Urinary Concentrations of Hydroxyproline and 3-Methyl Histidine in Postpartum Cow

The urinary concentrations of hydroxyproline (HYPRO)and 3 -methyl histidine (3 - MEHIS) were de- termined in 16 Chinese-Holstein cows. The objectives of the experiment were to find out thhe relationship between collagen and myosin ddegradation and uterine involution in the postpartum cow. The results in the experiment showed that the mean concentrations of HYPRO and 3-MEHIS were 138.32±22.99 and 37.09 ±3.90 nmol·mL-1,respectively,for the cows during the days between 60-90 postpartum,and for the cows immediately after calving the concentrations of HYPRO and 3 -MEHIS reduced from 284.30 and 65.48 nmol ·mL-1 on the day one after calving to the normal level of 109.18 and 33.51 nmol·mL^-1 on the day 50 post- partum,respectively. There was a good correlation between the urinary concentrations of both HYPRO and 3 -MEHIS and the diameters of the involuting uterus (r = 0. 79).

3种多芳环烃在海胆体内的富集动力学研究

为研究多芳环烃(PAHs)在虾夷马粪海胆Strongylocentrotus intermedius体内的富集动力学,系统认识其动力学参数特征,应用半静态双箱动力学模型拟合虾夷马粪海胆(壳直径2.0 cm±0.3 cm)对3,4-苯并[a]芘、9,10-二甲基蒽、3-甲基菲3种PAHs的生物富集过程,通过非线性拟合获得海胆对3种多环芳烃的吸收速率常数(K_1)、释放速率常数(K_2)、生物富集因子(BCF),以及平衡状态下海胆体内3种多环芳烃的含量(C_(max))、生物学半衰期(t_(1/2))等动力学参数。结果表明:海胆对3,4-苯并[a]芘富集动力学参数K_1、K_2、BCF、C_(max)、t_(1/2)的平均值分别为59.1、0.152、136.5、11.788μg/g和6.36 d;海胆对9,10-二甲基蒽富集动力学参数K_1,K_2、BCF、C_(max)、t_(1/2)的平均值分别为12.3、0.228、54.05、4.383μg/g和6.32 d;海胆对3-甲基菲富集动力学参数K_1、K_2、BCF、C_(max)、t_(1/2)的平均值分别为18.16、0.113、88.1、12.407μg/g和7.6 d;在5μg/L浓度条件下,海胆对3种多环芳烃的富集能力进行比较,依次为3,4-苯并[a]芘(14 d BCF=220)>3-甲基菲(14 d BCF=128.4)>9,10-二甲基蒽(14 d BCF=84.0)。研究表明,海胆对浓度为1、5、20μg/L的3,4-苯并[a]芘、浓度为5、100μg/L的3-甲基菲、浓度为5、10、50μg/L的9,10-二甲基蒽的生物富集过程均符合双箱动力学模型。

Reactivity of 3-Cyanoacetylindole Derivatives: Synthesisof 3-Hydrazonopyrazolyl and 3-Thiadiazolyl Indole Derivatives

The coupling reaction of 3-cyanoacetyl-2-methylindole 1a with the aromatic diazonium salts gave the corresponding arylhydrazones 2a-e. Compounds 2 were used for synthesis of 4-aminopyrazole-5-carbonitrile 4a-e and 5-amino-4-arylazo-3-pyrazoles 5a-e derivatives. Also, treatment of 3-cyanoacetyl-2-phenylindole 1b with phenyl isothiocyanate gave the corresponding thioacetanilide 7. The later compound 7 was utilized as the key intermediate for the synthesis of some new thiadiazole derivatives 9a-r. The structures of all new compounds were elucidated on the basis of elemental analysis and spectral data.

Synthesis and Crystal Structure of(E)-Ethyl 2-(4-(2,4-dimethoxybenzylideneamino)-5-(3,4,5-trimethoxyphenyl)-4H-1,2,4-triazol-3-ylthio)acetate

The crystal structure of the title compound(E)-ethyl 2-(4-(2,4-dimethoxy benzylide-neamino)-5-(3,4,5-trimethoxyphenyl)-4H-1,2,4-triazol-3-ylthio)acetate(4,C_(24)H_(28)N_(4)O_(7)S,Mr=516.17)was synthesized and determined by X-ray single-crystal diffraction.The crystal belongs to the monoclinic system,space group P2_(1)/n with a=13.162(2),b=8.4506(13),c=22.602(4)Å,β=99.888(3)°,μ=0.183 mm^(-1),V=2476.5(7)Å^(3),Z=4,D_(c)=1.385 g/cm^(3),F(000)=1088,T=110(2)K,R=0.0426 and wR=0.1216 for 3859 observed reflections with I 2σ(Ⅰ).

