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https://read.qxmd.com/read/30785464/a-concise-synthesis-and-biological-study-of-evodiamine-and-its-analogues
#1
Jie-Dan Deng, Shuai Lei, Yi Jiang, Hong-Hua Zhang, Xiao-Ling Hu, Huai-Xiu Wen, Wen Tan, Zhen Wang
Efficient access to evodiamine and its analogues is presented via Lewis acid catalysis. In this reaction, three chemical bonds and two heterocyclic-fused rings are constructed in one step. The reaction shows good functional group tolerance and atom economy, and various heteroatom-containing evodiamine analogues are obtained in moderate to excellent yields even on a gram scale. An anti-tumor study in vitro demonstrates compound 2b possesses potent efficacy against hepatoma cell line (IC50 = 5.7 μM).
February 20, 2019: Chemical Communications: Chem Comm
https://read.qxmd.com/read/30784920/bone-marrow-mesenchymal-stem-cells-suppress-growth-and-promote-the-apoptosis-of-glioma-u251-cells-through-downregulation-of-the-pi3k-akt-signaling-pathway
#2
Li Lu, Guohu Chen, Jingjing Yang, Zhanjun Ma, Yang Yang, Yan Hu, Yubao Lu, Zhangqi Cao, Yan Wang, Xuexi Wang
Mesenchymal stem cells (MSCs), with the capacity for self-renewal and differentiation into multiple cell types, exhibit the property of homing towards tumor sites and immunosuppression and have been used as tumor-tropic vectors for tumor therapy. However, few studies have investigated the underlying molecular mechanisms that link MSCs to targeted tumor cells. In this study, we elucidated the inhibitory effects and mechanisms of human bone marrow mesenchymal stem cells (hBMSCs) on human glioma U251 cells using a co-culture system in vitro...
February 19, 2019: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://read.qxmd.com/read/30784091/sirtuin-6-mitigated-lps-induced-human-umbilical-vein-endothelial-cells-inflammatory-responses-through-modulating-nuclear-factor-erythroid-2-related-factor-2
#3
Yi Qin, Lirong Cao, Lili Hu
BACKGROUND: Nuclear factor erythroid 2-related factor 2 (Nrf2) protects the lung from sepsis-induced injury through activating Nrf2-regulated multiple phase 2 detoxification genes, including NAD(P)H: quinine oxidoreductase-1 (NQO1) and heme oxygenase-1 (HO1). Based on the positive effect of Sirtuin 6 on Nrf2, we aim to explore the potential role of SIRT6 in the mechanism of sepsis-induced acute lung injury (ALI). METHODS: Mouse models of sepsis were constructed by instilling intratracheal of lipopolysaccharide (LPS; 4 ml/kg)...
February 19, 2019: Journal of Cellular Biochemistry
https://read.qxmd.com/read/30783440/regulation-of-tgf-%C3%AE-1-on-pi3kc3-and-its-role-in-hypertension-induced-vascular-injuries
#4
Qin Zhang, Hu Liu, Jun Yang
The aim of the present study was to investigate the expression and role of transforming growth factor (TGF)-β1/phosphatidylinositol 3-kinase catalytic subunit type 3 (PI3KC3) in the peripheral blood in patients with hypertension. A total of 28 patients with primary hypertension and 20 healthy control subjects were included. Peripheral blood samples were collected. The mRNA and protein expression levels were detected by reverse transcription-quantitative polymerase chain reaction and western blot analysis, respectively...
March 2019: Experimental and Therapeutic Medicine
https://read.qxmd.com/read/30783421/protective-effect-of-xin-ji-er-kang-on-cardiovascular-remodeling-in-high-salt-induced-hypertensive-mice
#5
Guangyao Huang, Pan Cheng, Ling Ding, Li Wang, Juan Hu, Yongxue Zhang, Guowei Cai, Meiling Chen, Aizong Shen, Shan Gao
The aim of the present study was to investigate the effects of Xin-Ji-Er-Kang (XJEK) on high salt-induced hypertensive mice. Mice with high-salt diet-induced hypertension were divided into four groups: Control (standard diet alone for 8 weeks), model (diet containing 8% NaCl for 8 weeks and intragastric administration of distilled water for the last 4 weeks), XJEK + high-salt-treated (diet containing 8% NaCl for 8 weeks and intragastric administration of XJEK for the last 4 weeks) and irbesartan + high-salt-treated (diet containing 8% NaCl for 8 weeks with intragastric administration of irbesartan for the last 4 weeks)...
