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https://www.readbyqxmd.com/read/28212338/synthesis-and-antitumor-activities-of-chiral-dipeptide-thioureas-containing-an-alpha-aminophosphonate-moiety
#1
Jingzi Liu, Peng Liao, Junfeng Hu, Hong Zhu, Yonglin Wang, Yongjun Li, Yan Li, Bin He
Thiourea derivatives demonstrate potent cytotoxic activity against various leukemias and many tumor cell lines. In our previous study, the combination of thiourea and phosphonate has been proven as an effective strategy for developing antitumor agents. Herein, we synthesized and evaluated a series of novel chiral dipeptide thioureas containing an α-aminophosphonate moiety as antitumor agents. Finally, we developed novel dipeptide thioureas 11d and 11f that showed comparable inhibition with that of Cisplatin against BGC-823 and A-549 cells, respectively...
February 16, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28211011/teoa-a-triterpenoid-from-actinidia-eriantha-induces-autophagy-in-sw620-cells-via-endoplasmic-reticulum-stress-and-ros-dependent-mitophagy
#2
Dandan Zhang, Cuixia Gao, Ruyi Li, Lin Zhang, Jingkui Tian
2α,3α,24-Thrihydroxyurs-12-en-28-oicacid (TEOA), a pentacyclic triterpenoid, isolated from the roots of Actinidia eriantha, exhibits significant cytotoxicity against SW620, BGC-823, HepG-2, A549 and PC-3 cancer cells. In this study, we investigated the underlying molecular mechanism of the anticancer activity of TEOA in SW620 cells. We demonstrated that TEOA induced apoptosis through cleavage of caspase-9 and PARP in SW620 cells. In addition, evidence of TEOA-mediated autophagy included the induction of autophagolysosomes and activation of autophagic markers LC-3B and p62...
February 16, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28209093/two-new-cytotoxic-glycosides-isolated-from-the-green-walnut-husks-of-juglans-mandshurica-maxim
#3
Yuan-Yuan Zhou, Quan-Yu Liu, Bing-You Yang, Yan-Qiu Jiang, Yu-Xin Liu, Ying Wang, Shuang Guo, Haixue Kuang
Two new glycosides including an alcohol glycoside and a phenolic glycoside: hexyl-1-O-α-d-arabinofuranosyl-(1 → 6)-β-d-glucopyranoside (1), 4-hydroxypropiophenone-4-O-β-d-glucopyranosyl(1 → 6)-β-d-glucopyranoside(2), along with six known naphthalenyl glucosides (3-8) were isolated from green walnut husks of Juglans mandshurica, and their structures were elucidated on the basis of spectroscopic studies. All compounds were evaluated for their inhibitory effects on tumour cells (BGC-823, HepG-2, MCF-7)...
June 2017: Natural Product Research
https://www.readbyqxmd.com/read/28208606/ustiloxin-g-a-new-cyclopeptide-mycotoxin-from-rice-false-smut-balls
#4
Xiaohan Wang, Jian Wang, Daowan Lai, Weixuan Wang, Jungui Dai, Ligang Zhou, Yang Liu
Ustiloxins were cyclopeptide mycotoxins from rice false smut balls (FSBs) that formed in rice spikelets infected by the fungal pathogen Ustilaginoidea virens. To investigate the chemical diversity of these metabolites and their bioactivities, one new cyclopeptide, ustiloxin G (1), together with four known congeners-ustiloxins A (2), B (3), D (4), and F (5)-were isolated from water extract of rice FSBs. Their structures were elucidated by analyses of their physical and spectroscopic data, including ultraviolet spectrometry (UV), infrared spectroscopy (IR), 1D and 2D nuclear magnetic resonance (NMR), and high-resolution electrospray ionization-mass spectrometry (HR-ESI-MS)...
February 10, 2017: Toxins
https://www.readbyqxmd.com/read/28197324/-125-i-f56-peptide-as-radioanalysis-agent-targeting-vegfr1-in-mice-xenografted-with-human-gastric-tumor
#5
Hua Zhu, Chuanke Zhao, Fei Liu, Lixin Wang, Junnan Feng, Chengchao Shou, Zhi Yang
(125)I-Radiolabeled F56 peptide was designed as a radioactive analogue of F56 (peptide WHSDMEWWYLLG) to bind with VEGFR1 receptor. It was synthesized in high radiochemical yield and specific activity. The in vitro stability of (125)I-F56 was tested, and the bioactivity of (125)I-F56 was confirmed by both cell uptake and binding affinity measurement in VEGFR1 positive BGC-823 cells. The time-radioactivity relationship and biodistribution of (125)I-F56 tracer were conducted using nude mice bearing human gastric carcinoma BGC-823, by noninvasive micro-SPECT/CT imaging...
