Objective: To synthesize inhibitors of the epidermal growth factor receptor tyrosine kinase such as 6-nitro-4-anilinoquinazolines and 6-amino-4-anilinoquinazolines,and to compare their anticancer effects in vitro. Met...Objective: To synthesize inhibitors of the epidermal growth factor receptor tyrosine kinase such as 6-nitro-4-anilinoquinazolines and 6-amino-4-anilinoquinazolines,and to compare their anticancer effects in vitro. Methods: The 4-anilinoquinazolines compounds were prepared by hydrolyzed, ringed, halagenated, substituded in turn from 2-amino-5-nitrobenzylcarbonitril. The synthesized 4- anilinoquinazoline compounds has been rudimentarily screened by using A431 tumor cell line which overexpresses epidermal growth factor receptor as model adopted MTT method. Results: Five 6-nitro-4-halo-sbstituted anilinoquinazolines and five 6-amino-4-halo-substituted anilinoquinazolines have been obtained,and all of them had anticancer activity. The anticancer activity of 6-amino substituted inhibitors was higher than that of 6-nitro substituted inhibitors. However, the difference of anticancer activity between two series of quinazoline was much less than that of their inhibiting EGFR tyrosine kinase activity. Conclusion: The probable reason for 6-nitro-4-anilinoquinazolines having anticancer activity in vitro was that they had been partially transformed to 6-amino-4-anilinoquinazolines through endocellular cytochrome oxidation-reduction system.展开更多
The effects of combined use of earthworm extract（912）and HpD-laser on the produc-tion of reactive oxygen and the biosynthesis of DNA in S<sub>180</sub> tumor cells were studied throughchemiluminescence m...The effects of combined use of earthworm extract（912）and HpD-laser on the produc-tion of reactive oxygen and the biosynthesis of DNA in S<sub>180</sub> tumor cells were studied throughchemiluminescence measurement and[<sup>3</sup>H]-TdR incorporation assay.The results showed that as com-pared with the control,the intensity of chemiluminescence emitted by tumor cells treatedsimultaneously with 912 and HpD-laser was enhanced more than ten-folds,while that treated with912 or HpD-laser alone was increased only 2～4 folds.The[<sup>3</sup>H]-TdR incorporation into tumorcells of the former group was inhibited upto 74.1%,and that of the latter groups decreased onlyby 42.2% and 40.0%,respectively.In accordance with these biochemical changes,the ultrastructuraldamage of tumor cells of the former,combinedly treated group appeared to be the most serious.This suggests an additive effect of 912 with HpD-laser on tumor cells.In addition,if free radicalscavengers,such as catalase and superoxide dismutase,were added to the reaction systembefore chemiluminescence assay,the luminescent enhancement effect mentioned above was dramaticallyalleviated,implying the presence of O<sub>2</sub><sup> </sup>and H<sub>2</sub>O<sub>2</sub> in the system.Therefore,as to the toxic effecton tumor cells,912 and HpD-laser are not only additive in efficiency,but also similar in theunderlying mechanism of action.展开更多
Cinchonine was employed as backbone for the synthesis of novel phosphite compounds with diol substituents. These monophosphinites were provided in one pot with the yields ranged from 63% to 75%. Their structures were ...Cinchonine was employed as backbone for the synthesis of novel phosphite compounds with diol substituents. These monophosphinites were provided in one pot with the yields ranged from 63% to 75%. Their structures were confirmed by NMR spectroscopy and HRMS. C 2009 Sheng Yong Zhang. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.展开更多
Vitamin E(tocopherol),one of the ma-jor vitamins a human being needs,is an impor-tant antioxidant as well as a radical scavengerin organisms.However,no determinations ofvitamin E concentration for dilatationcardiomyop...Vitamin E(tocopherol),one of the ma-jor vitamins a human being needs,is an impor-tant antioxidant as well as a radical scavengerin organisms.However,no determinations ofvitamin E concentration for dilatationcardiomyopathy have yet been reported athome or abroad.The authors have展开更多
