ABSTRACT
Based on the idea of modification of sugar drugs, or transforming other active substances with sugar molecules, sixteen D-glucosamine-fluoroquinolone (FQ) derivatives were designed by combining D-glucosamine with FQs and synthesized by a multi-step reaction with shared intermediates. The assay results of anti-human pathogenic bacteria and anti-citrus canker showed that the inhibitory activities of two target molecules TM2b and TM2d against Staphylococcus aureus ATCC14125 were stronger than those of all tested positive control drugs, and the inhibitory rates of target molecules TM2m and TM2n against citrus canker were higher than that of the positive control streptomycin at the concentrations of 0.5 and 0.2 µg·mL-1, respectively, which all were worthy of further study. In this study, a series of novel molecules composed of D-glucosamine and FQs were synthesized for the first time, and super antibacterial molecules were found, which expanded the types and biological activities of D-glucosamine derivatives.
ABSTRACT
Cephalosporins are widely used in the treatment of infectious diseases. The structural differences in cephalosporin drugs mainly lie in the C-7 amino side chain and the C-3 substituent. In this study, twenty-five haloacylated cephalosporins of five series were designed by using a strategy of introducing simple substituents at the C-7 amino group in four cephalosporin parent nucleus with different C-3 substituents and efficiently synthesized under optimized conditions. Their activities against human pathogenic bacteria, Pichia pastoris, citrus canker and citrus pathogenic fungi were evaluated. The results showed that most of the molecules had activity against human pathogenic bacteria, of which seven compounds including TM1f had stronger or equivalent inhibitory activities against eight human pathogens than the marketed drugs cefalotin, cefoxitin sodium and ceftizoxime sodium. The inhibitory activity of TM1s against Alternaria alternate Al.6 was stronger than that of cephalosporins and comparable to that of the positive control prochloraz. TM1f and TM1s are worthy of further study.
ABSTRACT
Objective: To establish the capillary GC fingerprint of Guominxing Biyan Granules and give a new method for quality control. Methods: The capillary GC was used. The ingredients of common peaks were analyzed by FID and MS. The HP-5 Phenyl Methyl Siloxane (30 m×0.32 mm, 0.25 μm) was used for capillary column. The chromatography conditions were as follows: the temperature of inlet was 200℃ in splitless sampling, the detector temperature was 250℃, the column initial temperature was 50℃, 3℃/min rose to 140℃, keeping 2 min and 10℃/min rose to 200℃, keeping 2 min. Results: Capillary GC fingerprint of volatile oil in Allergic Rhinitis Particles was established. Twelve peaks were selected as the fingerprint peaks of Allergic Rhinitis Particles. The ingredients of common peaks were designated by GC-MS. The similarity between the fingerprint of 10 batches of Allergic Rhinitis Particles Samples were 0.90. Conclusion: The established capillary GC fingerprint has desirable precision, reproducibility, and stability, and can be applied to the quality control of Guominxing Biyan Granules.
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To evaluate the rationality of alcohol precipitation technology of Biqiu granule by investigating its effect on serum histamine, IgE, IL-4, IFN and TNF-α. The contents of cafferic acid and rosmarinic acid were used as the evaluation indexes, and some factors affecting index were firstly evaluated by Plackett-Burman design; then alcohol precipitation technology was further optimized by Box-Behnken design to determine the optimal alcohol precipitation conditions. The best alcohol precipitation conditions were as follows: the relative density of herb liquor was 1.15 (65 ℃); the concentration of alcohol was 70%, and standing time was 12 hours. Optimal alcohol precipitation technology of Biqiu granules determined by pharmacodynamic screening, Plackett-Burman and Box-Behnken design tests, was stable and feasible with good predictability, providing reliable basis for the industrialization production of Biqiu granules.
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Objective: To establish an HPLC method for the simultaneous determination of cafferic acid and rosmarinic acid in Perilla frutescens leaves and Schizonepeta tenuifolia. Methods: The anaiysis was carried out on an Agilent C18 column (250 mm × 4.6 mm, 5 μm), and the mobile phase was composed of actonitrile and 0.1% phosphoric acid aqueous with gradient elution. The detection wavelength was 327 nm. The flow rate 1.0 mL/min at column temperature of 30 ℃. Results: Under the chromatographic condition, cafferic acid and rosmarinic acid were completely separated and other components had no effect on their determination. It showed a good linearity in the range of 0.69-22.12 and 3.65 -116.92 μg/mL. The average recoveries of P. frutescens leaves were 102.9% and 105.6%, and the RSD values were 1.8% and 1.9%. The average recoveries of S. tenuifolia were 101.2% and 101.0% and the RSD values were 2.4% and 1.9%. Conclusion: The established method is rapid, sensitive, accurate, and the test component peak separation degree is good, and could be used for the simultaneous determination of cafferic acid and rosmarinic acid in P. frutescens leaves and S. tenuifolia, which provides a scientific basis for the quality evaluation of P. frutescens leaves and S. tenuifolia.
