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Pharmacology

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https://www.readbyqxmd.com/read/28930747/quantification-of-bisoprolol-and-metoprolol-in-simultaneous-human-serum-and-cerebrospinal-fluid-samples
#1
Ali Sigaroudi, Martina Kinzig, Oliver Wahl, Christoph Stelzer, Michael Schroeter, Uwe Fuhr, Ulrike Holzgrabe, Fritz Sörgel
BACKGROUND: Bisoprolol and metoprolol are moderately lipophilic, beta(1)-selective betablockers reported to cause adverse effects in the central nervous system (CNS), such as sleep disturbance, suggesting that both drugs may reach relevant concentrations in the brain. CNS beta(2)-receptor blockade has been suspected to be related to such effects. The higher molecular size of bisoprolol (325 Dalton) and the higher beta(1)-selectivity compared to metoprolol (267 Dalton) would suggest a lower rate of CNS effects...
September 21, 2017: Pharmacology
https://www.readbyqxmd.com/read/28926842/pharmacotherapy-with-thymoquinone-improved-pancreatic-%C3%AE-cell-integrity-and-functional-activity-enhanced-islets-revascularization-and-alleviated-metabolic-and-hepato-renal-disturbances-in-streptozotocin-induced-diabetes-in-rats
#2
Adel Galal El-Shemi, Osama Adnan Kensara, Aiman Alsaegh, Mohammed Hasan Mukhtar
AIMS: This study is aimed at evaluating the antidiabetic effects of thymoquinone (TQ) on streptozotocin (STZ)-induced diabetes in rats, and exploring the possible underlying mechanisms. METHODS: Diabetes was induced in adult male Wistar rats by intraperitoneal injection of freshly prepared STZ (65 mg/kg). After disease induction, 42 rats were equally assigned to: controls, STZ-diabetic group, and STZ-diabetic group treated with oral TQ (35 mg/kg/day) for 5 weeks...
September 20, 2017: Pharmacology
https://www.readbyqxmd.com/read/28926841/beneficial-combination-of-lacosamide-with-retigabine-in-experimental-animals-an-isobolographic-analysis
#3
Jarogniew J Luszczki, Mirosław Zagaja, Barbara Miziak, Maria W Kondrat-Wrobel, Katarzyna Zaluska, Paula Wroblewska-Luczka, Piotr Adamczuk, Stanislaw J Czuczwar, Magdalena Florek-Luszczki
BACKGROUND/AIM: To isobolographically determine the types of interactions that occur between retigabine and lacosamide (LCM; two third-generation antiepileptic drugs) with respect to their anticonvulsant activity and acute adverse effects (sedation) in the maximal electroshock-induced seizures (MES) and chimney test (motor performance) in adult male Swiss mice. METHODS: Type I isobolographic analysis for nonparallel dose-response effects for the combination of retigabine with LCM (at the fixed-ratio of 1:1) in both the MES and chimney test in mice was performed...
September 20, 2017: Pharmacology
https://www.readbyqxmd.com/read/28898893/effects-of-artesunate-on-the-expressions-of-insulin-like-growth-factor-1-osteopontin-and-c-telopeptides-of-type-ii-collagen-in-a-rat-model-of-osteoarthritis
#4
Zhe Bai, Xiao-Hui Guo, Chi Tang, Si-Tong Yue, Long Shi, Bo Qiang
OBJECTIVE: The study aims to explore the effects of artesunate on insulin-like growth factor-1 (IGF-1), Osteopontin (OPN), and C-telopeptides of type II collagen (CTX-II) in serum, synovial fluid (SF), and cartilage tissues of rats with osteoarthritis (OA). METHODS: OA models were established. Normal model, artesunate, and Viatril-S groups (20 rats respectively) were set. Enzyme-linked immunosorbent assay, IHC staining, and quantitative real-time polymerase chain reaction were conducted to calculate IGF-1, OPN, and CTX-II levels in serum, SF, and cartilage tissues of rats...
September 13, 2017: Pharmacology
https://www.readbyqxmd.com/read/28848223/mechanistic-evaluation-of-the-protective-effect-of-carnosine-on-acute-lung-injury-in-sepsis-rats
#5
Chenliang Sun, Qinfeng Wu, Xuejie Zhang, Qianru He, Hongsheng Zhao
This study analyzes the sepsis healing therapeutic potential of carnosine against experimentally sepsis-induced male albino rats. Carnosine in 2 different doses, 25 mg/kg and 50 mg/kg, were administered for 30 consecutive days. At the end of the treatment, lipid peroxidation, catalase, superoxide dismutase, glutathione peroxidase and myeloperoxidase activities were measured. Lungs weight and total protein content were determined in the bronchoalveolar fluid (BALF). Cytokines such as macrophage inhibitory factor (MIF), interleukin-8 (IL-8) and tumour necrosis factor-alpha (TNF-α) were determined in the BALF...
