The 1,3,5-triazine diphosphine oxide ligands with donor-acceptor properties formed strong complexes with europium(Ⅲ) ion in acetonitrile. Spectrophotometric titrations and mass spectra indicated that two ligands co...The 1,3,5-triazine diphosphine oxide ligands with donor-acceptor properties formed strong complexes with europium(Ⅲ) ion in acetonitrile. Spectrophotometric titrations and mass spectra indicated that two ligands coordinated to one europium ion. The stability constants varied from 11.64 to 14.60 (log 13). Binary complexes exhibited rather weak luminescence in solution. 1,3,5-triazine diphosphine oxides engaged as co-ligands in Eu(Ⅲ) (2-thenoyltrifluoroacetonate)3 complex contributed to the overall photoluminescence and allowed for excitation with longer wavelengths than the parent complex.展开更多
A differential pulse voltammetric method was developed for the sensitive andselective determination of Cu(II) at 4-methoxy-2,6-bis(3,5-dimethylpyrazoyl)-l,3,5-triazine modifiedcarbon paste electrode in 0.05 mol/L KHC_...A differential pulse voltammetric method was developed for the sensitive andselective determination of Cu(II) at 4-methoxy-2,6-bis(3,5-dimethylpyrazoyl)-l,3,5-triazine modifiedcarbon paste electrode in 0.05 mol/L KHC_8H_4O_4 solution (pH = 4.02). The oxidation peak of Cu(II)was observed at 0.065 V(vs Ag/AgCl) by scanning the potential in positive direction. The analysisprocedure consisted of an open circuit accumulation step in stirred sample solution. It was followedby medium exchange to a clean solution and subsequently an anodic potential scan was affected toobtain the voltammetric peak. The current was proportional to the concentration of the Cu(II) ion ina range of 1 X 10^(-7) -1 X 10^(-4) mol/L for 6 min accumulation; the most of metal ions did notinterfere with the determination. The developed method was applied to Cu (II) determination incoal-ash sample, the results agreed with that of atomic adsorption spectroscopy (AAS).展开更多
A disubstituted triazine compound, namely, 2-amino-4,6-bis(diphenoxyl phosphorramide)-1,3,5-triazine, which is an inherent flame retardant monomer, was synthesized specifically, and its structure was characterized b...A disubstituted triazine compound, namely, 2-amino-4,6-bis(diphenoxyl phosphorramide)-1,3,5-triazine, which is an inherent flame retardant monomer, was synthesized specifically, and its structure was characterized by using NMR spectrum and X-ray single-crystal diffraction. Unit cell parameters: space group P21/c, Z=4, a=8.7494(15), b=27.518(5), c=12.511(2),β=109.323(16) , Z=4, V=2842.7(9)β3 , Dc=1.380 g/cm3 , F(000)=1224 and Mr=590.46. All the atoms are in the general positions.展开更多
Reaction products of 2,4,6-tris(4-phenyl-phenoxy)-1,3,5-triazine derived from 4-phenylphenol cyanate ester and phenyl glycidyl ether were analyzed. In addition to an isocyanurate compound and an oxazolidone compound w...Reaction products of 2,4,6-tris(4-phenyl-phenoxy)-1,3,5-triazine derived from 4-phenylphenol cyanate ester and phenyl glycidyl ether were analyzed. In addition to an isocyanurate compound and an oxazolidone compound which were well known as reaction products of cyanate esters and epoxy resins, compounds with hybrid ring structure of cyanurate/isocyanurate were determined. Gibbs free energies of the compound having hybrid ring structure of cyanurate/isocyanurate with two isocyanurate moiety were found to be lower than that of the compound with cyanurate ring structure through calculations. Calculation data supported the existence of hybrid ring structure of cy-anurate/isocyanurate. It was revealed that isomerization from cyanurate to isocyanurate occurs via hybrid ring structure of cyanurate/isocyanurate in the reaction of aryl cyanurate and epoxy.展开更多
