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Acta Pharmacologica Sinica

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https://read.qxmd.com/read/30765842/inhibition-of-g9a-by-a-small-molecule-inhibitor-unc0642-induces-apoptosis-of-human-bladder-cancer-cells
#1
Yue-Peng Cao, Jing-Ya Sun, Mei-Qian Li, Yu Dong, Yuan-Heng Zhang, Jun Yan, Rui-Min Huang, Xiang Yan
Urinary bladder cancer (UBC) is characterized by frequent recurrence and metastasis despite the standard chemotherapy with gemcitabine and cisplatin combination. Histone modifiers are often dysregulated in cancer development, thus they can serve as an excellent drug targets for cancer therapy. Here, we investigated whether G9a, one of the histone H3 methyltransferases, was associated with UBC development. We first analyzed clinical data from public databases and found that G9a was significantly overexpressed in UBC patients...
February 14, 2019: Acta Pharmacologica Sinica
https://read.qxmd.com/read/30760835/magnesium-lithospermate-b-ameliorates-microcirculation-perfusion-in-rats-by-promoting-vascular-no-production-via-activating-the-pi3k-akt-pathway
#2
Ying-Luo Liu, Xiao-Yu Zhou, Li-Jiang Xuan
Microcirculation morphologically refers to the blood flow in vessels of less than 150 μm in diameter, including arterioles, capillaries and venules, which provides nutrients and removes metabolic byproducts within tissues. Microcirculation dysfunction is involved in the pathological progress of many diseases, such as obesity, hypertension, and insulin resistance. In this study we investigated the effects of magnesium lithospermate B (MLB), an active compound of the traditional Chinese medicine Slavia miltiorrhiza, on the microcirculation dysfunction in rats and the underlying molecular mechanisms...
February 13, 2019: Acta Pharmacologica Sinica
https://read.qxmd.com/read/30760834/low-intensity-walking-as-mild-medication-for-pressure-control-in-prehypertensive-and-hypertensive-subjects-how-far-shall-we-wander
#3
Qin Lu, Sheng-Ming Wang, Yi-Xiao Liu, Hong Chen, Rui Zhang, Wen-Hui Zhang, Yuan-Yuan Zou, Jia-Wei Zhou, Xin-Yi Guo, Ying Zhang, Teng-Li Huang, Yu-Hang Liu, Si-Qi Zhang, Kyosuke Yamanishi, Hiromichi Yamanishi, Hideaki Higashino, Haruki Okamura
Successful prevention and treatment of hypertension depend on the appropriate combination of antihypertensive drug therapy and nondrug lifestyle modification. While most hypertension guidelines recommend moderate- to high-intensity exercise, we decided to explore a mild yet effective type of exercise to add to hypertension management, especially in populations with complications or frailty. After comparing the short-term cardiovascular effects of low-speed walking versus high-speed walking for 3 kilometers (km) (3 km/h versus 6 km/h) in young, healthy volunteers, we delivered low-speed walking (low-intensity walking, 2...
February 13, 2019: Acta Pharmacologica Sinica
https://read.qxmd.com/read/30728467/simvastatin-improves-olanzapine-induced-dyslipidemia-in-rats-through-inhibiting-hepatic-mtor-signaling-pathway
#4
Xue-Mei Liu, Xiao-Min Zhao, Chao Deng, Yan-Ping Zeng, Chang-Hua Hu
Second-generation antipsychotic drug (SGA)-induced metabolic abnormalities, such as dyslipidemia, are a major clinical problem for antipsychotic therapy. Accumulated evidences have shown the efficacy of statins in reducing SGA-induced dyslipidemia, but the underlying mechanisms are unclear. In this study, we explored whether mTOR signaling was involved in olanzapine (OLZ)-induced dyslipidemia as well as the lipid-lowering effects of cotreatment of simvastatin (Sim) in rats. Model rats received OLZ (1.0 mg/kg, t...