August 25, 2017: Pharmacology
https://www.readbyqxmd.com/read/28848215/inhibitory-effect-of-citalopram-on-the-pharmacokinetics-of-carvedilol-in-rats-and-in-vitro-models
#6
Maria Bianca Abrudan, Dana Maria Muntean, Daniela Saveta Popa, Ana-Maria Gheldiu, Maria Adriana Neag, Laurian Vlase
BACKGROUND/AIMS: The aim of this study was to investigate the drug-drug interaction between carvedilol and citalopram based on carvedilol metabolism in vitro and his pharmacokinetics (PKs) in vivo after the oral administration of the single drug and both drugs, and reveal citalopram effects on the PKs of carvedilol. METHODS: Each rat was cannulated on the femoral vein, prior to being connected to BASi Culex ABC®. Carvedilol was orally administrated in rats (3.57 mg/kg body weight [b...
August 19, 2017: Pharmacology
https://www.readbyqxmd.com/read/28848138/heat-shock-protein-27-a-novel-regulator-of-transforming-growth-factor-%C3%AE-induced-resistance-to-cisplatin-in-a549-cell
#7
Zhicheng Huang, Changliang Yang, Shuangyan Sun, Yingji Nan, Zhiguo Lang, Xiu Wang, Jihong Zhao, Ying Liu
Lung cancer is one of the major causes of cancer morbidity and mortality around the world, and the resistance to cisplatin is a critical issue to chemotherapy in lung cancer patients. Transforming growth factor β (TGF-β) signal pathway abnormality is widely observed in drug resistance during lung cancer chemotherapy. Here, we investigated the effects of heat-shock protein 27 (HSP27) in the TGF-β-induced cisplatin resistance in lung cancer cell. In this study, our results indicated that the mRNA and protein expression of HSP27 were significantly increased in human lung cancer tissues...
August 19, 2017: Pharmacology
https://www.readbyqxmd.com/read/28810242/mir-490-5p-suppresses-cell-proliferation-and-invasion-by-targeting-bub1-in-hepatocellular-carcinoma-cells
#8
Bin Xu, Tangpeng Xu, Huali Liu, Qian Min, Shidong Wang, Qibin Song
OBJECTIVE: To verify that miR-490-5p could influence hepatocellular carcinoma (HCC) cells' proliferation, invasion, cycle, and apoptosis by targeting BUB1. METHODS: Quantitative real time-PCR (QRT-PCR) was used to determine the miR-490-5p expression. Immunohistochemistry, qRT-PCR, and Western blot were employed to detect BUB1 and transforming growth factor-beta (TGFβ/Smad) signaling-related proteins expression in hepatic tissues and cells. The luciferase assay was used to confirm the targeting relationship between miR-490-5p and BUB1...
August 16, 2017: Pharmacology
https://www.readbyqxmd.com/read/28797008/resveratrol-attenuates-adriamycin-induced-focal-segmental-glomerulosclerosis-through-c3ar-c5ar-sphingosine-kinase-1-pathway
#9
Guoyong Liu, Qiang Wang, Yan Shi, Xiaofei Peng, Hong Liu, Youming Peng, Liyu He
BACKGROUND/AIM: Focal segmental glomerulosclerosis (FSGS) typically presents with nephrotic range proteinuria, which could eventually develop into end-stage renal disease. Resveratrol (RSV) is a natural polyphenol compound, which has been reported to suppress inflammatory response and renal interstitial fibrosis. This study is aimed at evaluating the renoprotective effect of RSV treatment on adriamycin-induced FSGS. METHODS: In Balb/c mice, adriamycin nephropathy was induced by adriamycin (10 mg/kg body weight, diluted in normal saline) via a tail vein on day 0...
August 11, 2017: Pharmacology
https://www.readbyqxmd.com/read/28797006/amiloride-is-effective-in-the-management-of-abiraterone-induced-mineralocorticoid-excess-syndrome-without-interfering-with-its-antineoplastic-activity
#10
Francesca Bedussi, Diego Galli, Martina Fragni, Francesca Valcamonico, Elisa Rossini, Alberto Dalla Volta, Sara Vezzoli, Elisa Roca, Vittorio Ferrari, Barbara Lazzari, Maurizio Memo, Sandra Sigala, Alfredo Berruti
BACKGROUND: The administration of abiraterone acetate (abiraterone) leads to an adrenocorticotropic hormone (ACTH)-driven increase in mineralocorticoid hormones, requiring glucocorticoid supplementation that may stimulate the growth of prostate cancer (PCa). Amiloride is a drug that selectively reduces the aldosterone-sensitive Na+/K+ exchange and could be effective in the management of mineralocorticoid excess syndrome (MCES). METHODS: The efficacy of amiloride + hydrochlorothiazide (HCT) in the clinical management of abiraterone-induced MCES was assessed in 5 consecutive patients with castration-resistant PCa (CRPC)...
