The residual metal impurities in cisplatin, carboplatin and oxaliplatin were determined by ICP-AES. The samples were ignited and dissolved with HCl:HNO 3 (3:1). The method is simple and accurate. By the determination ...The residual metal impurities in cisplatin, carboplatin and oxaliplatin were determined by ICP-AES. The samples were ignited and dissolved with HCl:HNO 3 (3:1). The method is simple and accurate. By the determination of the metal residues in the samples, the calculated actual daily exposure and concentration of the metal Pd, Ir, Rh, Ru, Mo, Ni, Cr, V, Cu, Mn, Fe and Zn that were less than the permitted daily exposures (PDE) and the limited concentration permitted in the EMEA guideline on the specification limits for residues of metal catalysts or metal reagents [1] . The metal residues can de adequately removed from the active pharmaceutical ingredients and the corresponding drugs. The trace metal residues will not affect human health and lead to the safety hazard by the intravenous injection.展开更多
Nucleotide pools in mammalian cells change due to the influence of antitumor drugs,which may help in evaluating the drug effect and understanding the mechanism of drug action.In this study,an ion-pair RP-HPLC method w...Nucleotide pools in mammalian cells change due to the influence of antitumor drugs,which may help in evaluating the drug effect and understanding the mechanism of drug action.In this study,an ion-pair RP-HPLC method was used for a simple,sensitive and simultaneous determination of the levels of 12 nucleotides in mammalian cells treated with antibiotic antitumor drugs(daunorubicin,epirubicin and dactinomycin D).Through the use of this targeted metabolomics approach to find potential biomarkers,UTP and ATP were verified to be the most appropriate biomarkers.Moreover,a holistic statistical approach was put forward to develop a model which could distinguish 4 categories of drugs with different mechanisms of action.This model can be further validated by evaluating drugs with different mechanismsof action.This targeted metabolomics study may provide a novel approach to predict the mechanism of action of antitumor drugs.展开更多
Traditional tumor models do not tend to accurately simulate tumor growth in vitro or enable personalized treatment and are particularly unable to discover more beneficial targeted drugs.To address this,this study desc...Traditional tumor models do not tend to accurately simulate tumor growth in vitro or enable personalized treatment and are particularly unable to discover more beneficial targeted drugs.To address this,this study describes the use of threedimensional(3D)bioprinting technology to construct a 3D model with human hepatocarcinoma SMMC-7721 cells(3DP-7721)by combining gelatin methacrylate(GelMA)and poly(ethylene oxide)(PEO)as two immiscible aqueous phases to form a bioink and innovatively applying fluorescent carbon quantum dots for long-term tracking of cells.The GelMA(10%,mass fraction)and PEO(1.6%,mass fraction)hydrogel with 3:1 volume ratio offered distinct pore-forming characteristics,satisfactorymechanical properties,and biocompatibility for the creation of the 3DP-7721 model.Immunofluorescence analysis and quantitative real-time fluorescence polymerase chain reaction(PCR)were used to evaluate the biological properties of the model.Compared with the two-dimensional culture cell model(2D-7721)and the 3D mixed culture cell model(3DM-7721),3DP-7721 significantly improved the proliferation of cells and expression of tumor-related proteins and genes.Moreover,we evaluated the differences between the three culture models and the effectiveness of antitumor drugs in the three models and discovered that the efficacy of antitumor drugs varied because of significant differences in resistance proteins and genes between the three models.In addition,the comparison of tumor formation in the three models found that the cells cultured by the 3DP-7721 model had strong tumorigenicity in nude mice.Immunohistochemical evaluation of the levels of biochemical indicators related to the formation of solid tumors showed that the 3DP-7721 model group exhibited pathological characteristics of malignant tumors,the generated solid tumors were similar to actual tumors,and the deterioration was higher.This research therefore acts as a foundation for the application of 3DP-7721 models in drug development research.展开更多
