Analgesic and Anti‐inflammatory Activities of the Ethanol Extract of Taxillus tsaii Chiu in Mice
This study was conducted to investigate the analgesic activities and mechanism of anti‐inflammatory activities of a 50% ethanol extract of Taxillus tsaii (ETT) in vivo using the acetic acid induced writhing test and formalin induced paw licking in mice. The anti‐inflammatory effect of ETT was evaluated using a mouse model of λ‐carrageenan (Carr)‐induced paw edema. ETT reduced the writhing in the acetic acid assay test at a dose 1.0 g/kg po and reduced the licking time in the late phase of the formalin test at doses of 0.5 and 1.0 g/kg po). Carr‐induced paw edema was reduced when ETT (0.5 and 1.0 g/kg po) was adm...
Source: Drug Development Research - May 1, 2015 Category: Drugs & Pharmacology Authors: Chia‐Yu Liu, Yung‐Jia Chiu, Chao‐Lin Kuo, Tzu‐Mei Chien, Lung‐Yuan Wu, Wen‐Huang Peng Tags: Research Article Source Type: research
Antioxidant‐Mediated Reversal of Oxidative Damage in Mouse Modeling of Complex I Inhibition
ABSTRACT
Mitochondrial dysfunction is a key component of various aging‐related pathologies of the brain that result in dementia. As such, it provides an important avenue in development of therapeutic interventions for a host of neurological disorders. A requirement for functional mitochondrial respiratory chain complex I (CI), to accomplish the normal physiological processes regulating memory, seems intuitive. In the present study, a synthetic lipoylcarnitine antioxidant (PMX‐500FI; 100 mg/kg/day po) was administered to female ICR mice (3–4‐month old) that were subsequently treated with the mitochondrial CI ...
Source: Drug Development Research - April 3, 2015 Category: Drugs & Pharmacology Authors: Kodeeswaran Parameshwaran, Michael H. Irwin, Kosta Steliou, Vishnu Suppiramaniam, Carl A. Pinkert Tags: Research Article Source Type: research
Phosphate and Thiophosphate Biphenyl Analogs as Steroid Sulfatase Inhibitors
ABSTRACT
In the present work, we report convenient methods for the synthesis and biological evaluation of phosphate and thiophosphate biphenyl derivatives exhibiting steroid sulfatase (STS) activity. The described synthesis is based on straightforward preparation of biphenyl‐4‐ol and 4′‐hydroxy‐biphenyl‐4‐carboxylic acid ethyl ester modified with various phosphate or thiophosphate moieties. The inhibitory effects of these compounds were tested on STS isolated from human placenta and led to two compounds of interest, 5a and 5d with IC50 values of 28.0 and 22.1 µM, respectively and that had interesting ...
Source: Drug Development Research - April 3, 2015 Category: Drugs & Pharmacology Authors: Sebastian Demkowicz, Witold Kozak, Mateusz Daśko, Maciej Masłyk, Konrad Kubiński, Janusz Rachon Tags: Research Article Source Type: research
Mitochondrially‐Imported RNA in Drug Discovery
ABSTRACT
The import of nuclear transcribed RNAs into mitochondria is an emerging area that presents a tremendous opportunity to develop human metabolic therapeutics. However, our knowledge base is quite limited. Much remains to be discovered regarding specific RNA localization and mechanisms of import. To identify novel RNAs imported into mitochondria, all RNAs within the mitochondria were characterized using next generation sequencing technology. Several nuclear transcribed RNAs were found within mitochondrial RNA (mtRNA) samples, including nuclear ribosomal RNAs, gamma satellite RNA and VL30 retroelement RNA. The ...
Source: Drug Development Research - April 3, 2015 Category: Drugs & Pharmacology Authors: Matthew V. Cannon, Michael H. Irwin, Carl A. Pinkert Tags: Research Article Source Type: research
Inhibition of LPS‐Induced TLR4 Signaling Products in Murine Macrophages by Phenylmethimazole: An Assay Methodology for Screening Potential Phenylmethimazole Analogs DOI:10.1002/ddr.21231, Vol 75, issue 8, 497–509.
(Source: Drug Development Research)
Source: Drug Development Research - March 31, 2015 Category: Drugs & Pharmacology Tags: Erratum Source Type: research
Effects of the Inhalation of the M3 Receptor Antagonist Bencycloquidium Bromide in A Mouse Cigarette Smoke‐Induced Airway Inflammation Model
ABSTRACT
Bencycloquidium bromide (BCQB), a novel M3 receptor antagonist, alleviates airway hyperresponsiveness, inflammation, and airway remodeling in a murine model of asthma. The aim of this study was to investigate the anti‐inflammatory activity of inhaled BCQB in a cigarette smoke (CS)‐induced model of acute lung inflammation. Mice exposed to CS developed chronic obstructive pulmonary disease (COPD). Inhalation of BCQB suppressed the accumulation of neutrophils and macrophages in airways and lung and also inhibited the CS‐induced increases in mRNA levels of keratinocyte‐derived chemokine, monocyte chemot...
