A5010922568- Pharmacogenetics and Drug Metabolism
- Plant-based Medicinal Research
- Natural Compounds in Disease Treatment
- Antimicrobial Resistance in Staphylococcus
- Quinazolinone synthesis and applications
- Pharmacological Effects of Natural Compounds
- Berberine and alkaloids research
- Cancer therapeutics and mechanisms
- Natural product bioactivities and synthesis
- Alkaloids: synthesis and pharmacology
- Liver Disease and Transplantation
- Protease and Inhibitor Mechanisms
- S100 Proteins and Annexins
- Traditional Chinese Medicine Analysis
- Hormonal and reproductive studies
- Phytochemical compounds biological activities
- Antibiotic Resistance in Bacteria
- Sexual Differentiation and Disorders
- Eicosanoids and Hypertension Pharmacology
- Glutathione Transferases and Polymorphisms
- Phytochemistry and biological activity of medicinal plants
- Signaling Pathways in Disease
- Sexual function and dysfunction studies
- Liver Disease Diagnosis and Treatment
- Wound Healing and Treatments
Hubei University
2007-2024
University of Notre Dame
2013-2019
University Gastroenterology
2011
In the face of clinical challenge posed by resistant bacteria, present needs for novel classes antibiotics are genuine. silico docking and screening, followed chemical synthesis a library quinazolinones, led to discovery (E)-3-(3-carboxyphenyl)-2-(4-cyanostyryl)quinazolin-4(3H)-one (compound 2) as an antibiotic effective in vivo against methicillin-resistant Staphylococcus aureus (MRSA). This impairs cell-wall biosynthesis documented functional assays, showing binding 2 penicillin-binding...
We recently reported on the discovery of a novel antibacterial (2) with 4(3H)-quinazolinone core. This was made by in silico screening 1.2 million compounds for binding to penicillin-binding protein and subsequent demonstration activity against Staphylococcus aureus. The first structure–activity relationship this scaffold is explored report evaluation 77 variants structural class. Eleven promising were further evaluated vitro toxicity, pharmacokinetics, efficacy mouse peritonitis model...
Infections caused by hard-to-treat methicillin-resistant Staphylococcus aureus (MRSA) are a serious global public-health concern, as MRSA has become broadly resistant to many classes of antibiotics. We disclose herein the discovery new class non-β-lactam antibiotics, oxadiazoles, which inhibit penicillin-binding protein 2a (PBP2a) MRSA. The oxadiazoles show bactericidal activity against vancomycin- and linezolid-resistant other Gram-positive bacterial strains, in vivo efficacy mouse model...
Rapid emergence of antibiotic resistance is one the most challenging global public health concerns. In particular, vancomycin-resistant Enterococcus faecium infections have been increasing in frequency, representing 25% enterococci intensive care units. A novel class 1,2,4-triazolo[1,5-a]pyrimidines active against E. reported herein. We used a three-component Biginelli-like heterocyclization reaction for synthesis series these derivatives based on reactions aldehydes, β-dicarbonyl compounds,...
A complication of diabetes is the inability wounds to heal in diabetic patients. Diabetic are refractory healing due involvement activated matrix metalloproteinases (MMPs), which remodel tissue resulting apoptosis. There no readily available methods that identify active unregulated MMPs. With use a novel inhibitor-tethered resin binds exclusively forms MMPs, coupled with proteomics, we quantified MMP-8 and MMP-9 mouse model wounds. Topical treatment selective inhibitor led acceleration wound...
The structure–activity relationship (SAR) for the newly discovered oxadiazole class of antibiotics is described with evaluation 120 derivatives lead structure. This was by in silico docking and scoring against crystal structure a penicillin-binding protein. They impair cell-wall biosynthesis exhibit activities Gram-positive bacterium Staphylococcus aureus, including methicillin-resistant S. aureus (MRSA) vancomycin-resistant linezolid-resistant aureus....
The quinazolinones are a new class of antibacterials with in vivo efficacy against methicillin-resistant Staphylococcus aureus (MRSA). target cell wall biosynthesis and have unique mechanism action by binding to the allosteric site penicillin-binding protein 2a (PBP 2a).
Objective This study was designed to determine whether a transjugular intrahepatic portosystemic shunt (TIPS) combined with embolotherapy superior TIPS alone. Methods Seventy-nine patients were included in the (43 and group 36 alone group). Embolotherapy performed after using coils tissue adhesive agent. The pressure gradient (PPG) lower than 12 mm Hg all patients. Multivariate analyses Cox regression model, probabilities of survival rebleeding estimated Kaplan-Meier method. Results Baseline...
Phillygenin is a bioactive intergradient in Osmanthus fragrans, well-known food additive and Chinese traditional medicine. This study was to investigate the hepatoprotective effects pharmacokinetics of phillygenin. The effect phillygenin assessed carbon tetrachloride- (CCl 4 -) intoxicated mice by monitoring levels serum tissue biomarkers. evaluated mouse after oral ( po , 24 mg / kg) or intravenous iv 12 mg/kg) administration. Results showed that has great on CCl4-induced liver injury owing...
Hepatocellular carcinoma (HCC) is the leading cause of death in patients with cirrhosis. Due to its poor response conventional chemotherapy drugs, prognosis for survival worst. NAD(P)H:quinone oxidoreductase 1 (NQO1) an attractive anticancer target due overexpression HCC. Although triptolide (TP) possesses potent antitumor activity, clinical practice greatly limited general toxicities and narrow therapeutic window. Herein, we develop NQO1-selective activated TP analog, named CX-23, which...
In this work, liquid chromatography-electrospray ionization tandem ion-trap mass spectrometry (LC-MS(n)) was used to investigate the in-vivo and in-vitro metabolism of tectoridin. After oral administration a single dose (100 mg kg(-1)) tectoridin healthy rats, faeces urine samples were collected for 0-48 h 0-24 h, respectively. Tectoridin also incubated with rat intestinal flora liver microsomes. Samples from studies purified using C(18) solid-phase extraction cartridge, then separated...
Abstract Palmatine is an isoquinoline alkaloid that has been widely used in China for the treatment of various inflammatory diseases such as gynecological inflammation, bacillary dysentery, enteritis, respiratory tract infection, urinary etc. In study reported this paper, a simple and rapid high‐performance liquid chromatography/electrospray ionization (ESI) tandem mass spectrometric method (MS/MS) was developed elucidation structures metabolites palmatine rat urine after administration...
The gelatinases, matrix metalloproteinases (MMP)-2 and MMP-9, are thought to be key mediators of secondary damage in adult animal models brain injury. Moreover, an acute increase these proteases plasma extracellular fluid patients with moderate-to-severe traumatic injuries (TBIs) is associated poorer clinical outcomes mortality. Nonetheless, their involvement after TBI the pediatric remains understudied. Using a murine model at postnatal day 21 (p21), approximating toddler-aged child, we saw...
MMP-9 plays a detrimental role in the pathology of several neurological diseases and, thus, represents an important target for intervention. The water-soluble prodrug ND-478 is hydrolyzed to active inhibitor ND-322, which turn N-acetylated even more potent metabolite ND-364. We used sensitive bioanalytical method based on ultraperformance liquid chromatography with multiple-reaction monitoring detection measure levels ND-478, and ND-364 plasma brain after administration metabolites. did not...