Talachalasins A-C,Undescribed Cytochalasans with a 16β-Methyl or 2-Oxabicyclo[3.3.1]nonan-3-one unit from the Deep-Sea-Derived Fungus Talaromyces muroii sp.SCSIO 40439

Comprehensive Summary Talachalasins A-C(1-3),three new cytochalasans(CYTs),were isolated from deep-sea-derived fungus Talaromyces muroii sp.SCSIO 40439.The structures of 1-3,including absolute configurations,were determined based on HRESIMS,NMR spectroscopic data,ECD comparison,and single crystal X-ray diffraction analysis.Talachalasins A-C(1-3)represented the first examples of cytochalasans possessing a unique 16β-methyl group,distinct from>500 reported CYTs.Talachalasin C(3)was an unprecedented 20,21-seco-cytochalasans characterized by a 2-oxabicyclo[3.3.1]nonan-3-one unit.Talachalasin A(1)displayed moderate cytotoxic activity against four tumor cell lines(IC_(50)3.40-10.02μM).Talachalasin B(2)showed comparable anti-RSV and HSV-1 activities(IC5012.5μM or IC5020.0μM).

Determination of 8,2′-diprenylquercetin 3-methyl ether in plasma by UPLC-MS-MS and its pharmacokinetic application in rats

8,2＇-Diprenylquercetin 3-methyl ether with significant anti-breast cancer activity is the main constituent of Tibetan medicine Sinopodophylli Fructus. In the present study, we developed and validated a rapid and sensitive ultra performance liquid chromatography-tandem mass spectrometry （UPLC-MS/MS） method for the determination of 8,2＇-diprenylquercetin 3-methyl ether in rat plasma. 8-Prenylkaempferol was used as the internal standard. The separation was carried out using Waters ACQUITY UPLC BEH C18 column （2.1 mm×100 ram, 1.7 μm） with a mobile phase consisting of acetonitrile and 0.1% formic acid in water on a gradient program at a flow rate of 0.4 mL＇min-1 and temperature of 30 ℃. Triple quadrupole mass spectrometric detection in negative ion mode was used for multiple-reaction monitoring of the transitions at m/z 451.30→177.25 and m/z 353.25→298.15 for 8,2＇-diprenylquercetin 3-methyl ether and 8-prenylkaempferol, respectively. The calibration curves were linear within the concentration range 0.1-2000 ng/mL （r = 0.9954）. The recoveries were 103%-115%, and the results were consistent across low, middle and high concentration levels. The intra- and inter-day precisions were within 15%, and the bias was between --6%-15%. This method was simple, rapid and sensitive, which could be applied to the determination of 8,2＇-diprenylquercetin 3-methyl ether in plasma and pharmacokinetic study in rats. Pharmacokinetic test indicated that the peak plasma concentration occurred in 2 h after the female rats were intragastrically administered with 8,2＇-diprenylquercetin 3-methyl ether at the dose of 100 mg/kg, and the biological half-life was 6.79 h. The blood drug concentration maintained equal amount for 20 h, which was conducive to the in vivo effects of drugs.

Global hypomethylation in hepatocellular carcinoma and its relationship to aflatoxin B_1 exposure

AIM:To determine global DNA methylation in paired hepatocellular carcinoma(HCC) samples using several different assays and explore the correlations between hypomethylation and clinical parameters and biomarkers,including that of aflatoxin B 1 exposure.METHODS:Using the radio labeled methyl acceptance assay as a measure of global hypomethylation,as well as two repetitive elements,including satellite 2(Sat2) by MethyLight and long interspersed nucleotide elements(LINE1),by pyrosequencing.RESULTS:By all three assays,mean methylation levels in tumor tissues were significantly lower than that in adjacent tissues.Methyl acceptance assay log(mean ± SD) disintegrations/min/ng DNA are 70.0 ± 54.8 and 32.4 ± 15.6,respectively,P = 0.040;percent methylation of Sat2 42.2 ± 55.1 and 117.9 ± 88.8,respectively,P < 0.0001 and percent methylation LINE1 48.6 ± 14.8 and 71.7 ± 1.4,respectively,P < 0.0001.Aflatoxin B 1 albumin(AFB 1-Alb) adducts,a measure of exposure to this dietary carcinogen,were inversely correlated with LINE1 methylation(r =-0.36,P = 0.034).CONCLUSION:Consistent hypomethylation in tumor compared to adjacent tissue was found by the three different methods.AFB 1 exposure is associated with DNA global hypomethylation,suggesting that chemical carcinogens may influence epigenetic changes in humans.