August 11, 2017: Pharmacology
https://www.readbyqxmd.com/read/28793305/paclitaxel-promotes-cell-apoptosis-in-uterine-leiomyomas
#11
Haiping Liu, Jianye Wang, Lianbing Sheng, Yan Zhang, Ning Tang, Yunfei Li, Tianyu Hao
Uterine leiomyomas are common clinical gynecological tumors, which are a major health concern for many women. In the current study, we aimed to investigate the effect of paclitaxel (PTX) on uterine leiomyomas. A mouse model of uterine leiomyomas was established by estradiol benzoate, followed by treatment with increasing doses of PTX. PTX showed no dose-limiting toxicity that affected the survival of mice, and was able to restore the apoptosis level of uterus tissues of the model mice to normal levels. In this study, we discovered that PTX played a critical role in promoting apoptosis in the mouse model of uterine leiomyomas, which provides a new insight into the therapy of uterine leiomyomas...
August 10, 2017: Pharmacology
https://www.readbyqxmd.com/read/28743115/cerebrospinal-fluid-levels-of-14-3-3-gamma-what-does-it-tell-us-about-sporadic-creutzfeldt-jakob-disease
#12
Christian Humpel, Thomas Benke
Clinical diagnosis of Creutzfeldt-Jakob disease (CJD) can be supported by the analysis of Tau and 14-3-3 in the cerebrospinal fluid (CSF). In this short report, we report about a retrospective analysis performed on 2,296 routinely collected CSF samples, and 44 samples with a ratio of phosphoTau181/Tau <0.075 were selected. Analysis was performed with a novel 14-3-3 gamma CircuLex Elisa. We show that control levels were around 6,000 AU/mL and samples from Alzheimer patients were not different from those collected from healthy controls...
July 26, 2017: Pharmacology
https://www.readbyqxmd.com/read/28743107/a-prozone-like-effect-influences-the-efficacy-of-the-monoclonal-antibody-abt-700-against-the-hepatocyte-growth-factor-receptor
#13
Kedar S Vaidya, Anatol Oleksijew, Lora A Tucker, William N Pappano, Mark G Anderson, Christine M Grinnell, Qian Zhang, Sarah J Heighton, Michael J Mitten, Sasmita Mishra, Joann P Palma, Jieyi Wang, Edward B Reilly, Erwin R Boghaert
ABT-700 is a therapeutic antibody against the hepatocyte growth factor receptor (MET). At doses or regimens that lead to exposures exceeding optimum in vivo, the efficacy of ABT-700 is unexpectedly reduced. We hypothesized that this reduction in efficacy was due to a "prozone-like" effect in vivo. A prozone-like effect, which is a reduction in efficacy beyond optimum exposure, is caused due a mechanism similar to the generation of false negative flocculation tests by excessive antibody titres. In vitro, we demonstrate that at higher ABT-700 concentrations, this "prozone-like" effect is mediated by a progressive conversion from bivalent to ineffective monovalent binding of the antibody...
July 26, 2017: Pharmacology
https://www.readbyqxmd.com/read/28728159/oxamate-enhances-the-anti-inflammatory-and-insulin-sensitizing-effects-of-metformin-in-diabetic-mice
#14
Mu-Chao Wu, Wei-Ran Ye, Yi-Jia Zheng, Shan-Shan Zhang
Metformin (MET) is the first-line drug for treating type 2 diabetes mellitus (T2DM). However, MET increases blood lactate levels in patients with T2DM. Lactate possesses proinflammatory properties and causes insulin resistance (IR). Oxamate (OXA), a lactate dehydrogenase inhibitor, can decrease tissue lactate production and blood lactate levels. This study was conducted to examine the effects of the combination of OXA and MET on inflammation, and IR in diabetic db/db mice. Supplementation of OXA to MET led to lowered tissue lactate production and serum lactate levels compared to MET alone, accompanied with further decreased tissue and blood levels of pro-inflammatory cytokines, along with better insulin sensitivity, beta-cell mass, and glycemic control in diabetic db/db mice...
