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Acta Pharmacologica Sinica

Yang Lv, Rong-Rong Hu, Manyi Jing, Tai-Yun Zhao, Ning Wu, Rui Song, Jin Li, Gang Hu
Increasing preclinical evidence demonstrates that dopamine D3 receptor (D3R) antagonists are a potential option for the treatment of drug addiction. The reinstatement of the addiction can be triggered by environmental stimuli that acquire motivational salience through repeated associations with the drug's effects. YQA14 is a novel D3R antagonist that has exhibited pharmacotherapeutic efficacy in reducing cocaine and amphetamine reward and relapse to drug seeking in mice. In this study we investigated the effects of YQA14 on morphine-induced context-specific locomotor sensitization in mice...
September 17, 2018: Acta Pharmacologica Sinica
Xu-Hong Fu, Xiong Zhang, Hong Yang, Xiao-Wei Xu, Zong-Long Hu, Juan Yan, Xing-Ling Zheng, Rong-Rui Wei, Zhu-Qing Zhang, Shi-Rui Tang, Mei-Yu Geng, Xun Huang
Pancreatic adenocarcinoma is a highly malignant cancer that often involves a deregulation of c-Myc. It has been shown that c-Myc plays a pivotal role in the regulation of a variety of physiological processes and is involved in early neoplastic development, resulting in poor progression. Hence, suppression of c-Myc overexpression is a potential strategy for pancreatic cancer therapy. CUDC-907 is a novel dual-acting inhibitor of phosphoinositide 3-kinase (PI3K) and histone deacetylase (HDAC). It has shown potential efficiency in patients with lymphoma, multiple myeloma, or thyroid cancer, as well as in solid tumors with c-Myc alterations, but the evidence is lacking for how CUDC-907 regulates c-Myc...
September 17, 2018: Acta Pharmacologica Sinica
Mei Han, Hui Gao, Jing Xie, Yin-Ping Yuan, Quan Yuan, Ming-Quan Gao, Kai-Li Liu, Xue-Hong Chen, Yan-Tao Han, Zhi-Wu Han
Hispidulin (4',5,7-trihydroxy-6-methoxyflavone) is a phenolic flavonoid isolated from the medicinal plant S. involucrata, which exhibits anti-neoplastic activity against several types of cancer. However, the mechanism underlying its anti-cancer activity against hepatocellular carcinoma (HCC) has not been fully elucidated. In this study, we investigated whether and how hispidulin-induced apoptosis of human HCC cells in vitro and in vivo. We showed that hispidulin (10, 20 μmol/L) dose-dependently inhibited cell growth and promoted apoptosis through mitochondrial apoptosis pathway in human HCC SMMC7721 cells and Huh7 cells...
September 14, 2018: Acta Pharmacologica Sinica
Bo-Yu Shen, Chong Chen, Yang-Fan Xu, Jia-Jia Shen, Hui-Min Guo, Hao-Feng Li, Xi-Nuo Li, Dian Kang, Yu-Hao Shao, Zhang-Pei Zhu, Xiao-Xi Yin, Lin Xie, Guang-Ji Wang, Yan Liang
The combinational administration of antioxidants and chemotherapeutic agents during conventional cancer treatment is among one of the most controversial areas in oncology. Although the data on the combinational usage of doxorubicin (DOX) and glutathione (GSH) agents have been explored for over 20 years, the duration, administration route, and authentic rationality have not yet been fully understood yet. In the current study, we systematically investigated the pharmacokinetics (PK) and pharmacodynamics (PD) with both in vivo and in vitro models to elucidate the influence of GSH on the toxicity and efficacy of DOX...
September 14, 2018: Acta Pharmacologica Sinica
Yue-Min Bian, Xi-Bing He, Yan-Kang Jing, Li-Rong Wang, Jun-Mei Wang, Xiang-Qun Xie
With treatment benefits in both the central nervous system and the peripheral system, the medical use of cannabidiol (CBD) has gained increasing popularity. Given that the therapeutic mechanisms of CBD are still vague, the systematic identification of its potential targets, signaling pathways, and their associations with corresponding diseases is of great interest for researchers. In the present work, chemogenomics-knowledgebase systems pharmacology analysis was applied for systematic network studies to generate CBD-target, target-pathway, and target-disease networks by combining both the results from the in silico analysis and the reported experimental validations...
