Abstract In this study, a series of new flavones (2‐phenyl‐chromone), 2‐naphthyl chromone, 2‐anthryl‐chromone, or 2‐biphenyl‐chromone derivatives containing 6 7‐substituted tertiary amine side chain were designed, synthesized, and evaluated in acetylcholinesterase (AChE) butyrylcholinesterase (BChE) inhibition. The results indicated that the alteration aromatic ring connecting to chromone scaffold brings about significant impact on biological activity. Compared with flavones, inhibitory...

A novel series of quinoline–indole derivatives were synthesized and evaluated as multitarget-directed ligands for the treatment Alzheimer's disease (AD). Biological evaluation revealed that had multifunctional profiles including antioxidant effects, blood–brain barrier (BBB) penetration, biometal chelation, Aβ aggregation modulation, neurotrophic neuroprotective properties. Moreover, several representative target demonstrated hippocampal cell proliferation in living adult mice by...

Melanoma is the most aggressive and treatment-resistant form of skin cancer. Curcumol a Chinese medicinal herb traditionally used as cancer remedy. However, molecular mechanisms underlying anticancer activity curcumol in melanoma remains largely unknown. In present study, we observed that decreased mouse B16 cell proliferation migration. The xenograft tumor assay showed reduced volume lung metastasis. upregulated expression E-cadherin downregulated N-cadherin, MMP2 MMP9 cell. Western blot...

To search for nano-drug preparations with high efficiency in tumor treatment, we evaluated the drug-loading capacity and cell-uptake toxicity of three kinds nanoparticles (NPs). Pullulan was grafted ethylenediamine hydrophobic groups to form cholesterol-modified amino-pullulan (CHAP) conjugates. Fourier transform infrared spectroscopy nuclear magnetic resonance were used identify CHAP structure calculate degree substitution cholesterol group. We compared types NPs close properties: CHAP,...

Most free drugs that cross the blood–brain barrier are characterized by high liposolubility, but they often have limited clinical applications because of poor dissolution and bioavailability. In this study, we prepared donepezil drug-loaded nanoparticles (DZP) with cholesterol-modified pullulan (CHP) as nanocarrier (DZP-CHP) surface modified to improve water solubility while enhancing its targeting sustained release. We determined drug loading encapsulation efficiency DZP-CHP at different...

Polyethylene glycolated (PEGylated)curcumin-grafted-chitosan (PCC) conjugates were synthesized with three PEG/chitosan feed molar ratios (1/5, 1/7.5, and 1/10), namely PCC1, PCC2 PCC3. Chemical structures of these characterized by Fourier transform infrared (FTIR) proton nuclear magnetic resonance (¹H NMR). The degrees substitution (DS) PEG 0.75%, 0.45% 0.33%, respectively, for PCC3by ¹H NMR analysis. Self-assembled PCC nanoparticles (NPs) spherical as observed in transmission electron...

Glioma is one of the most common malignant tumors affecting central nervous system. We screened active drugs from 12 classes to provide experimental data for study human glioma. Serum-free suspension clone formation was used induce glioma stem‑like cells (GSLCs) U251 cells. and observed their effects on number tumor balls. The results revealed that serum‑free successfully induced GSLCs. Six [curcumin, chrysin, apigenin, luteolin, casticin 8-bromo-7-methoxychrysin (BrMChR)] were identified by...

Neonatal hypoglycemia is tightly related to adverse neurodevelopmental and brain injury outcomes. A total of 195 infants who were born from diabetic mothers with a low blood glucose level (< 2.6 mM) within 0.5 h after birth enrolled in this prospective cohort study. Of these, 157 had neonatal (group A) followed up, group was further divided into A1 [blood concentration (BGC) < mM at 2 birth], A2 (BGC 2–24 birth), A3 > 24 birth). 144 whose no high risk for gestational diabetes mellitus up as...

Neuroglobin (Ngb) has been reported to be increased in early and moderately advanced Alzheimer’s disease (AD) stages but declined the severe stage. However, its regulatory mechanisms pathophysiological roles remain defined. In this study, we found that Ngb expression was significantly upregulated by low dose Aβ 25–35 , neurotoxic fragment of 1 - 40 42 not further a higher . Mutation analysis supershift assay demonstrated transcription factor Nuclear Factor κB (NF κB), κB2 κB3 sites located...