February 9, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28196062/elemene-induces-apoptosis-of-human-gastric-cancer-cell-line-bgc-823-via-extracellular-signal-regulated-kinase-erk-1-2-signaling-pathway
#6
Pihong Li, Xiang Zhou, Weijian Sun, Weiwei Sheng, Yangyang Tu, Yaojun Yu, Jianda Dong, Bing Ye, Zhiqiang Zheng, Mingdong Lu
BACKGROUND Elemene is extracted from a traditional herbal medicine and is commonly used in the treatment of cancer in China. However, its effect on gastric cancer cells remains unknown. The goal of this study was to investigate its effect on human gastric cancer cells. MATERIAL AND METHODS Human gastric cancer BGC-823 cells and a tumor-bearing mouse model were employed to be divided into 4 groups: control group, elemene group, PD98059 group (an ERK 1/2 signaling pathway inhibitor), and the combined group (elemene plus PD98059)...
February 14, 2017: Medical Science Monitor: International Medical Journal of Experimental and Clinical Research
https://www.readbyqxmd.com/read/28159956/microrna-495-inhibits-gastric-cancer-cell-migration-and-invasion-possibly-via-targeting-high-mobility-group-at-hook-2-hmga2
#7
Huashe Wang, Zhipeng Jiang, Honglei Chen, Xiaobin Wu, Jun Xiang, Junsheng Peng
BACKGROUND Gastric cancer is one of the most common malignancies, and has a high mortality rate. miR-495 acts as a suppressor in some cancers and HMGA2 (high mobility group AT-hook 2) is a facilitator for cell growth and epithelial-mesenchymal transition (EMT), but little is known about their effect in gastric cancer. This study aimed to investigate the role and mechanism of miR-495 in gastric cancer. MATERIAL AND METHODS miR-495 levels were quantitatively analyzed in gastric cancer tissue and GES-1, SGC-7901, BGC-823, and HGC-27 cell lines by qRT-PCR...
February 4, 2017: Medical Science Monitor: International Medical Journal of Experimental and Clinical Research
https://www.readbyqxmd.com/read/28155603/advances-in-chemistry-and-pharmacology-of-triterpenoid-synthetic-dimers
#8
Barbara Bednarczyk-Cwynar, Andrzej Günther
The publication focuses on advances in chemistry and pharmacology of synthetic triterpenoid dimers, obtained from natural compounds. Synthetic triterpenoid dimers were divided into specific subgroups basing on the structure of main triterpenoid monomeric skeleton. Synthetic triterpenoid derivatives of dimeric structure can be obtained through the covalent linkage of the C-3 hydroxyl or another group, via the C-2 atom or the C-17 carboxyl group (mainly anhydrides, amides or esters). Some triterpenes can undergo chemical transformations leading to the formation of cyclic dimers or other types of dimers...
February 2, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28137630/aristolochic-acid-derivatives-from-the-rhizome-of-arisolochia-championii
#9
Xin Wang, Guo-Ru Shi, Yan-Fei Liu, Li Li, Ruo-Yun Chen, De-Quan Yu
Four new aristolochic acid derivatives aristchamic A (1), aristchamic B (2), aristochamic C (3a), aristchamic D (3b) and one new aristolactam aristolactam-CV (4), together with 10 known compounds (5-14), were isolated from the rhizomes of Aristolochia championii. Their structures were assigned by detailed analysis of MS and NMR spectroscopic data. All of the isolated compounds were evaluated for their cytotoxic activities against HCT-116, HepG2, BGC-823, NCI-H1650, and A2780 cell. Compound 1 exhibited significant cytotoxic activity against HCT-116, HepG2, BGC-823, and NCI-H1650, with IC50 values of 0...
January 27, 2017: Fitoterapia
https://www.readbyqxmd.com/read/28132880/pseudolaric-acid-b-inhibits-gastric-cancer-cell-metastasis-in-vitro-and-in-haematogenous-dissemination-model-through-pi3k-akt-erk1-2-and-mitochondria-mediated-apoptosis-pathways
#10
Dan Wang, Yan Xin, Yanqiu Tian, Wenhui Li, Dan Sun, Yi Yang
Pseudolaric acid B (PAB) is the major bioactive constituent in the root bark of Pseudolarix kaempferi and has been reported to have cytotoxicity against tumor cells. Our in vivo experiments showed that PAB could inhibit gastric cancer cell lung metastasis in a nude mouse haematogenous dissemination model. To evaluate the anti-metastasis mechanism of PAB in gastric cancer cells, cytological experiments were performed. The results showed that PAB could inhibit the adhesion ability to matrigel, migration, invasion and colony formation ability of BGC-823 and MKN-45 cells...