In order to explore the novel anti-tumor agents,ten 6-arylmethyl-3-aryl-777-thiazolo[3,2-b],2,4-triazin-7-ones were designed and synthesized,and the structures were characterized by ^1H-NMR,MS,IR and X-ray single-crys...In order to explore the novel anti-tumor agents,ten 6-arylmethyl-3-aryl-777-thiazolo[3,2-b],2,4-triazin-7-ones were designed and synthesized,and the structures were characterized by ^1H-NMR,MS,IR and X-ray single-crystal diffraction analysis.The biological activity results showed that the target compounds exhibited certain inhibitory activity of osteosarcoma cells U2OS-EGFP.Compounds 6a,6g and 6j exhibited more than 70%inhibition ratio at the concentration of 50μmol·L^-1,and especially,the IC5o value of compound 6j was 11.58μmol·L^-1.The crystal of 6h was obtained and analyzed;some related weak interactions were discussed.The molecular docking results showed that the target compounds were supposed to be ERK1/2 inhibitors.展开更多
A dinuclear Zn( complex C66H48Cl4N24Zn2·2CH3OH·2H2O (1) was synthesized and characterized by X-ray crystallography. In the complex, two 2,4,6-tris[bis(2-pyridyl)amino]-1,3,5-triazine ligands are bridged toge...A dinuclear Zn( complex C66H48Cl4N24Zn2·2CH3OH·2H2O (1) was synthesized and characterized by X-ray crystallography. In the complex, two 2,4,6-tris[bis(2-pyridyl)amino]-1,3,5-triazine ligands are bridged together by two zinc( ions and stacked in a parallel manner. CCDC: 267649.展开更多
In an attempt to develop potent and selective anticancer agents,we designed and synthesized a series of novel bis(morpholino-1,3,5-triazine) derivatives beating aylmethylene hydrazine moiety and evaluated their cyto...In an attempt to develop potent and selective anticancer agents,we designed and synthesized a series of novel bis(morpholino-1,3,5-triazine) derivatives beating aylmethylene hydrazine moiety and evaluated their cytotoxicity,in vitro,against H460(non-small-cell lung cancer),HT-29(human colorectal cancer) and MDA-MB-231(human breast cancer) cell lines.The pharmacological results indicate that all the compounds exhibit enhanced cytotoxicity than BMCL-200908069-1,and six target compounds(7e,7h,7j,9a,9b,9c) were superior to PAC-1 against all the tested cancer cell lines.The most active compound 7j,with IC50(inhibitory concentration 50%)values of 0.75,0.34 and 0.60 μ mol/L against HT-29,H460 and MDA-MB-231 cancer cell lines,was 39-,28-,and 60-fold more potent than BMCL-200908069-1 (29.24,9.52 and 36.21 μmol/L),respectively.展开更多
The 1,3,5-triazine-water hydrogen bonding interactions have been investigated using the density functional theory B3LYP method and 6-31 ++G^** basis, obtaining one, two and seven energy minima of the ground states...The 1,3,5-triazine-water hydrogen bonding interactions have been investigated using the density functional theory B3LYP method and 6-31 ++G^** basis, obtaining one, two and seven energy minima of the ground states for the 1,3,5-triazine-water, 1,3,5-triazine-(water)2 and 1,3,5-triazine-(water)3 complexes respectively. The fully optimized geometries and binding energies were reported for the various stationary points. The global minima of 1,3,5-triazine-(water)2 and 1,3,5-triazine-(water)3 complexes have a hydrogen bond N…H-O and a chain of water molecules, terminated by a hydrogen bond O…H-C. The binding energies are 13.38, 39.52 and 67.79 kJ/mol for the most stable 1,3,5-triazine-water, 1,3,5-triazine-(water)2 and 1,3,5-triazine-(water)3 complexes respectively, after the basis set superposition error and zero point energy corrections. The H-O symmetric stretching modes of water in the complexes are red-shifted relative to those of the monomer water. In addition, the NBO analysis indicates that inter-molecule charge transfer is 0.02145 e, 0.02501 e and 0.02777 e for the most stable 1 : 1, 1 : 2 and 1 : 3 complexes between 1,3,5-triazine and water, respectively.展开更多