March 2019: Experimental and Therapeutic Medicine
https://read.qxmd.com/read/30783116/the-flavonoid-4-4-dimethoxychalcone-promotes-autophagy-dependent-longevity-across-species
#6
Didac Carmona-Gutierrez, Andreas Zimmermann, Katharina Kainz, Federico Pietrocola, Guo Chen, Silvia Maglioni, Alfonso Schiavi, Jihoon Nah, Sara Mertel, Christine B Beuschel, Francesca Castoldi, Valentina Sica, Gert Trausinger, Reingard Raml, Cornelia Sommer, Sabrina Schroeder, Sebastian J Hofer, Maria A Bauer, Tobias Pendl, Jelena Tadic, Christopher Dammbrueck, Zehan Hu, Christoph Ruckenstuhl, Tobias Eisenberg, Sylvere Durand, Noélie Bossut, Fanny Aprahamian, Mahmoud Abdellatif, Simon Sedej, David P Enot, Heimo Wolinski, Jörn Dengjel, Oliver Kepp, Christoph Magnes, Frank Sinner, Thomas R Pieber, Junichi Sadoshima, Natascia Ventura, Stephan J Sigrist, Guido Kroemer, Frank Madeo
Ageing constitutes the most important risk factor for all major chronic ailments, including malignant, cardiovascular and neurodegenerative diseases. However, behavioural and pharmacological interventions with feasible potential to promote health upon ageing remain rare. Here we report the identification of the flavonoid 4,4'-dimethoxychalcone (DMC) as a natural compound with anti-ageing properties. External DMC administration extends the lifespan of yeast, worms and flies, decelerates senescence of human cell cultures, and protects mice from prolonged myocardial ischaemia...
February 19, 2019: Nature Communications
https://read.qxmd.com/read/30781382/daphnetin-a-novel-anti-helicobacter-pylori-agent
#7
Genzhu Wang, Jing Pang, Xinxin Hu, Tongying Nie, Xi Lu, Xue Li, Xiukun Wang, Yun Lu, Xinyi Yang, Jiandong Jiang, Congran Li, Yan Q Xiong, Xuefu You
BACKGROUND: Antibiotic-resistant H. pylori was increasingly found in infected individuals, which resulted in treatment failure and required alternative therapeutic strategies. Daphnetin, a coumarin-derivative compound, has multiple pharmacological activities. METHODS: The mechanism of daphnetin on H. pylori was investigated focusing on its effect on cell morphologies, transcription of genes related to virulence, adhesion, and cytotoxicity to human gastric epithelial (GES-1) cell line...
February 15, 2019: International Journal of Molecular Sciences
https://read.qxmd.com/read/30779911/mir-1247-3p-mediates-apoptosis-of-cerebral-neurons-by-targeting-caspase-2-in-stroke
#8
Rong Zhang, Weipin Zhou, Zhijun Yu, Ling Yang, Guangqi Liu, Haotian Yu, Qianyi Zhou, Zhenli Min, Chunxiang Zhang, Qingming Wu, Xia-Min Hu, Qiong Yuan
Brain stroke is one of the leading causes of death worldwide. We explored a potential stroke-related role for a newly found microRNA, miR-1247-3p, and one of its target genes, caspase-2, predicted by TargetScanVert. In the present study, we found that miR-1247-3p was downregulated during ischemia/reperfusion (I/R) and that LV-miR-1247-3p overexpression attenuated brain impairment induced by I/R. Similar results were observed in neuro2a (N2a) cells treated with oxygen-glucose deprivation/reoxygenation (OGD/R)...
