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https://www.readbyqxmd.com/read/29775949/design-and-synthesis-of-some-new-carboxamide-and-propanamide-derivatives-bearing-phenylpyridazine-as-a-core-ring-and-the-investigation-of-their-inhibitory-potential-on-in-vitro-acetylcholinesterase-and-butyrylcholinesterase
#1
Burcu Kilic, Hayrettin O Gulcan, Fatma Aksakal, Tugba Ercetin, Nihan Oruklu, E Umit Bagriacik, Deniz S Dogruer
A series of new carboxamide and propanamide derivatives bearing phenylpyridazine as a core ring were designed, synthesized and evaluated for their ability to inhibit both cholinesterase enzymes. In addition, a series of carboxamide and propanamide derivatives bearing biphenyl instead of phenylpyridazine were also synthesized to examine the inhibitory effect of pyridazine moiety on both cholinesterase enzymes. The inhibitory activity results revealed that compounds 5b, 5f, 5h, 5j, 5l pyridazine-3-carboxamide derivative, exhibited selective acetylcholinesterase (AChE) inhibition with IC50 values ranging from 0...
May 8, 2018: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29775947/hit-optimization-studies-of-3-hydroxy-indolin-2-one-analogs-as-potential-anti-hiv-1-agents
#2
Subhash Chander, Cheng-Run Tang, Ashok Penta, Ping Wang, Deepak P Bhagwat, Nicolas Vanthuyne, Muriel Albalat, Payal Patel, Sanskruti Sankpal, Yong-Tang Zheng, Murugesan Sankaranarayanan
In the current study, twenty-two compounds based upon 3-hydroxy-3-(2-oxo-2-phenylethyl)indolin-2-one nucleus were designed, synthesized and in vitro evaluated for HIV-1 RT inhibition and anti-HIV-1 activity. Compounds 3d, 5c and 5e demonstrated encouraging potency against RT enzyme as well as HIV-1 in low micromolar to nanomolar concentration with good to excellent safety index. Structure activity relationship studies revealed that halogens such as bromo or chloro at 5th the position of oxindole ring remarkably enhanced the potency against RT...
May 9, 2018: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29775946/il-9-exhibits-elevated-expression-in-osteonecrosis-of-femoral-head-patients-and-promotes-cartilage-degradation-through-activation-of-jak-stat-signaling-in-vitro
#3
Wei Geng, Wen Zhang, Jinzhu Ma
Osteonecrosis of the femoral head (ONFH) often causes severe symptoms in young people and limits the mobility of the hip joint. Interleukin-9 (IL-9) is a multi-functional inflammatory factor that participates in lumbar disk herniation and arthritis and has been reported in many studies. However, the correlation between IL-9 and ONFH is unclear. The present study aimed to determine the role of IL-9 in the pathogenetic mechanism of osteonecrosis. To assess IL-9 expression in ONFH and femoral neck fracture patients, cartilage tissue was examined through western blot analysis and immunohistochemistry...
May 15, 2018: International Immunopharmacology
https://www.readbyqxmd.com/read/29775901/tricine-co-ligand-improved-the-efficacy-of-99m-tc-hynic-ser-3-j18-peptide-for-targeting-and-imaging-of-non-small-cell-lung-cancer
#4
Zahra Shaghaghi, Seyed Mohammad Abedi, Seyed Jalal Hosseinimehr
The early diagnosis of non-small cell lung cancer (NSCLC) is important for increasing survival rate and improving quality life of patients. The aim of this study was to investigate 99m  Tc-(tricine)-HYNIC-(Ser)3 -J18 for targeting and imaging of NSCLC in A-549 xenografted nude mice. The (Ser)3 -J18 peptide was conjugated with HYNIC and labeled with 99m  Tc using tricine as a co-ligand. The radiolabeled peptide was evaluated for its radiochemical purity, stability, receptor binding and internalization in vitro...
May 15, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29775898/particle-induced-sirt1-downregulation-promotes-osteoclastogenesis-and-osteolysis-through-er-stress-regulation
#5
Liang Zhang, Dongmei Bao, Peng Li, Zhidong Lu, Long Pang, Zhirong Chen, Haohui Guo, Zhihui Gao, Qunhua Jin
BACKGROUND: Sirtuin 1 (SIRT1) downregulation has been found to be induced by wear particles in aseptic prosthesis loosening (APL). Osteoclastogenesis and osteoclast activation are the main pathological factors associated with APL. However, whether SIRT1 downregulation contributes to the formation and activation of osteoclasts through the induction of endoplasmic reticulum (ER) stress is unclear. METHODS: To address this, an osteolysis mouse model was used in which animals were treated with the SIRT1 activator, resveratrol (RES), or an ER stress inhibitor, 4-PBA, for two weeks...
