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Acta Pharmacologica Sinica

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https://www.readbyqxmd.com/read/29323338/ulinastatin-attenuates-lps-induced-inflammation-in-mouse-macrophage-raw264-7-cells-by-inhibiting-the-jnk-nf-%C3%AE%C2%BAb-signaling-pathway-and-activating-the-pi3k-akt-nrf2-pathway
#1
Si-Tong Li, Qi Dai, Shu-Xian Zhang, Ya-Jun Liu, Qiu-Qiong Yu, Fei Tan, Shu-Hong Lu, Quan Wang, Jian-Wen Chen, He-Qing Huang, Pei-Qing Liu, Min Li
Ulinastatin (UTI) is a broad-spectrum serine protease inhibitor isolated and purified from human urine with strong anti-inflammatory and cytoprotective actions, which is widely used for the treatment of various diseases, such as pancreatitis and sepsis. Although the therapeutic effects of UTI are reported to be associated with a variety of mechanisms, the signaling pathways mediating the anti-inflammatory action of UTI remain to be elucidated. In the present study we carried out a systematic study on the anti-inflammatory and anti-oxidative mechanisms of UTI and their relationships in LPS-treated RAW264...
January 11, 2018: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29323337/regulatory-t-cells-as-a-new-therapeutic-target-for-atherosclerosis
#2
REVIEW
Han-Xiao Ou, Bing-Bing Guo, Qi Liu, Yu-Kun Li, Zhen Yang, Wen-Jie Feng, Zhong-Cheng Mo
Atherosclerosis is an autoimmune disease caused by self- and non-self-antigens contributing to excessive activation of T and B cell immune responses. These responses further aggravate vascular inflammation and promote progression of atherosclerosis and vulnerability to plaques via releasing pro-inflammatory cytokines. Regulatory T cells (Tregs) as the major immunoregulatory cells, in particular, induce and maintain immune homeostasis and tolerance by suppressing the immune responses of various cells such as T and B cells, natural killer (NK) cells, monocytes, and dendritic cells (DCs), as well as by secreting inhibitory cytokines interleukin (IL)-10, IL-35 and transcription growth factor β (TGF-β) in both physiological and pathological states...
January 11, 2018: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29323336/schisandrin-ameliorates-cognitive-impairment-and-attenuates-a%C3%AE-deposition-in-app-ps1-transgenic-mice-involvement-of-adjusting-neurotransmitters-and-their-metabolite-changes-in-the-brain
#3
Bin-Bin Wei, Ming-Yan Liu, Zai-Xing Chen, Min-Jie Wei
Neurotransmitters (NTs) in the brain are involved in neurodegenerative diseases, such as Alzheimer's disease (AD). Schisandrin is a major ingredient of Schisandra chinensis (Turcz.) Baill and has been used for the treatment of AD. In this study we examined the therapeutic effects of schisandrin in APP/PS1 transgenic mice, and correlated the beneficial effects on cognitive impairment with the adjustments in NTs and their metabolites in the mouse brains. APP/PS1 mice were treated with schisandrin (2 mg·kg-1·d-1, ip) for 2 weeks...
January 11, 2018: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29323335/tanshinol-alleviates-impaired-bone-formation-by-inhibiting-adipogenesis-via-klf15-ppar%C3%AE-2-signaling-in-gio-rats
#4
Ya-Jun Yang, Zhu Zhu, Dong-Tao Wang, Xin-le Zhang, Yu-Yu Liu, Wen-Xiu Lai, Yu-Lin Mo, Jin Li, Yan-Long Liang, Zhuo-Qing Hu, Yong-Jie Yu, Liao Cui
Glucocorticoid (GC)-induced osteoporosis (GIO) is characterized by impaired bone formation, which can be alleviated by tanshinol, an aqueous polyphenol isolated from Salvia miltiorrhiza Bunge. In this study we investigated the molecular mechanisms underlying GC-induced modulation of osteogenesis as well as the possibility of using tanshinol to interfere with GIO. Female SD rats aged 4 months were orally administered distilled water (Con), prednisone (GC, 5 mg·kg-1·d-1), GC plus tanshinol (Tan, 16 mg·kg-1·d-1) or GC plus resveratrol (Res, 5 mg·kg-1·d-1) for 14 weeks...