January 26, 2017: Experimental Cell Research
https://www.readbyqxmd.com/read/28125959/assessing-in-silico-the-recruitment-and-functional-spectrum-of-bacterial-enzymes-from-secondary-metabolism
#11
Valery Veprinskiy, Leonhard Heizinger, Maximilian G Plach, Rainer Merkl
BACKGROUND: Microbes, plants, and fungi synthesize an enormous number of metabolites exhibiting rich chemical diversity. For a high-level classification, metabolism is subdivided into primary (PM) and secondary (SM) metabolism. SM products are often not essential for survival of the organism and it is generally assumed that SM enzymes stem from PM homologs. RESULTS: We wanted to assess evolutionary relationships and function of bona fide bacterial PM and SM enzymes...
January 26, 2017: BMC Evolutionary Biology
https://www.readbyqxmd.com/read/28116768/acyl-histidines-new-n-acyl-amides-from-legionella-pneumophila
#12
Thomas Tørring, Stephanie R Shames, Wooyoung Cho, Craig R Roy, Jason Crawford
Legionella pneumophila, the causative agent of Legionnaire's disease, is a Gram-negative Gammaproteobacterial pathogen that infects and intracellularly replicates in a variety of protozoa and in human macrophages. L. pneumophila encodes an orphan biosynthetic gene cluster (BGC) that contains isocyanide-associated biosynthetic genes and is upregulated during infection. Because isocyanide-functionalized metabolites are known to harbor invertebrate innate immunosuppressive activities in bacterial pathogen-insect interactions, we used pathway-targeted molecular networking and tetrazine-based chemoseletive ligation chemistry to characterize the metabolites from the orphan pathway in L...
January 23, 2017: Chembiochem: a European Journal of Chemical Biology
https://www.readbyqxmd.com/read/28113080/microrna-200c-binding-to-fn1-suppresses-the-proliferation-migration-and-invasion-of-gastric-cancer-cells
#13
Hengchun Zhang, Zhiguo Sun, Yan Li, Dong Fan, Hao Jiang
We aimed to investigate the effects of miR-200c binding to fibronectin 1 (FN1) on proliferation, migration and invasion of gastric cancer (GC) cells. A total of 52 GC tissues and their corresponding normal adjacent tissue samples were collected. Then, miR-200c and FN1 were tested using quantitative real-time RT-PCR in the clinical specimens and GC cells, while immunohistochemistry and western blotting assay were carried out to detect FN1 expressions. Dual luciferase reporter gene assay was used to assess the effect of miR-200c on the luciferase activity of FN1 3'UTR...
January 20, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28108499/relay-balloon-technique-for-recanalization-of-acute-symptomatic-proximal-internal-carotid-artery-occlusion-with-short-balloon-tipped-guiding-catheter-landing-zone
#14
Sang Hun Lee, Dong Geun Lee, Sun U Kwon, Deok Hee Lee
BACKGROUND: Endovascular recanalization of a completely occluded proximal internal carotid artery (ICA) with underlying stenosis may be challenging owing to a possible thrombotic component. This is especially true when the landing zone for a balloon-tipped guiding catheter (BGC) at the bulb portion is insufficient. Sequential application of the balloons of a BGC and an angioplasty catheter may prevent thromboembolism during revascularization. This study analyzed the safety and effectiveness of this relay-balloon technique...
January 20, 2017: Journal of Neurointerventional Surgery
https://www.readbyqxmd.com/read/28107526/rab14-act-as-oncogene-and-induce-proliferation-of-gastric-cancer-cells-via-akt-signaling-pathway
#15
Bo Guo, Wenjing Wang, Zhenghao Zhao, Qian Li, Kaiyue Zhou, Lingyu Zhao, Lumin Wang, Juan Yang, Chen Huang
Rab14 is a member of RAS oncogene family, and its dysfunction has been reported to be involved in various types of human cancer. However, its expression and function were still unclear in gastric cancer. The aim of this study was to investigate the function and mechanism of Rab14 in gastric cancer cell lines. Quantitative real-time PCR (qRT-PCR) was performed in 17 gastric adenocarcinoma tissues and 4 cell lines to detect the expression of Rab14. 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyl-tetrazolium bromide (MTT), colony formation and flow cytometry assays were employed to determine the proliferative ability, cell cycle transition and apoptosis in vitro in BGC-823 or SGC-7901 cells...