May 15, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29775894/positive-effects-of-antitumor-drugs-in-combination-with-propolis-on-canine-osteosarcoma-cells-spos-2-and-mesenchymal-stem-cells
#6
Pedro Negri Bernardino, Paulo Ricardo Oliveira Bersano, João Ferreira Lima Neto, José Maurício Sforcin
The combination of lower concentrations of antitumor drugs (carboplatin - CARB, doxorubicin - DOX, and methotrexate - MET) with propolis was investigated against canine osteosarcoma (spOS-2) and mesenchymal stem cells (MSC) in vitro. The mechanism of action in the combinations was analyzed. spOS-2 cells were incubated up to 72 h with propolis (50 μg/ml) alone or in combination with CARB (10-400 μmol/l), DOX (0.5-2 μmol/l) or MET (50-200 μmol/l). Cell viability was assessed by MTT assay, apoptosis/necrosis by flow cytometry, and MSC was incubated with the optimum combination...
May 15, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29775892/microrna-135a-inhibits-cardiac-fibrosis-induced-by-isoproterenol-via-trpm7-channel
#7
Yan Wu, Yonghui Liu, Yitong Pan, Chunxiao Lu, Haonan Xu, Xiaozhi Wang, Tingting Liu, Kai Feng, Yiqun Tang
BACKGROUND: Cardiac fibrosis is a crucial factor of heart failure. It has been reported that several microRNAs (miRNAs, miRs) were involved in cardiac fibrosis, however, the role and possible regulatory mechanism of microRNA-135a (miR-135a) in cardiac fibrosis have not been investigated. Here, we explored the regulation mechanism of miR-135a on cardiac fibrosis. METHODS AND RESULTS: In vitro, cardiac fibroblasts (CFs) from neonatal rats were treated by isoproterenol (ISO) at the final concentration of 10 μM for 24 h and miR-135a expression was decreased obviously...
May 15, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29775891/protective-effect-of-atorvastatin-meditated-by-hmgcr-gene-on-diabetic-rats-with-atherosclerosis-an-in-vivo-and-in-vitro-study
#8
Yong-Zhi Wang, Lei Yang, Chuan-Fang Li
BACKGROUND: Accelerated atherosclerosis in patients suffering from diabetes represents a major cause of morbidity and mortality. The aim of present study was to investigate the protective effects conferred by atorvastatin (AVT) meditated by the HMGCR gene in diabetic rats with atherosclerosis. METHODS: Serum triglyceride (TG), total cholesterol (TC), high-density lipoprotein cholesterol (HDL-C), low-density lipoprotein cholesterol (LDL-C), very-low-density lipoprotein cholesterol (VLDL-C), fasting blood glucose (FBG) and serum insulin (INS) were all determined by means of in vivo experiments...
May 15, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29775890/triterpenic-acids-enriched-fraction-from-cyclocarya-paliurus-attenuates-non-alcoholic-fatty-liver-disease-via-improving-oxidative-stress-and-mitochondrial-dysfunction
#9
Meng-Ge Zhao, Xue-Ping Sheng, Ya-Ping Huang, Yi-Ting Wang, Cui-Hua Jiang, Jian Zhang, Zhi-Qi Yin
The effects of triterpenic acids-enriched fraction from Cyclocarya paliurus (CPT) on nonalcoholic fatty liver disease (NAFLD) were investigated using in vivo and in vitro models. In high fat diet-induced Wister rats, CPT significantly increased superoxide dismutase (SOD) activity and glutathione/oxidized glutathione (GSH/GSSG) ratio, reduced malondialdehyde (MDA) and protein carbonyl (PCO) levels. Moreover, CPT restored mitochondrial membrane potential dysfunction, decreased cytochrome P450 enzyme 2E1 (CYP2E1) activity, improved nuclear factor erythroid 2-related factor 2 (Nrf2) and Nrf2-mediated antioxidant enzyme heme oxygenase1 (HO-1) expression...
May 15, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29775889/lncrna-mir22hg-negatively-regulates-mir-141-3p-to-enhance-dapk1-expression-and-inhibits-endometrial-carcinoma-cells-proliferation
#10
Zhili Cui, Xin An, Jingxia Li, Qiaozhen Liu, Wenli Liu
Emerging evidence has indicated that long non-coding RNAs (lncRNAs) play critical roles in tumor development and progression. Recent studies reported that lncRNA MIR22HG could play important roles in hepatocellular carcinoma and lung cancer progression. However, the expression and underlying mechanism of MIR22HG in endometrial cancer (EC) remain unclear. In the present study, qRT-PCR showed that MIR22HG expression was significantly downregulated in EC tissues. In vitro function assays showed that increased MIR22HG expression significantly inhibited EC cells proliferation, induced EC cells apoptosis, and arrested EC cells in G0/G1 phase...
