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Naunyn-Schmiedeberg's Archives of Pharmacology

Chu Shan Tan, Mun Fei Yam
Previous studies have demonstrated that 3'-hydroxy-5,6,7,4'-tetramethoxyflavone (TMF) content in Orthosiphon stamineus fractions correlate with its vasorelaxation activity. Even with the availability of previous studies, there is still very little information on the vasorelaxation effect of TMF, and few scientific studies have been carried out. Therefore, the present study was designed to investigate the vasorelaxation activity and mechanism of action of the TMF. The vasorelaxation activity and the underlying mechanisms of TMF were evaluated on thoracic aortic rings isolated from Sprague Dawley rats...
March 19, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Mаhmoud Youns, Abeer ElKhoely, Rehab Kamel
Pancreatic cancer, the fourth most common cause of cancer-related deaths, is one of the most aggressive and devastating human malignancies with increasing incidence worldwide. To date, surgical resection is the only potentially curative therapy available for pancreatic cancer patients. Early diagnosis of pancreatic tumors is difficult, and hence, nearly 80% of patients cannot receive surgical resection. Natural products have always been a vital source for novel compounds for cancer treatment. The naturally occurring prenylated xanthone, gambogic acid, has been previously shown to exert potent anticancer, anti-inflammatory, apoptotic, antiangiogenic, and antioxidant activities...
March 15, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Ivana Vrhovac Madunić, Josip Madunić, Maja Antunović, Mladen Paradžik, Vera Garaj-Vrhovac, Davorka Breljak, Inga Marijanović, Goran Gajski
Apigenin is found in several dietary plant foods such as vegetables and fruits. To investigate potential anticancer properties of apigenin on human breast cancer, ER-positive MCF-7 and triple-negative MDA MB-231 cells were used. Moreover, toxicological safety of apigenin towards normal cells was evaluated in human lymphocytes. Cytotoxicity of apigenin towards cancer cells was evaluated by MTT assay whereas further genotoxic and oxidative stress parameters were measured by comet and lipid peroxidation assays, respectively...
March 14, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Kathrin Kaiser, Katja Prystaz, Anna Vikman, Melanie Haffner-Luntzer, Stephanie Bergdolt, Gudrun Strauss, Georg H Waetzig, Stefan Rose-John, Anita Ignatius
Patients with multiple injuries frequently suffer bone fractures and are at high risk to develop fracture healing complications. Because of its key role both in systemic posttraumatic inflammation and fracture healing, the pleiotropic cytokine interleukin-6 (IL-6) may be involved in the pathomechanisms of trauma-induced compromised fracture healing. IL-6 signals are transmitted by two different mechanisms: classic signaling via the membrane-bound receptor (mIL-6R) and trans-signaling via its soluble form (sIL-6R)...
March 1, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Sai Kiran S S Pindiprolu, Praveen T Krishnamurthy, Pavan Kumar Chintamaneni
Breast cancers contain small population of tumor-initiating cells called breast cancer stem cells (BCSCs), which are spared even after chemotherapy. Recently, BCSCs are implicated to be a cause of metastasis, tumor relapse, and therapy resistance in breast cancer. BCSCs have unique molecular mechanisms, which can be targeted to eliminate them. These include surface biomarkers, proteins involved in self-renewal pathways, drug efflux transporters, apoptotic/antiapoptotic proteins, autophagy, metabolism, and microenvironment regulation...
February 23, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Juliano Q D Rodrigues, Henrique Camara, Aron Jurkiewicz, Rosely O Godinho
Hypertension is a risk factor for cardiovascular diseases, which have been associated with dysfunction of sympathetic and purinergic neurotransmission. Therefore, herein, we evaluated whether modifications of adenosine receptor signaling may contribute to the cardiac dysfunction observed in hypertension. Isolated right atria from spontaneously hypertensive (SHR) or normotensive Wistar rats (NWR) were used to investigate the influence of adenosine receptor signaling cascade in the cardiac chronotropism. Our results showed that adenosine, the endogenous agonist of adenosine receptors, and CPA, a selective agonist of A1 receptor, decreased the atrial chronotropism of NWR and SHR in a concentration- and time-dependent manner, culminating in cardiac arrest (0 bpm)...
