Instruction to Authors
(Source: Drug Development Research)
Source: Drug Development Research - June 8, 2016 Category: Drugs & Pharmacology Tags: Instruction to Authors Source Type: research
Apocynin Suppresses Lipopolysaccharide ‐Induced Inflammatory Responses Through the Inhibition of MAP Kinase Signaling Pathway in RAW264.7 Cells
The objective of this study was to elucidate the anti‐inflammatory mechanism of apocynin in lipopolysaccharide (LPS)‐challenged RAW264.7 macrophage cells. Apocynin inhibited LPS‐induced extracellular secretion of the pro‐inflammatory mediators, nitric oxide (NO) and PGE2 and the expression of inducible nitric oxide synthase and cyclooxygenase‐2. Apocynin also suppressed LPS‐induced secretion of the pro‐inflammatory cytokine, tumor necrosis factor‐α and LPS‐induced degradation of IκB, which retains NF‐κB in the cytoplasm, consequently inhibiting the transcription of pro‐inflammatory genes by NF‐κ...
Source: Drug Development Research - May 31, 2016 Category: Drugs & Pharmacology Authors: Young ‐Jae Hwang, Sung Joon Lee, Jin‐Young Park, Wanjoo Chun, Seung‐Joo Nam, Jin Myung Park, Sung Chul Park, Dae Hee Choi, Chang Don Kang Tags: Research Article Source Type: research
Synthesis and Pharmacological Evaluation of Indole Derivatives as Deaza Analogues of Potent Human Neutrophil Elastase Inhibitors
ABSTRACT
A number of N‐benzoylindoles were designed and synthesized as deaza analogs of previously reported potent and selective HNE inhibitors with an indazole scaffold. The new compounds containing substituents and functions that were most active in the previous series were active in the micromolar range (the most potent had IC50 = 3.8 μM) or inactive. These results demonstrated the importance of N‐2 in the indazole nucleus. Docking studies performed on several compounds containing the same substituents but with an indole or an indazole scaffold, respectively, highlight interesting aspects concerning the ...
Source: Drug Development Research - May 31, 2016 Category: Drugs & Pharmacology Authors: Letizia Crocetti, Igor A. Schepetkin, Giovanna Ciciani, Maria Paola Giovannoni, Gabriella Guerrini, Antonella Iacovone, Andrei I. Khlebnikov, Liliya N. Kirpotina, Mark T. Quinn, Claudia Vergelli Tags: Research Article Source Type: research
Novel 5 ‐Hydroxy, 5‐Substituted Benzenesulfonamide Pyrimidine‐2,4,6‐Triones Attenuate Lipopolysaccharide‐Induced Acute Lung Injury via Inhibition of the Gelatinases, MMP‐2 and MMP‐9
ABSTRACT
A novel series of ten 5‐hydroxy, 5‐substituted benzene sulfonamide pyrimidine‐2,4,6‐triones were synthesized and their structures ascertained using 1H‐NMR, 13C‐NMR, mass and elemental analysis. These compounds were subsequently tested for inhibition of MMP‐2 and MMP‐9 where most exhibited activity with compound 5i being the most potent against MMP‐2 and MMP‐9 with IC50 values of 2.35 nM and 8.24 nM, respectively. Compound 5i was further analyzed in a mouse LPS‐induced acute lung injury model where it had protective activity. Histochemical studies indicated that 5i improved the vascular...
Source: Drug Development Research - May 31, 2016 Category: Drugs & Pharmacology Authors: Wei He, Jie Jiang, Ze ‐Qian Yu, Jia‐Hua Zhou Tags: Research Article Source Type: research
Nociceptive Alteration by High Sucrose Diet in Hypoestrogenic Wistar Rats
Abstract
Obesity is a risk factor associated with alterations in pain perception. The aim of this study was to analyse a time‐course of nociceptive responses (plantar test) in hypoestrogenic rats after the induction of obesity. Animals (hypoestrogenic and naïve) received either a hypercaloric or regular diet for 24 weeks. Thermal nociception and body weight were measured during this period. At the 4th and 17th weeks after treatment, oral glucose tolerance, blood insulin levels, abdominal fat weight, and uric acid levels were measured. The hypoestrogenic rats on a high sucrose diet had higher body weight and abdom...