The reaction of 2,4,6-tris(2-pyridyl)-1,3,5-triazine (tptz) and K2PdCl4 in THF/H2O (10:1) results in the hydrolysis of tptz to bis(2-pyridylcarbonyl)amide anion (bpca), and affords complex Pd(bpca)Cl 1, w...The reaction of 2,4,6-tris(2-pyridyl)-1,3,5-triazine (tptz) and K2PdCl4 in THF/H2O (10:1) results in the hydrolysis of tptz to bis(2-pyridylcarbonyl)amide anion (bpca), and affords complex Pd(bpca)Cl 1, which is the first example of Pd(Ⅱ)-promoted hydrolysis of ligands. Crystal data for 1: orthorhombic, space group Pbcn, a = 12.0136(17), b = 14.180(2), c = 6.9747(11)A, V= 1188.2(3) A3, Z = 4, Mr = 368.06, Dc = 2.058 g/cm3, F(000) = 720,μ = 1.786 mm^-1, λ(MoKα) = 0.71073 A, T= 293(2) K, 2θmax = 54.9°, GOOF = 1.085, the final R= 0.0647 and wR = 0.1051 for 1234 observed reflections with I 〉 2σ(I) (refinement on F2). Complex 1 is connected through hydrogen bonding to give a 2D network. And weak Pd...Pd interactions are also found between adjacent molecules with the distance of 3.6074(5) A, so the complex is further extended into a 3D supramolecular structure. Thermal gravity analysis (TGA) shows that 1 exhibits high thermal stability below 310℃. X-ray powder diffraction (XRD) and UV/Vis spectrum of 1 are also discussed.展开更多
In order to remove hexahydro-1,3,5-trinitro-1,3,5-triazine(RDX),the main impurity,in process of polymorphic transformation of octrahydro-1,3,5,7-tetranitro-1,3,5,7-tetrazocine(HMX),the solubility ofβ-HMX and RDX in a...In order to remove hexahydro-1,3,5-trinitro-1,3,5-triazine(RDX),the main impurity,in process of polymorphic transformation of octrahydro-1,3,5,7-tetranitro-1,3,5,7-tetrazocine(HMX),the solubility ofβ-HMX and RDX in acetonitrile(ACN)+water in the temperature range of 288.15-333.15 K and in nitric acid(HNO_(3))+water in the temperature range of 298.15-333.15 K were measured by laser dynamic method.The results showed that the solubility of bothβ-HMX and RDX in binary mixed solvents increased monotonously as the temperature increase at a given solvent composition or with increasing of mole fraction of solvent(ACN and nitric acid).Solubility data were well correlated by the modified Apelblat equation,Jouyban-Acree model,Yaws equation and van't Hoff equation,and the Yaws equation achieved the best fitting results according to the relative error and the mean square error root.Furthermore,the solubility ofβ-HMX and RDX in binary mixed solvent was compared,based on the solubility difference and the solvent's own properties,the best separation degree ofβ-HMX and RDX was found when the mole fraction of nitric acid was 0.22 at room temperature,which provided data support for HMX crystallization in mixed solvent.The solubility differences between RDX andβ-HMX in mixed solvents were explained from the formation of intermolecular and intramolecular hydrogen bonds.展开更多
Background:In the early metastasis of colon cancer,cancer cells detach,migrate,and infiltrate surrounding tissues,including lymph vessels and blood vessels.Tumor heterogeneity arises from both tumor cells and distinct...Background:In the early metastasis of colon cancer,cancer cells detach,migrate,and infiltrate surrounding tissues,including lymph vessels and blood vessels.Tumor heterogeneity arises from both tumor cells and distinct microenvironments.Maldistribution of blood vessels,creates hypoxic regions within the tumors,fostering cancer stem cell-like properties due to reduced oxygen and nutrient supply.Under hypoxia,tumor cells shift to a glycolytic pathway,producing more lactic acid that acidifies the microenvironment and leads to unstable heart rate variability(HRV)factors,weight disparity,and a higher