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Sheng Li, Yuhua Qu, Xiu-Yin Shen, Ting Ouyang, Wen-Bin Fu, Tao Luo, Hua-Qiao Wang
BACKGROUND: Crocetin is a carotenoid extracted from the traditional Chinese medical herb saffron. Previous studies have demonstrated that crocetin possesses anticancer properties that are effective against various cancers. As an extension of our earlier study, the present study explored the underlying mechanisms in crocetin's anticancer effect on KYSE-150 cells. The phosphatidylinositol-3-kinase (PI3K)/protein kinase B (AKT), Mitogen-activated protein kinases (MAPK), and p53/p21 signal pathways play an important role in carcinogenesis, progression, and metastasis of carcinoma cells...
February 15, 2019: Pharmacology
Fan Zhang, Yani Liu, Dandan Zhang, Xizhenzi Fan, Decheng Shao, Han Li
Osteoarthritic pain has a strong impact on patients' quality of life. Understanding the pathogenic mechanisms underlying osteoarthritic pain will likely lead to the development of more effective treatments. In the present study of osteoarthritic model rats, we observed a reduction of M-current density and a remarkable decrease in the levels of KCNQ2 and KCNQ3 proteins and mRNAs in dorsal root ganglia (DRG) neurons, which were associated with hyperalgesic behaviors. The activation of KCNQ/M channels with flupirtine significantly increased the mechanical threshold and prolonged the withdrawal latency of osteoarthritic model rats at 3-14 days after model induction, and all effects of flupirtine were blocked by KCNQ/M-channel antagonist, XE-991...
February 13, 2019: Pharmacology
Eri Usugi, Kenichiro Ishii, Yoshifumi Hirokawa, Kazuki Kanayama, Chise Matsuda, Katsunori Uchida, Taizo Shiraishi, Masatoshi Watanabe
BACKGROUND: Pirfenidone (PFD), which is an antifibrotic agent used for treatment of idiopathic pulmonary fibrosis, induces G0/G1 cell cycle arrest in fibroblasts. We hypothesized that PFD-induced G0/G1 cell cycle arrest might be achieved in other types of cells, including cancer cells. Here we investigated the effects of PFD on the proliferation of pancreatic cancer cells (PCCs) in vitro. METHOD: Human skin fibroblasts ASF-4-1 cells and human prostate stromal cells (PrSC) were used as fibroblasts...
February 7, 2019: Pharmacology
Adriana Papiez, Klara Odehnalova, Vladimir Sramek, Pavel Suk
BACKGROUND/AIMS: Administration of tablets via feeding tube (FT) is often associated with significant drug losses, as was confirmed by weighing. The aim of this study was to measure the proportion of active substance losses (ASLs) in an in vitro model. METHODS: A film-coated tablet (FilmCT) containing clopidogrel (Trombex®) and a tablet with enteric coating (EntericCT) containing pantoprazole (Controloc®) were crushed in a mortar and transferred by method A (tablet powder was transferred into the beaker, poured into the syringe and water added) and method B (water was added into the mortar, suspension drawn into the syringe) and administered via FT in an in vitro model...
February 6, 2019: Pharmacology
Kentaro Higashi, Asami Mori, Kenji Sakamoto, Kunio Ishii, Tsutomu Nakahara
We examined the effect of probucol, an antihyperlipidemic drug with potent antioxidant properties, on cataract formation in streptozotocin (STZ)-induced hyperglycemic rats that were given 5% D-glucose as drinking water. Probucol treatment was initiated immediately after the induction of hyperglycemia was confirmed. Using full horizontal-plane lens images captured with an original digital camera system, the opacity of central region of lens was assessed by measuring the opaque area in the region. Central opacities were detected after 3 weeks of hyperglycemia, and progressed in a time-dependent manner...
February 5, 2019: Pharmacology
Marwan Abdel-Latif Ibrahim, Alaa-Eldin Salah-Eldin
AIM: The present study aimed to elucidate the effects of tramadol on the testicular functions of adult male rats due to the chronic usage of tramadol and the effect of its withdrawal. METHOD: Adult male albino rats were classified into the following 3 groups: (I) a control administered with normal saline and (II) tramadol-treated rats (40 mg/kg b.w. orally) for 21 successive days; and (III) like the rats in the second group but kept for 4 weeks after the last tramadol dose to study the effect of tramadol withdrawal...
January 30, 2019: Pharmacology
Xiao-Jun Fu, Shuang-Yan Hu
BACKGROUND: Systemic oxidative stress has been reported to play a central role in the pathogenesis of kidney function decline. The nuclear factor erythroid 2-related factor 2 (Nrf2)/antioxidant response element (ARE) pathway is one of the important endogenous antioxidant stress pathways in cells. This study aims to investigate whether shenduning granule can ameliorate oxidative stress in kidney tissues by activating the Nrf2/ARE pathway, and explores the detailed underlying mechanism...
