Penicillin G acylase(PGA) was immobilized on the magnetic hydrophilic polymer microspheres with average pore size of 17.1 nm,specific surface area of 128.2 m2/g and saturate magnetization of 6.4 emu/g.The 96.7%ampicil...Penicillin G acylase(PGA) was immobilized on the magnetic hydrophilic polymer microspheres with average pore size of 17.1 nm,specific surface area of 128.2 m2/g and saturate magnetization of 6.4 emu/g.The 96.7%ampicillin yield with 1.60 of the synthesis/hydrolysis(S/H) ratio from 6-aminopenicillanic acid(6-APA) and D-(-)-alpha-phenylglycine methyl ester(D-PGME) can be achieved using the resultant magnetic biocatalyst in ethylene glycol,where only 82.1%yield with 1.40 of the S/H ratio was obtained using the free PGA under the identical reaction conditions.The immobilized PGA can be separated magnetically and recycled for five times without obvious loss of its catalytic activity.展开更多
Surface molecularly imprinted polymers （SMIPs） for selective adsorption of ampicillin sodium were synthesized using surface molecular imprinting technique with silica gel as a support. The physical and morphological...Surface molecularly imprinted polymers （SMIPs） for selective adsorption of ampicillin sodium were synthesized using surface molecular imprinting technique with silica gel as a support. The physical and morphological characteristics of the polymers were investigated by scanning electron microscope （SEM）, Fourier transform infrared spectroscopy （FT-IR）, thermogravimetric analysis （TGA）, elemental analysis and nitrogen adsorption-desorption test. The obtained results showed that the SMIPs displayed great adsorption capacity （13.5 lag/mg）, high recognition ability （the imprinted factor is 3.2） and good binding kinetics for ampicillin sodium. Finally, as solid phase extraction adsorbents, the SMIPs coupled with HPLC method were validated and applied for the enrichment, purification and determination of anapicillin sodium in real milk and blood samples. The averages of spiked accuracy ranged from 92.1% to 107.6%. The relative standard deviations of intra- and inter-day precisions were less than 4.6%. This study provides a new and promising method for enriching, extracting and determining ampicillin sodium in complex biological samples.展开更多
The aim of this study is a present of a simple solvothermal synthesis approach to preparation of Cu-based magnetic metal organic framework(MMOF)and subsequently its application as sorbent for ultrasound assisted magne...The aim of this study is a present of a simple solvothermal synthesis approach to preparation of Cu-based magnetic metal organic framework(MMOF)and subsequently its application as sorbent for ultrasound assisted magnetic solid phase extraction(UAMSPE)of ampicillin(AMP)from cow milk samples prior to high performance liquid chromatography-Ultraviolet(HPLC-UV)determination.Characteristics of prepared MMOF were fully investigated by different techniques which showed the exclusive properties of proposed sorbent in terms of proper functionality,desirable magnetic property and also high specific surface area.Different influential factors on extraction recovery including sorbent dosage,ultrasonic time,washing solvent volume and eluent solvent volume were assessed using central composite design(CCD)based response surface methodology(RSM)as an operative and powerful optimization tool.This is the first report for determination of AMP using MMOF.The proposed method addressed some drawbacks of other methods and sorbents for determination of AMP.The presented method decreases the extraction time(4 min)and also enhances adsorption capacity(250 mg/g).Moreover,the magnetic property of presented sorbent(15 emu/g)accelerates the extraction process which does not need filtration,centrifuge and precipitation procedures.Under the optimized conditions,the proposed method is applicable for linear range of 1.0-5000.0 μg/L with detection limit of 0.29 μg/L,satisfactory recoveries(≥95.0%)and acceptable repeatability(RSD less than 4.0%).The present study indicates highly promising perspectives of MMOF for highly effective analysis of AMP in complicated matrices.展开更多
