2019 Vol. 37, No. 5
Display Method:
2019, 37(5): 385-389,399.
doi: 10.3969/j.issn.1006-0111.2019.05.001
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Metabolomics is a new science to quantitatively or qualitatively analyze all the endogenous small molecule metabolites in biological system(cells,tissues,organs,living organisms),which reveals the metabolic nature of diseases by studying the laws between changes in metabolites and metabolic pathways and physiological and pathological changes.Leukemia is a common malignant tumor of the blood system,which occurrence and development are closely related to metabolism.Endogenous small molecule metabolites discovered by metabolomics had been widely used in the study of pathogenesis,diagnosis and pharmacodynamic mechanism of leukemia and made significant progress.The advances of metabolomics about the study of pathogenesis,diagnosis and pharmacodynamic mechanism of leukemia in recent years were reviewed in this paper in order to provide reference for further research.
Metabolomics is a new science to quantitatively or qualitatively analyze all the endogenous small molecule metabolites in biological system(cells,tissues,organs,living organisms),which reveals the metabolic nature of diseases by studying the laws between changes in metabolites and metabolic pathways and physiological and pathological changes.Leukemia is a common malignant tumor of the blood system,which occurrence and development are closely related to metabolism.Endogenous small molecule metabolites discovered by metabolomics had been widely used in the study of pathogenesis,diagnosis and pharmacodynamic mechanism of leukemia and made significant progress.The advances of metabolomics about the study of pathogenesis,diagnosis and pharmacodynamic mechanism of leukemia in recent years were reviewed in this paper in order to provide reference for further research.
2019, 37(5): 390-393,421.
doi: 10.3969/j.issn.1006-0111.2019.05.002
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Long non-coding RNA (lncRNA) covers most of the messages from the human DNA without protein-coding potential,which is a wide range of complicated molecules that consist of more than 90% of the whole genomic and present in different forms in the course of pathophysiology of cancers.In 2003,lncRNA MEG3 was firstly discovered as a potential tumor-inhibiting factor of pituitary adenomas.Later on,the roles and mechanisms in the regulation of gene expression,imprinting,transcription,and post-translation of MEG3 in meningioma,hepatocellular cancer,lung cancer,neuroendocrine tumor,prostate cancer and other kinds of tumors were further clarified,indicated that the expression of MEG3 was down-regulated or deficient in a wide range of tumors while the expression up-regulation of MEG was greatly correlated with tumor inhibition.The function of MEG3 and its research progress in tumorigenesis were summarized in this paper.
Long non-coding RNA (lncRNA) covers most of the messages from the human DNA without protein-coding potential,which is a wide range of complicated molecules that consist of more than 90% of the whole genomic and present in different forms in the course of pathophysiology of cancers.In 2003,lncRNA MEG3 was firstly discovered as a potential tumor-inhibiting factor of pituitary adenomas.Later on,the roles and mechanisms in the regulation of gene expression,imprinting,transcription,and post-translation of MEG3 in meningioma,hepatocellular cancer,lung cancer,neuroendocrine tumor,prostate cancer and other kinds of tumors were further clarified,indicated that the expression of MEG3 was down-regulated or deficient in a wide range of tumors while the expression up-regulation of MEG was greatly correlated with tumor inhibition.The function of MEG3 and its research progress in tumorigenesis were summarized in this paper.
2019, 37(5): 394-399.
doi: 10.3969/j.issn.1006-0111.2019.05.003
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Biotechnology drugs have attracted increasing attention as a hot topic in research and development of new drugs.The pharmacokinetics of biotechnology drugs shows uniqueness and complexity due to the different physical and chemical properties from those of small molecule drugs.In this paper,the concept of biotechnology drugs was described and four main analytical methods for biotechnology drugs were summarized,the absorption,distribution,metabolism and excretion of biotechnology drugs in vivo were reviewed and the differences in pharmacokinetics between monoclonal antibody drugs,one of the mainstreams of biotechnology drugs,and small molecule drugs were compared.This review was intended to provides a deep and fully understanding for the pharmacokinetic characteristics and mechanisms of biotechnology drugs,which can serve as a supporting reference for the new biotechnology drug screening,R&D,safety evaluation and clinical use of drugs.
Biotechnology drugs have attracted increasing attention as a hot topic in research and development of new drugs.The pharmacokinetics of biotechnology drugs shows uniqueness and complexity due to the different physical and chemical properties from those of small molecule drugs.In this paper,the concept of biotechnology drugs was described and four main analytical methods for biotechnology drugs were summarized,the absorption,distribution,metabolism and excretion of biotechnology drugs in vivo were reviewed and the differences in pharmacokinetics between monoclonal antibody drugs,one of the mainstreams of biotechnology drugs,and small molecule drugs were compared.This review was intended to provides a deep and fully understanding for the pharmacokinetic characteristics and mechanisms of biotechnology drugs,which can serve as a supporting reference for the new biotechnology drug screening,R&D,safety evaluation and clinical use of drugs.
