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Liu S.,Shijiazhuang University | Shang R.,Lanzhou Institute of Husbandry and Pharmaceutical science of CAAS | Shi L.,Shijiazhuang University | Wan D.C.-C.,Chinese University of Hong Kong | Lin H.,Chinese University of Hong Kong
European Journal of Medicinal Chemistry | Year: 2014

A series of 7H-thiazolo[3,2-b]-1,2,4-triazin-7-one derivatives 7a-i were synthesized and evaluated as novel acetylcholinesterase (AChE) inhibitors. All target compounds were evaluated in vitro for the inhibitory activities against AChE via Ellman colorimetric assay. Compound 7c showed an excellent (89.82%) inhibitory activity. The molecular docking studies revealed that 7c, 7d and 7g, with the lateral chain in the para position of the phenyl ring, possessed an optimal docking pose and can perfectly fit into the catalytic active site (CAS) and peripheral anionic site (PAS), simultaneously, and, consequently, exhibited higher inhibitory potency than 7b that bears the same lateral chain as 7g, but in the ortho position of the phenyl ring. © 2014 Elsevier Masson SAS. All rights reserved.


PubMed | Northwest Agriculture and Forestry University, Lanzhou Institute of Husbandry and Pharmaceutical science of CAAS, Guizhou University, University of Maryland University College and Sichuan Agricultural University
Type: | Journal: Scientific reports | Year: 2016

The goat (Capra hircus) is one of the first farm animals that have undergone domestication and extensive natural and artificial selection by adapting to various environments, which in turn has resulted in its high level of phenotypic diversity. Here, we generated medium-coverage (9-13) sequences from eight domesticated goat breeds, representing morphologically or geographically specific populations, to identify genomic regions representing selection signatures. We discovered ~10 million single nucleotide polymorphisms (SNPs) for each breed. By combining two approaches, ZH


PubMed | Lanzhou Institute of Husbandry and Pharmaceutical science of CAAS, Institute Pasteur Paris and Yancheng YouHua Pharmaceutical & Chemical Technology Co.
Type: | Journal: European journal of medicinal chemistry | Year: 2016

The alarming growth of multidrug-resistant bacteria such as methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococci (VRE) has become a major global health hazard. Therefore, urgent demand for new antibiotics with a unique mechanism of action is very necessary. The present study reports the design, synthesis, and antibacterial studies of a series of novel pleuromutilin derivatives with substituted 6-amino pyrimidine moieties. Most of the tested compounds exhibited highly potent anti-MRSA or Staphylococcus aureus (S.aureus) activities. 14-O-[(4,6-Diamino -pyrimidine-2-yl) thioacetyl] mutilin (3) and 14-O-[(2-((3R)-3-Hydroxymethylpiperidine-1-yl)-acetamido-6-aminopyrimidine-2-yl) thioacetyl] mutilin (5h) were the most active compounds and showed higher antibacterial activities. Compound 3 displayed rapid bactericidal activity and affected bacterial growth with the same manner as tiamulin fumarate. Docking experiments for compounds 3 and 5h carried out on the peptidyl transferase center (PTC) of 23S rRNA provided the information about the binding model. Invivo mouse systemic infection experimental results confirmed the therapeutic efficacy of compound 3, with ED


Wang D.,China Agricultural University | Wang D.,Xinjiang Academy of Animal Science | Wang Z.,Xinjiang Academy of Animal Science | Yan Z.,Lanzhou Institute of Husbandry and Pharmaceutical Science of CAAS | And 5 more authors.
Infection, Genetics and Evolution | Year: 2015

