A5100651793- Click Chemistry and Applications
- Chemical Synthesis and Analysis
- Synthetic Organic Chemistry Methods
- Cancer Treatment and Pharmacology
- Cancer therapeutics and mechanisms
- Microbial Natural Products and Biosynthesis
- HER2/EGFR in Cancer Research
- Asymmetric Synthesis and Catalysis
- RNA Interference and Gene Delivery
- Monoclonal and Polyclonal Antibodies Research
- Cancer-related Molecular Pathways
- Nanoparticle-Based Drug Delivery
- Immune Cell Function and Interaction
- Peptidase Inhibition and Analysis
- Catalytic Alkyne Reactions
- Marine Sponges and Natural Products
- Immunotherapy and Immune Responses
- Cyclopropane Reaction Mechanisms
- Adenosine and Purinergic Signaling
- Synthesis and pharmacology of benzodiazepine derivatives
- Health Literacy and Information Accessibility
- Glycosylation and Glycoproteins Research
- Estrogen and related hormone effects
- MicroRNA in disease regulation
- Autophagy in Disease and Therapy
University of Macau
2024-2025
Novartis (United States)
2021
Endocyte (United States)
2010-2020
First Hospital of Xi'an
2017-2020
Xian Central Hospital
2017-2020
Hangzhou Medical College
2020
Zhejiang Provincial People's Hospital
2020
Hubei University of Chinese Medicine
2020
Huazhong University of Science and Technology
2019
Central Hospital of Wuhan
2019
Sepsis‑induced cardiomyopathy (SIC) is a complication of severe sepsis and septic shock characterized by an invertible myocardial depression. This study sought to explore the potential effects mechanism luteolin, flavonoid polyphenolic compound, in lipopolysaccharide (LPS)‑induced injury. Experimental mice were randomly allocated into 3 groups (25 each group): The control group (NC), LPS (LPS) + luteolin (LPS Lut). Before SIC model was induced, dissolved DMSO injected intraperitoneally for...
China is experiencing a rapid increase in its aging population, leading to the emergence of significant challenges improve quality life (QoL) older adults. The study aims explore potential benefits using mobile health technology improving QoL for Chinese This utilized subsample adults aged 60 and above from cross-sectional, population-based national survey conducted among (N = 852). A moderated mediation analysis was investigate impact mHealth use on adults' QoL, focusing mediating roles...
Vintafolide is a potent folate-targeted vinca alkaloid small molecule drug conjugate (SMDC) that has shown promising results in multiple clinical oncology studies. Structurally, vintafolide consists of 4 essential modules: (1) folic acid, (2) hydrophilic peptide spacer, (3) disulfide-containing, self-immolative linker, and (4) the cytotoxic drug, desacetylvinblastine hydrazide (DAVLBH). Here, we report structure-activity study evaluating biological impact (i) substituting DAVLBH within with...
To better regulate the biodistribution of vinblastine-folate conjugate, EC145, a new folate-spacer that incorporates 1-amino-1-deoxy-D-glucitol-gamma-glutamate subunits into peptidic backbone, was synthesized. Synthesis Fmoc-3,4;5,6-di-O-isopropylidene-1-amino-1-deoxy-D-glucitol-gamma-glutamate 20, suitable for Fmoc-strategy solid-phase peptide synthesis (SPPS), achieved in four steps from delta-gluconolactone. Addition alternating glutamic acid and 20 moieties onto cysteine-loaded resin,...
Although peptides, antibodies/antibody fragments, siRNAs, antisense DNAs, enzymes, and aptamers are all under development as possible therapeutic agents, the breadth of their applications has been severely compromised by inability to reach intracellular targets. Thus, while macromolecules can often enter cells receptor-mediated endocytosis, missions frequently fail due an escape entrapping endosomes. In this paper, we describe a general method for promoting release any biologic material from...
Targeting of malignancies with folate-linked therapeutics has proven to be a promising endeavor due the preferential expression folate receptors (FR) on human tumors. We have shown that folic acid (pteroyl-glutamate) can used deliver an antigenic hapten, fluorescein, surface tumor cells promote their opsonization within fluorescein-immunized host. Here, we investigate structure–activity relationships among members another class folate–hapten conjugates (EC57, EC63, EC0293, and EC0294),...
Natural plants are considered as a huge treasure for anticancer. Amomum tsaoko, plant of Zingiberaceae, is used widely food and traditional medicine in East Asia. In previous studies, tsaoko has antitumor effect on liver cancer cells, but the mechanism not clear. Here, we demonstrated that ethanol extract from (At-EE) could inhibit ovarian decrease angiogenesis vivo. At-EE did influence vascular endothelial cells directly, decreased IL-6 VEGF secreted by to through inhibition p-STAT3 NF-kB...