January 30, 2019: Pharmacology
Seham Mustafa, Abdelhamid H Elgazzar, Nabil Kamal
BACKGROUND AND OBJECTIVE: Calcium channel blockers (CCBs) are among the most widely used prescribed drugs for the treatment of cardiovascular diseases. The present study investigates the effect of verapamil, which is most commonly used as a CCB, on kidney function using radionuclide imaging. METHODS: Ten New Zealand white rabbits were used in vitro (4) and in vivo (6) studies. Isometric tensions were recorded for isolated renal artery ring segments, while renographic studies were performed using Technetium-99m mercaptoacetyltriglycine and Gamma camera...
January 29, 2019: Pharmacology
Georg Hagn, Robert Westhofen, Ian Burkovskiy, Bruce Holbein, Juan Zhou, Christian Lehmann
Interstitial cystitis (IC) is a highly prevalent debilitating disease, with its cardinal symptoms being severe pain, urinary urgency and frequency. The associated pain may eventually lead as a last resort to removal of the bladder. Though the initial trigger for IC remains largely unknown, we propose novel iron chelators as a possible new treatment for this disease. Iron is a mandatory component for the generation of reactive oxygen species (ROS). A substantial decrease in ROS production and thus inflammation can be achieved by effectively sequestering host iron, which we believe may improve outcome and quality of life in IC patients...
January 29, 2019: Pharmacology
Keisuke Obara, Mayumi Michino, Masataka Ito, Lin Ao, Ayano Sawada, Fumiko Yamaki, Kazuhiro Matsuo, Takashi Yoshio, Yoshio Tanaka
BACKGROUND: A report examining whether clinically available antidepressants increase urethral smooth muscle contraction via antagonistic effects on the α2-adrenoceptor (α2-AR) is lacking. OBJECTIVES: The present study was performed to evaluate the potential of clinically available antidepressants to reverse α2-AR-mediated contractile inhibition in rat vas deferens, in order to predict whether they can induce voiding impairment. METHOD: The effects of 18 antidepressants of different classes on electrical field stimulation (EFS)-induced contractions suppressed by 10-8 mol/L clonidine (a selective α2-AR agonist) in isolated rat vas deferens were investigated and related to their respective clinical blood concentrations...
January 29, 2019: Pharmacology
Tobias Schupp, Michael Behnes, Dominik Ellguth, Julian Müller, Linda Reiser, Armin Bollow, Gabriel Taton, Thomas Reichelt, Niko Engelke, Seung-Hyun Kim, Christoph Nienaber, Muharrem Akin, Kambis Mashayekhi, Thomas Bertsch, Martin Borggrefe, Ibrahim Akin
OBJECTIVE: The study sought to assess the long-term prognostic impact of different pharmacotherapies, including angiotensin-converting enzyme inhibitor-inhibitor/angiotensin receptor blocker (ACEi/ARB), statins, and amiodarone in patients with electrical storm (ES). BACKGROUND: Data regarding the outcome of patients with ES is limited. METHODS: Consecutive patients with ES from 2002 to 2016 were included. Patients on ACEi/ARB were compared to patients without ACEi/ARB, respectively, for statin and amiodarone therapy...
January 29, 2019: Pharmacology
Zheng Ding, Huifeng Shi, Wei Yang
OBJECTIVES: Present investigation determines the protective effect of cimiracemate A against glucocorticoid-induced osteoporosis rat. METHODS: Osteoporosis was induced by injecting methylprednisolone acetate (21 mg/kg) for the period of 6 weeks, and the rats were treated with cimiracemate A 5 and 10 mg/kg, p.o. 60 min after the administration of methylprednisolone acetate (21 mg/kg) for the duration of 6 weeks. Effect of cimiracemate A was observed by estimating the microarchitecture of bone and histopathological changes by micro-CT scan and light microscope...
January 29, 2019: Pharmacology
Li Wu, Lu Li, Fang Wang, Xianwei Wu, Xin Zhao, Na Xue
The present manuscript intended to investigate the anti-inflammatory effect of ropivacaine on lipopolysaccharide-induced inflammation in RAW 264.7 macrophages. Results suggested that ropivacaine causes significant inhibition of generation of nitric oxide (NO), prostaglandin E2, tumor necrosis factor (TNF)-α, interleukin (IL)-6, and IL-1β, as well as expression of their synthesizing enzymes, inducible NO synthase, and cyclooxygenase-2. Moreover, ropivacaine causes inhibition of mitogen-activated protein kinases as well as nuclear factor-kappa B signaling pathway and apoptosis in RAW 264...