January 11, 2018: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29283175/ebp50-suppresses-the-proliferation-of-mcf-7-human-breast-cancer-cells-via-promoting-beclin-1-p62-mediated-lysosomal-degradation-of-c-myc
#5
Hong Liu, Wu-Li Zhao, Jia-Ping Wang, Bing-Mu Xin, Rong-Guang Shao
c-Myc, a key activator of cell proliferation and angiogenesis, promotes the development and progression of breast cancer. Ezrin-radixin-moesin-binding phosphoprotein-50 (EBP50) is a multifunctional scaffold protein that suppresses the proliferation of breast cancer cells. In this study we investigated whether the cancer-suppressing effects of EBP50 resulted from its regulation of c-Myc signaling in human breast cancer MCF-7 cells in vitro and in vivo. We first found a significant correlation between EBP50 and c-Myc expression levels in breast cancer tissue, and demonstrated that EBP50 suppressed cell proliferation through decreasing the expression of c-Myc and its downstream proteins cyclin A, E and Cdc25A in MCF-7 cells...
December 28, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29283174/nucleus-accumbens-a-new-sleep-regulating-area-through-the-integration-of-motivational-stimuli
#6
Sara Valencia Garcia, Patrice Fort
No abstract text is available yet for this article.
December 28, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29283173/cyp3a4-inducer-and-inhibitor-strongly-affect-the-pharmacokinetics-of-triptolide-and-its-derivative-in-rats
#7
Ye Xu, Yi-Fan Zhang, Xiao-Yan Chen, Da-Fang Zhong
Triptolide is the most active ingredient of Tripterygium wilfordii Hook F, which is used to treat rheumatoid arthritis. (5R)-5-Hydroxytriptolide is a hydroxylation derivative of triptolide with a reduced toxicity. To investigate the metabolic enzymes of the two compounds and the drug-drug interactions with enzyme inducers or inhibitors, a series of in vitro and in vivo experiments were conducted. In vitro studies using recombinant human cytochrome P450 enzyme demonstrated that cytochrome P450 3A4 (CYP3A4) was predominant in the metabolism of triptolide and (5R)-5-hydroxytriptolide, accounting for 94...
December 28, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29265109/humanin-decreases-mitochondrial-membrane-permeability-by-inhibiting-the-membrane-association-and-oligomerization-of-bax-and-bid-proteins
#8
Ze-Wei Ma, Dong-Xiang Liu
Humanin (HN) is a 24-residue peptide identified from the brain of a patient with Alzheimer's disease (AD). HN has been found to protect against neuronal insult caused by Aβ peptides or transfection of familial AD mutant genes. In order to elucidate the molecular mechanisms of HN neuroprotection, we explored the effects of HN on the association of Bax or Bid with lipid bilayers and their oligomerization in the membrane. By using single-molecule fluorescence and Förster resonance energy transfer techniques, we showed that Bax was mainly present as monomers, dimers and tetramers in lipid bilayers, while truncated Bid (tBid) enhanced the membrane association and tetramerization of Bax...
December 21, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29265108/prefrontal-ampa-receptors-are-involved-in-the-effect-of-methylphenidate-on-response-inhibition-in-rats
#9
Dong-Dong Zhang, Yu-Qiu Zhang, Xue-Han Zhang
Response inhibition is a critical executive control function in many species. Deficits in response inhibition have been observed in many disorders, eg, attention deficit/hyperactivity disorder (ADHD). The stop-signal task (SST) is a unique behavior task for evaluating response inhibition via measuring the covert latency of a stop process, and it is widely used in studies of humans, nonhuman primates and rodents. Methylphenidate (MPH; Ritalin®) is a psychostimulant that is widely used for the treatment of ADHD and that effectively improves response inhibition in individuals with ADHD and normal subjects...
December 21, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29239351/association-of-serum-uric-acid-levels-with-osteoporosis-and-bone-turnover-markers-in-a-chinese-population
#10
Dan-Dan Yan, Jie Wang, Xu-Hong Hou, Yu-Qian Bao, Zhen-Lin Zhang, Cheng Hu, Wei-Ping Jia
Recent evidence shows that uric acid is protective against some neurological diseases, but can be detrimental in many metabolic and cardiovascular disorders. In this study, we examined the association between serum uric acid levels and bone metabolism in Chinese males and postmenopausal females. A total of 943 males and 4256 postmenopausal females were recruited in Shanghai. The levels of serum uric acid and bone turnover markers (BTMs) were detected along with other biochemical traits. In addition, the fat distribution was calculated through MRI and image analysis software, and bone mineral density (BMD) was determined using dual-energy X-ray absorptiometry...