To overcome ampicillin-resistance of bacteria which is believed to attribute their endogenous B-lactamase, we designed three 10-23 DNAzymes（Dz1, Dz2. Dz3） targeting the coding region of B-lactamase mRNA and examined...To overcome ampicillin-resistance of bacteria which is believed to attribute their endogenous B-lactamase, we designed three 10-23 DNAzymes（Dz1, Dz2. Dz3） targeting the coding region of B-lactamase mRNA and examined their inhibitory capabilities of the ampicillin-resistance of TEM-1 and TEM-3 bacteria. Dz1 was a traditional 10-23 DNAzyme, Dz2 was the mutant of Dz1 by addition of the protected nucleotide to each ann of the enzyme, and Dz3 was a mutant of Dz1 at antisense arms of which phosphorothioate modifications were made. Kinetic analysis, bacterial growth, and β-lactamase activity measurement showed that all the three DNAzymes worked efficiently in vitro and in vivo. A 9 hours bacterial growth inhibition test showed that the inhibition rates of TEM-1 bacteria by Dz1, Dz2, and Dz3 were 27%, 50%, and 29%, respectively. In addition, the inhibition rates of TEM-3 bacteria by those three DNAzymes were found io be 49%, 58%, and 45%, respectively. The current findings suggest that DNAzymes may become potential candidates of alternative inhibitors for bacteria drug-resistance.展开更多
The stabilities of two kinds of solutions (30 mg/mL) of Ampicillin sodium in 0.9% NaCl in water (NS, normal saline) and in sterile water (SW) in the intravenous elastomeric infusion device (Accufuser®) were ev...The stabilities of two kinds of solutions (30 mg/mL) of Ampicillin sodium in 0.9% NaCl in water (NS, normal saline) and in sterile water (SW) in the intravenous elastomeric infusion device (Accufuser®) were evaluated based on recommended solutions and storage periods. The injectable NS- and SW-Ampicillin solutions in the Accufuser® device were stored and evaluated at controlled temperature (room temperature, 25℃ ± 2℃ and cold temperature, 4℃ ± 2℃) during 7 days. Effects of the periods of storage (from 0 to 7 days) and the temperatures of storage (RT and CT) on the physico-chemical appearances and concentrations of active compounds were determined. The visual clarity, pH, and concentrations of Ampicillin were determined by stability-indicating high-performance liquid chromatography (HPLC)-ultraviolet (UV) detection. The results showed that the amount of Ampicillin in studied solutions gradually decreased with time. The Ampicillin in NS, which was stored in CT, was relatively stable, retaining 94% of its original amount up to 7 days. The solution that showed least stability was Ampicillin in SW, which was stored in RT, retaining 80% of its original amount. Generally, solutions that were stored in CT were more stable than the solutions that were stored in RT. No significant changes in physical appearance or color of the solutions were observed during the study. Particles were not detected in any solution samples. In summary, two kinds of solutions of Ampicillin sodium, in NS and SW, showed different chemical stabilities with time in intravenous infusion device without any significant physical changes and retained about 94% vs 89% and 83% vs 80% of initial concentrations after 7 days in CT and RT, respectively. We suggest that 30 mg/mL of Ampicillin sodium in NS solution in an Accufuser® infusion device which is stored in CT can be applicable for 7 days in clinical situations.展开更多
多囊卵巢综合征(Polycystic ovary syndrome,PCOS)是一组生殖内分泌代谢紊乱的综合征,临床以稀发排卵、高雄激素体征、胰岛素抵抗为主要特征,其中育龄期发病率高,对女性生育力造成严重不良影响。PCOS的发生发展涉及多种信号通路,腺苷酸...多囊卵巢综合征(Polycystic ovary syndrome,PCOS)是一组生殖内分泌代谢紊乱的综合征,临床以稀发排卵、高雄激素体征、胰岛素抵抗为主要特征,其中育龄期发病率高,对女性生育力造成严重不良影响。PCOS的发生发展涉及多种信号通路,腺苷酸活化蛋白激酶(AMP-activated protein kinase,AMPK)及哺乳动物雷帕霉素靶蛋白(Mammalian target of rapamycin,mTOR)作为细胞能量感受器是其中两个关键靶点。二者在PCOS各个发病部位包括下丘脑-垂体-卵巢轴、子宫内膜、脂肪与骨骼肌中发挥重要的调节作用,通过影响细胞自噬、氧化应激、炎症、线粒体功能、葡萄糖摄取等,促进卵泡的发育和成熟,改善胰岛素抵抗。近年来,中医药因其成分多样、靶点众多等优势广泛应用于临床,研究人员已对PCOS的发病以及中药治疗及改善PCOS的机制进行了大量研究,结果提示AMPK与mTOR相关通路在其中发挥关键作用。通过总结中药干预AMPK与mTOR及其相关通路治疗PCOS的研究结果,为临床治疗及基础研究提供参考。展开更多
基金supported by The National Basic Research Program 973 of China(No.2010CB534916)the National Natural Science Foundation of China(Nos.50662004,20564002).