February 16, 2019: Brain Research
https://read.qxmd.com/read/30778296/the-genus-adonis-as-an-important-cardiac-folk-medicine-a-review-of-the-ethnobotany-phytochemistry-and-pharmacology
#9
REVIEW
Xiaofei Shang, Xiaolou Miao, Feng Yang, Chunmei Wang, Bing Li, Weiwei Wang, Hu Pan, Xiao Guo, Yu Zhang, Jiyu Zhang
The genus Adonis L. (Ranunculaceae), native to Europe and Asia, comprises 32 annual or perennial herbaceous species. Due to their cardiac-enhancing effects, Adonis spp. have long been used in European and Chinese folk medicine. These plants have been widely investigated since the late 19th century, when the cardiovascular activity of Adonis vernalis L. was noted in Europe. The present paper provides a review of the phytochemistry, biological activities and toxicology in order to highlight the future prospects of the genus...
2019: Frontiers in Pharmacology
https://read.qxmd.com/read/30777660/dual-inhibitors-of-raf-mek-erk-and-pi3k-pdk1-akt-pathways-design-synthesis-and-preliminary-anticancer-activity-studies-of-3-substituted-5-phenylamino-indolone-derivatives
#10
Zutao Yu, Zhuo Chen, Qiongli Su, Shiqi Ye, Hongbo Yuan, Mengni Kuai, Meng Lv, Zhijun Tu, Xiaoping Yang, RangRu Liu, Gaoyun Hu, Qianbin Li
The dysfunction and mutual compensatory activation of RAF-MEK-ERK and PI3K-PDK1-AKT pathways have been demonstrated as the hallmarks in several primary and recurrent cancers. The strategy of concurrent blocking of these two pathways shows clinical merits on effective cancer therapy, such as combinatory treatments and dual-pathway inhibitors. Herein, we report a novel prototype of dual-pathway inhibitors by means of merging the core structural scaffolds of a MEK1 inhibitor and a PDK1 inhibitor. A library of 43 compounds that categorized into three series (Series I-III) was synthesized and tested for antitumor activity in lung cancer cells...
January 26, 2019: Bioorganic & Medicinal Chemistry
https://read.qxmd.com/read/30777330/self-assembled-nanovehicle-mediated-co-encapsulation-of-inactivated-ev71-virus-and-cpg-oligonucleotides-elicits-potent-anti-ev71-humoral-and-cellular-immune-protective-responses
#11
Hao Liang, Xiangqian Xiao, Xiaofei Zhang, Qin Hu, Yishu Yang, Shan Cen, Xiongwei Deng, Wang Sheng
Inactivated vaccines are widely used for prevention of viral disease. Both humoral and cellular immune responses have been shown to play important roles in the control and clearance of virus infections. CpG motif containing oligodeoxynucleotides (ODN) have recently gained considerable interest and been used as vaccine adjuvant due to their potent abilities to modulate host immune response. In this study, CpG-ODN adjuvant and inactivated viral particles of enterovirus 71 (EV71) were co-encapsulated into nanoparticles (NP) generated by using protamine sulfate (PS) and carboxymethyl β-glucan (CMG) through a self-assembly approach...
February 16, 2019: Biochemical and Biophysical Research Communications
https://read.qxmd.com/read/30776588/inclusion-complex-of-saikosaponin-d-with-hydroxypropyl-%C3%AE-cyclodextrin-improved-physicochemical-properties-and-anti-skin-cancer-activity
#12
Stephen Chu-Sung Hu, Yi-Chien Lai, Chi-Ling Lin, Wen-Sheng Tzeng, Feng-Lin Yen
BACKGROUND: Saikosaponin-d (SSD) is a triterpene saponin isolated from Bupleurum plants. It has been shown to exhibit antioxidant, anti-inflammatory, and anticancer activities. However, its biomedical applications are limited by its poor water solubility. Cyclodextrins are highly water soluble oligosaccharide compounds which can form inclusion complexes with lipophilic drugs. PURPOSE: We complexed SSD with hydroxypropyl-β-cyclodextrin (HPBCD) in various ratios to form SSD-HPBCD inclusion complexes...