January 28, 2019: Pharmacology
Takeaki Wajima, Reina Kinugawa, Tetsuya Yamada, Hideaki Ikoshi, Norihisa Noguchi
BACKGROUND: In traditional Chinese medicine, Panax notoginseng is used to treat inflammation and bleeding but has not been shown to affect bacterial pathogens. OBJECTIVES: Our aim was to assess the antibacterial potential of Panax notoginseng extract (PNE) against bacterial pathogens. METHODS: PNE was dissolved in autoclaved distilled water. Antimicrobial activity was measured by the disc diffusion test and bacterial growth curve assays, in which the concentration of bacterial colony forming units was monitored at several time points in the presence or absence of PNE...
January 28, 2019: Pharmacology
Yu-Sheng Chen, Quan-Zhan Chen, Zhen-Jiong Wang, Chun Hua
BACKGROUND: Ganoderma lucidum Polysaccharides (GLPS) were found to possess various pharmacological properties including anti-inflammatory and hepatoprotective activities. However, the effect and possible mechanism of GLPS treatment on liver injury have not yet been reported. Therefore, this study aimed to explore the potential anti-inflammatory and hepatoprotective effects and possible mechanism of GLPS in carbon tetrachloride (CCl4)-induced acute liver injury mice. SUMMARY: GLPS significantly reduced the activation of NLRP3 inflammasome and improved liver function in liver injury mice...
January 23, 2019: Pharmacology
Emese Bogáthy, Diana Kostyalik, Peter Petschner, Szilvia Vas, Gyorgy Bagdy
The endocannabinoid and serotonin (5-HT) systems have key roles in the regulation of several physiological functions such as motor activity and food intake but also in the development of psychiatric disorders. Here we tested the hypothesis, whether blockade of serotonin 2C (5-HT2C) receptors prevents the reduced locomotor activity and other behavioral effects caused by a cannabinoid 1 (CB1) receptor antagonist. As a pretreatment, we administered SB-242084 (1 mg/kg, ip.), a 5-HT2C receptor antagonist or vehicle (VEH) followed by the treatment with AM-251 (5 or 10 mg/kg, ip...
January 23, 2019: Pharmacology
Guizhen Guo, Qing Zhao, Qinghua Wang, Enze Li
To investigate the effect of Tanshinone IIA (TSA) on viral myocarditis (VMC). VMC animal model was established using BALB/c mice by intraperitoneally injecting Coxsackie virus B3 (CVB3). The mice were randomly divided into control group, model group, and TSA group. We detected the survival rate, the heart weight to body weight (HW/BW) ratio and hemodynamic and cardiac function parameters. The pathological features of VMC were measured through H&E staining. The expression of serum enzyme, inflammatory cytokines, and T helper (Th)1/Th2 markers was also investigated...
January 2, 2019: Pharmacology
Xiaoli Song, Gang Dong, Yun Zhou
Isofraxidin is a Coumarin compound widely distributed in plants, such as the Umbelliferae or Chloranthaceae, and it possesses numerous pharmacological activities. However, whether isofraxidin affects the activity of human liver cytochrome P450 (CYP) enzymes remains unclear. In this study, the inhibitory effects of isofraxidin on the 8 human liver CYP isoforms (i.e., 1A2, 3A4, 2A6, 2E1, 2D6, 2C9, 2C19, and 2C8) were investigated in vitro using human liver microsomes. The results showed that isofraxidin inhibited the activity of CYP1A2, 3A4, and 2E1, with IC50 values of 23...
December 13, 2018: Pharmacology
Mohammad Raziya Banu, Muhammed Ibrahim, K Prabhu, Srinivasagam Rajasankar
Withaferin A (WA) was evaluated for its neuro-protective efficacy on ageing induced striatal dopamine (DA) and behavioural changes in aged rats. Wistar albino rats were divided into group I - young (3 months), Group II - aged (24 months), Group III - aged rats supplemented with WA (50 mg/kg b.w once in a day for 30 days) and Group IV - young rats supplemented with WA (50 mg/kg b.w). The HPLC assay revealed significant decline in the levels of DA and homovanillic acid (HVA) in substantia nigra (SN) and striatum (ST) of aged rat...
December 13, 2018: Pharmacology
Gabriele Cortellini, Domenico Lippolis, Silvia Amati, Giancarlo Piovaccari, Fabio Cortellini, Giorgio Ballardini
To date, aspirin desensitization is employed with patients with nonsteroidal anti-inflammatory drugs (NSAIDs) exacerbated respiratory diseases (NERD) or with aspirin or NSAIDs hypersensitive patients needing a stent procedure for coronary artery disease. On the other hand, few data exist regarding aspirin desensitization in other cardiological features and particularly we haven't data on different NSAIDs desensitization. Only for NERD patients we have data on ketorolac use. We report an efficacious desensitization procedure for ibuprofen in urticaria/angioedema patient with pericarditis and myocarditis associated...
December 13, 2018: Pharmacology
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