Source: Drug Development Research - March 1, 2015 Category: Drugs & Pharmacology Authors: Shui‐Juan Zhang, Jun‐Xia Jiang, Qian‐Qian Ren, Qiang‐Min Xie, Yao‐Kang Xiong Tags: Research Article Source Type: research
Antimetastatic Effects of Gambogic Acid are Mediated via the Actin Cytoskeleton and NF‐κB Pathways in SK‐HEP1 Cells
In this study, the influence of GA on migration and invasion of SK‐HEP1 cells was evaluated. At concentrations above 0.6 μM, GA reduced cell proliferation in SK‐HEP1 cells without affecting proliferation of noncancerous HEK‐293 cells. GA also suppressed migration and invasion of SK‐HEP1 cells. GA downregulated the expression of the integrin β1/rho family GTPase signaling pathway, suppressed the actin rearrangement related to cell cytoskeleton and migration and decreased matrix metalloproteinases MMP‐2, MMP‐9, and NF‐κB expression involved in cancer invasion. These results suggest that GA may be a potenti...
Source: Drug Development Research - March 1, 2015 Category: Drugs & Pharmacology Authors: Min‐Seok Park, Nan‐Hee Kim, Chang‐Won Kang, Chul‐Woong Oh, Gun‐Do Kim Tags: Research Article Source Type: research
Biodistribution of the Multidentate Hydroxypyridinonate Ligand [14C]‐3,4,3‐LI(1,2‐HOPO), a Potent Actinide Decorporation Agent
ABSTRACT
The pharmacokinetics and biodistribution of the 14C‐labeled actinide decorporation agent 3,4,3‐LI(1,2‐HOPO) were investigated in young adult Swiss Webster mice and Sprague Dawley rats, after intravenous, intraperitoneal, and oral dose administration. In all routes investigated, the radiolabeled compound was rapidly distributed to various tissues and organs of the body. In mice, the 24 h fecal elimination profiles suggested that the biliary route is the predominant route of elimination. In contrast, lower fecal excretion levels were observed in rats. Tissue uptake and retention of the compound did not ...
Source: Drug Development Research - February 1, 2015 Category: Drugs & Pharmacology Authors: Taylor A. Choi, Aaron N. Endsley, Deborah I. Bunin, Christophe Colas, Dahlia D. An, Joel A. Morales‐Rivera, Jonathan A. Villalobos, Walter M. Shinn, Jack E. Dabbs, Polly Y. Chang, Rebecca J. Abergel Tags: Research Article Source Type: research
Self‐Nanoemulsifying Drug Delivery System of trans‐Cinnamic acid: Formulation Development and Pharmacodynamic Evaluation in Alloxan‐induced Type 2 Diabetic Rat Model
The objective of this study was to formulate a self‐nanoemulsifying oral drug delivery system (SNEDDS) for the poorly water‐soluble trans‐Cinnamic acid (t‐CA SNEDDS) that could be evaluated for its antihyperglycemic efficacy in comparison to the parent t‐CA in an alloxan‐induced diabetic rat model. A SNEDDS formulation consisting of 60% surfactant (Kolliphor EL), 10% co‐surfactant (PEG 400) and 30% oil (isopropyl myristate) proved to be optimal. t‐CA SNEDDS (80 mg/kg, p.o.), t‐CA suspension (80 mg/kg, p.o.), and Metformin Hydrochloride Tablets (230 mg/kg, p.o.) were administer qdfor 30 days to diabe...
Source: Drug Development Research - February 1, 2015 Category: Drugs & Pharmacology Authors: Houyong Wang, Qiang Li, Wenwen Deng, E. Omari‐siaw, Qilong Wang, Shicheng Wang, Shengli Wang, Xia Cao, Ximing Xu, Jiangnan Yu Tags: Research Article Source Type: research
Mitochondrial Drugs Come of Age
(Source: Drug Development Research)
Source: Drug Development Research - February 1, 2015 Category: Drugs & Pharmacology Authors: Walter H. Moos, James A. Dykens Tags: Editorial Source Type: research
5‐HT2B Receptor Antagonists Reduce Nerve Injury‐Induced Tactile Allodynia and Expression of 5‐HT2B Receptors
ABSTRACT
This work was performed to assess the effects of intrathecal serotonin 2B (5‐HT2B) receptor antagonists in rats with neuropathic pain. With RS‐127445, its effect was also determined on 5‐HT2B receptor expression. Neuropathic pain was induced by L5/L6 spinal nerve ligation. Western blotting was used to determine 5‐HT2B receptor expression. Dose‐response curves with the 5‐HT2B receptor antagonists 2‐amino‐4‐(4‐fluoronaphth‐1‐yl)‐6‐isopropylpyridine (RS‐127445, 1–100 nmol) and 1‐[(2‐chloro‐3,4‐dimethoxyphenyl)methyl]‐2,3,4,9‐tetrahydro‐6‐methyl‐1H‐pyrido[3,4...