November 8, 2018: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://read.qxmd.com/read/30776481/pd-l1-promotes-colorectal-cancer-stem-cell-expansion-by-activating-hmga1-dependent-signaling-pathways
#13
Fang Wei, Tong Zhang, Shu-Chou Deng, Jian-Chang Wei, Ping Yang, Qiang Wang, Zhuan-Peng Chen, Wang-Lin Li, Hua-Cui Chen, He Hu, Jie Cao
PD-L1 is critical for tumor cell escape from immune surveillance by inhibiting T cell function via the PD-1 receptor. Accumulating evidence demonstrates that anti-PD-L1 monoclonal antibodies might potently enhance antitumor effects in various tumors, but the effect of PD-L1 on colorectal cancer stem cells (CSCs) remains unclear. We observed high PD-L1 expression in CD133+ CD44+ colorectal CSCs and CSC-enriched tumorspheres. Altering PD-L1 expression promoted colorectal CSC self-renewal by increasing the expression of stemness genes, the CD133+ CD44+ cell population sizes and the ability to form tumorspheres...
February 15, 2019: Cancer Letters
https://read.qxmd.com/read/30775851/chemotherapy-combined-with-endostar-as-salvage-treatment-for-egfr-tyrosine-kinase-inhibitor-primary-resistance-in-an-advanced-non-small-cell-lung-cancer-patient-with-egfr-l858r-mutation-and-ros1-fusion-a-case-report
#14
Dong Qiu, Yu Zhang, Ying-Bo Xue, Qi Shen, Hang Li, Ping Huang, Jian-Jun Hu, Yong-Sheng Wang
EGFR-activating mutations have been recognized as the most important predictor of response to EGFR-tyrosine kinase inhibitors (TKIs); however, 20-30% of patients harboring EGFR-activating mutations show poor responses. The mechanisms of such EGFR-TKI primary resistance are still poorly understood. In our case, a non-small cell lung cancer patient developed intrinsic EGFR-TKI resistance and was then confirmed to simultaneously harbor an L858R mutation and ROS1 rearrangement. Salvage chemotherapy plus Endostar showed enduring therapeutic effects, achieving a disease-free survival period of 24 months and overall survival of 30 months...
February 18, 2019: Thoracic Cancer
https://read.qxmd.com/read/30772808/in-vitro-anti-platelet-aggregation-effects-of-fourteen-fruits-and-vegetables
#15
Cen Chen, Qian Zhang, Feng-Qin Wang, Chun-Hong Li, Yuan-Jia Hu, Zhi-Ning Xia, Feng-Qing Yang
In the present study, the anti-platelet aggregation activity of 14 vegetables and fruits was tested in vitro. The aqueous, 90% ethanol and ethyl acetate extracts, as well as concentrated juices of 14 foods (fruits and vegetables) were prepared, and the anti-platelet aggregation activity of those extracts was analyzed on a platelet aggregation analyzer in vitro with adenosine 5'-diphosphate (ADP), bovine thrombin (THR) and arachidonic acid (AA) as aggregation inducers, respectively. Aspirin (ASP) was used as the positive control...
January 2019: Pakistan Journal of Pharmaceutical Sciences
https://read.qxmd.com/read/30771312/propofol-specifically-reduces-pma-induced-neutrophil-extracellular-trap-formation-through-inhibition-of-p-erk-and-hocl
#16
Ming-Shan Chen, Wen-Chun Lin, Hsuan-Te Yeh, Chia-Lin Hu, Shew-Meei Sheu
Neutrophil extracellular traps (NETs) are net-like chromatin fibers that can trap and kill microorganisms. Although several anti-inflammatory effects of intravenous anesthetics have been reported, it has not been investigated whether intravenous anesthetics influence NET formation. AIMS: To compare the effects of four intravenous anesthetics (propofol, thiamylal sodium, midazolam, and ketamine) on phorbol myristate acetate (PMA)-induced NET formation and analyze the associated signaling pathways...