Changes of 5-hydroxytryptamine(5-HT)and 5-hydroxyindoleacetic acid(5-HIAA)levels in brain cortex and serum were studied using spectrofluorometer follow-ing brain injury in rats.Cyproheptadine,a receptor antagonist of ...Changes of 5-hydroxytryptamine(5-HT)and 5-hydroxyindoleacetic acid(5-HIAA)levels in brain cortex and serum were studied using spectrofluorometer follow-ing brain injury in rats.Cyproheptadine,a receptor antagonist of 5-HT,was employedand its effect on alterations of 5-HT and 5-HIAA contents in brain cortex and serum af-ter brain injury was investigated.The results showed that after brain injury levels of5-HT and 5-HIAA in the brain cortex increased markedly,The increase of 5-HT in thebrain cortex reached its peak at 48h after brain injury,and its value was 4.29±0.44μg/g,which was 4.8 times of control value.The increase of 5-HIAA in the brain cortexreached its peak at 24h after brain injury,and its value was 5.48±0.41μg/g,which was5.8times of control value.The change of 5-HT in the serum was not significant,but thelevel of 5-HIAA in the serum was increased significantly.Cyproheptadine could reducelevels of 5-HT and 5-HIAA in this experiment.The value of 5-HT in the brain cortexdecreased to 1.32±0.09μg/g,and the value of 5-HIAA decreased to 1.36±0.10μg/g.Thelevel of 5-HIAA in the serum was also reduced significantly.It was 0.27±0.03μg/ml.展开更多
The efficient synthesis of N-（diphenylmethylene） glycine alkyl esters was achieved for the first microwave irradiation under solvent-free condition, using PEG or quaternary ammonium salts as phase transfer catalysts...The efficient synthesis of N-（diphenylmethylene） glycine alkyl esters was achieved for the first microwave irradiation under solvent-free condition, using PEG or quaternary ammonium salts as phase transfer catalysts （PTCs）. Under the optimum conditions, N-（diphenylmethylene） glycine alkyl esters were obtained in excellent yields in most cases.展开更多
In this study, we found, through biochemical synthesis of DNA with the incorporation of ~3HTdR and morphological observation of the tumor cells, that aidiron (912), an extract from earthworm, had a stronger kilting ef...In this study, we found, through biochemical synthesis of DNA with the incorporation of ~3HTdR and morphological observation of the tumor cells, that aidiron (912), an extract from earthworm, had a stronger kilting effect (27%) on mouse ascitic hepatoma tumor cells (H_(22)) in vitro, and that laser-hematoporphyrin derivative (HpD) combined with 912 markedly enhanced the kilting effect (74%) on tumor cells. By means of the fluoresoence spectrophotography we also dis- covered that the killing effect of laser-HpD-912 on tumor calls was closely related with the produc- tion of free radicals and lipid peroxidation.展开更多
In this study,six thiourea derivatives of cinchona alkaloids with 9-nat or 9-epi-configuration were synthesized.After characterized the structures,we adopted them to the asymmetric'interrupted'Feist-Benary(IFB...In this study,six thiourea derivatives of cinchona alkaloids with 9-nat or 9-epi-configuration were synthesized.After characterized the structures,we adopted them to the asymmetric'interrupted'Feist-Benary(IFB) reaction ofα-haloketones withβ-dicarbonyl compounds,to give optically active dihydrofurans.Various thiourea derivatives as organocatalysts were examined.The corresponding chiral hydroxyl dihydrofurans have been obtained in excellent yields and moderate ees.To the acyclic substrate,we obtained excitin...展开更多