Source: Drug Development Research - January 25, 2015 Category: Drugs & Pharmacology Authors: Jorge B. Pineda‐Farias, Isabel Velázquez‐Lagunas, Paulino Barragán‐Iglesias, Claudia Cervantes‐Durán, Vinicio Granados‐Soto Tags: Research Article Source Type: research
Antioxidant Activities of Caralluma tuberculata on Streptozotocin‐Induced Diabetic Rats
Abstract
The aim of this study was to elucidate the antioxidant effects of Caralluma tuberculata (C. tuberculata) in streptozotocin (STZ)‐induced diabetic rats. Diabetes was induced in male Wistar rats with an intraperitoneal injection of STZ at dose of 60 mg/kg body weight. Three days after diabetes induction, powdered aerial part of plant at doses of 100 and 200 mg/kg body weight were gavaged orally for a period of 45 days. The diabetes significantly decreased the activities of superoxide dismutase, catalase, glutathione peroxidase, glutathione reductase, and level of total thiol in liver, kidney, and heart of a...
Source: Drug Development Research - January 25, 2015 Category: Drugs & Pharmacology Authors: Jafar Poodineh, Abdurrashid Khazaei Feizabad, Alireza Nakhaee Tags: Research Article Source Type: research
The Role of Potassium Channels in the Vasodilatation Induced by Resveratrol and Naringenin in Isolated Human Umbilical Vein
Abstract
Potassium (K+) channels have a key role in the maintenance of smooth muscle tone; a variety of agonists can modify the tone by altering K+‐channel activity. The aim of this study was assess the effects of the phenols, resveratrol, and naringenin on K+‐channels of the vascular smooth muscle. Segments of human umbilical vein (HUV) without endothelium were precontracted using serotonin (100 μM) or 100 mM K+ to derive cumulative concentration‐response curves using increasing concentrations of resveratrol or naringenin. K+‐channel inhibitors were added in the bath before resveratrol (1–100 μM) or nar...
Source: Drug Development Research - January 25, 2015 Category: Drugs & Pharmacology Authors: Dragana Protić, Nebojša Radunović, Svetlana Spremović‐Rađenović, Vladimir Živanović, Helmut Heinle, Aleksandar Petrović, Ljiljana Gojković‐Bukarica Tags: Research Article Source Type: research
Dalbergia odorifera Extract Ameliorates UVB‐Induced Wrinkle Formation by Modulating Expression of Extracellular Matrix Proteins
This study examined the antiwrinkle effects of ethanol extracts of D. odorifera in UVB‐irradiated human skin cells. Ethanol extracts of D. odorifera and thier constituents, dalbergin and sativanone, induced expression of collagen type I and transforming growth factor (TGF)‐β1 in human dermal fibroblasts. In HR‐1 hairless mice exposed to UVB, the ethanol extract reduced wrinkle formation and skin thickness. This inhibitory effect of ethanol extract was associated with the restoration of collagen type I, TGF‐β1, and elastin to levels approaching those in skin tissues not exposed to UVB, which was accompanied by the...
Source: Drug Development Research - January 25, 2015 Category: Drugs & Pharmacology Authors: Sun Ah Ham, Eun Sil Kang, Taesik Yoo, Hyun Ho Lim, Won Jin Lee, Jung Seok Hwang, Kyung Shin Paek, Han Geuk Seo Tags: Research Article Source Type: research
Quercetin Induces Antiproliferative Activity Against Human Hepatocellular Carcinoma (HepG2) Cells by Suppressing Specificity Protein 1 (Sp1)
ABSTRACT
Quercetin, found in red onions and red apple skin can induce apoptosis insome malignant cells. However, the apoptotic effect of quercetin in hepatocellular carcinoma HepG2 cells via regulation of specificity protein 1 (Sp1) has not been studied. Here, we demonstrated that quercetin decreased cell growth and induce apoptosis in HepG2 cells via suppression of Sp1 using 3‐(4,5‐dimethyl‐2‐yl)‐5‐(3‐carboxymethoxyphenyl)‐2‐(4‐sulfophenyl)‐2H‐tetrazolium, inner salt (MTS) assay, 4′,6‐diamidino‐2‐phenylindole (DAPI) staining, Annexin V, and Western blot analysis, an effect that was d...
Source: Drug Development Research - January 25, 2015 Category: Drugs & Pharmacology Authors: Ra Ham Lee, Jin Hyoung Cho, Young‐Joo Jeon, Woong Bang, Jung‐Jae Cho, Nag‐Jin Choi, Kang Seok Seo, Jung‐Hyun Shim, Jung‐Il Chae Tags: Research Article Source Type: research