文摘Penicillin G acylase(PGA) was immobilized on the magnetic hydrophilic polymer microspheres with average pore size of 17.1 nm,specific surface area of 128.2 m2/g and saturate magnetization of 6.4 emu/g.The 96.7%ampicillin yield with 1.60 of the synthesis/hydrolysis(S/H) ratio from 6-aminopenicillanic acid(6-APA) and D-(-)-alpha-phenylglycine methyl ester(D-PGME) can be achieved using the resultant magnetic biocatalyst in ethylene glycol,where only 82.1%yield with 1.40 of the S/H ratio was obtained using the free PGA under the identical reaction conditions.The immobilized PGA can be separated magnetically and recycled for five times without obvious loss of its catalytic activity.
基金financially supported by the National Natural Science Foundation of China (Nos. 81573391 and 81173024)the National Key Projects of China (No. 812277802)
文摘Surface molecularly imprinted polymers （SMIPs） for selective adsorption of ampicillin sodium were synthesized using surface molecular imprinting technique with silica gel as a support. The physical and morphological characteristics of the polymers were investigated by scanning electron microscope （SEM）, Fourier transform infrared spectroscopy （FT-IR）, thermogravimetric analysis （TGA）, elemental analysis and nitrogen adsorption-desorption test. The obtained results showed that the SMIPs displayed great adsorption capacity （13.5 lag/mg）, high recognition ability （the imprinted factor is 3.2） and good binding kinetics for ampicillin sodium. Finally, as solid phase extraction adsorbents, the SMIPs coupled with HPLC method were validated and applied for the enrichment, purification and determination of anapicillin sodium in real milk and blood samples. The averages of spiked accuracy ranged from 92.1% to 107.6%. The relative standard deviations of intra- and inter-day precisions were less than 4.6%. This study provides a new and promising method for enriching, extracting and determining ampicillin sodium in complex biological samples.
基金This work was financially supported by Graduate School and Research Council of Yasouj University.
文摘The aim of this study is a present of a simple solvothermal synthesis approach to preparation of Cu-based magnetic metal organic framework(MMOF)and subsequently its application as sorbent for ultrasound assisted magnetic solid phase extraction(UAMSPE)of ampicillin(AMP)from cow milk samples prior to high performance liquid chromatography-Ultraviolet(HPLC-UV)determination.Characteristics of prepared MMOF were fully investigated by different techniques which showed the exclusive properties of proposed sorbent in terms of proper functionality,desirable magnetic property and also high specific surface area.Different influential factors on extraction recovery including sorbent dosage,ultrasonic time,washing solvent volume and eluent solvent volume were assessed using central composite design(CCD)based response surface methodology(RSM)as an operative and powerful optimization tool.This is the first report for determination of AMP using MMOF.The proposed method addressed some drawbacks of other methods and sorbents for determination of AMP.The presented method decreases the extraction time(4 min)and also enhances adsorption capacity(250 mg/g).Moreover,the magnetic property of presented sorbent(15 emu/g)accelerates the extraction process which does not need filtration,centrifuge and precipitation procedures.Under the optimized conditions,the proposed method is applicable for linear range of 1.0-5000.0 μg/L with detection limit of 0.29 μg/L,satisfactory recoveries(≥95.0%)and acceptable repeatability(RSD less than 4.0%).The present study indicates highly promising perspectives of MMOF for highly effective analysis of AMP in complicated matrices.