2019, 37(5): 400-405,426.
doi: 10.3969/j.issn.1006-0111.2019.05.004
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Objective To investigate the effect of p62 protein on the lipid autophagy and the expression of inflammatory cytokines in macrophage-derived foam cells. Methods RAW264.7 cells were stimulated by oxidized low density lipoprotein to mimic the formation of macrophage-derived foam cells.The levels of p62 protein and mRNA in macrophage-derived foam cells were detected by Western blot and real-time qPCR.The protein levels of LC3,Plin2 and PEX2 were measured by Western blot in Ox-LDL treated Raw264.7 cells to determine the effects of p62 on autophagy in macrophage-derived foam cells.The TNFα and IL-6 mRNA levels were detected by real-time PCR. Results Ox-LDL up-regulated both autophagy levels and p62 protein levels in RAW264.7 cells.After interfering the expression of p62,the level of LC3-Ⅱ protein decreased,but the protein levels of lipid droplet-related protein Plin2 did not change significantly.The peroxisome-related protein PEX2 level increased.The expression of TNFα and IL-6 also increased.Further studies showed that Nrf2 interference significantly inhibited the up-regulation of p62 by Ox-LDL. Conclusion Ox-LDL mediates the upregulation of p62 through Nrf2 in macrophage-derived foam cells,and p62 may play a protective role in atherosclerosis.
Objective To investigate the effect of p62 protein on the lipid autophagy and the expression of inflammatory cytokines in macrophage-derived foam cells. Methods RAW264.7 cells were stimulated by oxidized low density lipoprotein to mimic the formation of macrophage-derived foam cells.The levels of p62 protein and mRNA in macrophage-derived foam cells were detected by Western blot and real-time qPCR.The protein levels of LC3,Plin2 and PEX2 were measured by Western blot in Ox-LDL treated Raw264.7 cells to determine the effects of p62 on autophagy in macrophage-derived foam cells.The TNFα and IL-6 mRNA levels were detected by real-time PCR. Results Ox-LDL up-regulated both autophagy levels and p62 protein levels in RAW264.7 cells.After interfering the expression of p62,the level of LC3-Ⅱ protein decreased,but the protein levels of lipid droplet-related protein Plin2 did not change significantly.The peroxisome-related protein PEX2 level increased.The expression of TNFα and IL-6 also increased.Further studies showed that Nrf2 interference significantly inhibited the up-regulation of p62 by Ox-LDL. Conclusion Ox-LDL mediates the upregulation of p62 through Nrf2 in macrophage-derived foam cells,and p62 may play a protective role in atherosclerosis.
2019, 37(5): 406-415.
doi: 10.3969/j.issn.1006-0111.2019.05.005
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Objective To identify the chemical constituents in Fuzheng Huayu capsule by ultra performance liquid chromatography-high resolution time of flight mass spectrometry(UHPLC-TOF/MS). Methods ACQUITY UPLCHSS T3(2.1mm×100mm,1.8μm) was used to chromatographic separation; mobile phase 0.1% formic acid aqueous solution(A) -0.1% formic acid acetonitrile solution(B),gradient elution conditions:0-3min,2% B; 3-18 min,2%-50% B; 18-22 min,50%-95% B; 22-25 min,95% B.The equilibration time was 10 min,the flow rate was 0.40 ml/min,and the analysis time was 25 min.Mass spectrometry was performed by an electrospray ion source using a positive-negative ion mode scan with a range of 100-1 100 m/z. Results 154 components were identified at one time,of which 28 were positive and negative ion modes. Conclusion The composition of Fuzheng Huayu capsule was comprehensively clarified in this study,which laid a foundation for further research of this compound.
Objective To identify the chemical constituents in Fuzheng Huayu capsule by ultra performance liquid chromatography-high resolution time of flight mass spectrometry(UHPLC-TOF/MS). Methods ACQUITY UPLCHSS T3(2.1mm×100mm,1.8μm) was used to chromatographic separation; mobile phase 0.1% formic acid aqueous solution(A) -0.1% formic acid acetonitrile solution(B),gradient elution conditions:0-3min,2% B; 3-18 min,2%-50% B; 18-22 min,50%-95% B; 22-25 min,95% B.The equilibration time was 10 min,the flow rate was 0.40 ml/min,and the analysis time was 25 min.Mass spectrometry was performed by an electrospray ion source using a positive-negative ion mode scan with a range of 100-1 100 m/z. Results 154 components were identified at one time,of which 28 were positive and negative ion modes. Conclusion The composition of Fuzheng Huayu capsule was comprehensively clarified in this study,which laid a foundation for further research of this compound.
