A5009495444- Chemical Synthesis and Analysis
- Aldose Reductase and Taurine
- Synthesis of Organic Compounds
- Saffron Plant Research Studies
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Phytochemistry and Biological Activities
- Phagocytosis and Immune Regulation
- Natural Compound Pharmacology Studies
- Medicinal Plants and Neuroprotection
- Wood and Agarwood Research
- Carbohydrate Chemistry and Synthesis
- Identification and Quantification in Food
- Cholinesterase and Neurodegenerative Diseases
- Natural Antidiabetic Agents Studies
- Biological Activity of Diterpenoids and Biflavonoids
- Cancer Treatment and Pharmacology
- Glycosylation and Glycoproteins Research
- Neurological Disorders and Treatments
- Neuroscience and Neuropharmacology Research
- RNA and protein synthesis mechanisms
- Tea Polyphenols and Effects
- Organic and Inorganic Chemical Reactions
- Bioactive Compounds and Antitumor Agents
- Medicinal Plants and Bioactive Compounds
Jinan University
2016-2025
Guangdong Pharmaceutical University
2012-2022
Shanghai Institute of Materia Medica
2013-2017
Chinese Academy of Sciences
2013-2017
Guangzhou Experimental Station
2014
Sun Yat-sen University
2012-2014
China Pharmaceutical University
2010
University of Wuppertal
2009
Shantou University
2005
University of Hong Kong
2002-2003
Psiguadials A (1) and B (2), two novel sesquiterpenoid-diphenylmethane meroterpenoids with unusual skeletons, along a pair of known epimers, psidial (3) guajadial (4), were isolated from the leaves Psidium guajava. Their structures absolute configurations elucidated by means NMR, X-ray diffraction, quantum chemical CD calculation. Compounds 1, 2, 4 exhibited potent inhibitory effects on growth human hepatoma cells.
Blood vessels in the tumor periphery have high pericyte coverage and are resistant to vascular disrupting agents (VDAs). VDA treatment resistance leads a viable peripheral rim that contributes failure disease recurrence. Here, we provide evidence support hypothesis shifting target of VDAs from vessel endothelial cells pericytes disrupts rim, circumventing resistance. Through chemical engineering, developed Z-GP-DAVLBH (from tubulin-binding desacetylvinblastine monohydrazide [DAVLBH]) as...
Gardenamide A (GA) protects the rat retinal ganglion (RGC-5) cells against cell apoptosis induced by H2O2. The protective effect of GA was completely abrogated specific phosphoinositide 3-kinase (PI3K) inhibitor LY294002, and protein kinase B (Akt) Akt VIII respectively, indicating that mechanism is mediated PI3K/Akt signaling pathway. extracellular signal-regulated (ERK1/2) PD98059 could not block neuroprotection GA. attenuated levels reactive oxygen species (ROS) malondialdehyde (MDA)...
Abstract Oxidative stress has been suggested to play a causative role in the development of obesity‐induced insulin resistance and type 2 diabetes. Given antioxidant potency previously reported xanthones isolated from Swertia mussotii . These natural products were further evaluated against other targets diabetes, aldose reductase α‐glucosidase, order identify novel multitarget‐directed antidiabetic agents. Among 14 screened, 1,3,7,8‐tetrahydroxyxanthone ( 6 ), 1,3,5,8‐tetrahydroxyxanthone 7...
Sunitinib is a multikinase inhibitor used to treat patients with advanced renal cell carcinoma (RCC). However, sunitinib toxicity makes it double-edged sword. Potent immune modulation by extends nuclear interactions. To address these issues, there an urgent need for delivery vectors suitable treatment. We developed PEGylated liposomes as precisely target (lipo-sunitinib) RCC tumors. Further investigations, including RNA sequencing (RNA-seq), were performed evaluate transcriptomic changes in...
ABSTRACT Infection with respiratory syncytial virus (RSV) is a major cause of acute lower tract disease in young children and older people. Despite intensive efforts over the past few decades, no direct-acting small-molecule agents against RSV are available. Most candidates targeting fusion (F) protein pose considerable risk inducing drug-resistant mutations. Here, we explored vitro vivo virological properties K394R variant, cross-resistant mutant capable evading multiple inhibitors. Our...