incidence of aberrant crypt foci(ACF).These hypoxic-induced parameters promote cancer cell invasion,increase radiation resistance,and facilitate cancer cell migration.Methods:In this study,we induced hypoxia-preneoplastic colon damage in albino Wister rats by administrating 1,2-dimethyl hydrazine(DMH).After successfully creating a hypoxic environment in albino Wister rats,resulting in preneoplastic colon damage,we randomly allocated Wistar albino rats into seven groups,each containing 8 animals,and conducted a 6-week study.Group 1-Normal control(administered 1 mM EDTA+saline,2 ml/kg/day,p.o.);group 2-Toxic control(administered DMH,30 mg/kg/week,s.c.);group 3-Standard treatment(DMH,30 mg/kg/week,s.c.for 6 weeks),followed by 5-fluorouracil and Leucovorin(25 mg/kg each on 1^(st),3^(rd),7^(th),and 10^(th) days,i.p.after 6 weeks administration of DMH);group 4-Low dose of P1(DMH,30 mg/kg/week,s.c.+P1,2 mg/kg,i.v.,weekly for 3 weeks);group 5-High dose P1(DMH,30 mg/kg/week,s.c.+P1,4 mg/kg,i.v.,weekly for 3 weeks),group 6-Low dose of P2(DMH,30 mg/kg/week,s.c.,+P2,2 mg/kg,i.v.,weekly for 3 weeks),group 7-High dose of P2(DMH,30 mg/kg/week,s.c.,+P2,4 mg/kg,i.v.weekly for 3 weeks).Results:DMH-treated rats exhibited alterations in HRV factors,weight disparity,elevated gastric pH,increased total acidity,a higher incidence of ACF,and changes in antioxidant markers(TBARs,SOD,catalase,GSH).Brightfield microscopy at 40x magnification revealed the presence of large crypts within aberrant crypt foci in the toxic control group.Conclusion:Treatment groups P1 and P2 containing triazine derivatives initiated proteasomal degradation of Hypoxia Inducible Factor-1α(HIF-1α)by activating Prolyl Hydroxylase(PHDs)pathways.HIF-1αunder a hypoxic environment is responsible for activating a multitude of genes involved in angiogenesis,metastasis,invasiveness,pH changes,metabolic reprogramming,stem cell maintenance,resistance to radiation,and downstream regulation of the immune system.Treatment with P1 and P2 groups helped minimize the ACF count and restored HRV factors,weight disparity,pH levels,total acidity,and oxidative balance.Our findings emphasize the potential role of 1,2,4-triazine derivatives in suppressing hypoxia-induced colon carcinogenesis.展开更多
A new s-triazine derivative modified graphene composite, in which 2,4,6-tri(2,4-dihydroxyphenyl)-1,3,5- triazine (TDTA) was attached onto reduced graphene oxide (rGO) via the noncovalent functionalization approa...A new s-triazine derivative modified graphene composite, in which 2,4,6-tri(2,4-dihydroxyphenyl)-1,3,5- triazine (TDTA) was attached onto reduced graphene oxide (rGO) via the noncovalent functionalization approach, named TDTA/rGO, was reported. And the TDTA was synthesized via a Friedel-Crafts reaction. FTIR and NMR spectroscopic characterizations were carried out to confirm the synthesis of TDTA. UV-Vis, XPS and TEM revealed that TDTA molecules were successfully loaded onto graphene sheets by π-π stacking, and the composite is found to improve greatly the dispersity ofrGO in DMF and to be a good UV-absorber.展开更多
基金support from the Polish Ministry of Science and Higher Education (3T09A 081 28)
文摘The 1,3,5-triazine diphosphine oxide ligands with donor-acceptor properties formed strong complexes with europium(Ⅲ) ion in acetonitrile. Spectrophotometric titrations and mass spectra indicated that two ligands coordinated to one europium ion. The stability constants varied from 11.64 to 14.60 (log 13). Binary complexes exhibited rather weak luminescence in solution. 1,3,5-triazine diphosphine oxides engaged as co-ligands in Eu(Ⅲ) (2-thenoyltrifluoroacetonate)3 complex contributed to the overall photoluminescence and allowed for excitation with longer wavelengths than the parent complex.