2019, 37(5): 416-421.
doi: 10.3969/j.issn.1006-0111.2019.05.006
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Objective To study the effects of microneedle-roller insertion times on skin permeation. Methods Tretinoin was used as model drug.The in vitro transdermal characteristics in nude mice were studied with Franz diffusion cell and the tissue homogenization method.The drug distribution in nude mice skin was investigated by methylene blue staining and confocal lasers scanning microscope.The skin irritation was evaluated by trans-epidermal water-loss (TEWL) measurement and laser Doppler flowmetry. Results Within the microneedle roller insertion times 1,3,5,8,and 10,the better penetration effect and drug accumulation in skin were achieved with the increment of insertion times.However,there was no significant difference in the skin accumulation between 8 and 10 times of the insertion(P>0.05).The results from methylene blue staining and microscope confocal lasers scanning indicated that the uniformity of needle hole distribution was increased with the increased insertion times.However,some needle hole overlap and skin damages were observed from methylene blue staining when insertion times were more than five.The in vivo drug absorption study indicated that the drug accumulation was inhomogeneous in nude mice skin after one treatment.It was significantly improved after three treatments.The results from TEWL measurements suggested that the recovery time of skin barrier function was 24 hours if insertion was less than five times and 36 hours if more than eight times.The results of laser Doppler flowmetry indicated that the recovery time of skin barrier function was 1 hour if insertion times were less than five,and 2 hours if more than eight times. Conclusion The optimal microneedle insertion time was five times,which could ensure the safety and effectiveness of the skin permeation study in nude mice.
Objective To study the effects of microneedle-roller insertion times on skin permeation. Methods Tretinoin was used as model drug.The in vitro transdermal characteristics in nude mice were studied with Franz diffusion cell and the tissue homogenization method.The drug distribution in nude mice skin was investigated by methylene blue staining and confocal lasers scanning microscope.The skin irritation was evaluated by trans-epidermal water-loss (TEWL) measurement and laser Doppler flowmetry. Results Within the microneedle roller insertion times 1,3,5,8,and 10,the better penetration effect and drug accumulation in skin were achieved with the increment of insertion times.However,there was no significant difference in the skin accumulation between 8 and 10 times of the insertion(P>0.05).The results from methylene blue staining and microscope confocal lasers scanning indicated that the uniformity of needle hole distribution was increased with the increased insertion times.However,some needle hole overlap and skin damages were observed from methylene blue staining when insertion times were more than five.The in vivo drug absorption study indicated that the drug accumulation was inhomogeneous in nude mice skin after one treatment.It was significantly improved after three treatments.The results from TEWL measurements suggested that the recovery time of skin barrier function was 24 hours if insertion was less than five times and 36 hours if more than eight times.The results of laser Doppler flowmetry indicated that the recovery time of skin barrier function was 1 hour if insertion times were less than five,and 2 hours if more than eight times. Conclusion The optimal microneedle insertion time was five times,which could ensure the safety and effectiveness of the skin permeation study in nude mice.
2019, 37(5): 422-426.
doi: 10.3969/j.issn.1006-0111.2019.05.007
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Objective To establish rat polycystic ovary syndrome model with letrozole combined high fat diet. Methods Eighteen 21-day-old female rats were fed with 45% high-fat diet for 16 weeks.Letrozole was started at the 6th week of age until the end of modeling.Eight rats in control group were fed with regular diet and Saline without letrozole at the 6th week of age.The vaginal smear and ovarian histological changes were investigated.The changes in body mass,organ weight,blood testosterone level,glucose tolerance,blood lipid level,fasting insulin and insulin sensitivity index were measured. Results In the model group,the ovary of the rats showed a multi-cystic change,the granulosa cell layer decreased,and the tunica albuginea increased.Compared with the control group,the body weight of the model group increased,the weight of the ovary and inguinal fat increased,the weight and weight index of the uterus and pituitary gland decreased,the triglyceride and low density lipoprotein increased,the area under the glucose tolerance curve increased,the blood testosterone level increased,the fasting insulin increased,and the insulin sensitivity decreased. Conclusion Letrozole combined with high fat diet could establish an effective PCOS model of abnormal endocrine and metabolic phenotype.
Objective To establish rat polycystic ovary syndrome model with letrozole combined high fat diet. Methods Eighteen 21-day-old female rats were fed with 45% high-fat diet for 16 weeks.Letrozole was started at the 6th week of age until the end of modeling.Eight rats in control group were fed with regular diet and Saline without letrozole at the 6th week of age.The vaginal smear and ovarian histological changes were investigated.The changes in body mass,organ weight,blood testosterone level,glucose tolerance,blood lipid level,fasting insulin and insulin sensitivity index were measured. Results In the model group,the ovary of the rats showed a multi-cystic change,the granulosa cell layer decreased,and the tunica albuginea increased.Compared with the control group,the body weight of the model group increased,the weight of the ovary and inguinal fat increased,the weight and weight index of the uterus and pituitary gland decreased,the triglyceride and low density lipoprotein increased,the area under the glucose tolerance curve increased,the blood testosterone level increased,the fasting insulin increased,and the insulin sensitivity decreased. Conclusion Letrozole combined with high fat diet could establish an effective PCOS model of abnormal endocrine and metabolic phenotype.
2019, 37(5): 427-432.
doi: 10.3969/j.issn.1006-0111.2019.05.008
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Objective To investigate the correlation between anti-insomnia effects and HPLC fingerprint of compound caulis polygoni multiflori mixture. Methods A fingerprinting method was established by high performance liquid chromatography and then used to analyze different batches of compound caulis polygoni multiflori mixture.Rat insomnia model was established by intraperitoneal injection of p-chlorophenylalanine,5-HT in rat hippocampus was determined by ELISA.Then the orthogonal partial least squares (OPLS)analysis was used to investigate the spectrum-effect relationship. Results 21 common peaks were identified from the fingerprints,the variable projection importance (VIP)values of these 12 peaks were more than 1.0,indicated that the 3 peaks had played an important role in the anti-insomnia activity of compound caulis polygoni multiflori mixture. Conclusion The anti-insomnia activity of compound caulis polygoni multiflori mixture was the result of synergistic effect of multiple components,its material basis could be analyzed by spectrum-effect relationship,which could provide basis for the quality control of preparation.