December 14, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29239350/suppression-of-eef-2k-mediated-autophagy-enhances-the-cytotoxicity-of-raddeanin-a-against-human-breast-cancer-cells-in-vitro
#11
Yi-di Guan, Shi-Long Jiang, Pian Yu, Mei Wen, Yi Zhang, Song-Shu Xiao, Xiao-Jun Xu, Yan Cheng
Recent evidence shows that raddeanin A (RA), an oleanane-type triterpenoid saponin extracted from Anemone raddeana Regel, exerts remarkable cytotoxicity against cancer cells in vitro and in vivo. In addition, RA has also been found to activate autophagy in human gastric cancer cells. In this study, we investigated the molecular mechanisms underlying RA-induced autophagy as well as the relationship between RA-induced autophagy and its cytotoxicity in human breast cancer cells in vitro. Treatment with RA (2-8 μmol/L) dose-dependently enhanced autophagy, as evidenced by increased LC3 levels in breast cancer cell lines T47D, MCF-7 and MDA-MB-231...
December 14, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29239349/influences-of-ivabradine-treatment-on-serum-levels-of-cardiac-biomarkers-sst2-gdf-15-supar-and-h-fabp-in-patients-with-chronic-heart-failure
#12
Peter Jirak, Dzeneta Fejzic, Vera Paar, Bernhard Wernly, Rudin Pistulli, Ilonka Rohm, Christian Jung, Uta C Hoppe, P Christian Schulze, Michael Lichtenauer, Atilla Yilmaz, Daniel Kretzschmar
Chronic heart failure (CHF) represents a major cause of hospitalization and death. Recent evidence shows that novel biomarkers such as soluble suppression of tumorigenicity (sST2), growth-differentiation factor-15 (GDF-15), soluble urokinase plasminogen activator receptor (suPAR) and heart-type fatty acid binding protein (H-FABP) are correlated with inflammatory and ischemic responses in CHF patients. In this study we examined the effects of Ivabradine that inhibited the hyperpolarization-activated cyclic nucleotide-gated channel (HCN channel, also called funny current If), thereby leading to selective heart rate reduction and improved myocardial oxygen supply on the cardiac biomarkers sST2, GDF-15, suPAR and H-FABP in 50 CHF patients at the University Hospital of Jena...
December 14, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29219950/exosomes-new-molecular-targets-of-diseases
#13
REVIEW
Saheli Samanta, Sheeja Rajasingh, Nicholas Drosos, Zhigang Zhou, Buddhadeb Dawn, Johnson Rajasingh
Extracellular vesicles (EVs) comprise apoptotic bodies, microvesicles and exosomes, and they perform as key regulators in cell-to-cell communication in normal as well as diseased states. EVs contain natural cargo molecules, such as miRNA, mRNA and proteins, and transfer these functional cargos to neighboring cells or more distant cells through circulation. These functionally active molecules then affect distinct signaling cascades. The message conveyed to the recipient cells is dependent upon the composition of the EV, which is determined by the parent cell and the EV biogenesis...
December 7, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29219949/a-micrna-200c-cathepsin-l-feedback-loop-determines-paclitaxel-resistance-in-human-lung-cancer-a549-cells-in-vitro-through-regulating-epithelial-mesenchymal-transition
#14
Yi-Fan Zhao, Mei-Ling Han, Ya-Jie Xiong, Long Wang, Yao Fei, Xiao Shen, Ying Zhu, Zhong-Qin Liang
Cathepsin L (CTSL), a cysteine protease, is closely related to tumor occurrence, development, and metastasis, and possibly regulates cancer cell resistance to chemotherapy. miRNAs, especially the miR-200 family, have been implicated in drug-resistant tumors. In this study we explored the relationship of CTSL, micRNA-200c and drug resistance, and the potential regulatory mechanisms in human lung cancer A549 cells and A549/TAX cells in vitro. A549/TAX cells were paclitaxel-resistant A549 cells overexpressing CTSL and characterized by epithelial-mesenchymal transition (EMT)...
December 7, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29219948/asperosaponin-vi-promotes-angiogenesis-and-accelerates-wound-healing-in-rats-via-up-regulating-hif-1%C3%AE-vegf-signaling
#15
Cheng-Gui Wang, Yi-Ting Lou, Min-Ji Tong, Li-Lian Zhang, Zeng-Jie Zhang, Yong-Zeng Feng, Shi Li, Hua-Zi Xu, Cong Mao
Wound therapy remains a clinical challenge due to the complexity of healing pathology and high demand of achieving functional and aesthetically satisfactory scars. Newly formed blood vessels are essential for tissue repair since they can support cells at the wound site with nutrition and oxygen. In this study, we investigated the effects of Asperosaponin VI (ASA VI) isolated from a traditional Chinese medicine, the root of Dipsacus asper Wall, in promoting angiogenesis, as well as its function in wound therapeutics...