February 6, 2019: Acta Pharmacologica Sinica
https://read.qxmd.com/read/30728466/nlrp3-inflammasome-pathway-is-involved-in-olfactory-bulb-pathological-alteration-induced-by-mptp
#5
Ying Chen, Qiu-Shuang Zhang, Qian-Hang Shao, Shuo Wang, Yu-He Yuan, Nai-Hong Chen, Hong-Bo Wang
Olfactory bulb, as one of sensory organs opening to the outside, is susceptible to toxic environment and easy to deteriorate. Recent studies in Parkinson's disease (PD) patients and 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-treated monkeys have shown that abnormal α-synuclein is accumulated in the olfactory glomeruli, suggesting that the lesions of PD are not only confined to the substantia nigra (SN) but also located in the olfactory bulb. Thus, olfactory bulb might be the region of onset in PD pathogenesis and a targeted region for diagnosis and treatment of PD...
February 6, 2019: Acta Pharmacologica Sinica
https://read.qxmd.com/read/30670816/cannabis-cannabinoid-receptors-and-endocannabinoid-system-yesterday-today-and-tomorrow
#6
EDITORIAL
Jie Wu
No abstract text is available yet for this article.
January 22, 2019: Acta Pharmacologica Sinica
https://read.qxmd.com/read/30670815/histone-methyltransferase-nsd2-mediates-the-survival-and-invasion-of-triple-negative-breast-cancer-cells-via-stimulating-adam9-egfr-akt-signaling
#7
Jun-Jian Wang, June X Zou, Hong Wang, Zhi-Jian Duan, Hai-Bin Wang, Peng Chen, Pei-Qing Liu, Jian-Zhen Xu, Hong-Wu Chen
Triple-negative breast cancer (TNBC) is a heterogeneous disease with a poor prognosis due to the lack of an effective targeted therapy. Histone lysine methyltransferases (KMTs) have emerged as attractive drug targets for cancer therapy. However, the function of the majority of KMTs in TNBC has remained largely unknown. In the current study, we found that KMT nuclear receptor binding SET domain protein 2 (NSD2) is overexpressed in TNBC tumors and that its overexpression is associated with poor survival of TNBC patients...
January 22, 2019: Acta Pharmacologica Sinica
https://read.qxmd.com/read/30644422/costunolide-alleviates-hksa-induced-acute-lung-injury-via-inhibition-of-macrophage-activation
#8
Yun-Tian Chen, Yao Du, Bo Zhao, Li-Xing Gan, Kai-Kai Yu, Lei Sun, Jian Wang, Feng Qian
Staphylococcus aureus (S. aureus) infection leads to a severe inflammatory response and causes acute lung injury (ALI), eventually threatening human life. Therefore, it is of importance to find an agent to inhibit inflammation and reduce ALI. Here, we found that costunolide, a sesquiterpene lactone, displays anti-inflammatory effects and ameliorates heat-killed S. aureus (HKSA)-induced pneumonia. Costunolide treatment attenuated HKSA-induced murine ALI in which pulmonary neutrophil infiltration was inhibited, lung edema was decreased, and the production of pro-inflammatory cytokines was significantly reduced...
January 15, 2019: Acta Pharmacologica Sinica
https://read.qxmd.com/read/30643210/shr-a1403-a-novel-c-met-antibody-drug-conjugate-exerts-encouraging-anti-tumor-activity-in-c-met-overexpressing-models
#9
Chang-Yong Yang, Lei Wang, Xing Sun, Mi Tang, Hai-Tian Quan, Lian-Shan Zhang, Li-Guang Lou, Shao-Hua Gou
Emerging evidence demonstrates that a c-Met antibody-drug conjugate (ADC) has superior efficacy and safety profiles compared with those of currently available small molecules or antibody inhibitors for the treatment of c-Met-overexpressing cancers. Here we described both the in vitro and in vivo efficacies of SHR-A1403, a novel c-Met ADC composed of a humanized IgG2 monoclonal antibody against c-Met conjugated to a novel cytotoxic microtubule inhibitor. SHR-A1403 showed high affinity to c-Met proteins derived from human or monkey and potent inhibitory effects in cancer cell lines with high c-Met protein expression...