Objective To investigate the correlation between anti-insomnia effects and HPLC fingerprint of compound caulis polygoni multiflori mixture. Methods A fingerprinting method was established by high performance liquid chromatography and then used to analyze different batches of compound caulis polygoni multiflori mixture.Rat insomnia model was established by intraperitoneal injection of p-chlorophenylalanine,5-HT in rat hippocampus was determined by ELISA.Then the orthogonal partial least squares (OPLS)analysis was used to investigate the spectrum-effect relationship. Results 21 common peaks were identified from the fingerprints,the variable projection importance (VIP)values of these 12 peaks were more than 1.0,indicated that the 3 peaks had played an important role in the anti-insomnia activity of compound caulis polygoni multiflori mixture. Conclusion The anti-insomnia activity of compound caulis polygoni multiflori mixture was the result of synergistic effect of multiple components,its material basis could be analyzed by spectrum-effect relationship,which could provide basis for the quality control of preparation.
2019, 37(5): 433-439.
doi: 10.3969/j.issn.1006-0111.2019.05.009
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Objective To study the regulation and mechanism of hsa-miRNA-30a-5p on the proliferation of human lung cancer A549 cells. Methods Five pairs of lung cancer and para-carcinoma tissues were harvested in clinical and measured for hsa-miRNA-30a-5p and SCARA5 levels by real-time PCR and western blotting,respectively.The theoretical binding site of hsa-miRNA-30a-5p in SCARA5's 3'UTR was predicted by bioinformatics,and validated by luciferase report assay.A549 cells were transfected with pshRNA-SCARA5 and miRNA-30a-5p inhibitor and 48 h later,the proliferation of A549 cells after genetic intervention was assayed by the MTT method,and the cell growth curve was plotted to observe the effect of hsa-miRNA-30a-5p knockdown on cell proliferation. Results For all five pairs of samples tested,hsa-miRNA-30a-5p was higher in the cancer tissues than in the adjacent tissue(P<0.05),and SCARA5 protein was lower in the cancer tissues than in the adjacent tissue (P<0.05).The bioinformatics analysis showed that there was a theoretical binding site of hsa-miRNA-30a-5p in SCARA5's 3'UTR.The luciferase assay showed that miRNA-30a mimics inhibited the luciferase expressed by the luciferase reporter vector carrying a wild-type SCARA5's 3'UTR(pGL3-WT- SCARA5)(P<0.05,vs pGL3-WT-SCARA5 alone),and miRNA-30a-5p inhibitor enhanced the luciferase activity(P<0.05,vs pGL3-WT- SCARA5 alone).No change was observed when miRNA-30a-5p mimics or miRNA-30a-5p inhibitor was co-transfected with the luciferase reporter vector carrying a mutant SCARA5's 3'UTR(pGL3-MT- SCARA5)(P>0.05,vs pGL3-WT- SCARA5 alone).Hsa-miRNA-30a-5p level in A549 cells transfected with miRNA-30a inhibitor for 48 h was significantly decreased(P<0.05,vs cell control or NC),and there was no difference in hsa-miRNA-30a-5p between the negative control and the transfection control(P>0.05).The proliferation of A549 cells was suppressed by transfection with miRNA-30a-5p inhibitor 24-72 h after transfection(P<0.05,vs control or NC). Conclusion Hsa-miRNA-30a-5p could increase the proliferation in A549 cells via suppressing the expression of SCARA5,and transfection of miRNA-30a-5p inhibitor could inhibit the proliferation of A549 cells via up-regulating SCARA5 expression.
