A5102010575- Veterinary medicine and infectious diseases
- Pharmacological Effects of Natural Compounds
- Toxin Mechanisms and Immunotoxins
- Bioactive Compounds and Antitumor Agents
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Synthesis and Biological Evaluation
- Humic Substances and Bio-Organic Studies
- Probiotics and Fermented Foods
- Clostridium difficile and Clostridium perfringens research
- RNA modifications and cancer
- Cancer-related molecular mechanisms research
- Mosquito-borne diseases and control
- Advanced biosensing and bioanalysis techniques
- RNA Interference and Gene Delivery
- Genomics, phytochemicals, and oxidative stress
- Bee Products Chemical Analysis
- Viral Infections and Immunology Research
- Immune cells in cancer
- Meat and Animal Product Quality
- Gut microbiota and health
- HVDC Systems and Fault Protection
- Microbial metabolism and enzyme function
- Microbial Natural Products and Biosynthesis
- Vector-borne infectious diseases
Shandong Academy of Agricultural Sciences
2022-2025
Poultry Research Institute
2025
Peking University
2022-2024
Lanzhou Institute of Husbandry and Pharmaceutical Sciences
2014-2023
Ministry of Agriculture and Rural Affairs
2020-2023
Chinese Academy of Agricultural Sciences
2013
The quantitative structure–activity relationship (QSAR) is one of the most popular methods for virtual screening new drug leads and optimization. Herein, we collected a dataset 955 MIC values pleuromutilin derivatives to construct 2D-QSAR model with an accuracy 80% 3D-QSAR non-cross-validated correlation coefficient (r2) 0.9836 cross-validated (q2) 0.7986. Based on obtained QSAR models, designed synthesized compounds 1 2 thiol-functionalized side chains. Compound displayed highest...
Several pleuromutilin derivatives possessing thiadiazole moieties were synthesized via acylation reactions under mild conditions. The in vitro antibacterial activities of the against methicillin-resistant S. aureus, epidermidis, E. coli, and B. cereus tested by agar dilution method Oxford cup assay. All screened compounds displayed potent activity. Compound 6d was most active agent because its lowest MIC value largest inhibition zone. Docking experiments performed to understand possible mode...
MicroRNAs (miRNAs) play indispensable roles in post-transcriptional gene regulation. The identification of target mRNAs is essential for dissecting the recognition basis, dynamics, and regulatory mechanism miRNA–mRNA interactions. However, lack an unbiased method detecting weak interactions remains a long-standing obstacle miRNA research. Here, we develop provide proof-of-concept evidence demonstrating chemical G-clamp-enhanced photo-cross-linking strategy covalent capture intracellular...
Halicin, the first antibacterial agent discovered by artificial intelligence, exerts broad-spectrum effects and has a unique structure. Our study found that halicin had good inhibitory effect on clinical isolates of drug-resistant strains Clostridium perfringens ( C. ). The safety was evaluated acute oral toxicity, genotoxicity subchronic toxicity studies. results test indicated halicin, as low-toxicity compound, an LD 50 2018.3 mg/kg. sperm malformation, bone marrow chromosome aberration...
Heat-stress-induced oxidative and inflammatory responses were important factors contributing to chicken intestinal damage. The purpose of this study was based on the antioxidant anti-inflammatory activities Physalis Calyx seu Fructus (Jin Deng Long, JDL) investigate its efficacy mechanism in relieving heat stress Primary embryo duodenum cells 90 30-day-old specific-pathogen-free randomly divided into control JDL groups establish models vitro vivo. mitigating effect assessed through...
Escherichia coli (E. coli) has the ability to induce clinical and subclinical mastitis in dairy cows, causing a huge loss for industry. In this study, 51 isolates 36 from eight provinces of China between 2019 2021 were used investigate differences their biological characteristics. The results showed that B1 (52.9%) A (39.1%) predominant phylogroups; R1 (50.6%) was lipopolysaccharide (LPS) core type; 44 STs (ST10 ST58 most sequence-prevalent STs) 2 new (ST14828 ST14829) identified; however,...
Abstract While studies of various carcinomas have reported aberrant metal metabolism, much remains unknown regarding their spatial accumulation and regulatory impacts in tumors. Here, elevated copper levels are detected breast cancer tumors from patients animal models, specifically exhibiting a zonate pattern. Spatially resolved multiomics analyses reveal that zonation drives tumor metabolic preference for oxidative phosphorylation (OXPHOS) over glycolysis promotes metastatic immune‐desert...
A new pleuromutilin derivative with excellent antibacterial activity, 14-O-[(2-amino-1,3,4-thiadiazol-5-yl) thioacetyl] mutilin (ATTM), may serve as a possible lead compound for the development of drugs. However, in vivo efficacy and toxicity evaluations this have not been performed. In study, we evaluated ATTM by measuring survival mice after lethal challenge methicillin-resistant Staphylococcus aureus (MRSA), 50% effective dose (ED50) was 5.74 mg/kg intravenous route. an oral single-dose...
A series of pleuromutilin derivatives were synthesized by two synthetic procedures under mild reaction conditions and characterized Nuclear Magnetic Resonance (NMR), Infrared Spectroscopy (IR), High Resolution Mass Spectrometer (HRMS). Most the with heterocyclic groups at C-14 side exhibited excellent in vitro antibacterial activities against Staphylococcus aureus, methicillin-resistant aureus (MRSA), epidermidis (MRSE), vancomycin-resistant Enterococcus (VRE) activity. The which contained...
Novel pleuromutilin derivatives designed based on the structure of valnemulin were synthesized and evaluated for their in vitro antibacterial activities. These with substituted amino moiety exhibited excellent activities against methicillin-resistant Staphylococcus aureus, epidermidis, Escherichia coli, Streptococcus agalactiae. Compound 5b showed highest even exceeded tiamulin. Moreover, docking experiments provided information about binding model between compounds peptidyl transferase...
Infections caused by methicillin-resistant Staphylococcus aureus (MRSA) have threated the public health worldwide, which emphasizes urgent need for new drugs with novel mechanism of actions. 14-O-[(5-ethoxycarbonyl-4,6-dimethylpyrimidine-2-yl) thioacetyl] mutilin (EDT) is a pleuromutilin compound high activity against several Gram-positive bacteria in vitro and vivo. This study aimed to verifying potential anti-MRSA evaluating safety EDT. In antibacterial assays, EDT exhibited potent MRSA...
To investigate the effect of polymer blends on in vitro release/degradation and pharmacokinetics moxidectin-loaded PLGA microspheres (MOX-MS), four formulations (F1, F2, F3 F4) were prepared using O/W emulsion solvent evaporation method by blending high (75/25, 75 kDa) low (50/50, 23 molecular weight with different ratios. The addition low-molecular-weight did not change release mechanism microspheres, but sped up drug drastically shortened lag phase. degradation results show that consisted...