May 15, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29775866/identification-of-udp-glucosyltransferases-from-the-aluminum-resistant-tree-eucalyptus-camaldulensis-forming-%C3%AE-glucogallin-the-precursor-of-hydrolyzable-tannins
#11
Ko Tahara, Mitsuru Nishiguchi, Andrej Frolov, Juliane Mittasch, Carsten Milkowski
In the highly aluminum-resistant tree Eucalyptus camaldulensis, hydrolyzable tannins are proposed to play a role in internal detoxification of aluminum, which is a major factor inhibiting plant growth on acid soils. To understand and modulate the molecular mechanisms of aluminum detoxification by hydrolyzable tannins, the biosynthetic genes need to be identified. In this study, we identified and characterized genes encoding UDP-glucose:gallate glucosyltransferase, which catalyzes the formation of 1-O-galloyl-β-d-glucose (β-glucogallin), the precursor of hydrolyzable tannins...
May 15, 2018: Phytochemistry
https://www.readbyqxmd.com/read/29775846/reproductive-stage-and-sex-steroid-hormone-levels-influence-the-expression-of-mesenchymal-stromal-cell-msc-markers-in-the-equine-endometrium
#12
B Elisabeth Rink, Juliane Kuhl, Cristina L Esteves, Hilari M French, Elaine Watson, Christine Aurich, F Xavier Donadeu
Mesenchymal stem or stromal cells (MSCs) play key roles in tissue homeostasis. In the cyclic equine endometrium, this may be regulated by changes in serum concentrations of sex steroid hormones. This study was designed to investigate the changes in endometrial expression of MSC markers during reproductive cycles in mares and the influence of sex steroid hormones on endometrial MSC proliferation in vitro. Endometrial biopsies were collected from pony mares at different reproductive stages (estrus; day 5 and 13 after ovulation; seasonal anestrus; 20 h and 7days post-partum; n = 5 per stage) and were analyzed by RT-qPCR...
May 4, 2018: Theriogenology
https://www.readbyqxmd.com/read/29775835/analysis-of-the-cytotoxic-effects-of-combined-ultrasound-microbubble-and-nucleoside-analog-combinations-on-pancreatic-cells-in-vitro
#13
Julia Mariglia, Shadab Momin, Imogen R Coe, Raffi Karshafian
Ultrasonically-stimulated microbubbles enhance the therapeutic effects of various chemotherapy drugs. However, the application of ultrasound and microbubbles (USMB) for enhancing the therapeutic effect of nucleoside analogs, which are used as front-line treatments in a range of cancers, and its underlying mechanism is not well understood. This study investigated the effect of gemcitabine, a nucleoside analog drug, in combination with USMB in increasing cell cytotoxicity relative to either treatment alone in BxPC3 pancreatic cancer cells...
May 5, 2018: Ultrasonics
https://www.readbyqxmd.com/read/29775819/facile-synthesis-of-yolk-shell-structured-monodisperse-mesoporous-organosilica-nanoparticles-by-a-mild-alkalescent-etching-approach
#14
Jun Tao, Meng Dang, Xiaodan Su, Qing Hao, Junjie Zhang, Xiaobo Ma, Guangming Lu, Yunlei Zhang, Ying Tian, Lixing Weng, Zhaogang Teng, Lianhui Wang
In the work, yolk-shell structured mesoporous organosilica nanoparticles (YSMONs) are successfully prepared by a mild alkalescent etching approach. The method is very convenient, in which mesostructured organosilica nanospheres are directly transformed into yolk-shell structures after etching with mild alkalescent solution (e.g. sodium carbonate solution). The prepared YSMONs have ethane-bridged frameworks, a monodisperse diameter (320 nm), a large pore volume (1.0 cm3  g-1 ), a uniform mesopore (2.4 nm) and a high surface area (1327 m2  g-1 )...
May 15, 2018: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/29775778/the-genus-cordyceps-an-extensive-review-of-its-traditional-uses-phytochemistry-and-pharmacology
#15
REVIEW
Opeyemi Joshua Olatunji, Jian Tang, Adesola Tola, Florence Auberon, Omolara Oluwaniyi, Zhen Ouyang
The genus Cordyceps has about 750 identified species which are distributed in many regions of the World, but mainly found in South Asia, Europe and North America. The species of the genus are highly priced and are widely used as food and medicine for the treatment of various ailments. This present review compiles literature information on the ethno-medicinal, phytochemistry and pharmacological properties of species in the genus Cordyceps. In addition, the review also suggest recommendations for the future researches...