文摘A differential pulse voltammetric method was developed for the sensitive andselective determination of Cu(II) at 4-methoxy-2,6-bis(3,5-dimethylpyrazoyl)-l,3,5-triazine modifiedcarbon paste electrode in 0.05 mol/L KHC_8H_4O_4 solution (pH = 4.02). The oxidation peak of Cu(II)was observed at 0.065 V(vs Ag/AgCl) by scanning the potential in positive direction. The analysisprocedure consisted of an open circuit accumulation step in stirred sample solution. It was followedby medium exchange to a clean solution and subsequently an anodic potential scan was affected toobtain the voltammetric peak. The current was proportional to the concentration of the Cu(II) ion ina range of 1 X 10^(-7) -1 X 10^(-4) mol/L for 6 min accumulation; the most of metal ions did notinterfere with the determination. The developed method was applied to Cu (II) determination incoal-ash sample, the results agreed with that of atomic adsorption spectroscopy (AAS).
文摘A disubstituted triazine compound, namely, 2-amino-4,6-bis(diphenoxyl phosphorramide)-1,3,5-triazine, which is an inherent flame retardant monomer, was synthesized specifically, and its structure was characterized by using NMR spectrum and X-ray single-crystal diffraction. Unit cell parameters: space group P21/c, Z=4, a=8.7494(15), b=27.518(5), c=12.511(2),β=109.323(16) , Z=4, V=2842.7(9)β3 , Dc=1.380 g/cm3 , F(000)=1224 and Mr=590.46. All the atoms are in the general positions.
文摘Reaction products of 2,4,6-tris(4-phenyl-phenoxy)-1,3,5-triazine derived from 4-phenylphenol cyanate ester and phenyl glycidyl ether were analyzed. In addition to an isocyanurate compound and an oxazolidone compound which were well known as reaction products of cyanate esters and epoxy resins, compounds with hybrid ring structure of cyanurate/isocyanurate were determined. Gibbs free energies of the compound having hybrid ring structure of cyanurate/isocyanurate with two isocyanurate moiety were found to be lower than that of the compound with cyanurate ring structure through calculations. Calculation data supported the existence of hybrid ring structure of cy-anurate/isocyanurate. It was revealed that isomerization from cyanurate to isocyanurate occurs via hybrid ring structure of cyanurate/isocyanurate in the reaction of aryl cyanurate and epoxy.
基金supported by the National Natural Science Foundation of China(No.21342006)the Program for Innovative Research Team of the Ministry of Education of China(No.IRT_14R36)
文摘In order to explore the novel anti-tumor agents,ten 6-arylmethyl-3-aryl-777-thiazolo[3,2-b],2,4-triazin-7-ones were designed and synthesized,and the structures were characterized by ^1H-NMR,MS,IR and X-ray single-crystal diffraction analysis.The biological activity results showed that the target compounds exhibited certain inhibitory activity of osteosarcoma cells U2OS-EGFP.Compounds 6a,6g and 6j exhibited more than 70%inhibition ratio at the concentration of 50μmol·L^-1,and especially,the IC5o value of compound 6j was 11.58μmol·L^-1.The crystal of 6h was obtained and analyzed;some related weak interactions were discussed.The molecular docking results showed that the target compounds were supposed to be ERK1/2 inhibitors.
文摘A dinuclear Zn( complex C66H48Cl4N24Zn2·2CH3OH·2H2O (1) was synthesized and characterized by X-ray crystallography. In the complex, two 2,4,6-tris[bis(2-pyridyl)amino]-1,3,5-triazine ligands are bridged together by two zinc( ions and stacked in a parallel manner. CCDC: 267649.
文摘In an attempt to develop potent and selective anticancer agents,we designed and synthesized a series of novel bis(morpholino-1,3,5-triazine) derivatives beating aylmethylene hydrazine moiety and evaluated their cytotoxicity,in vitro,against H460(non-small-cell lung cancer),HT-29(human colorectal cancer) and MDA-MB-231(human breast cancer) cell lines.The pharmacological results indicate that all the compounds exhibit enhanced cytotoxicity than BMCL-200908069-1,and six target compounds(7e,7h,7j,9a,9b,9c) were superior to PAC-1 against all the tested cancer cell lines.The most active compound 7j,with IC50(inhibitory concentration 50%)values of 0.75,0.34 and 0.60 μ mol/L against HT-29,H460 and MDA-MB-231 cancer cell lines,was 39-,28-,and 60-fold more potent than BMCL-200908069-1 (29.24,9.52 and 36.21 μmol/L),respectively.