Even-carbon predominance of Monomethyl branched alkanes in Humic coal from Junggar Basin,NW China

A series of Monomethyl branched alkanes compounds were detected between nC14-nC36,in immature and low maturity Jurassic humic coal,Junggar basin.2-methyl alkanes and 3-methyl alkanes accounted for the vast majority of the compounds.It is worth noting that the2-methyl alkanes in the humic coal samples show an obvious distribution of even carbon predominances rarely reported in the literature.The results show that with the increase of Pr/Ph(pristane/phytane),the even carbon dominance of 2-methyl alkanes is more obvious,while the odd carbon number distribution of 3-methyl alkanes is weakened.As Pr/Ph increases in the humic coal,the relative content of the hopanes increased,while the relative content of 2-methyl alkanes and 3-methyl alkanes increases first and then decreases.

Indole Alkaloids from the Roots of Ervatamia hainanensis

Two new indole alkaloids, named ibogamine-18-carboxylic acid, 3, 4-didehydro-7, 8-dioxo-methyl ester 1, ibogamine-18-carboxylic acid, 16, 17-didehydro-9, 17-dihydro-9-hydroxy （2-oxopropyl）-methyl ester 2, were isolated from Ervatamia hainanensis. Their structures were elucidated on the basis of spectroscopic methods.

Effect of Chemical Doping and Ion Implantation on Cond uctivity of Poly(p-phenylene vinylene) Derivatives

The surface conductivity of poly [ 2-methoxy-5-（3＇-methyl） butoxy]-p-phenylene vinylene （PMOMBOPV） films doped with FeCl3 and H2SO4 by chemical method and implanted by N^＋ ions was studied and the comparison of environmental stability of conductive behavior was also investigated. The energy and dose of N^＋ ions were in the rang 15～35 keV and 3. 8×10^15～9. 6×10^16 ions/cm^2, respectively. The conductivity of PMOMBOPV film was enhanced remarkably with the increases of the energy and dose of N^＋ ions. For example, the conductivity of PMOMBOPV film was 3. 2×10^-2S/cm when ion implantation was performed with an energy of 35 keV at a dose of 9. 6 × 10^14 ions/cm^2 , which was almost seven orders of magnitude higher than that of film unimplanted. The environmental stability of conductive behavior for ionimplanted film was much better than that of chemical doped films. Moreover, the conductive activation energy of ion-implanted films was measured to be about 0.17 eV.

Screening of chemokine receptor CCR4 antagonists by capillary zone electrophoresis

CC chemokine receptor 4(CCR4)is a kind of G-protein-coupled receptor,which plays a pivotal role in allergic inflammation.The interaction between 2-(2-(4-chloro-phenyl)-5-{[(naphthalen-1-ylmethyl)-carbamlyl]-methyl-4-oxo-thiazolidin-3-yl)-N-(3-morpholin-4-yl-propyi)-acetamide(S009)and the N-terminal extracellular tail(ML40)of CCR4 has been validated to be high affinity by capillary zone electrophoresis(CZE).The S009 is a known CCR4 antagonist.Now,a series of new thiourea derivatives have been synthesized.Compared with positive control S009,they were screened using ML40 as target by CZE to find some new drugs for allergic inflammation diseases.The synthesized compounds XJH-5,XJH-4,XJH-17 and XJH-1 displayed the interaction with ML40,but XJH-9,XJH-10,XJH-I 1,XJH-12,XJH-13,XJH-14,XJH-3,XJH-8,XJH-6,XJH-7,XJH-15,XJH-16 and XJH-2 did not bind to ML40.Both qualification and quantification characterizations of the binding were determined.The affinity of the four compounds was valued by the binding constant,which was similar with the results of chemotactic experiments.The established CEZ method is capable of sensitive and fast screening for a series of lactam analogs in the drug discovery for allergic inflammation diseases.

A New 10-Hydroxyl Anthrone Glycoside from Cassia siamea Lam

A new 10-hydroxyl anthrone glycoside, 1, 8, 10 - trihydroxyl-1ObDglucopyrano- syl-3-methyl-10- C (S) b D- glucopyranosyl-anthrone-9 1 was isolated from the stem of Cassia siamea Lam. The structure was elucidated by spectral evidences, especially by 2 D techniques.