February 13, 2019: Life Sciences
https://read.qxmd.com/read/30770785/applying-an-innovative-biodegradable-self-assembly-nanomicelles-to-deliver-%C3%AE-mangostin-for-improving-anti-melanoma-activity
#17
Shuping Yang, Xiang Gao, Yihong He, Yuzhu Hu, Bocheng Xu, Zhiqiang Cheng, Mingli Xiang, Yongmei Xie
α-Mangostin (αM), a traditional natural product with promising application of treating a series of diseases, was limited use in clinical due to its hydrophobicity. Herein, MPEG-PCL nanomicelles were used to embed the αM for resolving hydrophobicity and improving the anti-melanoma effect of the αM. The anti-melanoma activity and potential mechanisms of biodegradable αM/MPEG-PCL nanomicelles were investigated. The αM/MPEG-PCL nanomicelles possessed a stronger effect on anti-melanoma compared to the free αM both in vitro and in vivo with a low cytotoxicity in non-tumor cell lines...
February 15, 2019: Cell Death & Disease
https://read.qxmd.com/read/30769844/synthesis-characterization-and-biological-activity-of-a-novel-series-of-benzo-4-5-imidazo-2-1-b-thiazole-derivatives-as-potential-epidermal-growth-factor-receptor-inhibitors
#18
Xinshan Deng, Xiaoyu Tan, Tiantian An, Qingqing Ma, Zhe Jin, Ce Wang, Qingguo Meng, Chun Hu
Based on the analysis of epidermal growth factor receptor (EGFR) complexes with gefitinib with molecular docking, the scaffold-hopping strategy, combination of the active substructures, and structural optimization of EGFR inhibitors, a novel series of benzo[4,5]imidazo[2,1- b ]thiazole derivatives was designed, synthesized, and evaluated for antitumor activity in human cancer cell lines and cellular toxicity against human normal cell lines using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) colorimetric assay and EGFR inhibitory activities in vitro...
February 14, 2019: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://read.qxmd.com/read/30768595/anti-inflammatory-microrna-146a-protects-mice-from-diet-induced-metabolic-disease
#19
Marah C Runtsch, Morgan C Nelson, Soh-Hyun Lee, Warren Voth, Margaret Alexander, Ruozhen Hu, Jared Wallace, Charisse Petersen, Vanja Panic, Claudio J Villanueva, Kimberley J Evason, Kaylyn M Bauer, Timothy Mosbruger, Sihem Boudina, Mary Bronner, June L Round, Micah J Drummond, Ryan M O'Connell
Identifying regulatory mechanisms that influence inflammation in metabolic tissues is critical for developing novel metabolic disease treatments. Here, we investigated the role of microRNA-146a (miR-146a) during diet-induced obesity in mice. miR-146a is reduced in obese and type 2 diabetic patients and our results reveal that miR-146a-/- mice fed a high-fat diet (HFD) have exaggerated weight gain, increased adiposity, hepatosteatosis, and dysregulated blood glucose levels compared to wild-type controls. Pro-inflammatory genes and NF-κB activation increase in miR-146a-/- mice, indicating a role for this miRNA in regulating inflammatory pathways...
February 15, 2019: PLoS Genetics
https://read.qxmd.com/read/30768161/a-14-day-esomeprazole-and-amoxicillin-containing-high-dose-dual-therapy-regimen-achieves-a-high-eradication-rate-as-first-line-anti-helicobacter-pylori-treatment-in-taiwan-a-prospective-randomized-trial
#20
Wei-Chen Tai, Chih-Ming Liang, Chung-Mou Kuo, Pao-Yuan Huang, Cheng-Kun Wu, Shih-Cheng Yang, Yuan-Hung Kuo, Ming-Tsung Lin, Chen-Hsiang Lee, Chien-Ning Hsu, Keng-Liang Wu, Tsung-Hui Hu, Seng-Kee Chuah
BACKGROUND: The first-line eradication rate of standard triple therapy for Helicobacter pylori infection has declined to <80%, and alternative therapies with >90% success rates are needed. Inconsistent eradication rates were reported for proton pump inhibitor- and amoxicillin-containing high-dose dual therapy. OBJECTIVES: We performed a prospective, randomized controlled study to assess the efficacy of esomeprazole- and amoxicillin-containing high-dose dual therapy and investigated the influencing clinical factors...
February 14, 2019: Journal of Antimicrobial Chemotherapy
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