At different,time after copper wire induced into the vitreous of the rabbits,malondialdehydes(MDA)in the retinas and trace element coppar in the aqueous humor and Pa-thology were observed.One day after the induction o...At different,time after copper wire induced into the vitreous of the rabbits,malondialdehydes(MDA)in the retinas and trace element coppar in the aqueous humor and Pa-thology were observed.One day after the induction of copper,the level of MDA increasedabout three times in the retinas of experimental eyes as compared with the control eyes(p【0.01)and the amplitude of electroretinography(ERG)dropped rapidily following increase ofcopper ions in the vitreous.The tncrease of concentration of copper ions in the vitreous wasclosely correlated with that of MDA in the retinas (p【0.01).Early EM examination of ex-perimental eyes reveaisd damage of retinal membranous structure rich in oxygen andpolyunsaturated acid(PUFA),including the ovaer and inner segments of the photoreceptors.These results indicate thu copper-induced isptd peroxidation is an important cause of retinaldumage.展开更多
文摘Objective: To synthesize inhibitors of the epidermal growth factor receptor tyrosine kinase such as 6-nitro-4-anilinoquinazolines and 6-amino-4-anilinoquinazolines,and to compare their anticancer effects in vitro. Methods: The 4-anilinoquinazolines compounds were prepared by hydrolyzed, ringed, halagenated, substituded in turn from 2-amino-5-nitrobenzylcarbonitril. The synthesized 4- anilinoquinazoline compounds has been rudimentarily screened by using A431 tumor cell line which overexpresses epidermal growth factor receptor as model adopted MTT method. Results: Five 6-nitro-4-halo-sbstituted anilinoquinazolines and five 6-amino-4-halo-substituted anilinoquinazolines have been obtained,and all of them had anticancer activity. The anticancer activity of 6-amino substituted inhibitors was higher than that of 6-nitro substituted inhibitors. However, the difference of anticancer activity between two series of quinazoline was much less than that of their inhibiting EGFR tyrosine kinase activity. Conclusion: The probable reason for 6-nitro-4-anilinoquinazolines having anticancer activity in vitro was that they had been partially transformed to 6-amino-4-anilinoquinazolines through endocellular cytochrome oxidation-reduction system.
基金Supported by the National Natural Science Foundation of China No.3860835
文摘The effects of combined use of earthworm extract（912）and HpD-laser on the produc-tion of reactive oxygen and the biosynthesis of DNA in S<sub>180</sub> tumor cells were studied throughchemiluminescence measurement and[<sup>3</sup>H]-TdR incorporation assay.The results showed that as com-pared with the control,the intensity of chemiluminescence emitted by tumor cells treatedsimultaneously with 912 and HpD-laser was enhanced more than ten-folds,while that treated with912 or HpD-laser alone was increased only 2～4 folds.The[<sup>3</sup>H]-TdR incorporation into tumorcells of the former group was inhibited upto 74.1%,and that of the latter groups decreased onlyby 42.2% and 40.0%,respectively.In accordance with these biochemical changes,the ultrastructuraldamage of tumor cells of the former,combinedly treated group appeared to be the most serious.This suggests an additive effect of 912 with HpD-laser on tumor cells.In addition,if free radicalscavengers,such as catalase and superoxide dismutase,were added to the reaction systembefore chemiluminescence assay,the luminescent enhancement effect mentioned above was dramaticallyalleviated,implying the presence of O<sub>2</sub><sup> </sup>and H<sub>2</sub>O<sub>2</sub> in the system.Therefore,as to the toxic effecton tumor cells,912 and HpD-laser are not only additive in efficiency,but also similar in theunderlying mechanism of action.
基金the National Natural Science Foundation of China(Nos.20842007,30600163)Natural Science Basic Research Plan in Shaanxi Province of China(No.SJ08-ZT02) for financial support.
文摘Cinchonine was employed as backbone for the synthesis of novel phosphite compounds with diol substituents. These monophosphinites were provided in one pot with the yields ranged from 63% to 75%. Their structures were confirmed by NMR spectroscopy and HRMS. C 2009 Sheng Yong Zhang. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.