February 22, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
José M Centeno, Luis Miranda-Gómez, Mikahela A López-Morales, Teresa Jover-Mengual, María C Burguete, Vannina G Marrachelli, María Castelló-Ruiz, Alicia Aliena-Valero, Enrique Alborch, Francisco J Miranda
Diabetic nephropathy is associated with increased risk of cardiovascular disease. B-type natriuretic peptide (BNP) plays an important role in cardiovascular pathophysiology and therapeutics. The aim of the present study was to investigate the influence of experimental diabetes on the mechanisms that regulate the relaxant response of the rabbit renal artery to BNP. Arterial relaxations to BNP were enhanced in diabetic rabbits. Indomethacin enhanced BNP-induced relaxation in control rabbits but showed no effect in diabetic rabbits...
February 21, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Kohei Takahara, Tadashi Yamamoto, Keiichiro Uchida, Hai-Lei Zhu, Atsushi Shibata, Tetsuichiro Inai, Mitsuru Noguchi, Mari Yotsu-Yamashita, Noriyoshi Teramoto
Molecular investigations were performed in order to determine the major characteristics of voltage-gated Na + channel β-subunits in mouse vas deferens. The use of real-time quantitative PCR showed that the expression of Scn1b was significantly higher than that of other β-subunit genes (Scn2b - Scn4b). Immunoreactivity of Scn1b proteins was also detected in the inner circular and outer longitudinal smooth muscle of mouse vas deferens. In whole-cell recordings, the actions of 4,9-anhydroTTX on voltage-gated Na + current peak amplitude in myocytes (i...
February 16, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Bruno Pradier, Edda Erxlebe, Astrid Markert, Ildikó Rácz
Chronic alcohol abuse leads to severe brain damage. Although the underlying neuropathological processes are largely unknown, recent studies show that chronic alcohol consumption leads to neuroinflammation and may result in neurodegeneration and impaired neuronal connectivity. Long-term alcohol consumption promotes the production of pro-inflammatory cytokines, such as TNF-α and IL-1β, and activates microglia cells in the brain. As it has not yet been investigated to what extent these processes dependent on the duration of alcohol consumption or whether microglia are source of pro-inflammatory cytokines in vivo, this study investigated the expression of the pro-inflammatory cytokine, IL-1β, in microglia at different time points in mice chronically exposed to alcohol...
February 14, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Suresh Palle, Prasad Neerati
The objective of the present study was to evaluate the protective effect of resveratrol nanoparticles (NRSV) against rotenone-induced neurodegeneration in rats. NRSV were prepared by temperature-controlled antisolvent precipitation method and characterized for its particle size, shape, and dissolution properties. Moreover, NRSV effects compared with the free resveratrol (RSV). Animals were divided into four groups: (I) control, (II) rotenone (2 mg/kg s.c.), (III) RSV (40 mg/kg, p.o.) + rotenone, and (IV) NRSV (40 mg/kg, p...
February 6, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Carlos Moya, Salvador Máñez
Atherosclerosis is one of the leading causes of death in Western countries, with high-density lipoproteins (HDL) playing an important protective role due to their ability to inhibit oxidation of low-density lipoproteins (LDL), thus relieving vascular subendothelial damage. One of the proteins constituting HDL particles is paraoxonase-1 (PON1), an enzyme able to hydrolyze aryl esters, lactones, and organophosphates. Other closely related paraoxonases are designated as PON2, which is a protein localized inside many different kinds of cells, and PON3, not only present in HDL but also in mitochondria and endoplasmic reticulum, as well...
February 6, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Agata Szymaszkiewicz, Marta Zielinska, Kun Li, Mani Ramanathan, Safiul Alam, Duen-Ren Hou, Jakub Fichna, Martin Storr
Cannabinoid-1 (CB1) receptors are broadly distributed in the central and peripheral nervous systems; among others, they are located in the enteric nervous system. In the gastrointestinal (GI) system, they participate in regulation of intestinal motility or ion transport. The aim of our study was to assess the effect of 1,2,3-triazole derivatives (compound 1: 2-[4,5-bis(2,4-dichlorophenyl)-2H-1,2,3-triazol-2-yl]-N-(2-fluorobenzyl)acetamide, compound 2: 2-[4,5-bis(2,4-dichlorophenyl)-2H-1,2,3-triazol-2-yl]-N-(4-fluorobenzyl)acetamide, compound 3: N-benzyl-2-[4-(4-chlorophenyl)-5-(2,4-dichlorophenyl)-2H-1,2,3-triazol-2-yl]acetamide]), characterized in vitro as CB1 antagonists with high CB1 over CB2 selectivity, in the mouse GI tract...