Objective To study the regulation and mechanism of hsa-miRNA-30a-5p on the proliferation of human lung cancer A549 cells. Methods Five pairs of lung cancer and para-carcinoma tissues were harvested in clinical and measured for hsa-miRNA-30a-5p and SCARA5 levels by real-time PCR and western blotting,respectively.The theoretical binding site of hsa-miRNA-30a-5p in SCARA5's 3'UTR was predicted by bioinformatics,and validated by luciferase report assay.A549 cells were transfected with pshRNA-SCARA5 and miRNA-30a-5p inhibitor and 48 h later,the proliferation of A549 cells after genetic intervention was assayed by the MTT method,and the cell growth curve was plotted to observe the effect of hsa-miRNA-30a-5p knockdown on cell proliferation. Results For all five pairs of samples tested,hsa-miRNA-30a-5p was higher in the cancer tissues than in the adjacent tissue(P<0.05),and SCARA5 protein was lower in the cancer tissues than in the adjacent tissue (P<0.05).The bioinformatics analysis showed that there was a theoretical binding site of hsa-miRNA-30a-5p in SCARA5's 3'UTR.The luciferase assay showed that miRNA-30a mimics inhibited the luciferase expressed by the luciferase reporter vector carrying a wild-type SCARA5's 3'UTR(pGL3-WT- SCARA5)(P<0.05,vs pGL3-WT-SCARA5 alone),and miRNA-30a-5p inhibitor enhanced the luciferase activity(P<0.05,vs pGL3-WT- SCARA5 alone).No change was observed when miRNA-30a-5p mimics or miRNA-30a-5p inhibitor was co-transfected with the luciferase reporter vector carrying a mutant SCARA5's 3'UTR(pGL3-MT- SCARA5)(P>0.05,vs pGL3-WT- SCARA5 alone).Hsa-miRNA-30a-5p level in A549 cells transfected with miRNA-30a inhibitor for 48 h was significantly decreased(P<0.05,vs cell control or NC),and there was no difference in hsa-miRNA-30a-5p between the negative control and the transfection control(P>0.05).The proliferation of A549 cells was suppressed by transfection with miRNA-30a-5p inhibitor 24-72 h after transfection(P<0.05,vs control or NC). Conclusion Hsa-miRNA-30a-5p could increase the proliferation in A549 cells via suppressing the expression of SCARA5,and transfection of miRNA-30a-5p inhibitor could inhibit the proliferation of A549 cells via up-regulating SCARA5 expression.
2019, 37(5): 440-443,449.
doi: 10.3969/j.issn.1006-0111.2019.05.010
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Objective To investigate the physicochemical constants such as the solubility and the apparent oil-water partition coefficient of total flavonoids from Oxytropis falcata Bunge and study the in vitro percutaneous permeability for providing the reference for the design and preparation of transdermal drug formulations. Methods The solubility of total flavonoids from Oxytropis falcata Bunge in water and different solvents were determined by ultraviolet spectrophotometry. The apparent oil-water partition coefficient of n-octanol/water buffer solution was also determined. Percutaneous penetration of total flavonoids from Oxytropis falcata Bunge was investigated by a double-chamber osmotic diffusion device with rat isolated skin as a model. Results The total flavonoids from Oxytropis falcata Bunge had good solubility in methanol, ethanol and phosphate buffer at pH 5.0-7.4. The apparent oil-water partition coefficient(P) of total flavonoids from Oxytropis falcata Bunge had a certain relationship with the pH of the solution. At 2.5-7.4, the lgP value of total flavonoids decreased with increasing pH value and the lgP value is between 0.38 and 1.34. The cumulative amount of drug in 24 hours is 155.44 μg/cm2 and the time lag was (11.52±0.95) h. Conclusion The total flavonoids from Oxytropis falcata Bunge had poor water solubility, but were more soluble in ethanol, methanol and phosphate buffer at pH 5.0-7.4. The skin permeability was not high, and the cumulative transmittances was low with a time lag. The above characteristics should be considered comprehensively in the design of transdermal drug dosage forms.
Objective To investigate the physicochemical constants such as the solubility and the apparent oil-water partition coefficient of total flavonoids from Oxytropis falcata Bunge and study the in vitro percutaneous permeability for providing the reference for the design and preparation of transdermal drug formulations. Methods The solubility of total flavonoids from Oxytropis falcata Bunge in water and different solvents were determined by ultraviolet spectrophotometry. The apparent oil-water partition coefficient of n-octanol/water buffer solution was also determined. Percutaneous penetration of total flavonoids from Oxytropis falcata Bunge was investigated by a double-chamber osmotic diffusion device with rat isolated skin as a model. Results The total flavonoids from Oxytropis falcata Bunge had good solubility in methanol, ethanol and phosphate buffer at pH 5.0-7.4. The apparent oil-water partition coefficient(P) of total flavonoids from Oxytropis falcata Bunge had a certain relationship with the pH of the solution. At 2.5-7.4, the lgP value of total flavonoids decreased with increasing pH value and the lgP value is between 0.38 and 1.34. The cumulative amount of drug in 24 hours is 155.44 μg/cm2 and the time lag was (11.52±0.95) h. Conclusion The total flavonoids from Oxytropis falcata Bunge had poor water solubility, but were more soluble in ethanol, methanol and phosphate buffer at pH 5.0-7.4. The skin permeability was not high, and the cumulative transmittances was low with a time lag. The above characteristics should be considered comprehensively in the design of transdermal drug dosage forms.
2019, 37(5): 444-449.
doi: 10.3969/j.issn.1006-0111.2019.05.011
Abstract:
Objective The marine cyclopeptide stylissamide Ⅰ was synthesized through a solid phase synthesis and cyclization in solution(SPS-CS). Methods 2-chlorotrityl chloride resin was used as solid support for the total synthesis.Each amino acid protected by 9-fluorenylmethyloxycarbonyl(Fmoc) group was coupled with N,N-diisopropylethylamine(DIPEA)/O-(6-chloro-1-hydrocibenzotriazol-1-yl)-1,1,3,3-tetramethyluronium hexafluoro- phosphat(HCTU) as condensing agents.The linear peptide was cleaved from resin by 2,2,2-trifluoroethanol(TFE) and cyclized in the presence of(7-azabenzotriazol-1-yloxy)tripyrrolidinophosphonium hexafluorophosphate(PyAOP)/1-hydroxy-7-azabenzotriazole(HOAt)/N-methyl morphofine(NMM).Finally,the crude cyclopeptide was obtained through global deprotection with trifluoroacetic acid(TFA).The target compound was purified by preparative RP-HPLC to 98.9% pure and its structure was identified by 1H-NMR,13C-NMR and Q-TOF LC/MS. Results The first total synthesis of the marine cyclopeptide stylissamide Ⅰ was successfully realized with a yield of 67%. Conclusion A rapid,simple and high-efficient method of stylissamide Ⅰ total synthesis was successfully established.
