A5020744768- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Drug Transport and Resistance Mechanisms
- Pharmacogenetics and Drug Metabolism
- Crystallography and molecular interactions
- Magnetism in coordination complexes
- Berberine and alkaloids research
- Metabolomics and Mass Spectrometry Studies
- HIV/AIDS drug development and treatment
- Antibiotics Pharmacokinetics and Efficacy
- Metal-Organic Frameworks: Synthesis and Applications
- Analytical Chemistry and Chromatography
- HIV Research and Treatment
- Metal complexes synthesis and properties
- Alkaloids: synthesis and pharmacology
- Advanced Steganography and Watermarking Techniques
- Cancer-related Molecular Pathways
- Natural Compounds in Disease Treatment
- Pharmacological Effects and Toxicity Studies
- Receptor Mechanisms and Signaling
- Digital Media Forensic Detection
- Cholinesterase and Neurodegenerative Diseases
- Liver physiology and pathology
- Chemical Synthesis and Analysis
- Advancements in Transdermal Drug Delivery
Sun Yat-sen University
2004-2024
The Seventh Affiliated Hospital of Sun Yat-sen University
2021-2024
Key Laboratory of Guangdong Province
2021
Zhongshan Hospital
2009-2020
Sanofi (United States)
2019
Zhongshan Hospital of Xiamen University
2019
Institute of Pharmacology
2014-2018
Takeda (United States)
2013
Millennium Engineering and Integration (United States)
2013
Shandong Normal University
2011-2012
Abstract Circular RNAs (circRNAs) play important roles in gastric cancer progression but the regulatory role of circRNAs controlling macrophage function remains elusive. Exosomes serve as cargo for and a crucial mediators facilitating communication between cells tumor microenvironment. In this study, we found that circATP8A1, previously unreported circular RNA, is highly expressed both tissues exosomes derived from plasma. Increased circATP8A1 was associated with advanced TNM stage worse...
The dinuclear copper(II) cryptate [Cu2L](ClO4)4 (1) cleaves the C−C bond of acetonitrile at room temperature to produce a cyanide bridged complex [Cu2L(CN)](ClO4)3·2CH3CN·4H2O (2). cleavage mechanism is presented on basis results crystal structure 2, electronic absorption spectra, ESI-MS spectroscopy, and GC spectra 1, respectively.
The past five decades have witnessed remarkable advancements in the field of inhaled medicines targeting lungs for respiratory disease treatment. As a non-invasive drug delivery route, inhalation therapy offers numerous benefits to patients, including rapid and targeted exposure at specific sites, quick onset action, bypassing first-pass metabolism, beyond. Understanding characteristics pulmonary transporters metabolizing enzymes is crucial comprehending efficient clearance processes within...
Evidence suggests that gut microbiome changes upon hypobaric hypoxia exposure; however, it remains elusive whether this change is a merely derivational reflection of host physiological alteration, or synergizes to exacerbate high-altitude diseases. We intervened in the rat model prolonged challenge and found intervention could alleviate symptoms pathological cardiac hypertrophy, microbial dysbiosis, metabolic disruptions certain metabolites plasma induced by hypoxia.
Schisantherin A and schisandrin A, the most abundant active ingredients of Wuzhi capsule, are known to inhibit tacrolimus metabolism by inhibiting CYP3A4/5. We aimed predict contribution schisantherin drug-drug interaction (DDI) between capsule using physiologically-based pharmacokinetic (PBPK) modelling. Firstly, inhibition mechanism on CYP3A4/5 was investigated. Thereafter, PBPK models were established. Finally, pharmacokinetics evaluated after combined use with or A. The blood area under...
Abstract Triptolide (TP) is the major active principle of Tripterygium wilfordii Hook f. and very effective in treatment autoimmune diseases. However, TP induced hepatotoxicity limited its clinical applications. Our previous study found that was a substrate P-glycoprotein hepatobiliary clearance markedly affected by P-gp modulation sandwich-cultured rat hepatocytes. In this study, small interfering RNA (siRNA) specific inhibitor tariquidar were used to investigate impact down regulation on...
Background and Aims: Cell fate can be directly reprogrammed from accessible cell types (e.g., fibroblasts) into functional by exposure to small molecule stimuli. However, no chemical reprogramming method has been reported date that successfully generates hepatocyte‐like cells repopulate liver tissue, casting doubt over the feasibility of approaches obtain desirable for therapeutic applications. Approach Results: Here, through induction phenotypic plasticity, we provide a proof‐of‐concept...
Naturally occurring furanocoumarin compounds psoralen (PRN) and isopsoralen (IPRN) are bioactive constituents found in herbaceous plants. They widely used as active ingredients several Chinese herbal medicines. In this study, the CYP1A2 inhibitory potential of PRN IPRN was investigated rats vitro vivo well human liver microsomes. Both exhibited reversible time-dependent inhibition toward rat microsomal cyp1a2. The IC<sub>50</sub>, <i>k</i><sub>inact</sub>, <i>K</i><sub>I</sub> values were...