December 7, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29219947/dendritic-cell-nuclear-protein-1-regulates-melatonin-biosynthesis-by-binding-to-bmal1-and-inhibiting-the-transcription-of-n-acetyltransferase-in-c6-cells
#16
Dong Chen, Yi-Pei Li, Yan-Xia Yu, Tian Zhou, Chao Liu, Er-Kang Fei, Feng Gao, Chen-Chen Mu, Hai-Gang Ren, Guang-Hui Wang
Dendritic cell nuclear protein-1 (DCNP1) is a protein associated with major depression. In the brains of depression patients, DCNP1 is up-regulated. However, how DCNP1 participates in the pathogenesis of major depression remains unknown. In this study, we first transfected HEK293 cells with EGFP-DCNP1 and demonstrated that the full-length DCNP1 protein was localized in the nucleus, and RRK (the residues 117-119) composed its nuclear localization signal (NLS). An RRK-deletion form of DCNP1 (DCNP1ΔRRK) and truncated form (DCNP11-116), each lacking the RRK residues, did not show the specific nuclear localization like full-length DCNP1 in the cells...
December 7, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29219946/c1206-a-novel-curcumin-derivative-potently-inhibits-hsp90-and-human-chronic-myeloid-leukemia-cells-in-vitro
#17
Ying-Juan Fan, Yi-Xiang Zhou, Lian-Ru Zhang, Qiao-Fa Lin, Ping-Zhang Gao, Fang Cai, Li-Ping Zhu, Bi Liu, Jian-Hua Xu
4-(4-Pyridinyl methylene) curcumin (C1206) is a new derivative of curcumin that is more active than curcumin in inhibition of heat shock protein 90 (Hsp90) and antitumor action. In this study we investigated the relationship between C1206-induced inhibition of Hsp90 and its anti-leukemic effects. The fluorescence quenching experiments showed that C1206 seemed to bind the middle dimerization domain of Hsp90. The interaction between C1206 and Hsp90 was driven mainly by electrostatic interaction. In in vitro enzyme activity assay, C1206 dose-dependently inhibited Hsp90 ATPase activity with an IC50 value of 4...
December 7, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29188803/activation-of-human-smooth-muscle-bk-channels-by-hydrochlorothiazide-requires-cell-integrity-and-the-presence-of-bk-%C3%AE-1-subunit
#18
Pedro Martín, Melisa Moncada, Guruprasad Kuntamallappanavar, Alex M Dopico, Verónica Milesi
Thiazide-like diuretics are the most commonly used drugs to treat arterial hypertension, with their efficacy being linked to their chronic vasodilatory effect. Previous studies suggest that activation of the large conductance voltage- and Ca2+-dependent K+ (BK) channel (Slo 1, MaxiK channel) is responsible for the thiazide-induced vasodilatory effect. But the direct electrophysiological evidence supporting this claim is lacking. BK channels can be associated with one small accessory β-subunit (β1-β4) that confers specific biophysical and pharmacological characteristics to the current phenotype...
November 30, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29188802/the-lpi-gpr55-axis-enhances-human-breast-cancer-cell-migration-via-hbxip-and-p-mlc-signaling
#19
Xiao-Lei Zhou, Xin Guo, Yu-Pin Song, Chong-Yue Zhu, Wei Zou
The G protein-coupled receptor 55 (GPR55) is expressed in multiple tissues, and has been implicated in cancer pathogenesis, but little is known about its role in the migratory behavior of cancer cells, particularly breast cancer cells. In this study we first showed that GPR55 expression levels in 38 metastatic lymph nodes of breast cancer patients were profoundly elevated, and were positively associated in human breast cancer cells with their migratory ability. Moreover, the plasma levels of GPR55 endogenous agonist L-a-lysophosphatidylinositol (LPI) were significantly increased in breast cancer patients compared with healthy individuals...
November 30, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29188801/pharmacokinetic-and-pharmacodynamic-evidence-for-developing-an-oral-formulation-of-octreotide-against-gastric-mucosal-injury
#20
Xi-Nuo Li, Tai Rao, Yang-Fan Xu, Kang-Rui Hu, Zhang-Pei Zhu, Hao-Feng Li, Dian Kang, Yu-Hao Shao, Bo-Yu Shen, Xiao-Xi Yin, Lin Xie, Guang-Ji Wang, Yan Liang
Among the somatostatin analogues, octreotide (OCT) is the most commonly used in clinic via intravenous or subcutaneous injection to treat various diseases caused by increased secretion of growth hormone, gastrin or insulin. In order to assesse the feasibility of developing oral formulations of OCT, we conducted systematical pharmacokinetic and pharmacodynamic analyses of OCT in several animal models. The pharmacokinetic studies in rats showed that intragastric administration of OCT had extremely low bioavailability (<0...
November 30, 2017: Acta Pharmacologica Sinica
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