January 14, 2019: Acta Pharmacologica Sinica
https://read.qxmd.com/read/30643209/cp-25-reverses-prostaglandin-e4-receptor-desensitization-induced-fibroblast-like-synoviocyte-dysfunction-via-the-g-protein-coupled-receptor-kinase-2-in-autoimmune-arthritis
#10
Xiao-Yi Jia, Yan Chang, Fang Wei, Xing Dai, Yu-Jing Wu, Xiao-Jing Sun, Shu Xu, Hua-Xun Wu, Chun Wang, Xue-Zhi Yang, Wei Wei
Paeoniflorin-6'-O-benzene sulfonate (CP-25) is a novel compound derived from paeoniflorin that has been demonstrated to have therapeutic effects in a rat model of rheumatoid arthritis (RA). However, the underlying mechanism has not been elucidated to date. We explored this mechanism in the present study by treating rats with adjuvant arthritis (AA) with CP-25. We found that the membrane EP4 protein level was downregulated; whereas, GRK2 was upregulated, in fibroblast-like synoviocyte (FLS)s of AA rats. Prostaglandin (PGE)2 stimulated FLS proliferation and enhanced the membrane EP4 receptor protein level; the latter was reversed by the administration of an EP4 receptor agonist, whereas the membrane GRK2 protein level gradually increased...
January 14, 2019: Acta Pharmacologica Sinica
https://read.qxmd.com/read/30643208/discovery-of-%C3%AE-arrestin-biased-%C3%AE-2-adrenoceptor-agonists-from-2-amino-2-phenylethanol-derivatives
#11
Anthony Yiu-Ho Woo, Xin-Yue Ge, Li Pan, Gang Xing, Yong-Mei Mo, Rui-Juan Xing, Xiao-Ran Li, Yu-Yang Zhang, Irving W Wainer, Mao-Sheng Cheng, Rui-Ping Xiao
β-Arrestins are a small family of proteins important for signal transduction at G protein-coupled receptors (GPCRs). β-Arrestins are involved in the desensitization of GPCRs. Recently, biased ligands possessing different efficacies in activating the G protein- versus the β-arrestin-dependent signals downstream of a single GPCR have emerged, which can be used to selectively modulate GPCR signal transduction in such a way that desirable signals are enhanced to produce therapeutic effects while undesirable signals of the same GPCR are suppressed to avoid side effects...
January 14, 2019: Acta Pharmacologica Sinica
https://read.qxmd.com/read/30617294/magnesium-lithospermate-b-protects-the-endothelium-from-inflammation-induced-dysfunction-through-activation-of-nrf2-pathway
#12
Fei Gao, Jiao-Meng Li, Cong Xi, Hui-Hui Li, Ying-Luo Liu, Yi-Ping Wang, Li-Jiang Xuan
Magnesium lithospermate B (MLB) is an active component of Salvia miltiorrhiza Radix, a traditional Chinese herb used in treating cardiovascular diseases. In this study, we investigated the protective effects of MLB against inflammation-induced endothelial dysfunction in vitro and in vivo, and the underlying mechanisms. Endothelial dysfunction was induced in human dermal microvascular endothelial cells (HMEC-1) in vitro by lipopolysaccharide (LPS, 1 μg/mL). We showed that pretreatment with MLB (10-100 μM) dose-dependently inhibited LPS-induced upregulation of inflammatory cytokines ICAM1, VCAM1, and TNFα, which contributed to reduced leukocytes adhesion and attenuation of endothelial hyperpermeability in HMEC-1 cells...