Triptolide (TP), a main bioactive component of <i>Tripterygium wilfordii Hook F.</i>, is promising agent for treatment autoimmune diseases. However, high incidence dose-limiting hepatotoxicity was observed in the clinic. Sandwich-cultured rat hepatocyte model used this study to identify involvement P-glycoprotein (P-gp) TP disposition and evaluate TP-induced after modulation P-gp by known inhibitors, ritonavir tariquidar, inducers, phenobarbital, quercetin, H<sub>2</sub>O<sub>2</sub>. Our...
Fentanyl is a rapid-acting, short duration opioid analgesic agent. In recent years, increased prescription and illicit use of fentanyl drugs have led to major safety concerns growing death toll. However, the causes fentanyl-induced fatal adverse effects not been thoroughly researched. This study investigated P-glycoprotein (P-gp) modulated blood-brain barrier penetration its resulting toxicity in vitro vivo. ATPase assays were performed together with bi-directional transport using Caco-2...
The recent outbreak of novel coronavirus pneumonia (COVID-19) caused by a new has posed great threat to public health. Identifying safe and effective antivirals is urgent demand cure the huge number patients. Virus-encoded proteases are considered potential drug targets. human immunodeficiency virus protease inhibitors (lopinavir/ritonavir) been recommended in global Solidarity Trial March launched World Health Organization. However, there currently no experimental evidence support or...
Different from most antiretroviral drugs that act as passive defenders to inhibit HIV-1 replication inside the host cell, virus inactivators can attack and inactivate virions without relying on their cycle. Herein, we describe discovery of a hydrocarbon double-stapled helix peptide, termed D26. D26 is based gp41 protein lentiviral lytic peptide-3 motif (LLP3) sequence, which efficiently infection cell-free virions. It was noted highly resistant proteolytic degradation exhibited remarkably...
We previously reported that dinuclear copper(II) cryptate [Cu(2)L](4+) cleaves the C-C bond of acetonitrile at room temperature to produce a cyano-bridged and methanol, whereby reaction mechanism has not yet become clear. have now systemically investigated this reaction, four cryptates, [Cu(2)L](ClO(4))(4) (1), [Zn(2)L](ClO(4))(4) (2), [Cu(2)L(H(2)O)(2)](CF(3)SO(3))(4) (5), [Cu(2)L(OH)(OH(2))](ClO(4))(3) (6) are here. Cryptates 1 2 can cleave C--C bonds acetonitrile, propionitrile,...
Organophosphorus pesticides are the most widely used in modern agricultural systems to ensure good harvests. Isocarbophos (ICP), with a potent acetylcholinesterase inhibitory effect is utilized control variety of leaf-eating and soil insects. However, characteristics bioactivation detoxification ICP humans remain unclear. In this study, oxidative metabolism, esterase hydrolysis, chiral inversion human liver microsomes (HLMs) were investigated aid stereoselective LC/MS/MS method. The...
Gossypol was considered a promising male contraceptive but finally failed due to two side effects: hypokalemia and the irreversibility of its effect. Here we demonstrate that sustained zero-order release could be solution for these problems. The in vitro gossypol from gossypol/PEG layer-by-layer films follows perfect kinetics. In vivo tests indicate can maintain plasma drug concentration constant SD rats ∼20 days 30-bilayer film. is 2 orders magnitude lower than peak when administered orally...
Schizandrol A (SZA) and schizandrol B (SZB) are two active ingredients of Wuzhi capsule (WZC), a Chinese proprietary medicine commonly prescribed to alleviate tacrolimus (FK-506)-induced hepatoxicity in China. Due their inhibitory effects on cytochrome P450 (CYP) 3A enzymes, SZA/SZB may display drug–drug interaction (DDI) with tacrolimus. To identify the extent this DDI, enzymes’ profiles, including 50% concentration (IC50) shift, reversible inhibition (RI) time-dependent (TDI) were examined...
The crystal structures of [Co 2L(Cl)](ClO 4) 3 ( 1), 2L(Br)](ClO 2), 2L(OH)(OH 2)]I 3), and 2L (1)(Cl)](ClO 4), the density functional theory calculations, as well binding constants 2L] (4+) toward Cl (-) Br (1)] (-), are reported in this paper (L = N[(CH 2) 2NHCH 2(C 6H 4- p)CH 2NH(CH 2] 3N, L (1) m)CH 3N). rigid dicobalt(II) cryptate shows recognition but not F I because size matching to its cavity. We also found that relative tripodal skeleton than results higher affinity (-). Magnetic...
Radix Angelicae dahuricae is a well-known medicinal herb in number of preparations for medical uses. In this study, rapid and selective method using liquid chromatography with tandem mass spectrometry was developed the separation simultaneous quantitation nine furanocoumarins from A. dahuricae, namely imperatorin, isoimperatorin, oxypeucedanin hydrate, bergapten, oxypeucedanin, xanthotoxol, xanthotoxin, isopimpinellin, psoralen. Chromatographic achieved on CAPCELL PAK MG II C18 analytical...