Objective The marine cyclopeptide stylissamide Ⅰ was synthesized through a solid phase synthesis and cyclization in solution(SPS-CS). Methods 2-chlorotrityl chloride resin was used as solid support for the total synthesis.Each amino acid protected by 9-fluorenylmethyloxycarbonyl(Fmoc) group was coupled with N,N-diisopropylethylamine(DIPEA)/O-(6-chloro-1-hydrocibenzotriazol-1-yl)-1,1,3,3-tetramethyluronium hexafluoro- phosphat(HCTU) as condensing agents.The linear peptide was cleaved from resin by 2,2,2-trifluoroethanol(TFE) and cyclized in the presence of(7-azabenzotriazol-1-yloxy)tripyrrolidinophosphonium hexafluorophosphate(PyAOP)/1-hydroxy-7-azabenzotriazole(HOAt)/N-methyl morphofine(NMM).Finally,the crude cyclopeptide was obtained through global deprotection with trifluoroacetic acid(TFA).The target compound was purified by preparative RP-HPLC to 98.9% pure and its structure was identified by 1H-NMR,13C-NMR and Q-TOF LC/MS. Results The first total synthesis of the marine cyclopeptide stylissamide Ⅰ was successfully realized with a yield of 67%. Conclusion A rapid,simple and high-efficient method of stylissamide Ⅰ total synthesis was successfully established.
2019, 37(5): 450-452,480.
doi: 10.3969/j.issn.1006-0111.2019.05.012
Abstract:
Objective To establish a HPLC method for the assay of palmitul 3-(3,4-dihydroxyphenyl)-2-hydroxypropanoate (PDSS) in liposomes. Methods The separation was performed with an Agilent ZORBAX Eclipse Plus C18 column (4.6 mm×200 mm,5 μm) at room temperature.The mobile phase was acetonitrile-aqueous solution (500 ml water + 0.1 ml triethylamine + 0.1 ml formic acid,pH=6-7) (50:50) with the flow rate of 1 ml/min.Zidovudine palmitate was detected at 280 nm. Results PDSS had a good linear recovery between 0.05-0.45 mg/ml.The intra-day and inter-day RSD were <2%.The extracted recovery was in the range of 96% to 102%.The assay results for three batches were 97.81%,101.20% and 98.53%. Conclusion This method is simple,accurate and reliable.It can be used for the determination of PDSS in liposomes.
Objective To establish a HPLC method for the assay of palmitul 3-(3,4-dihydroxyphenyl)-2-hydroxypropanoate (PDSS) in liposomes. Methods The separation was performed with an Agilent ZORBAX Eclipse Plus C18 column (4.6 mm×200 mm,5 μm) at room temperature.The mobile phase was acetonitrile-aqueous solution (500 ml water + 0.1 ml triethylamine + 0.1 ml formic acid,pH=6-7) (50:50) with the flow rate of 1 ml/min.Zidovudine palmitate was detected at 280 nm. Results PDSS had a good linear recovery between 0.05-0.45 mg/ml.The intra-day and inter-day RSD were <2%.The extracted recovery was in the range of 96% to 102%.The assay results for three batches were 97.81%,101.20% and 98.53%. Conclusion This method is simple,accurate and reliable.It can be used for the determination of PDSS in liposomes.
2019, 37(5): 453-459.
doi: 10.3969/j.issn.1006-0111.2019.05.013
Abstract:
Objective To understand the research trends and hot issues of the research literature on the rational drug use of hypertension in Chinese hospital,and provide reference for promoting rational drug use of hypertension. Methods Literature of rational drug use in CNKI,Wanfang Database and VIP Database from 2010 to 2017 was retrieved,Bibliographic information system(BICOMB 2.0)was used to extract keywords,yeas and the corresponding literature quantity,journals,authors and institutions for literature metrology,article matrix about high-frequency keywords was established; the article matrix were imported into SPSS 21.0 for cluster analysis;and finally,graphical cluster toolkit(gCLUTO 1.0)was applied for co-occurrence analysis and visualized cluster analysis. Results 1 010 related literatures were retrieved from CNKI,Wanfang Database and VIP Database.According to the publication of every year,the rational drug use of hypertension had been a hot topic.According to the distribution of periodicals,the literature on rational drug use of hypertension was distributed in 262 journals,and the rational drug use of hypertension was widely concerned in various journals.According to the author,China had not formed the core strength of rational drug use research; According to the distribution of author units,the distribution organization was dispersed,most of which were hospitals.High-frequency key words focus on "anti-hypertension drugs,rational drug use,hypertension,analysis of drugs use,etc". Conclusion Researches on rational drug use of hypertension in our country were mainly to evaluate the rationality of the medication of patients with hypertension in a single hospital or the clinical application of antihypertensive drugs.Therefore,the field of research still need to shift from simple qualitative analysis to multi-regional,multi-level,large sample quantitative analysis,in order to better promote the rational drug use of hypertension.
