Binghu Fang

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Organization: South China Agricultural University
Department: Department of Veterinary Pharmacology and Toxicology, College of Veterinary Medicine
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Co-reporter:Liangzhu Chen;Dexue Yang;Zhikun Pan;Lihong Lai;Jianhua Liu;Shuning Shi
Chemical Biology & Drug Design 2015 Volume 86( Issue 2) pp:239-245
Publication Date(Web):
DOI:10.1111/cbdd.12486

A series of novel hybrid molecules between sulfonamides and active antimicrobial 14-o-(3-carboxy-phenylsulfide)-mutilin were synthesized, and their in vitro antibacterial activities were evaluated by the broth microdilution. Results indicated that these compounds displayed potent antimicrobial activities in vitro against various drug-susceptible and drug-resistant Gram-positive bacteria such as Staphylococci and streptococci, including methicillin-resistant Staphylococcus aureus, and mycoplasma. In particular, sulfapyridine analog (6c) exhibited more potent inhibitory activity against Gram-positive bacteria and mycoplasma, including Staphylococcus aureus (MIC = 0.016–0.063 μg/mL), methicillin-resistant Staphylococcus aureus (MIC = 0.016 μg/mL), Streptococcus pneumoniae (MIC = 0.032–0.063 μg/mL), Mycoplasma gallisepticum (MIC = 0.004 μg/mL), with respect to other synthesized compounds and reference drugs sulfonamide (MIC = 8–128 μg/mL) and valnemulin (MIC = 0.004–0.5 μg/mL). Furthermore, comparison between MIC values of pleuromutilin-sulfonamide hybrids 6a–f with pleuromutilin parent compound 3 revealed that these modifications at 14 position side chain of the pleuromutilin with benzene sulfonamide could greatly improve the antibacterial activity especially against Gram-positives.

Co-reporter:Lixiao Xu;Guijun Zhang;Chunna Guo;Yaping Zhang;Yi Zhang;Jianlong Zheng;Haicui Yang;Dexue Yang;Limin He;Zhenling Zeng
Journal of Separation Science 2014 Volume 37( Issue 6) pp:642-649
Publication Date(Web):
DOI:10.1002/jssc.201301014

In this study, a specific and sensitive LC–MS/MS method for the simultaneous analysis of type-B trichothecenes (deoxynivalenol, 3-acetyldeoxynivalenol, and 15-acetyldeoxynivalenol) and the de-epoxy metabolite of deoxynivalenol (de-epoxy-deoxynivalenol) in chicken muscle, liver, kidney, and fat tissues was developed and validated. The method involved an extraction step using ethyl acetate, followed by the evaporation of the supernatant, which was further purified by an Oasis HLB SPE cartridge (Waters, Milford, MA, USA). Chromatographic separation was performed on a C18 column by detection with MS in multiple-reaction monitoring mode and using a gradient elution program with 0.1% formic acid in water and methanol. The correlation coefficients (r) for each calibration curve were >0.99 within the experimental concentration range. The extraction recoveries ranged from 73.7 to 106.4%, with intraday and interday RSD < 11.6% at three levels of concentrations of 2, 10, and 100 μg/kg. The decision limits and the detection capabilities of the analytes in the chicken tissues ranged from 0.16 to 0.92 and 0.68 to 2.07 μg/kg, respectively. The results demonstrated the applicability of this sensitive procedure to the determination of trichothecenes in chicken tissue samples.