Miriplatin, a novel lipophilic platinum complex has been developed to treat hepatocellular carcinoma. An improvd synthetic route was designed and used to prepare the target compound. The intermediate Pt(C6H14N2)(I) 2 ...Miriplatin, a novel lipophilic platinum complex has been developed to treat hepatocellular carcinoma. An improvd synthetic route was designed and used to prepare the target compound. The intermediate Pt(C6H14N2)(I) 2 was synthesized from K 2 PtCl 4 , KI and (1R,2R)-1,2-cyclohexanediamine, Pt(C 6 H 14 N 2 )(I) 2 was reacted with AgNO 3 to prepare Pt(C 6 H 14 N 2 )(H 2 O) 2 (NO 3 ) 2 solution then was subsequently reacted with CH 3 (CH 2 ) 12 COONa in n-butanol to give target compound with satisfied yield 81%(based on Pt(C 6 H 14 N 2 )I 2 ). The structure of the target compound was identified by elemental analysis, ESI-MS, FT-IR, 1H-NMR, thermal analysis, the structure was consistent with the target compound.展开更多
We isolated a novel lectin(AHL)from Artocarpus hypargyreus Hance and showed its immunomodulatory activities.In this study,the amino acid sequence of AHL was determined by cDNA sequencing.AHL cDNA(875bp)contains a 456-...We isolated a novel lectin(AHL)from Artocarpus hypargyreus Hance and showed its immunomodulatory activities.In this study,the amino acid sequence of AHL was determined by cDNA sequencing.AHL cDNA(875bp)contains a 456-bp open reading frame(ORF),which encodes a protein with 151 amino acids.AHL is a new member of jacalin-related lectin family(JRLs),which share high sequence similarities to KM+and Morniga M,and contain the conserved carbohydrate binding domains.The antitumor activity of AHL was also explored using Jurkat T cell lines.AHL exhibits a strong binding affinity to cell membrane,which can be effectively inhibited by methyl-α-D-galactose.AHL inhibits cell proliferation in a time-and dose-dependent manner through apoptosis,evidenced by morphological changes,phosphatidylserine externalization,poly ADP-ribose polymerase(PARP)cleavage,Bad and Bax up-regulation,and caspase-3 activation.We further showed that the activation of ERK and p38 signaling pathways is involved for the pro-apoptotic effect of AHL.展开更多
基金The national SME technology innovation fund(11C26215305898)Kunming SME technology innovation fund(CJ2011040)
文摘The residual metal impurities in cisplatin, carboplatin and oxaliplatin were determined by ICP-AES. The samples were ignited and dissolved with HCl:HNO 3 (3:1). The method is simple and accurate. By the determination of the metal residues in the samples, the calculated actual daily exposure and concentration of the metal Pd, Ir, Rh, Ru, Mo, Ni, Cr, V, Cu, Mn, Fe and Zn that were less than the permitted daily exposures (PDE) and the limited concentration permitted in the EMEA guideline on the specification limits for residues of metal catalysts or metal reagents [1] . The metal residues can de adequately removed from the active pharmaceutical ingredients and the corresponding drugs. The trace metal residues will not affect human health and lead to the safety hazard by the intravenous injection.
基金supported financially by the Natural Science Foundation of Liaoning Province,China (No.201102210)the Program for Liaoning Innovative Research Team in University (No.LH2012018)
文摘Nucleotide pools in mammalian cells change due to the influence of antitumor drugs,which may help in evaluating the drug effect and understanding the mechanism of drug action.In this study,an ion-pair RP-HPLC method was used for a simple,sensitive and simultaneous determination of the levels of 12 nucleotides in mammalian cells treated with antibiotic antitumor drugs(daunorubicin,epirubicin and dactinomycin D).Through the use of this targeted metabolomics approach to find potential biomarkers,UTP and ATP were verified to be the most appropriate biomarkers.Moreover,a holistic statistical approach was put forward to develop a model which could distinguish 4 categories of drugs with different mechanisms of action.This model can be further validated by evaluating drugs with different mechanismsof action.This targeted metabolomics study may provide a novel approach to predict the mechanism of action of antitumor drugs.
基金supported by the National Natural Science Foundation of China(Nos.51975400 and 62031022)Shanxi Provincial Key Medical Scientific Research Project(Nos.2020XM06 and 2021XM12)+3 种基金Fundamental Research Program of Shanxi Province(No.202103021224081)Shanxi Provincial Basic Research Project(Nos.202103021221006 and 202103021223040)Scientific and Technological Innovation Programs of Higher Education Institutions in Shanxi(No.2021L044)Shanxi-Zheda Institute of Advanced Materials and Chemical Engineering(No.2022SX-TD026).