The aim of present study was to detect new trends of methicillin-resistant Staphylococcus aureus (MRSA) and methicillin-sensitive Staphylococcus aureus (MSSA) towards antibiotic susceptibility, resistance genes and molecular typing by methods of disc diffusion, multiplex PCR assay and multilocus sequence typing (MLST). A total of 219 S. aureus strains were isolated from bovine mastitis cases from six provinces of China, including 34 MRSA strains. The results revealed that more than 70% isolated strains showed resistance to various antibiotics, and multiple-drugs resistance to more than five categories of antibiotics was found more common. The ermC was the most prevalent resistance gene, followed by other genes; however, ermA was the least frequently detected gene. Twenty-eight mecA-negative MRSA and six mecA-positive MRSA strains were detected, and in which three strains were ST97-MRSA-IV, others were ST965-MRSA-IV, ST6-MRSA-IV and ST9-MRSA-SCC. mec-NT. The mecA-negative MRSA strains were found resistant to most of the antibiotics, and harbored aac(6')/. aph(2''), aph(3')-III and tetM genes higher than MSSA strains. The resistance to most of the antibiotics was significantly higher in MRSA than in MSSA strains. The MLST profiles showed that these strains mainly belonged to CC5, CC398, CC121 and CC50 lineage, especially within ST97 and ST398, while some novel sequence types (ST2154, ST2165 and ST2166) were identified and deposited in the MLST database. This indicates that the resistance of S. aureus is becoming more complicated by changes in multi-drug resistance mechanism and appearance of mecA-negative MRSA isolates, and importantly, MRSA-IV strains in different MLST types are emerging. © 2015 Elsevier B.V.


PubMed | Lanzhou Institute of Husbandry and Pharmaceutical science of CAAS, Lanzhou University of Technology and Yancheng Shunbao Chemical Co.
Type: Journal Article | Journal: Molecules (Basel, Switzerland) | Year: 2016

A series of novel pleuromutilin derivatives with substituted benzimidazole moieties were designed and synthesized from pleuromutilin and 5-amino-2-mercaptobenzimidazole through sequential reactions. All the newly synthesized compounds were characterized by IR, NMR, and HRMS. Each of the derivatives was evaluated in vitro for their antibacterial activity against


Shang R.,Lanzhou Institute of Husbandry and Pharmaceutical science of CAAS | Pu X.,Lanzhou University of Technology | Xu X.,Guiyang Medical University | Xin Z.,CAS Lanzhou Institute of Modern Physics | And 4 more authors.
Journal of Medicinal Chemistry | Year: 2014

A series of novel pleuromutilin derivatives possessing thiadiazole moieties were synthesized via acylation reactions under mild conditions. The in vitro antibacterial activities of the derivatives against methicillin-resistant Staphylococcus aureus, methicillin-resistant Staphylococcus epidermidis, Escherichia coli, and Streptococcus agalactiae were tested by the agar dilution method and Oxford cup assay. The majority of the tested compounds displayed moderate antibacterial activities. Importantly, the three compounds with amino or tertiary amine groups in their side chains, 11, 13b, and 15c, were the most active antibacterial agents. Docking experiments carried out on the peptidyl transferase center (PTC) of 23S rRNA proved that there is a reasonable direct correlation between the binding free energy (ΔGb, kcal/mol) and the antibacterial activity. Moreover, the pharmacokinetic profiles of 11 and 15c in rat were characterized by moderate clearance and oral bioavailability. © 2014 American Chemical Society.


Shen Y.,Lanzhou Institute of Husbandry and Pharmaceutical Science of CAAS | Liu X.,Lanzhou Institute of Husbandry and Pharmaceutical Science of CAAS | Yang Y.,Lanzhou Institute of Husbandry and Pharmaceutical Science of CAAS | Li J.,Lanzhou Institute of Husbandry and Pharmaceutical Science of CAAS | And 2 more authors.
Biomedical Chromatography | Year: 2015

Aspirin eugenol ester (AEE) is a promising drug candidate for treatment of inflammation, pain and fever and prevention of cardiovascular diseases with fewer side effects than its precursor, aspirin. Investigation into its metabolic process in target animal species will help to illustrate its mechanism of action and to establish its residual mark compound to formulate its dosage. Six beagle dogs were orally given a dose of 20 mg kg-1 of AEE and one dog was used to prepare blank liver microsomes. Their liver microsomes were prepared for in vitro study and their plasma and urine were collected for in vivo metabolic analysis using liquid chromatography tandem mass spectrometry. In this study we identified 10 metabolites, M1, M2, M3, M4, M5 in phase I and M6, M7, M8, M9, M10 in phase II. Based on the metabolites of AEE, the pathways of AEE metabolism in dog were demonstrated. © 2014 John Wiley & Sons, Ltd.