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An analysis method has been established to test 27 elements (Li, Be, B, Mg, Al, Sc, Ti, V, Cr, Mn, Fe, Co, Ni, Cu, Zn, Ga, As, Sr, Mo, Cd, Sn, Sb, Ba, La, Hg, Pb, Bi) in Maca nationality's medicine with microwave digestion-ICP-MS. Sample solutions were analyzed by ICP-MS after microwave digestion, and the contents of elements were calculated according to their calibration curves, and internal standard method was adopted to reduce matrix effect and other interference effects. The experimental results showed that the linear relations of all the elements were very good; the correlation coefficient (r) was 0.9994-1.0000 (Hg was 0.9982) ; the limits of detection were 0.003-2.662 microg x L(-1); the relative standard deviations for all elements of reproducibility were lower than 5% (except the individual elements); the recovery rate were 78.5%-123.7% with RSD lower than 5% ( except the individual elements). The analytical results of standard material showed acceptable agreement with the certified values. This method was applicable to determinate the contents of multi-elements in Maca which had a high sensitivity, good specificity and good repeatability, and provide basis for the quality control of Maca.
Subject(s)
Lepidium , Chemistry , Mass Spectrometry , Methods , Microwaves , Reproducibility of Results , Trace Elements , ChemistryABSTRACT
First with the qualified rate of granules as the evaluation index, significant influencing factors were firstly screened by Plackett-Burman design. Then, with the qualified rate and moisture content as the evaluation indexes, significant factors that affect one-step pelletization technology were further optimized by Box-Behnken design; experimental data were imitated by multiple regression and second-order polynomial equation; and response surface method was used for predictive analysis of optimal technology. The best conditions were as follows: inlet air temperature of 85 degrees C, sample introduction speed of 33 r x min(-1), density of concrete 1. 10. One-step pelletization technology of Biqiu granules by Plackett-Burman design and Box-Behnken response surface methodology was stable and feasible with good predictability, which provided reliable basis for the industrialized production of Biqiu granules.
Subject(s)
Chemistry, Pharmaceutical , Methods , Drugs, Chinese Herbal , Chemistry , TemperatureABSTRACT
With inlet temperature, specific gravity, feeding speed as independent variables, the comprehensive evaluating indexes of content of schisandrin and arctiin as dependent variable, the experimental data were fitted to a second order polynomial equation. Based on establishing the mathematical relationship between the comprehensive evaluating indexes and respective variables, Box-Benhnken central composite test and response surface analysis method was employed to optimize the spray drying technology of Biqiu granules ethanol extract. The optimal drying parameter was as follows: the inlet temperature was 175 degrees C, the specific gravity was 1.10, feeding speed was 32 r x min(-1). Under these conditions, the comprehensive evaluating indexes of spraying dry processes was 92.68, which was close to the model prediction. The spraying dry technology of Biqiu granules ethanol extract optimized by response surface methodology was accurate and feasible, which provided theoretical experiment basis for the industrialization production.
Subject(s)
Chemistry, Pharmaceutical , Methods , Chromatography, High Pressure Liquid , Drugs, Chinese Herbal , Chemistry , EthanolABSTRACT
<p><b>OBJECTIVE</b>The present study is concerning qualitative and quantitative detection of Poria cocos quality based on FT-near infrared (FT-NIR) spectroscopy combined with chemometrics.</p><p><b>METHOD</b>The Poria cocos polysaccharides contents were determined by UV. Transmission mode was used in the collection of NIR spectral samples. The pretreatment method was first derivation and vector normalization. Then principal component analysis (PCA) was used to build classification model and partial least square (PLS) to build the calibration model.</p><p><b>RESULT</b>The results showed that conventional criteria such as the R, root mean square error of calibration (RMSEC), and the root mean square error of prediction (RMSEP) are 0.944 0, 0.072 1 and 0.076 2, respectively. The misclassified sample is 0 using the qualitative model built by PCA.</p><p><b>CONCLUSION</b>The prediction models based on NIR have a better performance with high precision, good stability and adaptability and can be used to predict the polysaccharose content of Poria cocos rapidly, which can provide a fast approach to discriminate the different parts of Poria cocos.</p>
Subject(s)
Fungal Polysaccharides , Least-Squares Analysis , Poria , Chemistry , Principal Component Analysis , Spectroscopy, Near-Infrared , MethodsABSTRACT
The HPLC fingerprint determination method of Jinzhen oral solution was established to provide a new method for quality control of Jinzhen oral solution. RP-HPLC was used for phenomenex Luna C18 (4.6 mm x 250 mm, 5 μm) chromatographic column, with 0.1% H3 PO4 water solution and acetonitrile as the mobile phase for gradient elution. The detection wavelength was 280 nm. HPLC fingerprint of Jinzhen oral solution was established to identify 17 common peaks in Jinzhen oral solution. The similarity of fingerprints of 10 batches of finished products was more than 0. 90. The established HPLC fingerprint has a better precision, reproducibility and stability, and can be applied in quality control of Jinzhen oral solution.