文摘Vitamin E(tocopherol),one of the ma-jor vitamins a human being needs,is an impor-tant antioxidant as well as a radical scavengerin organisms.However,no determinations ofvitamin E concentration for dilatationcardiomyopathy have yet been reported athome or abroad.The authors have
文摘Changes of 5-hydroxytryptamine(5-HT)and 5-hydroxyindoleacetic acid(5-HIAA)levels in brain cortex and serum were studied using spectrofluorometer follow-ing brain injury in rats.Cyproheptadine,a receptor antagonist of 5-HT,was employedand its effect on alterations of 5-HT and 5-HIAA contents in brain cortex and serum af-ter brain injury was investigated.The results showed that after brain injury levels of5-HT and 5-HIAA in the brain cortex increased markedly,The increase of 5-HT in thebrain cortex reached its peak at 48h after brain injury,and its value was 4.29±0.44μg/g,which was 4.8 times of control value.The increase of 5-HIAA in the brain cortexreached its peak at 24h after brain injury,and its value was 5.48±0.41μg/g,which was5.8times of control value.The change of 5-HT in the serum was not significant,but thelevel of 5-HIAA in the serum was increased significantly.Cyproheptadine could reducelevels of 5-HT and 5-HIAA in this experiment.The value of 5-HT in the brain cortexdecreased to 1.32±0.09μg/g,and the value of 5-HIAA decreased to 1.36±0.10μg/g.Thelevel of 5-HIAA in the serum was also reduced significantly.It was 0.27±0.03μg/ml.
基金the National Natural Science Foundation of China(Nos.20572131, 20702063).
文摘The efficient synthesis of N-（diphenylmethylene） glycine alkyl esters was achieved for the first microwave irradiation under solvent-free condition, using PEG or quaternary ammonium salts as phase transfer catalysts （PTCs）. Under the optimum conditions, N-（diphenylmethylene） glycine alkyl esters were obtained in excellent yields in most cases.
文摘In this study, we found, through biochemical synthesis of DNA with the incorporation of ~3HTdR and morphological observation of the tumor cells, that aidiron (912), an extract from earthworm, had a stronger kilting effect (27%) on mouse ascitic hepatoma tumor cells (H_(22)) in vitro, and that laser-hematoporphyrin derivative (HpD) combined with 912 markedly enhanced the kilting effect (74%) on tumor cells. By means of the fluoresoence spectrophotography we also dis- covered that the killing effect of laser-HpD-912 on tumor calls was closely related with the produc- tion of free radicals and lipid peroxidation.
基金the National Natural Science Foundation of China(Nos.20572131,20372083,20972189,20672141,30901883)
文摘In this study,six thiourea derivatives of cinchona alkaloids with 9-nat or 9-epi-configuration were synthesized.After characterized the structures,we adopted them to the asymmetric'interrupted'Feist-Benary(IFB) reaction ofα-haloketones withβ-dicarbonyl compounds,to give optically active dihydrofurans.Various thiourea derivatives as organocatalysts were examined.The corresponding chiral hydroxyl dihydrofurans have been obtained in excellent yields and moderate ees.To the acyclic substrate,we obtained excitin...
文摘At different,time after copper wire induced into the vitreous of the rabbits,malondialdehydes(MDA)in the retinas and trace element coppar in the aqueous humor and Pa-thology were observed.One day after the induction of copper,the level of MDA increasedabout three times in the retinas of experimental eyes as compared with the control eyes(p【0.01)and the amplitude of electroretinography(ERG)dropped rapidily following increase ofcopper ions in the vitreous.The tncrease of concentration of copper ions in the vitreous wasclosely correlated with that of MDA in the retinas (p【0.01).Early EM examination of ex-perimental eyes reveaisd damage of retinal membranous structure rich in oxygen andpolyunsaturated acid(PUFA),including the ovaer and inner segments of the photoreceptors.These results indicate thu copper-induced isptd peroxidation is an important cause of retinaldumage.