September 10, 2018: Acta Pharmacologica Sinica
Kun-Kun Xia, Jian-Xin Shen, Ze-Bing Huang, Hui-Min Song, Ming Gao, De-Jie Chen, Shui-Jun Zhang, Jie Wu
We recently reported that a CB2 R agonist, GW405833 (GW), reduced both the ACh-induced Ca2+ oscillations and the L-arginine-induced Ca2+ signal enhancement in mouse pancreatic acinar cells, suggesting that GW-induced inhibition may prevent the pathogenesis of acute pancreatitis. In this study, we aim to evaluate the effects of other cannabinoid ligands on Ca2+ signaling in acinar cells. Patch-clamp whole-cell recordings were applied to measure ACh-induced intracellular Ca2+ oscillations in pancreatic acinar cells acutely dissociated from wild-type (WT), CB1 R knockout (KO), and CB2 R KO mice, and the pharmacological effects of various cannabinoid ligands on the Ca2+ oscillations were examined...
September 10, 2018: Acta Pharmacologica Sinica
Qing-Rong Liu, Nicholas S Huang, Hong Qu, Jennifer F O'Connell, Isabel Gonzalez-Mariscal, Sara Santa-Cruz-Calvo, Maire E Doyle, Zheng-Xiong Xi, Yun Wang, Emmanuel S Onaivi, Josephine M Egan
Targeting peripheral CB1R is desirable for the treatment of metabolic syndromes without adverse neuropsychiatric effects. We previously reported a human hCB1b isoform that is selectively enriched in pancreatic beta-cells and hepatocytes, providing a potential peripheral therapeutic hCB1R target. It is unknown whether there are peripherally enriched mouse and rat CB1R (mCB1 and rCB1, respectively) isoforms. In this study, we found no evidence of peripherally enriched rodent CB1 isoforms; however, some mCB1R isoforms are absent in peripheral tissues...
September 10, 2018: Acta Pharmacologica Sinica
Hang Li, Zhen Wang, Mian Jiang, Run-Ping Fang, Hui Shi, Yu Shen, Xiao-Li Cai, Qian Liu, Kai Ye, Sai-Jun Fan, Wei-Ying Zhang, Li-Hong Ye
Mammalian hepatitis B X-interacting protein (HBXIP) is an 18-kDa protein that regulates a large number of transcription factors such as TF-IID, E2F1, SP1, STAT3, c-Myc, and LXR by serving as an oncogenic transcription coactivator and plays an important role in the development of breast cancer. We previously showed that HBXIP as an oncoprotein could enhance the promoter activity of MDM2 through coactivating p53, promoting the MDM2 transcription in breast cancer. In this study we investigated the molecular mechanisms underlying the modulation of MDM2/p53 interaction by HBXIP in human breast cancer MCF-7 cells in vitro and in vivo...
September 4, 2018: Acta Pharmacologica Sinica
Yong-Qing Liu, Shi-Kang Wang, Qing-Qing Xu, Hui-Qing Yuan, Yan-Xia Guo, Qian Wang, Feng Kong, Zhao-Min Lin, De-Qing Sun, Rong-Mei Wang, Hong-Xiang Lou
Acquired docetaxel-resistance of prostate cancer (PCa) remains a clinical obstacle due to the lack of effective therapies. Acetyl-11-keto-β-boswellic acid (AKBA) is a pentacyclic triterpenic acid isolated from the fragrant gum resin of the Boswellia serrata tree, which has shown intriguing antitumor activity against human cell lines established from PCa, colon cancer, malignant glioma, and leukemia. In this study, we examined the effects of AKBA against docetaxel-resistant PCa in vitro and in vivo as well as its anticancer mechanisms...
August 31, 2018: Acta Pharmacologica Sinica
Matthew E Sloan, Caroline W Grant, Joshua L Gowin, Vijay A Ramchandani, Bernard Le Foll
Endocannabinoid signaling is implicated in an array of psychopathologies ranging from anxiety to psychosis and addiction. In recent years, radiotracers targeting the endocannabinoid system have been used in positron emission tomography (PET) studies to determine whether individuals with psychiatric disorders display altered endocannabinoid signaling. We comprehensively reviewed PET studies examining differences in endocannabinoid signaling between individuals with psychiatric illness and healthy controls. Published studies evaluated individuals with five psychiatric disorders: cannabis use disorder, alcohol use disorder, schizophrenia, post-traumatic stress disorder, and eating disorders...
