, and 1996 are acquired; (3) integration of series of temporal-spatial Tupu, reconstruction series of "Arising" Tupu, spatial-temporal Process Tupu and the spatial temporal Pattern Tupu on land-use change by remap tables; (4) Pattern Tupu analysis on land-use change in YRD during 1956-1996; and (5) spatial difference of the Pattern Tupu analysis by dynamic Tupu units. The various landform units and seven sub-deltas generated by the Yellow River since 1855 are different. The Tupu analysis on land-use in the paper is a promising try on the comprehensive research of "spatial pattern of dynamic process" and "temporal process of spatial pattern" in LUCC research. The Tupu methodology would be a powerful and efficient tool on integrated studies of spatial pattern and temporal process in Geo-science.