We describe the development of methodology which allows for introduction a second disulfide bond into molecular framework with pre-existing linker system. Compounds contain an S-9-fluorenylmethyl-protected thiol and additional linkage are deprotected in situ trapped activated thiophile. This allowed synthesis first molecule possessing two different biologically active agents covalently attached to folate receptor targeting ligand unit via disulfide-based release systems.
Folate receptor (FR)-β has been identified as a promising target for antimacrophage and antiinflammatory therapies. In the present study, we investigated EC0565, folic acid-derivative of everolimus, FR-specific inhibitor mammalian rapamycin (mTOR). Because its amphiphilic nature, EC0565 was first evaluated water solubility, critical micelle formation, stability in culture FR-binding specificity. Using FR-expressing macrophages, effect on mTOR signaling cellular proliferation studied. The...
The cycloaddition between 1,3-cyclohexadiene and various enones enals (methyl vinyl ketone, ethyl methacrolien) is accomplished at room temperature in yields ranging from 51 to 68% without the use of Lewis acids, high pressures, or microwave reactors. This normally sluggish cyclization by precoordination diene a π-basic molybdenum complex. η2-bound metal thought promote Michael reaction uncoordinated portion enone, resulting enolate then closes form cycloalkene product. organic cycloadduct...
Provoked by sterile/nonsterile insults, prolonged monocyte mobilization and uncontrolled monocyte/macrophage activation can pose imminent or impending harm to the affected organs. Curiously, folate receptor beta (FRβ), with subnanomolar affinity for vitamin folic acid (FA), is upregulated during immune in hematopoietic cells of myeloid lineage. This phenomenon has inspired a strong interest exploring FRβ-directed diagnostics/therapeutics. Previously, we have reported that FA-targeted...
Pyrrolobenzodiazepines (PBDs) and their dimers (bis-PBDs) have emerged as some of the most potent chemotherapeutic compounds, are currently under development novel payloads in antibody-drug conjugates (ADCs). However, when used stand-alone therapeutics or warheads for small molecule drug (SMDCs), dose-limiting toxicities often observed. As an elegant solution to this inherent problem, we designed diazepine-ring-opened conjugated prodrugs lacking imine moiety. Once prodrug (pro-PBD) conjugate...
To observe the therapeutic effect of electroacupuncture (EA) at five Back-Shu points on sleep, hippocampal peripheral benzodiazepine receptor (PBR) expression and hypothalamic 5-hydroxytryptamine (5-HT), 5-hydroxyindoleacetic acid (5-HIAA), tumor necrosis factor alpha (TNF-α) interleukin (IL)-1β contents in insomnia rats, so as to explore its mechanisms underlying improvement insomnia.Forty male SD rats were randomly divided into control, model, EA medication (Diazepam) groups (n=10 each...
China has a longstanding tradition of alcohol consumption, yet excessive drinking poses significant health risks, particularly for individuals with cardiovascular conditions such as hypertension. While existing literature indicates that both information scanning and seeking behaviors can impact beliefs actions, their effects on prevention remain understudied. Utilizing data from national survey in China, this study investigates the influence risk knowledge frequency among hypertensive...
Reactions are reported for the TpW(NO)(PMe3) complex of either 2-methylfuran or 2,5-dimethylfuran with various dipolarophiles (N-methylmaleimide, N-phenylmaleimide, acrylonitrile). The resulting 7-oxanorbornene complexes thought to be formed from a two-step reaction sequence. first step involves metal shifting coordination site C4−C5 C3−C4, an action that renders furan similar carbonyl ylide. This is followed by 1,3-dipolar cycloaddition. In case maleimides, high preference (>10:1) exo...
The rhenium furan complexes TpRe(CO)(MeIm)(η2-2-methylfuran) (1) and TpRe(CO)(MeIm)(η2-2,5-dmethylfuran) (2) undergo Lewis acid-promoted cyclopentannulation reactions with enones enals to generate 3-acetylcyclopentene complexes. During the reaction, a rearrangement occurs such that α β carbons of enone are incorporated into new carbocycle. Treatment these an oxidant (H2O2 or silver triflate) liberates acetylcyclopentene. When resolved form complex is used, acetylcyclopentenes can be obtained...
TpRe(CO)(MeIm)(η2-2-methylfuran) (1; Tp = hydridotris(pyrazolyl)borate and MeIm N-methylimidazole) TpRe(CO)(MeIm)(η2-2,5-dimethylfuran) (9) undergo Lewis acid promoted cyclopentannulation reactions with enones enals to generate 3-acetylcyclopentene complexes. During the reaction, a rearrangement occurs such that α- β-carbons of enone or enal are incorporated into new carbocycle. The completely regioselective. Yields vary from 26 78%, depending on reaction conditions. Diastereomer ratios...