Co-reporter:Yongxue Sun, Guijun Zhang, Haiyan Zhao, Jianlong Zheng, Fangyuan Hu, Binghu Fang
Journal of Chromatography B 2014 Volume 958() pp:75-82
Publication Date(Web):1 May 2014
DOI:10.1016/j.jchromb.2014.03.010
•LC–MS/MS was developed for analysis of T-2 toxin and its metabolites in swine samples.•Good linearity, precision and selectivity were observed upon LC–MS/MS analysis.•It was successfully applied for toxicokinetics, tissue distribution and excretion studies in pigs.•The results provide important information for evaluating human exposure to residual toxins.A rapid and sensitive high-performance liquid chromatography–tandem mass spectrometry (LC–MS/MS) method was developed and validated for quantitatively analyzing T-2 toxin and its major metabolites (HT-2 toxin and T-2 triol) in swine biological samples. For all matrices, liquid–liquid extraction (ethyl acetate or acetonitrile) and Varian Bond-Elut MycoSep cartridges for solid phase extraction were used for sample preparation. The analytes were separated via a Zorbax XDB-C18 column and were detected using LC–MS/MS with an electrospray ionization interface in positive ion mode. The resulting calibration curves offered satisfactory linearity (r2 > 0.992) within the test range. The limits of quantification for T-2 toxin, HT-2 toxin, and T-2 triol were 1 ng/mL (μg/kg), 2 ng/mL (μg/kg), and 5 ng/mL (μg/kg), respectively. The recovery rates in different matrices ranged from 74.3% to 102.4%, and the interday and intraday precisions were all less than 10.2% for the target analytes. The developed method was successfully applied to toxicokinetics, tissue distribution, and excretion studies of T-2 toxin and its major metabolites after intravenous (i.v.) administration in pigs. The results provide important information for evaluating and controlling human exposure to residual T-2 toxin and its major metabolites in animal-derived food.
Co-reporter:Yan Yong, Yahong Liu, Limin He, Lixiao Xu, Yaping Zhang, Binghu Fang
Journal of Chromatography B 2013 s 919–920() pp: 30-37
Publication Date(Web):1 March 2013
DOI:10.1016/j.jchromb.2012.12.038
A convenient, rapid and sensitive liquid chromatography-tandem mass spectrometry method was firstly established for the simultaneous determination of quinocetone and its 4 major metabolites: 1-desoxyquinocetone, di-deoxyquinocetone, carbonyl reduced metabolite from di-deoxyquinocetone and 3-methyl-quinoxaline-2-carboxylic acid in chicken muscle, liver, kidney and fat. Sample was extracted with acetonitrile and chloroform, and further purified by Oasis MAX SPE cartridge. Analysis was performed on a C18 column by detection with mass spectrometry in multiple reaction monitoring mode and using a gradient elution program with 0.1% formic acid solution and acetonitrile. The correlation coefficients (r) for each calibration curves are higher than 0.99 within the experimental concentration range. The recoveries of the five target analytes at three spiking levels were between 77.1% and 95.2%, with relative standard deviations less than 15%. The decision limits of the five analytes in chicken edible tissues ranged from 0.24 to 0.76 μg kg−1, and the detection capabilities were below 2.34 μg kg−1. The developed method demonstrated a satisfactory applicability in incurred chicken tissue samples.Highlights► Quinocetone and its four metabolites. ► Chicken muscle, liver, kidney and fat tissues. ► A rapid and sensitive LC–MS/MS method is firstly developed. ► The elimination curves of quinocetone and its metabolites are obtained.
VALNEMULIN
Trichothec-9-en-8-one,15-(acetyloxy)-12,13-epoxy-3,7-dihydroxy-, (3a,7a)-
3-METHYL-QUINOXALINE-2-CARBOXYLIC ACID
2-cyano-N-[(E)-(1-hydroxy-4-oxidoquinoxalin-4-ium-2-ylidene)methyl]iminoacetamide
Trichothec-9-en-8-one,3-(acetyloxy)-12,13-epoxy-7,15-dihydroxy-, (3a,7a)-
Trichothec-9-ene-3,4,8,15-tetrol,12,13-epoxy-, 8-(3-methylbutanoate), (3a,4b,8a)-
2-Acetyl-3-methylquinoxaline 1,4-dioxide
carbadox
Trichothec-9-ene-3,4,15-triol,12,13-epoxy-, (3a,4b)-
ACETONITRILE