August 30, 2018: Acta Pharmacologica Sinica
Ji-Hyun Lee, Pyo-Yoon Kang, Young-Eun Jang, Eun-Hee Kim, Jin-Tae Kim, Hee-Soo Kim
It is essential to monitor the end-tidal carbon dioxide (ETCO2 ) during general anesthesia and adjust the tidal volume and respiratory rate (RR). For the purpose of this study, we used a population pharmacodynamic modeling approach to establish the relationship between RR versus ETCO2 data during general anesthesia in children, and to identify the clinical variables affecting this relationship. A prospective observational study was designed to include 51 patients (aged ≤ 12 years), including users of antiepileptic drugs (levetiracetam, valproic, or phenobarbital (n = 21)) and non-users (n = 30), scheduled to receive general anesthesia during elective surgery...
August 30, 2018: Acta Pharmacologica Sinica
Cong Wang, Ying Li, Yong-Wen Li, Hong-Bing Zhang, Hao Gong, Yin Yuan, Wei-Ting Li, Hong-Yu Liu, Jun Chen
The abnormal expression of the long noncoding RNA (lncRNA) HOX transcript intergenic antisense RNA (HOTAIR) plays an important role in the development of various cancers; however, single nucleotide polymorphisms (SNPs) in HOTAIR and their association with primary lung cancer susceptibility have not yet been reported. Here, we performed a case-control study including 262 primary lung cancer patients and 451 cancer-free control individuals to investigate the association between four haplotype-tagging SNPs (rs920778, rs12826786, rs4759314, and rs1899663) in the HOTAIR lncRNA and the risk of developing primary lung cancer...
August 28, 2018: Acta Pharmacologica Sinica
Xiao-Juan Quan, Chun-Lian Liang, Ming-Zhu Sun, Lin Zhang, Xiu-Li Li
Hyperglycemia is a major factor in vascular endothelial injury that finally leads to a cardiovascular event. Steroid receptor coactivators (SRCs) are a group of non-DNA binding proteins that induce structural changes in steroid receptors (nuclear receptors) critical for transcriptional activation. SRCs, namely, SRC-1, SRC-2, and SRC-3, are implicated in the regulation of vascular homeostasis. In this study we investigate the role of SRCs in hyperglycemia-induced endothelial injury. Aortic endothelial cells were prepared from normal and diabetic rats, respectively...
August 8, 2018: Acta Pharmacologica Sinica
Shou-Yan Wu, Shi-Chao Cui, Le Wang, Yi-Ting Zhang, Xiao-Xia Yan, Heng-Lei Lu, Guo-Zhen Xing, Jin Ren, Li-Kun Gong
Cholestasis is a common feature of liver injury, which manifests as bile acid excretion and/or enterohepatic circulation disorders. However, very few effective therapies exist for cholestasis. Recently, 18β-Glycyrrhetinic acid (18b-GA), a major metabolic component of glycyrrhizin, which is the main ingredient of licorice, was reported to protect against alpha-naphthylisothiocyanate (ANIT)-induced cholestasis. However, its protective mechanism remains unclear. We hypothesized that 18b-GA may stimulate the signaling pathway of bile acid (BA) transportation in hepatocytes, resulting its hepatoprotective effect...
July 30, 2018: Acta Pharmacologica Sinica
Xin-Wei Liu, Jun-Ling Yang, Wei Niu, Wei-Wei Jia, Olajide E Olaleye, Qi Wen, Xiao-Na Duan, Yü-Hong Huang, Feng-Qing Wang, Fei-Fei Du, Chen-Chun Zhong, Yan-Fen Li, Fang Xu, Qi Gao, Li Li, Chuan Li
Terpene lactones are a class of bioactive constituents of standardized preparations of Ginkgo biloba leaf extract, extensively used as add-on therapies in patients with ischemic cardiovascular and cerebrovascular diseases. This investigation evaluated human pharmacokinetics of ginkgo terpene lactones and impact of their carboxylation in blood. Human subjects received oral YinXing-TongZhi tablet or intravenous ShuXueNing, two standardized ginkgo preparations. Their plasma protein-binding and platelet-activating factor antagonistic activity were assessed in vitro...