January 7, 2019: Acta Pharmacologica Sinica
https://read.qxmd.com/read/30593588/c-myc-promotes-tubular-cell-apoptosis-in-ischemia-reperfusion-induced-renal-injury-by-negatively-regulating-c-flip-and-enhancing-fasl-fas-mediated-apoptosis-pathway
#13
Dan Xu, Bao Wang, Pan-Pan Chen, Yan-Zhe Wang, Nai-Jun Miao, Fan Yin, Qian Cheng, Zhuan-Li Zhou, Hong-Yan Xie, Li Zhou, Jun Liu, Xiao-Xia Wang, Hong Xue, Wei Zhang, Li-Min Lu
c-Myc plays an important role in cell proliferation, differentiation, and cell apoptosis. FasL/Fas pathway is a key regulator of cell apoptosis. This study was aimed to investigate the effects of c-Myc on the FasL/Fas pathway in ischemia-reperfusion (I/R)-induced renal injury. Rats were objected to bilateral renal ischemia for 60 min and reperfused for 24 or 48 h. NRK-52E cells were treated with hypoxia-reoxygenation (H/R) or FasL. Immunohistochemistry was used to identify the distribution of c-Myc. Cell apoptosis was assessed by TUNEL staining...
December 28, 2018: Acta Pharmacologica Sinica
https://read.qxmd.com/read/30573812/a-novel-asbt-inhibitor-imb17-15-repressed-nonalcoholic-fatty-liver-disease-development-in-high-fat-diet-fed-syrian-golden-hamsters
#14
Mao-Xu Ge, Wei-Xiao Niu, Jin-Feng Ren, Shi-Ying Cai, Dong-Ke Yu, Hong-Tao Liu, Na Zhang, Yi-Xuan Zhang, Yu-Cheng Wang, Rong-Guang Shao, Ju-Xian Wang, Hong-Wei He
The manipulation of bile acid (BA) homeostasis by blocking the ileal apical Na+ -dependent bile salt transporter (ASBT/SLC10A2) may have therapeutic effects in nonalcoholic fatty liver disease. We developed a novel ASBT inhibitor, an N-(3,4-o-dichlorophenyl)-2-(3-trifluoromethoxy) benzamide derivative referred to as IMB17-15, and investigated its therapeutic effects and the molecular mechanisms underlying the effects. Syrian golden hamsters were challenged with high-fat diet (HFD) to induce NAFLD and were subsequently administered 400 mg/kg IMB17-15 by gavage daily for 21 days...
December 20, 2018: Acta Pharmacologica Sinica
https://read.qxmd.com/read/30568253/magnesium-isoglycyrrhizinate-ameliorates-high-fructose-induced-liver-fibrosis-in-rat-by-increasing-mir-375-3p-to-suppress-jak2-stat3-pathway-and-tgf-%C3%AE-1-smad-signaling
#15
Yan-Zi Yang, Xiao-Juan Zhao, Hong-Jiang Xu, Shan-Chun Wang, Ying Pan, Shui-Juan Wang, Qiang Xu, Rui-Qing Jiao, Hong-Mei Gu, Ling-Dong Kong
Increasing evidence has demonstrated that excessive fructose intake induces liver fibrosis. Epithelial-mesenchymal transition (EMT) driven by transforming growth factor-β1 (TGF-β1)/mothers against decapentaplegic homolog (Smad) signaling activation promotes the occurrence and development of liver fibrosis. Magnesium isoglycyrrhizinate is clinically used as a hepatoprotective agent to treat liver fibrosis, but its underlying molecular mechanism has not been identified. Using a rat model, we found that high fructose intake reduced microRNA (miR)-375-3p expression and activated the janus-activating kinase 2 (JAK2)/signal transducer and activator of transcription 3 (STAT3) cascade and TGF-β1/Smad signaling, which is consistent with the EMT and liver fibrosis...
December 19, 2018: Acta Pharmacologica Sinica
https://read.qxmd.com/read/30560904/sulfuretin-protects-hepatic-cells-through-regulation-of-ros-levels-and-autophagic-flux
#16
Yu-Ting Lu, Yu-Feng Xiao, Yu-Feng Li, Jia Li, Fa-Jun Nan, Jing-Ya Li
Palmitate (PA) exposure induces stress conditions featuring ROS accumulation and upregulation of p62 expression, resulting in autophagic flux blockage and cell apoptosis. Sulfuretin (Sul) is a natural product isolated from Rhus verniciflua Stokes; the cytoprotective effect of Sul on human hepatic L02 cells and mouse primary hepatocytes under PA-induced stress conditions was investigated in this study. Sul induced mitophagy by activation of p-TBK1 and LC3 and produced a concomitant decline in p62 expression...