2017: PloS One
https://www.readbyqxmd.com/read/28100567/mecp2-regulated-glycogenes-contribute-to-proliferation-and-apoptosis-of-gastric-cancer-cells
#16
Yannan Qin, Lingyu Zhao, Xiaofei Wang, Dongdong Tong, Christopher Hoover, Fei Wu, Yingxun Liu, Lumin Wang, Liying Liu, Lei Ni, Tusheng Song, Chen Huang
Aberrant glycogene and glycan expression is intimately associated with carcinogenesis, invasion, and metastasis of gastric cancer (GC); however the regulatory mechanisms for glycogenes in GC cells remain unclear. Methyl-CpG-binding protein 2 (MeCP2) regulates genes by binding to methylated promoters, and in our previous work we found that it is overexpressed in GC cell lines and tissues, functioning as an oncogene. In this study we detected the expression of 212 glycogenes in MeCP2 silenced GC cells versus control using the Agilent Whole Human Genome Microarray and mining the data through bioinformatic analysis...
January 18, 2017: Glycobiology
https://www.readbyqxmd.com/read/28099141/antitumor-activity-of-a-trans-thiosemicarbazone-schiff-base-palladium-ii-complex-on-human-gastric-adenocarcinoma-cells
#17
Bingchang Zhang, Haiqing Luo, Qinjuan Xu, Lirong Lin, Bing Zhang
The development of transition-metal-based antitumor drug candidates increases the metallopharmaceuticals study dramatically. Two trans-thiosemicarbazone-based, Schiff base palladium (Pd) (II) complexes, DMABTSPd (TSPd) and DMABPTSPd (PTSPd), were prepared and characterized as described in our previous study. Here, we investigated whether the two complexes have antitumor effect on human gastric adenocarcinoma cell lines, BGC-823 and SGC-7901, compared with normal human gastric mucosal epithelial cell line, Ges-1...
January 13, 2017: Oncotarget
https://www.readbyqxmd.com/read/28092748/optimizing-selective-cutting-strategies-for-maximum-carbon-stocks-and-yield-of-moso-bamboo-forest-using-biome-bgc-model
#18
Fangjie Mao, Guomo Zhou, Pingheng Li, Huaqiang Du, Xiaojun Xu, Yongjun Shi, Lufeng Mo, Yufeng Zhou, Guoqing Tu
The selective cutting method currently used in Moso bamboo forests has resulted in a reduction of stand productivity and carbon sequestration capacity. Given the time and labor expense involved in addressing this problem manually, simulation using an ecosystem model is the most suitable approach. The BIOME-BGC model was improved to suit managed Moso bamboo forests, which was adapted to include age structure, specific ecological processes and management measures of Moso bamboo forest. A field selective cutting experiment was done in nine plots with three cutting intensities (high-intensity, moderate-intensity and low-intensity) during 2010-2013, and biomass of these plots was measured for model validation...
January 13, 2017: Journal of Environmental Management
https://www.readbyqxmd.com/read/28088540/multiplexed-site-specific-genome-engineering-for-overproducing-bioactive-secondary-metabolites-in-actinomycetes
#19
Lei Li, Guosong Zheng, Jun Chen, Mei Ge, Weihong Jiang, Yinhua Lu
Actinomycetes produce a large variety of pharmaceutically active compounds, yet production titers often require to be improved for discovery, development and large-scale manufacturing. Here, we describe a new technique, multiplexed site-specific genome engineering (MSGE) via the 'one integrase-multiple attB sites' concept, for the stable integration of secondary metabolite biosynthetic gene clusters (BGCs). Using MSGE, we achieved five-copy chromosomal integration of the pristinamycin II (PII) BGC in Streptomyces pristinaespiralis, resulting in the highest reported PII titers in flask and batch fermentations (2...
January 11, 2017: Metabolic Engineering
https://www.readbyqxmd.com/read/28073676/sulfamic-and-succinic-acid-derivatives-of-25-oh-ppd-and-their-activities-to-mcf-7-a-549-hct-116-and-bgc-823-cell-lines
#20
Wu-Xi Zhou, Jia-Qing Cao, Xu-De Wang, Jun-Hui Guo, Yu-Qing Zhao
In the search for new anti-tumor agents with higher potency than our previously identified compound 1 (25-OH-PPD, 25-hydroxyprotopanaxadiol), 12 novel sulfamic and succinic acid derivatives that could improve water solubility and contribute to good drug potency and pharmacokinetic profiles were designed and synthesized. Their in vitro anti-tumor activities in MCF-7, A-549, HCT-116, and BGC-823 cell lines and one normal cell line were tested by standard MTT assay. Results showed that compared with compound 1, compounds 2, 3, and 7 exhibited higher cytotoxic activity on A-549 and BGC-823 cell lines, together with lower toxicity in the normal cell...
December 21, 2016: Bioorganic & Medicinal Chemistry Letters
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