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 collag...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).展开更多
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-a...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.展开更多
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 determin...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).展开更多
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 dete...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).展开更多
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 sens...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.展开更多
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,includ...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.展开更多
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...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.展开更多
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 isola...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.展开更多
基金supported financially by Heilongjiang(C- 9702)and Chinese National (39870572)Natural and Scicntificfunds.
文摘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).
文摘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.
基金supported by the Science Foundation of the Southern Medical University for New Excellent Talents(No.B1000374)the Natural Science Foundation of Guangdong Province(No.10451051501004725)
文摘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).
基金supported in part by the National Natural Science Technology Project of Hainan Province(ZDKJ202018)K.C.Wong Education Foundation(GJTD-2020-12)+1 种基金the Guangdong Provincial Special Fund for Marine Economic Development Project(GDNRC[2021]48)Southern Marine Science and Engineering Guangdong Laboratory(Guangzhou)(GML2019ZD0406).
文摘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).
基金National Natural Science Foundation of China(Grant No.81673590)National Key Technology R&D Program "New Drug Innovation" of China(Grant No.2013ZX09103002-006)
文摘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.
基金Supported by A grant from the National Institute of Health,No. ES005116 and No.P30ES009089
文摘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.
基金This research was financially supported by the National Natural Science Foundation of China(No.41772124)National Science and Technology Major Project(No.2016ZX05007001-002).
文摘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.
文摘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.