基金Project supported by the Sichuan Province Scientific Foundation for Youth and the Sichuan Province Scientific Foundation (No. 06ZQ026-019) and the National Natural Science Foundation of China (No. 50473062).
文摘The 1,3,5-triazine-water hydrogen bonding interactions have been investigated using the density functional theory B3LYP method and 6-31 ++G^** basis, obtaining one, two and seven energy minima of the ground states for the 1,3,5-triazine-water, 1,3,5-triazine-(water)2 and 1,3,5-triazine-(water)3 complexes respectively. The fully optimized geometries and binding energies were reported for the various stationary points. The global minima of 1,3,5-triazine-(water)2 and 1,3,5-triazine-(water)3 complexes have a hydrogen bond N…H-O and a chain of water molecules, terminated by a hydrogen bond O…H-C. The binding energies are 13.38, 39.52 and 67.79 kJ/mol for the most stable 1,3,5-triazine-water, 1,3,5-triazine-(water)2 and 1,3,5-triazine-(water)3 complexes respectively, after the basis set superposition error and zero point energy corrections. The H-O symmetric stretching modes of water in the complexes are red-shifted relative to those of the monomer water. In addition, the NBO analysis indicates that inter-molecule charge transfer is 0.02145 e, 0.02501 e and 0.02777 e for the most stable 1 : 1, 1 : 2 and 1 : 3 complexes between 1,3,5-triazine and water, respectively.
基金supported by 973 Program (2006CB932900)the National Natural Science Foundation of China (20571074)
文摘The reaction of 2,4,6-tris(2-pyridyl)-1,3,5-triazine (tptz) and K2PdCl4 in THF/H2O (10:1) results in the hydrolysis of tptz to bis(2-pyridylcarbonyl)amide anion (bpca), and affords complex Pd(bpca)Cl 1, which is the first example of Pd(Ⅱ)-promoted hydrolysis of ligands. Crystal data for 1: orthorhombic, space group Pbcn, a = 12.0136(17), b = 14.180(2), c = 6.9747(11)A, V= 1188.2(3) A3, Z = 4, Mr = 368.06, Dc = 2.058 g/cm3, F(000) = 720,μ = 1.786 mm^-1, λ(MoKα) = 0.71073 A, T= 293(2) K, 2θmax = 54.9°, GOOF = 1.085, the final R= 0.0647 and wR = 0.1051 for 1234 observed reflections with I 〉 2σ(I) (refinement on F2). Complex 1 is connected through hydrogen bonding to give a 2D network. And weak Pd...Pd interactions are also found between adjacent molecules with the distance of 3.6074(5) A, so the complex is further extended into a 3D supramolecular structure. Thermal gravity analysis (TGA) shows that 1 exhibits high thermal stability below 310℃. X-ray powder diffraction (XRD) and UV/Vis spectrum of 1 are also discussed.
文摘In order to remove hexahydro-1,3,5-trinitro-1,3,5-triazine(RDX),the main impurity,in process of polymorphic transformation of octrahydro-1,3,5,7-tetranitro-1,3,5,7-tetrazocine(HMX),the solubility ofβ-HMX and RDX in acetonitrile(ACN)+water in the temperature range of 288.15-333.15 K and in nitric acid(HNO_(3))+water in the temperature range of 298.15-333.15 K were measured by laser dynamic method.The results showed that the solubility of bothβ-HMX and RDX in binary mixed solvents increased monotonously as the temperature increase at a given solvent composition or with increasing of mole fraction of solvent(ACN and nitric acid).Solubility data were well correlated by the modified Apelblat equation,Jouyban-Acree model,Yaws equation and van't Hoff equation,and the Yaws equation achieved the best fitting results according to the relative error and the mean square error root.Furthermore,the solubility ofβ-HMX and RDX in binary mixed solvent was compared,based on the solubility difference and the solvent's own properties,the best separation degree ofβ-HMX and RDX was found when the mole fraction of nitric acid was 0.22 at room temperature,which provided data support for HMX crystallization in mixed solvent.The solubility differences between RDX andβ-HMX in mixed solvents were explained from the formation of intermolecular and intramolecular hydrogen bonds.