Objective To understand the research trends and hot issues of the research literature on the rational drug use of hypertension in Chinese hospital,and provide reference for promoting rational drug use of hypertension. Methods Literature of rational drug use in CNKI,Wanfang Database and VIP Database from 2010 to 2017 was retrieved,Bibliographic information system(BICOMB 2.0)was used to extract keywords,yeas and the corresponding literature quantity,journals,authors and institutions for literature metrology,article matrix about high-frequency keywords was established; the article matrix were imported into SPSS 21.0 for cluster analysis;and finally,graphical cluster toolkit(gCLUTO 1.0)was applied for co-occurrence analysis and visualized cluster analysis. Results 1 010 related literatures were retrieved from CNKI,Wanfang Database and VIP Database.According to the publication of every year,the rational drug use of hypertension had been a hot topic.According to the distribution of periodicals,the literature on rational drug use of hypertension was distributed in 262 journals,and the rational drug use of hypertension was widely concerned in various journals.According to the author,China had not formed the core strength of rational drug use research; According to the distribution of author units,the distribution organization was dispersed,most of which were hospitals.High-frequency key words focus on "anti-hypertension drugs,rational drug use,hypertension,analysis of drugs use,etc". Conclusion Researches on rational drug use of hypertension in our country were mainly to evaluate the rationality of the medication of patients with hypertension in a single hospital or the clinical application of antihypertensive drugs.Therefore,the field of research still need to shift from simple qualitative analysis to multi-regional,multi-level,large sample quantitative analysis,in order to better promote the rational drug use of hypertension.
2019, 37(5): 460-463.
doi: 10.3969/j.issn.1006-0111.2019.05.014
Abstract:
Objective To establish an assay method for three flavonoid glycosides:kaempferol-3-O-L-rhamnopyranosyl(1→2)-β-D-glucopyranoside,kaempferol-3-O-glucoside and kaemperol-3-O-α-L-rhamnopyranosyl(1→2)-[6-O-acetyl]-β-D-glucopyranoside in Thesium chinensis Turcz by HPLC. Methods Dikma C18 column (520 mm×4.6 mm,5 μm) was used with the mobile phase of acetonitrile-water (21:79,adjusted pH to 4.61 with acetic acid) at a flow rate of 1.0 ml/min.The detection wavelength was set at 346 nm,and the column temperature was 25℃. Results The linear range of those three flavonoid glycosides was 125-200 μg/ml,2.5-40 μg/ml and 5.0-80 μg/ml (r=0.999 9).The average recoveries (n=6) were 101.63%,99.82% and 102.02%.RSD was 1.72%,2.34% and 1.94%(n=6) respectively. Conclusion This method is simple and accurate.It can be used for the quality control of Thesium chinensis Turcz and related preparations.
Objective To establish an assay method for three flavonoid glycosides:kaempferol-3-O-L-rhamnopyranosyl(1→2)-β-D-glucopyranoside,kaempferol-3-O-glucoside and kaemperol-3-O-α-L-rhamnopyranosyl(1→2)-[6-O-acetyl]-β-D-glucopyranoside in Thesium chinensis Turcz by HPLC. Methods Dikma C18 column (520 mm×4.6 mm,5 μm) was used with the mobile phase of acetonitrile-water (21:79,adjusted pH to 4.61 with acetic acid) at a flow rate of 1.0 ml/min.The detection wavelength was set at 346 nm,and the column temperature was 25℃. Results The linear range of those three flavonoid glycosides was 125-200 μg/ml,2.5-40 μg/ml and 5.0-80 μg/ml (r=0.999 9).The average recoveries (n=6) were 101.63%,99.82% and 102.02%.RSD was 1.72%,2.34% and 1.94%(n=6) respectively. Conclusion This method is simple and accurate.It can be used for the quality control of Thesium chinensis Turcz and related preparations.
2019, 37(5): 464-465,469.
doi: 10.3969/j.issn.1006-0111.2019.05.015
Abstract:
Objective To establish a method for determination of ethanol content in intermediate products during the production of blood products by GC. Methods DB-624 column was used with FID detection.The temperature of the injector and detector was 230℃,280℃,respectively.The column temperature was kept at 40℃ for 5 minutes,then increased to 80℃ at 10℃ per minute,and finally to 230℃ at 50℃ per minute for 3 minutes.N-propanol was used as the internal standard. Results The standard curve was linear in the range of 0.05%-5%(r=1.000 0) for ethanol.The average recovery was 99.28% with RSD of 0.01%(n=9). Conclusion This method was simple,sensitive,accurate and reliable.It is suitable for the determination of ethanol content in intermediate products during the production of blood products.