December 18, 2018: Acta Pharmacologica Sinica
https://read.qxmd.com/read/30560903/profiling-and-targeting-of-cellular-mitochondrial-bioenergetics-inhibition-of-human-gastric-cancer-cell-growth-by-carnosine
#17
Jiao-Yan Cheng, Jian-Bo Yang, Yuan Liu, Min Xu, Yu-Yan Huang, Jing-Jing Zhang, Pei Cao, Jian-Xin Lyu, Yao Shen
L-Carnosine (β-alanyl-L-histidine) is a naturally occurring dipeptide distributed in various organs of mammalians. We previously showed that carnosine inhibited proliferation of human gastric cancer cells through targeting both mitochondrial bioenergetics and glycolysis pathway. But the mechanism underlying carnosine action on mitochondrial bioenergetics of tumor cells remains unclear. In the current study we investigated the effect of carnosine on the growth of human gastric cancer SGC-7901 cells in vitro and in vivo...
December 18, 2018: Acta Pharmacologica Sinica
https://read.qxmd.com/read/30518829/human-pharmacology-of-positive-gaba-a-subtype-selective-receptor-modulators-for-the-treatment-of-anxiety
#18
REVIEW
Xia Chen, Joop van Gerven, Adam Cohen, Gabriel Jacobs
Anxiety disorders arise from disruptions among the highly interconnected circuits that normally serve to process the streams of potentially threatening stimuli. The resulting imbalance among these circuits can cause a fundamental misinterpretation of neural sensory information as threatening and can lead to the inappropriate emotional and behavioral responses observed in anxiety disorders. There is considerable preclinical evidence that the GABAergic system, in general, and its α2- and/or α5-subunit-containing GABA(A) receptor subtypes, in particular, are involved in the pathophysiology of anxiety disorders...
December 5, 2018: Acta Pharmacologica Sinica
https://read.qxmd.com/read/30487651/state-of-the-art-functional-fluorescent-probes-for-bioimaging-and-pharmacological-research
#19
Lu Lu, Zhou-Yue Wu, Xin Li, Feng Han
Cardiovascular diseases, neuropsychiatric disorders, and cancers seriously endanger human health. Mechanistic and pharmacological mechanisms of candidate drugs are central to the translational paradigm. Since many signal transduction and molecular events are implicated in these diseases, a novel method to interrogate the key pharmacological mechanisms is required to accelerate innovative drug discovery. Much attention now focuses on the real-time visualization of molecular disease events to yield new insights to the pathogenesis of the diseases...
November 28, 2018: Acta Pharmacologica Sinica
https://read.qxmd.com/read/30487650/c11-a-novel-fibroblast-growth-factor-receptor-1-fgfr1-inhibitor-suppresses-breast-cancer-metastasis-and-angiogenesis
#20
Zhuo Chen, Lin-Jiang Tong, Bai-You Tang, Hong-Yan Liu, Xin Wang, Tao Zhang, Xian-Wen Cao, Yi Chen, Hong-Lin Li, Xu-Hong Qian, Yu-Fang Xu, Hua Xie, Jian Ding
The fibroblast growth factor receptors (FGFRs) are increasingly considered attractive targets for therapeutic cancer intervention due to their roles in tumor metastasis and angiogenesis. Here, we identified a new selective FGFR inhibitor, C11, and assessed its antitumor activities. C11 was a selective FGFR1 inhibitor with an IC50 of 19 nM among a panel of 20 tyrosine kinases. C11 inhibited cell proliferation in various tumors, particularly bladder cancer and breast cancer. C11 also inhibited breast cancer MDA-MB-231 cell migration and invasion via suppression of FGFR1 phosphorylation and its downstream signaling pathway...
November 28, 2018: Acta Pharmacologica Sinica
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