基金C.Karthikeyan,Indira Gandhi National Tribal University,Lalpur,Amarkantak,Anuppur,Madhya Pradesh,484887,India,for providing the gift sample of 1,2,4-triazine derivatives used for the study.
文摘Background:In the early metastasis of colon cancer,cancer cells detach,migrate,and infiltrate surrounding tissues,including lymph vessels and blood vessels.Tumor heterogeneity arises from both tumor cells and distinct microenvironments.Maldistribution of blood vessels,creates hypoxic regions within the tumors,fostering cancer stem cell-like properties due to reduced oxygen and nutrient supply.Under hypoxia,tumor cells shift to a glycolytic pathway,producing more lactic acid that acidifies the microenvironment and leads to unstable heart rate variability(HRV)factors,weight disparity,and a higher incidence of aberrant crypt foci(ACF).These hypoxic-induced parameters promote cancer cell invasion,increase radiation resistance,and facilitate cancer cell migration.Methods:In this study,we induced hypoxia-preneoplastic colon damage in albino Wister rats by administrating 1,2-dimethyl hydrazine(DMH).After successfully creating a hypoxic environment in albino Wister rats,resulting in preneoplastic colon damage,we randomly allocated Wistar albino rats into seven groups,each containing 8 animals,and conducted a 6-week study.Group 1-Normal control(administered 1 mM EDTA+saline,2 ml/kg/day,p.o.);group 2-Toxic control(administered DMH,30 mg/kg/week,s.c.);group 3-Standard treatment(DMH,30 mg/kg/week,s.c.for 6 weeks),followed by 5-fluorouracil and Leucovorin(25 mg/kg each on 1^(st),3^(rd),7^(th),and 10^(th) days,i.p.after 6 weeks administration of DMH);group 4-Low dose of P1(DMH,30 mg/kg/week,s.c.+P1,2 mg/kg,i.v.,weekly for 3 weeks);group 5-High dose P1(DMH,30 mg/kg/week,s.c.+P1,4 mg/kg,i.v.,weekly for 3 weeks),group 6-Low dose of P2(DMH,30 mg/kg/week,s.c.,+P2,2 mg/kg,i.v.,weekly for 3 weeks),group 7-High dose of P2(DMH,30 mg/kg/week,s.c.,+P2,4 mg/kg,i.v.weekly for 3 weeks).Results:DMH-treated rats exhibited alterations in HRV factors,weight disparity,elevated gastric pH,increased total acidity,a higher incidence of ACF,and changes in antioxidant markers(TBARs,SOD,catalase,GSH).Brightfield microscopy at 40x magnification revealed the presence of large crypts within aberrant crypt foci in the toxic control group.Conclusion:Treatment groups P1 and P2 containing triazine derivatives initiated proteasomal degradation of Hypoxia Inducible Factor-1α(HIF-1α)by activating Prolyl Hydroxylase(PHDs)pathways.HIF-1αunder a hypoxic environment is responsible for activating a multitude of genes involved in angiogenesis,metastasis,invasiveness,pH changes,metabolic reprogramming,stem cell maintenance,resistance to radiation,and downstream regulation of the immune system.Treatment with P1 and P2 groups helped minimize the ACF count and restored HRV factors,weight disparity,pH levels,total acidity,and oxidative balance.Our findings emphasize the potential role of 1,2,4-triazine derivatives in suppressing hypoxia-induced colon carcinogenesis.
文摘A new s-triazine derivative modified graphene composite, in which 2,4,6-tri(2,4-dihydroxyphenyl)-1,3,5- triazine (TDTA) was attached onto reduced graphene oxide (rGO) via the noncovalent functionalization approach, named TDTA/rGO, was reported. And the TDTA was synthesized via a Friedel-Crafts reaction. FTIR and NMR spectroscopic characterizations were carried out to confirm the synthesis of TDTA. UV-Vis, XPS and TEM revealed that TDTA molecules were successfully loaded onto graphene sheets by π-π stacking, and the composite is found to improve greatly the dispersity ofrGO in DMF and to be a good UV-absorber.