July 27, 2018: Acta Pharmacologica Sinica
Di Ge, Hong-Wei Yue, Hong-Hong Liu, Jing Zhao
Sphingosylphosphorylcholine (SPC) is a bioactive sphingolipid in blood plasma that is metabolized from the hydrolysis of the membrane sphingolipid. SPC maintains low levels in the circulation under normal conditions, which makes studying its origin and action difficult. In recent years, however, it has been revealed that SPC may act as a first messenger through G protein-coupled receptors (S1P1-5 , GPR12) or membrane lipid rafts, or as a second messenger mediating intracellular Ca2+ release in diverse human organ systems...
July 26, 2018: Acta Pharmacologica Sinica
Maria Scherma, Paolo Masia, Valentina Satta, Walter Fratta, Paola Fadda, Gianluigi Tanda
Anandamide is a lipid mediator that acts as an endogenous ligand of CB1 receptors. These receptors are also the primary molecular target responsible for the pharmacological effects of Δ9-tetrahydrocannabinol, the psychoactive ingredient in Cannabis sativa. Several studies demonstrate that anandamide exerts an overall modulatory effect on the brain reward circuitry. Several reports suggest its involvement in the addiction-producing actions of other abused drugs, and it can also act as a behavioral reinforcer in animal models of drug abuse...
July 26, 2018: Acta Pharmacologica Sinica
Grace Qun Gong, Ke Wang, Xin-Chuan Dai, Yan Zhou, Rajesh Basnet, Yi Chen, De-Hua Yang, Woo-Jeong Lee, Christina Maree Buchanan, Jack Urquhart Flanagan, Peter Robin Shepherd, Ying Chen, Ming-Wei Wang
The serum and glucocorticoid-regulated kinase (SGK) family has been implicated in the regulation of many cellular processes downstream of the PI3K pathway. It plays a crucial role in PI3K-mediated tumorigenesis, making it a potential therapeutic target for cancer. SGK family consists of three isoforms (SGK1, SGK2, and SGK3), which have high sequence homology in the kinase domain and similar substrate specificity with the AKT family. In order to identify novel compounds capable of inhibiting SGK3 activity, a high-throughput screening campaign against 50,400 small molecules was conducted using a fluorescence-based kinase assay that has a Z' factor above 0...
July 23, 2018: Acta Pharmacologica Sinica
Hong-Mei Liu, Yi Jia, Ying-Xian Zhang, Jun Yan, Ning Liao, Xiao-Hui Li, Yuan Tang
Pulmonary arterial hypertension (PAH) is the most common form of pulmonary hypertension. Pulmonary arterial remodeling is closely related to the abnormal proliferation of pulmonary artery smooth muscle cells (PASMCs), which leads to the thickening of the medial layer of muscular arteries and then results in the narrowing or occlusion of the precapillary arterioles and PAH. However, the mechanisms underlying the abnormal proliferation of PASMCs remain unclear. In this study, we established rat primary PAH models using monocrotaline (MCT) injection or hypoxic exposure, then investigated the expression patterns of seven miRNAs associated with multiple pathogenic pathways central to pulmonary hypertension, and further explored the roles and the possible mechanisms of miR-135a during the development of PAH...
July 23, 2018: Acta Pharmacologica Sinica
Bo Yin, Xu-Wei Hou, Mei-Li Lu
Astragaloside IV (AsIV) is an active saponin extracted from Astragalus membranaceus, which has shown cardioprotective effects in a number of experimental animals. In this study we investigated the molecular mechanisms by which AsIV attenuated the myocardial ischemia reperfusion (MI/R)-induced injury in vitro and in vivo by focusing on calcium-sensing receptor (CaSR) and extracellular signal-regulated kinase 1/2 (ERK1/2). Rat neonatal cardiac myocytes were subjected to a hypoxia/reoxygenation (H/R) procedure in vitro, which significantly decreased the cell viability, increased lactate dehydrogenase (LDH) release, induced cardiomyocyte apoptosis, and increased [Ca2+ ]i ...
July 20, 2018: Acta Pharmacologica Sinica
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