Source: Drug Development Research - May 31, 2016 Category: Drugs & Pharmacology Authors: Osmar Antonio Jaramillo ‐Morales, Josué Vidal Espinosa‐Juárez, Janette Nallely Corona‐Ramos, Francisco Javier López‐Muñoz Tags: Research Article Source Type: research
Synthesis and Evaluation of a New Series of 8 ‐(2‐Nitroaryl)Xanthines as Adenosine Receptor Ligands
Abstract
A new series of 1,3‐dimethylxanthine derivatives bearing 8‐(2‐nitroaryl) residue was synthesized and evaluated for affinity for recombinant human adenosine receptors subtypes. Nitrate esters of 7‐substituted‐1,3‐dimethyl‐8‐phenylxanthines were also synthesized and tested. Introducing a nitro substituent at the 2‐position of the 8‐substituted phenyl ring resulted in generally low affinity for adenosine receptors (ARs), selectivity toward the A2A subtype was enhanced in some of the compounds. 8‐(4‐Cyclopentyloxy‐5‐methoxy‐2‐nitrophenyl)‐1,3‐dimethylxanthine (9e) proved to b...
Source: Drug Development Research - May 31, 2016 Category: Drugs & Pharmacology Authors: Ranju Bansal, Gulshan Kumar, Suman Rohilla, Karl ‐Norbert Klotz, Sonja Kachler, Louise C. Young, Alan L. Harvey Tags: Research Article Source Type: research
Synthesis and Evaluation of a New Series of 8‐(2‐Nitroaryl)Xanthines as Adenosine Receptor Ligands
Abstract
A new series of 1,3‐dimethylxanthine derivatives bearing 8‐(2‐nitroaryl) residue was synthesized and evaluated for affinity for recombinant human adenosine receptors subtypes. Nitrate esters of 7‐substituted‐1,3‐dimethyl‐8‐phenylxanthines were also synthesized and tested. Introducing a nitro substituent at the 2‐position of the 8‐substituted phenyl ring resulted in generally low affinity for adenosine receptors (ARs), selectivity toward the A2A subtype was enhanced in some of the compounds. 8‐(4‐Cyclopentyloxy‐5‐methoxy‐2‐nitrophenyl)‐1,3‐dimethylxanthine (9e) proved to b...
Source: Drug Development Research - May 31, 2016 Category: Drugs & Pharmacology Authors: Ranju Bansal, Gulshan Kumar, Suman Rohilla, Karl‐Norbert Klotz, Sonja Kachler, Louise C. Young, Alan L. Harvey Tags: Research Article Source Type: research
Sanguinarine Induces Apoptosis of Human Oral Squamous Cell Carcinoma KB Cells via Inactivation of the PI3K/Akt Signaling Pathway
ABSTRACT
Sanguinarine, an alkaloid isolated from the root of Sanguinaria canadensis and other plants of the Papaveraceae family, selectively induces apoptotic cell death in a variety of human cancer cells, but its mechanism of action requires further elaboration. The present study investigated the pro‐apoptotic effects of sanguinarine in human oral squamous cell carcinoma KB cells. Sanguinarine treatment increased DR5/TRAILR2 (death receptor 5/TRAIL receptor 2) expression and enhanced the activation of caspase‐8 and cleavage of its substrate, Bid. Sanguinarine also induced the mitochondrial translocation of pro...
Source: Drug Development Research - May 31, 2016 Category: Drugs & Pharmacology Authors: Tae Kyung Lee, Cheol Park, Soon‐Jeong Jeong, Moon‐Jin Jeong, Gi‐Young Kim, Wun‐Jae Kim, Yung Hyun Choi Tags: Research Article Source Type: research
The Antinociceptive Effects of Tramadol and/or Gabapentin on Rat Neuropathic Pain Induced by a Chronic Constriction Injury
Abstract
The current work evaluates the interaction between two commonly used drugs, tramadol (Tra) and gabapentin (Gbp). Dose‐response curves (DRC) and isobolographic analysis were used to confirm their synergistic antihyperalgesic and anti‐allodynic responses in a rat neuropathic pain model involving chronic constriction injury of the sciatic nerve and in von Frey and acetone tests. Tra and Gbp produced dose‐dependent antihyperalgesic and anti‐allodynic effects. Dose‐response studies of combinations of Tra and Gbp in combination showed the DRC was leftward‐shifted compared to the DRCs for each compound...