July 21, 2017: Pharmacology
https://www.readbyqxmd.com/read/28723688/trigonelline-inhibits-inflammation-and-protects-%C3%AE-cells-to-prevent-fetal-growth-restriction-during-pregnancy-in-a-mouse-model-of-diabetes
#15
Ji-Yin Zhou, Xiao-Huang Du, Zuo Zhang, Gui-Sheng Qian
BACKGROUND: As an active component from traditional Chinese medicine, trigonelline has a protective effect on diabetes. This study evaluated the protective effects of trigonelline on diabetic mice during pregnancy. METHODS: Diabetes was induced in female mice by intraperitoneal injection for continuous 5-day of 40 mg/kg/day streptozotocin. Female mice were divided into 4 groups after they were allowed to mate with normal male mice: nondiabetic, nondiabetic treated with trigonelline (70 mg/kg) for 18 days, diabetic, and diabetic treated with trigonelline (70 mg/kg)...
July 20, 2017: Pharmacology
https://www.readbyqxmd.com/read/28728150/fisher-discrimination-of-metabolic-changes-in-rats-treated-with-aspirin-and-ibuprofen
#16
Jing Zhang, Huanchun Song, Shuying Jiang, Zhibin Chen, Shuhua Tong, Feiyan Lin, Congcong Wen, Xiuhua Zhang, Lufeng Hu
BACKGROUND: Aspirin and ibuprofen are the most frequently prescribed non-steroidal anti-inflammatory drugs in the world. However, both are associated with a variety of toxicities. We applied serum metabonomics and Fisher discrimination for the early diagnosis of its toxic reaction in order to help diagnose these toxicities. METHODS: A total of 45 rats were randomly divided into Control group, Aspirin group, and Ibuprofen groups. The experiment groups were given intragastric aspirin (15 mg/kg) or ibuprofen (15 mg/kg) for 3 weeks...
2017: Pharmacology
https://www.readbyqxmd.com/read/28715803/antinociceptive-effects-of-isosakuranetin-in-a-rat-model-of-peripheral-neuropathy
#17
Shushan Jia, Yong Zhang, Jingui Yu
Chronic pain remains a challenging clinical reality, yet currently available analgesics are insufficient to meet clinical needs. Increasing attention has been paid to bioactive compounds from natural plants, which may be efficacious against pain. This study examined the antinociceptive effects of isosakuranetin, a plant-derived transient receptor potential melastatin 3 blocker, in a rat model of peripheral neuropathy. Adult male Sprague-Dawley rats were first allowed to go through the chronic constriction injury surgery to develop neuropathic pain...
2017: Pharmacology
https://www.readbyqxmd.com/read/28704834/gper-mediates-functional-endothelial-aging-in-renal-arteries
#18
Matthias R Meyer, Thomas Rosemann, Matthias Barton, Eric R Prossnitz
Aging is associated with impaired renal artery function, which is partly characterized by arterial stiffening and a reduced vasodilatory capacity due to excessive generation of reactive oxygen species by NADPH oxidases (Nox). The abundance and activity of Nox depends on basal activity of the heptahelical transmembrane receptor GPER; however, whether GPER contributes to age-dependent functional changes in renal arteries is unknown. This study investigated the effect of aging and Nox activity on renal artery tone in wild-type and GPER-deficient (Gper-/-) mice (4 and 24 months old)...
2017: Pharmacology
https://www.readbyqxmd.com/read/28668949/naringin-reverses-neurobehavioral-and-biochemical-alterations-in-intracerebroventricular-collagenase-induced-intracerebral-hemorrhage-in-rats
#19
Navdeep Singh, Yashika Bansal, Ranjana Bhandari, Lovish Marwaha, Raghunath Singh, Kanwaljit Chopra, Anurag Kuhad
Intracerebral hemorrhage (ICH) contributes to 10-15% of all strokes and is a high risk factor for morbidity and mortality as compared to other subtypes of stroke, that is, cerebral ischemia and subarachnoid hemorrhage. Oxidative stress (OS)-induced neuroinflammation and neuronal cell death contribute towards the hallmarks of ICH. Spared antioxidant levels, increased inflammatory cytokines and free radicals in ICH lead to neuronal death and exaggerate the hallmarks of ICH. Intracerebroventricular (ICV) collagenase (COL-induced neuronal cell damage and cognitive deficits form a widely recognized experimental model for ICH...
2017: Pharmacology
https://www.readbyqxmd.com/read/28641304/hyperemesis-gravidarum-a-review-of-recent-literature
#20
Viktoriya London, Stephanie Grube, David M Sherer, Ovadia Abulafia
BACKGROUND: In the United States, hyperemesis gravidarum is the most common cause of hospitalization during the first half of pregnancy and is second only to preterm labor for hospitalizations in pregnancy overall. In approximately 0.3-3% of pregnancies, hyperemesis gravidarum is prevalent and this percentage varies on account of different diagnostic criteria and ethnic variation in study populations. Despite extensive research in this field, the mechanism of the disease is largely unknown...
2017: Pharmacology
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