Two new xanthones, 1,8-dihydroxy-3-methoxyxanthone 7-<i>O</i>-[<i>α</i>-L-rhamnopyranosyl(1 → 2)-<i>β</i>-D-glucopyranoside] (<b>1</b>) and 1,8- dihydroxy-3-methoxyxanthone 3)-<i>α</i>-L-rhamno-pyranosyl (1 2)-<i>β</i>-D-xylopyranoside] (<b>2</b>), together with 26 known xanthones (<b>3</b>–<b>28</b>), were isolated from the aqueous ethanol extract of traditional Chinese herb <i>Swertia mussotii</i>. Their structures elucidated via spectroscopic analyses including 2D NMR. The inhibition...
Vinca alkaloids, the well-known tubulin-binding agents, are widely used for clinical treatment of malignant tumors. However, little attention has been paid to their vascular disrupting effects, and underlying mechanisms remain largely unknown. This study aims investigate effect vinca alkaloids. Methods: The capillary disruption assay aortic ring were performed evaluate in vitro desacetylvinblastine monohydrazide (DAVLBH), a derivate vinblastine, vivo was assessed on HepG2 xenograft model...
The synthesis of water soluble star-block copolypeptides and their encapsulation properties are described. copolypeptides, obtained by ring-opening polymerization amino acid N-carboxyanhydrides, consist a PEI core, hydrophobic polyphenylalanine or polyleucine inner shell, negatively charged polyglutamate outer shell. study showed that these soluble, amphiphilic could simultaneously encapsulate versatile compounds ranging from to anionic cationic hydrophilic guest molecules.
Modifications at C1, C7, C8, and C10 of genipin were conducted, the neurotrophic effects all derivatives studied. Genipin 1-4 obtained in mild to high yield. Compounds 1 4 are more stable than if exposed nucleophiles. All display higher activities genipin. Compound is most active, with least optimal dose. Both up-regulated activity nNOS PC12 cells. The effect inhibited not only by 7-NI, a specific inhibitor nNOS, but also L-NIO, eNOS; case genipin, its 7-NI. results indicate that promising...
Abstract Bioactivity focus on α-cyano-4-hydroxycinnamic acid (CHCA) scaffold results in a small library of novel multifunctional aldose reductase (ALR2) inhibitors. All the entities displayed good to excellent inhibition with IC 50 72–405 nM. ( R , E )- N -(3-(2-acetamido-3-(benzyloxy)propanamido)propyl)-2-cyano-3-(4-hydroxy phenyl)acrylamide 5f ) was confirmed as most active inhibitor (IC 72.7 ± 1.6 nM), and best antioxidant. bound ALR2 new mode without affecting aldehyde (ALR1) activity,...
Sporormiellin A (<bold>1</bold>), the first tetrahydrofuran-fused furochromone with an unprecedented tetracyclic skeleton, has been obtained from fungal strain <italic>Sporormiella minima</italic>.
Detection of Hyperacute Reactions Desacetylvinblastine Monohydrazide in a Xenograft Model Using Intravoxel Incoherent Motion DWI and R2* MappingJianye Liang1, Rong Ma2, Heru Chen3, Dongmei Zhang3, Wencai Ye3, Changzheng Shi1 Liangping Luo1Audio Available | Share
Abstract A four‐step synthetic process has been developed to prepare 1,3,5,8‐tetrahydroxyxanthone ( 2a ) and its isomer 1,3,7,8‐tetrahydroxyxanthone 2b ). 25 more xanthones were also synthesized by a modified scheme. Xanthone was identified as the most active inhibitor against both α‐glucosidase aldose reductase (ALR2), with IC 50 values of 7.8 ± 0.5 μM 63.2 0.6 nM, respectively, which far than acarbose (35.0 0.1 μM), little epalrestat (67.0 3.0 nM). confirmed antioxidant in vitro EC value...
Abstract Genipin is a Chinese herbal medicine with both neuroprotective and neuritogenic activity. Because of its unstable nature, efforts have been to develop more stable genipin derivatives improved biological activities. Among the new compounds reported in literature, (1 R )‐isopropyloxygenipin (IPRG001) but less active compound compared parent, genipin. Here, two IPRG001 generated by stereoselective reduction C 6 =C 7 double bond were synthesized. The 1 S isomers (4a ,7 ,7a...
Two amantadine (ATD)-gardenamide A (GA) ligands have been designed and synthesized. The bonding of ATD with GA through a methylene carbonyl brigde (L1) enhances the neuroprotective effect against corticosterone (CORT)-induced impairments in PC12 cells; while succinyl (L2) does not. L1 reduces level reactive oxygen species (ROS) cell apoptosis generated by CORT. It restores CORT-changed morphology to state that is closed normal cells. One mechanism attenuate CORT-induced adjustment both...