A New Sesquiterpene-substituted Benzoic Acid from the Brown Alga Dictyopteris divaricata

A new sesquiterpene-substituted benzoic acid has been isolated from the brown Alga Dictyopteris divaricata Okam.. Its structure was elucidated as 3-[(2-hydroxy-2,5,5,8a-tetra- methyldecahydro-1-naphthalenyl)methyl]-4-hydroxybenzoic acid, named dictyvaric acid on the basis of spectroscopic methods including IR, HRFABMS, 1D and 2D NMR techniques.

Tribological Properties of Functionalized Ionic Liquids Containing Ester-group as Lubricants for Steel-Steel System

A series of functionalized ionic liquids （ILs） containing ester-group were synthesized and their tribological prop- erties as lubricants for steel-steel contact were studied and compared with a non-functionalized ionic liquid and perfluo- ropolyethers （PFPE）. The morphology and chemical composition of the worn scars were analyzed by scanning electron mi- croscopy and X-ray photoelectron spectroscopy, respectively, and the possible lubrication mechanism of ILs was discussed. As a result, all ILs demonstrated a better lubricity and a much higher load-carrying capacity than PFPE used as lubricants for the steel-steel tribomates system. The functionalized ILs with ester-group showed slightly worse friction reducing abil- ity than their nonfunctionalized counterparts at relatively lower loads owing to their higher viscosity, but then exhibited better antiwear ability because the ester group they contained had not only physical but also strong chemical reactions with the freshly exposed steel surface and formed chemical adsorption boundary films on the worn surface during friction pro- cess. Under high loads, some triboehemical reactions took place between the active elements, such as fluorine which were released from the ILs, and fresh metal surfaces of rubbing pairs to form the admixture reaction films, which were mainly composed of ferric fluoride mixed with ferric oxide, leading to lower friction coefficients and good wear resistance.

Effect of an Organic Inhibitor on the Electrical Properties of High Carbon Steel in Simulated Acid Environment

The effect of 1-Phenyl-3-Methyl Pyrazol-5-one (HPMP) on the electrical properties of high carbon steel in Hydrochloric acid (HCI), Trioxonitrate (v) acid (HNO3) and Perchloric acid (HCIO4) was studied by weight loss method. The acidic medium caused a complete degradation of the electrical properties of the coated and uncoated high carbon steel. However, the attack was more on the uncoated coupons, which showed that HPHP is an effective corrosion inhibitor. HNO3 had the most severe effect on the metal. The coupons coated with HPMP generally had higher values of resistance (0.0155 Ω) and conductivity (6.20 mho/m) in HCI environment than the uncoated coupons (0.0043 Ω) and (1.72 mho/m). Similar results were obtained for HNO3 and HCIO4 environments. These values are lower than the values obtained for as-received coupons: -0.0466 and 8.64 mho/m respectively.

新齐墩果酸衍生物抑制人肝癌SMMC-7721细胞增殖及诱导凋亡的研究

目的探讨一种新齐墩果酸衍生物(3β-hydroxyolea-12-en-28-oic acid-3,5,6-trimethylpyrazin-2-methyl ester,简称为受试物)对人肝细胞癌细胞株SMMC-7721细胞的抗肿瘤作用机制。方法应用四甲基偶氮唑蓝(MTT)法及细胞形态学观察新齐墩果酸衍生物对SMMC-7721细胞增殖及形态的影响;Annexin V联合PI染色法检测新齐墩果酸衍生物对细胞膜以及用JC-1染色法检测线粒体膜电位的损伤程度;Western blotting检测新齐墩果酸衍生物对凋亡相关蛋白Bcl-2,Bax,caspase-9 and caspase-3的表达。结果新齐墩果酸衍生物能抑制人SMMC-7721细胞增殖力,与浓度和时间呈正相关,作用细胞48 h后,细胞出现核固缩,细胞裂解,产生凋亡小体等形态学改变,细胞膜完整性被破坏,线粒体膜电位(Δψm)被降低,Bax、pro-caspase-9、cleaved caspase-9、pro-caspase-3以及cleaved caspase-3蛋白表达水平被上调,Bcl-2蛋白表达水平被下调。结论这种新齐墩果酸衍生物在人SMMC-7721细胞中发挥抗癌作用可能与其破坏了线粒体功能有关。