AIM:To evaluate pretreatment serum carcinoembryonic antigen (CEA) as a predictor of survival for patients with locally advanced gastric cancer receiving perioperative chemotherapy. METHODS:We retrospectively studied cohort 228 who underwent D2 gastrectomy combined chemotherapy at the Sun Yat-sen University Cancer Center between January 2005 and December 2009.Among them, 168 received 6-12 cycles oxaliplatin-based adjuvant (post-operative) chemotherapy, while 60 (2 FOLFOX6 or XELOX before...

Transient receptor potential melastatin 2 (TRPM2) is an important ion channel that represents a target for treating injury caused by cerebral ischemia. However, it unclear whether reducing TRPM2 expression can help repair injury, and if so what the mechanism underlying this process involves. This study investigated protective effect of on pheochromocytoma (PC12) cells injured oxygen-glucose deprivation (OGD). PC12 were transfected with plasmid encoding shRNAS, then subjected to OGD...

Insulin-like growth factor–binding protein 7 (IGFBP7) has been identified as a tumor suppressor in solid tumors. In acute leukemia, the role of IGFBP7 is largely unknown. The authors used quantitative reverse transcriptase–polymerase chain reaction (qRT-PCR) to investigate expression level gene bone marrow (BM) specimen from 66 children with myeloid leukemia (AML) at different stages and 30 nonleukemia patients control. Furthermore, U937 cells were transfected siRNA-2 (as U937R) for 24...

Biatractylolide, isolated from the ethyl acetate extract of Atractylodes macrocephala , has shown various pharmacological activities such as antitumor and antioxidant activities. In this work, we aim to study protective effect biatractylolide on glutamate‐induced rat adrenal pheochromocytoma cell (PC12) human bone marrow neuroblastoma line (SH‐SY5Y) injury preliminarily explore its mechanism. The results showed that glutamate was cytotoxic with an inhibitory concentration 50% (IC50) 8.5 mM...

Previously, we designed, synthesized, and evaluated a series of quinolone-benzofuran derivatives as multitargeted anti-Alzheimer's disease (anti-AD) compounds, discovered that WBQ5187 possesses superior anti-AD bioactivity. In this work, investigated the pharmacokinetics new molecule, well its therapeutic efficacy in restoring cognition neuropathology, APP/PS1 mouse model AD. Pharmacokinetic analyses demonstrated possessed rational oral bioavailability, metabolic stability, excellent...

Biatractylolide was isolated from ethyl acetate extract of dried Atractylodis Macrocephalae Rhizoma root by multistep chromatographic processing. Structure biatractylolide confirmed 1 H‐NMR and 13 C‐NMR. The IC 50 on acetylcholinesterase (AChE) activity 6.5458 μ g/mL when the control value huperzine A 0.0192 g/mL. Molecular Docking Software (MOE) used to discover molecular sites action between AChE protein regular docking approaches. Moreover, downregulated expression MEF 293T cells in a...

Abstract The present study investigated the composition, abundance, and diversity of gut microbes in full-term late-preterm infants from a medical center eastern China. A total 144 genomes stool samples were captured for 16S rRNA metagenomic analyses. high abundance commensal intestinal bacteria was detected these such as Phocaeicola vulgatus, Escherichia coli, Faecalibacterium prausnitzii , indicating relatively consistent aged 38–40 weeks. However, late preterm (n = 50) with mandatory...

Objective: To study antimicrobial activity of aqueous extract maize silk. Methods: Choose Staphylococcus aureus, Pseudomonas aeruginosa, Bacillus cereus, coli and Candida albicans as detected germs. Using methods agar plated diffusions tube continuous dilution to detect minimum inhibitory concentration Results:(1) Aqueous silk has against bacteria such aureus subtilis, the diameter bacteriostatic circle is 17 28 millimeter; also inhibited by its 24 millimeter.(2)The subtilis 500mg/ml...

To study antimicrobial activity of ethanolic extract maize silk. Staphylococcus aureus, Pseudomonas aeruginosa, Bacillus cereus, coli and Candida albicans were chosen as detected germs. Using methods agar plated diffusions and tube continuous dilution to detect MIC (minimum inhibitory concentration) silk. Ethanolic silk can inhibit microbial against bacteria such as S. aureus, P. aeruginosa, B. cereus, B. coli and C. albicans and the diameter bacteriostatic circle is 19, 20, 28, 15 21...

Histone modification is dysregulated in various types of cancers, including hematological malignancies. However, the expression profile histone-modifying enzymes pediatric acute monoblastic leukemia (AML FAB M5) has not been investigated. In this study, we evaluated mRNA 85 genes that encode involved histone-modification 27 AML M5 samples by using a novel real-time PCR array. We obtained gene cluster consisting total 28 (15 up-regulated and 13 down-regulated genes). This signature revealed...