Objective To establish a method for determination of ethanol content in intermediate products during the production of blood products by GC. Methods DB-624 column was used with FID detection.The temperature of the injector and detector was 230℃,280℃,respectively.The column temperature was kept at 40℃ for 5 minutes,then increased to 80℃ at 10℃ per minute,and finally to 230℃ at 50℃ per minute for 3 minutes.N-propanol was used as the internal standard. Results The standard curve was linear in the range of 0.05%-5%(r=1.000 0) for ethanol.The average recovery was 99.28% with RSD of 0.01%(n=9). Conclusion This method was simple,sensitive,accurate and reliable.It is suitable for the determination of ethanol content in intermediate products during the production of blood products.
2019, 37(5): 466-469.
doi: 10.3969/j.issn.1006-0111.2019.05.016
Abstract:
Objective To analyze the participation effect of clinical pharmacist during the treatment process of sodium valproate in a patient with secondary epilepsy after stroke. Methods The correct dose and usage of sodium valproate under TDM,the most common ADR and the potential DI were introduced by clinical pharmacists who participated in the whole course treatment of sodium valproate. Results The convulsion was controlled and the liver damage caused by sodium valproate was recovered. Conclusion Clinical pharmacist should not only pay attention to ADRs under normal usage and dosage,but also pay special attention to the ability to deal with drug errors,so as to promote rational and individualized drug use.
Objective To analyze the participation effect of clinical pharmacist during the treatment process of sodium valproate in a patient with secondary epilepsy after stroke. Methods The correct dose and usage of sodium valproate under TDM,the most common ADR and the potential DI were introduced by clinical pharmacists who participated in the whole course treatment of sodium valproate. Results The convulsion was controlled and the liver damage caused by sodium valproate was recovered. Conclusion Clinical pharmacist should not only pay attention to ADRs under normal usage and dosage,but also pay special attention to the ability to deal with drug errors,so as to promote rational and individualized drug use.
2019, 37(5): 470-472.
doi: 10.3969/j.issn.1006-0111.2019.05.017
Abstract:
Objective To analyze the reason of gynecomastia in a male patient with heart failure and provide safer references for clinical prescriptions. Methods The patient's clinical symptoms,signs and laboratory findings in great detail were learned and the analysis and advice of treatment regimens were given by the clinical pharmacist learned individually. Results Gynecomastia was possible from the result of drugs,the reduction of the dose of the suspicious drug spironolactone and were put forward and adopted. Conclusions As for gynecomastia appeared in the drug treatment process,the clinical pharmacist could analyze and sort out suspicious drugs,then reflect to the prescriber.
Objective To analyze the reason of gynecomastia in a male patient with heart failure and provide safer references for clinical prescriptions. Methods The patient's clinical symptoms,signs and laboratory findings in great detail were learned and the analysis and advice of treatment regimens were given by the clinical pharmacist learned individually. Results Gynecomastia was possible from the result of drugs,the reduction of the dose of the suspicious drug spironolactone and were put forward and adopted. Conclusions As for gynecomastia appeared in the drug treatment process,the clinical pharmacist could analyze and sort out suspicious drugs,then reflect to the prescriber.
2019, 37(5): 473-480.
doi: 10.3969/j.issn.1006-0111.2019.05.018
Abstract:
Objective To evaluate the efficacy and safety of once-daily fluticasone furoate/vilanterol compared with ICS alone or twice-daily ICS/LABA formulations in patients with asthma. Methods Systematic search was performed for randomized controlled trials in the CNKI,PubMed,Embase and Cochrane Library. Results 10 citations contained 9 811 patients with asthma met the selection criteria. In terms of efficacy,compared with the control group,the patient's trough forced expiratory volume in one second[WMD=0.09,95% Cl(0.05,0.13) P=0.000] and asthma control Test score[WMD=0.63,95% CI(0.24,1.03),P=0.002] were increased in the FF/VI group. In terms of safety,the risk of adverse reaction events associated with treatment in patients was not increased in the FF/VI group compared to the control group[RR=1.15,95% CI(0.98,1.36),P=0.000]. Conclusion FF/VI had advantages and better tolerance in treating asthma patients. It is recommended to be used for its once-daily use of the frequency,which was the advantage of improving patient adherence.
Objective To evaluate the efficacy and safety of once-daily fluticasone furoate/vilanterol compared with ICS alone or twice-daily ICS/LABA formulations in patients with asthma. Methods Systematic search was performed for randomized controlled trials in the CNKI,PubMed,Embase and Cochrane Library. Results 10 citations contained 9 811 patients with asthma met the selection criteria. In terms of efficacy,compared with the control group,the patient's trough forced expiratory volume in one second[WMD=0.09,95% Cl(0.05,0.13) P=0.000] and asthma control Test score[WMD=0.63,95% CI(0.24,1.03),P=0.002] were increased in the FF/VI group. In terms of safety,the risk of adverse reaction events associated with treatment in patients was not increased in the FF/VI group compared to the control group[RR=1.15,95% CI(0.98,1.36),P=0.000]. Conclusion FF/VI had advantages and better tolerance in treating asthma patients. It is recommended to be used for its once-daily use of the frequency,which was the advantage of improving patient adherence.
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