Pu W.,Lanzhou Institute of Husbandry and Pharmaceutical science of CAAS | Su Y.,Lanzhou Institute of Husbandry and Pharmaceutical science of CAAS | Li J.,Lanzhou Institute of Husbandry and Pharmaceutical science of CAAS | Li C.,Lanzhou Institute of Husbandry and Pharmaceutical science of CAAS | And 3 more authors.
PLoS ONE | Year: 2014

Staphylococcus aureus is a main cause of bovine mastitis and a major pathogen affecting human health. The emergence and spread of methicillin-resistant Staphylococcus aureus (MRSA) has become a significant concern for both animal health and public health. This study investigated the incidence of MRSA in milk samples collected from dairy cows with clinical mastitis and characterized the MRSA isolates using antimicrobial susceptibility tests and genetic typing methods. In total, 103 S. aureus isolates were obtained from dairy farms in 4 different provinces in China, including Gansu, Shanghai, Sichuan, and Guizhou. Antimicrobial susceptibility testing of these isolates revealed that the resistance rates to penicillin and sulfamethoxazole were high, while the resistance rates to ciprofloxacin and vancomycin were low. Among the 103 isolates, 49 (47.6%) were found to be mecA-positive, indicating the high incidence of MRSA. However, 37 of the 49 mecA-positive isolates were susceptible to oxacillin as determined by antimicrobial susceptibility assays and were thus classified as oxacillin-susceptible mecA-positive S. aureus (OS-MRSA). These isolates could be misclassified as methicillin susceptible Staphylococcus aureus (MSSA) if genetic detection of mecA was not performed. Molecular characterization of selected mecA-positive isolates showed that they were all negative with Panton-Valentine leukocidin (PVL), but belonged to different spa types and SCCmec types. These results indicate that OS-MRSA is common in bovine mastitis in China and underscore the need for genetic methods (in addition to phenotypic tests) to accurately identify MRSA. © 2014 Pu et al.


Wang R.,CAS Lanzhou Institute of Chemical Physics | Li J.-Y.,Lanzhou Institute of Husbandry and Pharmaceutical science of CAAS | Qi H.-Y.,CAS Lanzhou Institute of Chemical Physics | Shi Y.-P.,CAS Lanzhou Institute of Chemical Physics
Journal of Asian Natural Products Research | Year: 2013

The phytochemical investigation of the flower buds of Daphne genkwa yielded four highly oxygenated tigliane diterpene esters (1-4), including two new phorbol derivatives, 12-O-(2′E,4′E-decadienoyl)-7-oxo-5-ene-phorbol- 13-acetate (1) and 12- O-neodecanoyl-7-oxo-5-ene-phorbol-13-acetate (2). The molecular structures of the isolated compounds were elucidated on the basis of extensive spectroscopic analysis, including 1D and 2D NMR. © 2013 Taylor & Francis.


PubMed | Lanzhou Institute of Husbandry and Pharmaceutical science of CAAS
Type: | Journal: Food chemistry | Year: 2016

This study developed and validated a simple and reliable method for detecting and quantifying DVD, TMP and OMP in feed using dichloromethane extraction followed by HPLC-MS/MS. A matrix effect evaluation was performed using the post-extraction spiking method, and levels were less than 15% in all three feeds with their corresponding concentrations. LOD and LOQ, CC and CC were 20gkg(-1) and 40gkg(-1), 8.68-15.55gkg(-1) and 10.61-18.92gkg(-1) for all analytes, respectively. Calibration curves were linear for DVD, TMP and OMP with R(2)0.990 and r0.995, respectively. Recoveries of low, medium and high concentrations using the proposed method ranged from 74.4 to 105.2%. Repeatability and within-laboratory reproducibility were <7.4% (RSD). The chosen seven factors had no a significant influence on robustness. The method showed good performance when it was applied to analyze other laboratory-prepared or actual feed samples.

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