基金the National Natural Science Foundation of China(Nos.20771030 and 20671025)
文摘To overcome ampicillin-resistance of bacteria which is believed to attribute their endogenous B-lactamase, we designed three 10-23 DNAzymes（Dz1, Dz2. Dz3） targeting the coding region of B-lactamase mRNA and examined their inhibitory capabilities of the ampicillin-resistance of TEM-1 and TEM-3 bacteria. Dz1 was a traditional 10-23 DNAzyme, Dz2 was the mutant of Dz1 by addition of the protected nucleotide to each ann of the enzyme, and Dz3 was a mutant of Dz1 at antisense arms of which phosphorothioate modifications were made. Kinetic analysis, bacterial growth, and β-lactamase activity measurement showed that all the three DNAzymes worked efficiently in vitro and in vivo. A 9 hours bacterial growth inhibition test showed that the inhibition rates of TEM-1 bacteria by Dz1, Dz2, and Dz3 were 27%, 50%, and 29%, respectively. In addition, the inhibition rates of TEM-3 bacteria by those three DNAzymes were found io be 49%, 58%, and 45%, respectively. The current findings suggest that DNAzymes may become potential candidates of alternative inhibitors for bacteria drug-resistance.
基金supported by Division of Molecular Therapeutics Development,Hanyang Biomedical Research Institute,Hanyang University and Woo Young Medical Co.LTD.,Seoul,South Korea.
文摘The stabilities of two kinds of solutions (30 mg/mL) of Ampicillin sodium in 0.9% NaCl in water (NS, normal saline) and in sterile water (SW) in the intravenous elastomeric infusion device (Accufuser®) were evaluated based on recommended solutions and storage periods. The injectable NS- and SW-Ampicillin solutions in the Accufuser® device were stored and evaluated at controlled temperature (room temperature, 25℃ ± 2℃ and cold temperature, 4℃ ± 2℃) during 7 days. Effects of the periods of storage (from 0 to 7 days) and the temperatures of storage (RT and CT) on the physico-chemical appearances and concentrations of active compounds were determined. The visual clarity, pH, and concentrations of Ampicillin were determined by stability-indicating high-performance liquid chromatography (HPLC)-ultraviolet (UV) detection. The results showed that the amount of Ampicillin in studied solutions gradually decreased with time. The Ampicillin in NS, which was stored in CT, was relatively stable, retaining 94% of its original amount up to 7 days. The solution that showed least stability was Ampicillin in SW, which was stored in RT, retaining 80% of its original amount. Generally, solutions that were stored in CT were more stable than the solutions that were stored in RT. No significant changes in physical appearance or color of the solutions were observed during the study. Particles were not detected in any solution samples. In summary, two kinds of solutions of Ampicillin sodium, in NS and SW, showed different chemical stabilities with time in intravenous infusion device without any significant physical changes and retained about 94% vs 89% and 83% vs 80% of initial concentrations after 7 days in CT and RT, respectively. We suggest that 30 mg/mL of Ampicillin sodium in NS solution in an Accufuser® infusion device which is stored in CT can be applicable for 7 days in clinical situations.
文摘多囊卵巢综合征(Polycystic ovary syndrome,PCOS)是一组生殖内分泌代谢紊乱的综合征,临床以稀发排卵、高雄激素体征、胰岛素抵抗为主要特征,其中育龄期发病率高,对女性生育力造成严重不良影响。PCOS的发生发展涉及多种信号通路,腺苷酸活化蛋白激酶(AMP-activated protein kinase,AMPK)及哺乳动物雷帕霉素靶蛋白(Mammalian target of rapamycin,mTOR)作为细胞能量感受器是其中两个关键靶点。二者在PCOS各个发病部位包括下丘脑-垂体-卵巢轴、子宫内膜、脂肪与骨骼肌中发挥重要的调节作用,通过影响细胞自噬、氧化应激、炎症、线粒体功能、葡萄糖摄取等,促进卵泡的发育和成熟,改善胰岛素抵抗。近年来,中医药因其成分多样、靶点众多等优势广泛应用于临床,研究人员已对PCOS的发病以及中药治疗及改善PCOS的机制进行了大量研究,结果提示AMPK与mTOR相关通路在其中发挥关键作用。通过总结中药干预AMPK与mTOR及其相关通路治疗PCOS的研究结果,为临床治疗及基础研究提供参考。