Subject(s)
Chromatography, High Pressure Liquid , Methods , Drugs, Chinese Herbal , Chemistry , Quality ControlABSTRACT
This paper was focused on establishing a ICP-MS method with microwave digestion for simultaneous determination of lead, copper, arsenic, cadmium, mercury, magnesium, manganese, nickel, thallium in cassia tuckahoe capsule and its five raw herbal materials. Internal standard method was adopted to reduce matrix effect and other interference effects. The method established was shown to be simple with high sensitivity, strong specificity and good reproducibility. Linear relationship is good as R2 ≥ 0.999 3 while the average recovery was among 75.84% - 118.9%. The detection limit was 0.016 - 4.593 μg x L(-1). Data in this paper provided the basis for control of deleterious element in Guizhi Fuling capsules, and further more it was with referencing values for control of deleterious element in other crude drug.
Subject(s)
Capsules , Drugs, Chinese Herbal , Reproducibility of ResultsABSTRACT
<p><b>OBJECTIVE</b>To establish an analytical method for the fingerprint of triterpenoid constituents of Poria by HPLC and compare the fingerprints of different medicinal parts of Poria in order to provide basis for controlling Poria quality.</p><p><b>METHOD</b>The HPLC chromatographic conditions were Waters Symmetry C18 column (4.6 mm x 250 mm, 5 μm), 0.1% phosphoric acid (A) and acetonitrile (B) as gradient mobile phases, flow rate being 1.0 mL x min(-1), column temperature at 30 degrees C, The detection wavelength was set at 210 nm; The cluster analysis was carried on by SPSS 15.0.</p><p><b>RESULT</b>The HPLC fingerprints of triterpenoid constituents of Poria were set up. There were 16 common peaks in different medicinal parts. The results of method validation met technical requirement of fingerprints; Triterpenoid constituents in White Poria and Poria cum Radix Pini were different from Poria. The content of pachymic acid was the highest in Poria. The effect of habitat on the quality was no obvious difference.</p><p><b>CONCLUSION</b>The method is stable, reliable, reproducible, and can be used as an effective means of Poria quality evaluation.</p>
Subject(s)
Chromatography, High Pressure Liquid , Methods , Cluster Analysis , Poria , Chemistry , TriterpenesABSTRACT
<p><b>OBJECTIVE</b>To control the quality of the product, quantitative fingerprint was used to evaluate the composition of the amino acids in the Xingnao Tongluo injection.</p><p><b>METHOD</b>The method of the quantitative fingerprint to the amino acids composition was established through AccQ Tag precolumn derivatization. The quality was evaluated by the quantitative test of the amino acids and the similarity in ten batches.</p><p><b>RESULT</b>The Xingnao Tongluo injection contained 12 amino acids and the contents of these amino acids were stable. All the ten batches of the samples had similarity of more than 0.90.</p><p><b>CONCLUSION</b>The method was accurate, feasible and could be a simple and effective way to evaluate the quality of the traditional Chinese medicine.</p>
Subject(s)
Amino Acids , Chemistry , Chromatography, High Pressure Liquid , Methods , Drugs, Chinese Herbal , Chemistry , Quality ControlABSTRACT
An antibiotic-producing bacterium, which was numbered as 20 #-5, was separated from the soil in Chongqing. It was identified as the member of pseudomonas. Gram positive bacteria are badly suppressed by it. The antibiotic secreted by 20 #-5 can endure 100℃ for half an hour, and it can also go through the ultrafiltration membrane with pores of 0.22?m.