May 15, 2018: Fitoterapia
https://www.readbyqxmd.com/read/29775748/microrna-204-5p-regulates-3t3-l1-preadipocyte-proliferation-apoptosis-and-differentiation
#16
Jingjing Du, Peiwen Zhang, Mailin Gan, Xue Zhao, Yan Xu, Qiang Li, Yanzhi Jiang, Guoqing Tang, Mingzhou Li, Jinyong Wang, Xuewei Li, Shunhua Zhang, Li Zhu
Obesity due to excessive lipid accumulation is closely associated with metabolic diseases such as type 2 diabetes, insulin resistance and inflammation. Therefore, a detailed understanding of the molecular mechanisms that underlie adipogenesis is crucial to develop treatments for diseases related to obesity. Here, we found that the microRNA-204-5p (miR-204-5p) was expressed at low levels in fat tissues from obese mice fed long-term with a high-fat diet (HFD). Overexpression or inhibition of miR-204-5p in vitro in 3T3-L1 preadipocytes significantly inhibited or promoted 3T3-L1 proliferation, respectively, an effect mediated by regulating cell proliferation factors...
May 15, 2018: Gene
https://www.readbyqxmd.com/read/29775739/effects-of-environmental-factors-on-c-type-lectin-recognition-to-zooxanthellae-in-the-stony-coral-pocillopora-damicornis
#17
Zhi Zhou, Shuimiao Zhao, Junyi Ni, Yilu Su, Lingui Wang, Yanlai Xu
C-type lectin is a superfamily of Ca2+ -dependent carbohydrate-recognition proteins that play significant roles in nonself-recognition and pathogen clearance. In the present study, a C-type lectin (PdC-Lectin) was chosen from stony coral Pocillopora damicornis to understand its recognition characteristics to zooxanthellae. PdC-Lectin protein contained a signal peptide and a carbohydrate-recognition domain with EPN motif in Ca2+ -binding site 2. The PdC-Lectin recombinant protein was expressed and purified in vitro...
May 15, 2018: Fish & Shellfish Immunology
https://www.readbyqxmd.com/read/29775732/il4-10-fusion-protein-has-chondroprotective-anti-inflammatory-and-potentially-analgesic-effects-in-the-treatment-of-osteoarthritis
#18
C Steen-Louws, J Popov-Celeketic, S C Mastbergen, K Coeleveld, C E Hack, N Eijkelkamp, M Tryfonidou, S Spruijt, J A G van Roon, F P J G Lafeber
OBJECTIVE: Effective disease-modifying drugs for osteoarthritis (DMOAD) should preferably have chondroprotective, anti-inflammatory, and analgesic activity combined in a single molecule. We developed a fusion protein of IL4 and IL10 (IL4-10 FP), in which the biological activity of both cytokines is preserved. The present study evaluates the chondroprotective, anti-inflammatory, and analgesic activity of IL4-10 FP in in vitro and in vivo models of osteoarthritis. METHODS: Human osteoarthritic cartilage tissue and synovial tissue were cultured with IL4-10 FP...
May 15, 2018: Osteoarthritis and Cartilage
https://www.readbyqxmd.com/read/29775731/targeted-and-controlled-drug-delivery-by-multifunctional-mesoporous-silica-nanoparticles-with-internal-fluorescent-conjugates-and-external-polydopamine-and-graphene-oxide-layers
#19
Anh-Vy Tran, KyuHwan Shim, Thu-Thao Vo Thi, Jeong-Keun Kook, Seong Soo A An, Sang-Wha Lee
This study demonstrated the targeted delivery and controlled release of cisplatin drug molecules from doubly decorated mesoporous silica nanoparticles (MSNs), which were internally grafted with fluorescent conjugates and externally coated with polydopamine (PDA) and graphene oxide (GO) layers. The brush-like internal conjugates conferred fluorescent functionality and high capacity of cisplatin loading into MSNs, as well as contributing to a sustained release of the cisplatin through a porous channel with the assistance of external PDA layer...
May 15, 2018: Acta Biomaterialia
https://www.readbyqxmd.com/read/29775730/an-integrated-biomanufacturing-platform-for-the-large-scale-expansion-and-neuronal-differentiation-of-human-pluripotent-stem-cell-derived-neural-progenitor-cells
#20
Gayathri Srinivasan, Daylin Morgan, Divya Varun, Nicholas Brookhouser, David A Brafman
Human pluripotent stem cell derived neural progenitor cells (hNPCs) have the unique properties of long-term in vitro expansion as well as differentiation into the various neurons and supporting cell types of the central nervous system (CNS). Because of these characteristics, hNPCs have tremendous potential in the modeling and treatment of various CNS diseases and disorders. However, expansion and neuronal differentiation of hNPCs in quantities necessary for these applications is not possible with current two dimensional (2-D) approaches...
May 15, 2018: Acta Biomaterialia
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