文摘Traditional tumor models do not tend to accurately simulate tumor growth in vitro or enable personalized treatment and are particularly unable to discover more beneficial targeted drugs.To address this,this study describes the use of threedimensional(3D)bioprinting technology to construct a 3D model with human hepatocarcinoma SMMC-7721 cells(3DP-7721)by combining gelatin methacrylate(GelMA)and poly(ethylene oxide)(PEO)as two immiscible aqueous phases to form a bioink and innovatively applying fluorescent carbon quantum dots for long-term tracking of cells.The GelMA(10%,mass fraction)and PEO(1.6%,mass fraction)hydrogel with 3:1 volume ratio offered distinct pore-forming characteristics,satisfactorymechanical properties,and biocompatibility for the creation of the 3DP-7721 model.Immunofluorescence analysis and quantitative real-time fluorescence polymerase chain reaction(PCR)were used to evaluate the biological properties of the model.Compared with the two-dimensional culture cell model(2D-7721)and the 3D mixed culture cell model(3DM-7721),3DP-7721 significantly improved the proliferation of cells and expression of tumor-related proteins and genes.Moreover,we evaluated the differences between the three culture models and the effectiveness of antitumor drugs in the three models and discovered that the efficacy of antitumor drugs varied because of significant differences in resistance proteins and genes between the three models.In addition,the comparison of tumor formation in the three models found that the cells cultured by the 3DP-7721 model had strong tumorigenicity in nude mice.Immunohistochemical evaluation of the levels of biochemical indicators related to the formation of solid tumors showed that the 3DP-7721 model group exhibited pathological characteristics of malignant tumors,the generated solid tumors were similar to actual tumors,and the deterioration was higher.This research therefore acts as a foundation for the application of 3DP-7721 models in drug development research.
基金The Yunnan science and technology project(2010DH021)Kunming Wuhua Zoon science and technology project(201037)
文摘Miriplatin, a novel lipophilic platinum complex has been developed to treat hepatocellular carcinoma. An improvd synthetic route was designed and used to prepare the target compound. The intermediate Pt(C6H14N2)(I) 2 was synthesized from K 2 PtCl 4 , KI and (1R,2R)-1,2-cyclohexanediamine, Pt(C 6 H 14 N 2 )(I) 2 was reacted with AgNO 3 to prepare Pt(C 6 H 14 N 2 )(H 2 O) 2 (NO 3 ) 2 solution then was subsequently reacted with CH 3 (CH 2 ) 12 COONa in n-butanol to give target compound with satisfied yield 81%(based on Pt(C 6 H 14 N 2 )I 2 ). The structure of the target compound was identified by elemental analysis, ESI-MS, FT-IR, 1H-NMR, thermal analysis, the structure was consistent with the target compound.
基金the National Natural Science Foundation of China(No.81160366)the Natural Science Foundation of Guangxi Province,China(Nos.0832130 and 2011 GXNSFA 018195).
文摘We isolated a novel lectin(AHL)from Artocarpus hypargyreus Hance and showed its immunomodulatory activities.In this study,the amino acid sequence of AHL was determined by cDNA sequencing.AHL cDNA(875bp)contains a 456-bp open reading frame(ORF),which encodes a protein with 151 amino acids.AHL is a new member of jacalin-related lectin family(JRLs),which share high sequence similarities to KM+and Morniga M,and contain the conserved carbohydrate binding domains.The antitumor activity of AHL was also explored using Jurkat T cell lines.AHL exhibits a strong binding affinity to cell membrane,which can be effectively inhibited by methyl-α-D-galactose.AHL inhibits cell proliferation in a time-and dose-dependent manner through apoptosis,evidenced by morphological changes,phosphatidylserine externalization,poly ADP-ribose polymerase(PARP)cleavage,Bad and Bax up-regulation,and caspase-3 activation.We further showed that the activation of ERK and p38 signaling pathways is involved for the pro-apoptotic effect of AHL.