February 5, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Juan Antonio García-Carmona, Polymnia Georgiou, Panos Zanos, Alexis Bailey, Maria Luisa Laorden
Methamphetamine (METH) addiction is a major public health problem in some countries. There is evidence to suggest that METH use is associated with increased risk of developing cardiovascular problems. Here, we investigated the effects of chronic METH administration and withdrawal on the activation of the brain stress system and cardiac sympathetic pathways. Mice were treated with METH (2 mg/kg, i.p.) for 10 days and left to spontaneous withdraw for 7 days. The number of corticotrophin-releasing factor (CRF), c-Fos, and CRF/c-Fos neurons was measured by immunohistochemistry in the paraventricular nucleus of the hypothalamus (PVN) and the oval region of the bed nucleus of stria terminalis (ovBNST), two regions associated with cardiac sympathetic control...
January 30, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Sara A Khedr, Ahmed A Elmelgy, Omnyah A El-Kharashi, Hadwa A Abd-Alkhalek, Manal L Louka, Hoda A Sallam, Sawsan Aboul-Fotouh
Several hypotheses link high fat diet (HFD) with the pathophysiology of depression and its response to antidepressants. This study aimed to determine the effect of metformin (MET) on the cognitive and antidepressant activity of fluoxetine (FLU) through its effect on c-Jun expression. Behavioral, cognitive function, biochemical, and histopathological studies were performed in non-HFD- and HFD-fed rats exposed to chronic restraint stress (CRS). Stressed group showed cognitive impairment, depressive-like symptoms, disturbed glucose homeostasis and lipid profile, reduced adiponectin level, brain-derived neurotrophic factor (BDNF) expression, and increased corticosterone and c-Jun...
January 29, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Andreas Friebe, Peter Sandner, Achim Schmidtko
The article "Meeting report of the 8 th International Conference on "cGMP BcGMP: generators, effectors, and therapeutic implications" at Bamberg, Germany, from June 23 to 25, 2017" was originally published Online First without open access. After publication in volume 390, issue 12, pages 1177-1188, the author decided to opt for Open Choice and to make the article an open access publication.
January 24, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Orawan Wongmekiat, Wachirasek Peerapanyasut, Anongporn Kobroob
Nephrotoxicity is recognized as a serious disorder affected by chronic cadmium exposure. Imbalance between radical generation and elimination is considered a critical factor involved in the initiation and progression of renal injury caused by this heavy metal. The present study investigated the possible protection by catechin, a natural phenolic antioxidant, against cadmium nephrotoxicity and elucidated its potential mechanism. Male Wistar rats were assigned to receive vehicle, cadmium (CdCl2 2 mg/kg, i.p...
January 22, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Tunde Barta, Agnes Tosaki, David Haines, Gyorgy Balla, Istvan Lekli, Arpad Tosaki
Endothelin-1 (ET-1), a potent vasoconstrictor normally active in maintaining vascular tone, may mediate significant pathogenic effects, contributing to several serious diseases when aberrantly expressed or regulated. The present study evaluates the capacity of ET-1 to affect endothelin-1-associated hypertrophic activity and decreased expression of heme oxygenase-1 by H9c2 rat cardiomyoblasts in vitro, corresponding to in vivo processes underlying cardiovascular diseases (CVDs). Beta estradiol (β-E) is tested for its capacity to alter the effects of ET-1...
January 21, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Marc Le Vée, Elodie Jouan, Olivier Fardel
The lung is a preferential organ site for accumulation of lipophilic basic amine drugs, so-called pneumophilic drugs and belonging to various pharmacological classes, which can result in lung toxicity. In order to investigate the mechanism involved in such pulmonary accumulation of drugs, uptake of clonidine, used here as a prototypical basic amine drug, was characterized in cultured human lung cells. Clonidine accumulation in lung alveolar A549 cells was found to be temperature- and pH-dependent; it was saturable, with a Michaelis-Menten affinity constant (Km) value of 569...
January 19, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
Na Li, Dobromir Dobrev
No abstract text is available yet for this article.
January 11, 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
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