Source: Drug Development Research - May 31, 2016 Category: Drugs & Pharmacology Authors: Janette Nallely Corona‐Ramos, Minarda De la O‐Arciniega, Myrna Déciga‐Campos, José Raúl Medina‐López, Adriana Miriam Domínguez‐Ramírez, Osmar Antonio Jaramillo‐Morales, Josué Vidal Espinosa‐Juárez, Francisco Javier López‐Muñoz Tags: Research Article Source Type: research
Issue Information‐TOC
(Source: Drug Development Research)
Source: Drug Development Research - May 31, 2016 Category: Drugs & Pharmacology Tags: Issue Information ‐TOC Source Type: research
Topical Anti ‐Inflammatory and Analgesic Effects of Multiple Applications of S(+)‐Flurbiprofen Plaster (SFPP) in a Rat Adjuvant‐Induced Arthritis Model
Abstract
The aim of this study was to evaluate the efficacy of multiple applications of S(+)‐flurbiprofen plaster (SFPP), a novel Nonsteroidal anti‐inflammatory drug (NSAID) patch, for the alleviation of inflammatory pain and edema in rat adjuvant‐induced arthritis (AIA) model as compared to other NSAID patches. The AIA model was induced by the injection of Mycobacterium butyricum and rats were treated with a patch (1.0 cm × 0.88 cm) containing each NSAID (SFP, ketoprofen, loxoprofen, diclofenac, felbinac, flurbiprofen, or indomethacin) applied to the paw for 6 h per day for 5 days. The pain threshold was eva...
Source: Drug Development Research - May 30, 2016 Category: Drugs & Pharmacology Authors: Masanori Sugimoto, Yoshihisa Toda, Miyuki Hori, Akiko Mitani, Takahiro Ichihara, Shingo Sekine, Shinsuke Kaku, Noboru Otsuka, Hideo Matsumoto Tags: Research Article Source Type: research
Antinociceptive Effect of Racemic Flurbiprofen and Caffeine Co ‐Administration in an Arthritic Gout‐Type Pain in Rats
The objective of this work was to evaluate the combination of rac‐Flur + caffeine oral in arthritic gout‐type pain in rats. The antinociceptive effects of the rac‐Flur alone and in combination with caffeine were analyzed on a pain‐induced functional impairment model in rat. rac‐Flur induced a dose‐dependent antinociceptive effect and caffeine did not present any effect. The combination of rac‐Flur and caffeine achieve a higher percentage of antinociceptive effect compared with the individual administration of rac‐Flur. The dose‐response curve (DRCs) shows that the combination of rac‐Flur (31.6 mg/kg...
Source: Drug Development Research - May 30, 2016 Category: Drugs & Pharmacology Authors: Ricardo Li évano‐Reyes, Hermínia Ines Pérez‐Méndez, Aida Solís‐Oba, Osmar Antonio Jaramillo‐Morales, Josué Vidal Espinosa‐Juárez, Francisco Javier López‐Muñoz Tags: Research Article Source Type: research
Topical Anti‐Inflammatory and Analgesic Effects of Multiple Applications of S(+)‐Flurbiprofen Plaster (SFPP) in a Rat Adjuvant‐Induced Arthritis Model
ABSTRACT
The aim of this study was to evaluate the efficacy of multiple applications of S(+)‐flurbiprofen plaster (SFPP), a novel Nonsteroidal anti‐inflammatory drug (NSAID) patch, for the alleviation of inflammatory pain and edema in rat adjuvant‐induced arthritis (AIA) model as compared to other NSAID patches. The AIA model was induced by the injection of Mycobacterium butyricum and rats were treated with a patch (1.0 cm × 0.88 cm) containing each NSAID (SFP, ketoprofen, loxoprofen, diclofenac, felbinac, flurbiprofen, or indomethacin) applied to the paw for 6 h per day for 5 days. The pain threshold was eva...
Source: Drug Development Research - May 30, 2016 Category: Drugs & Pharmacology Authors: Masanori Sugimoto, Yoshihisa Toda, Miyuki Hori, Akiko Mitani, Takahiro Ichihara, Shingo Sekine, Shinsuke Kaku, Noboru Otsuka, Hideo Matsumoto Tags: Research Article Source Type: research
Antinociceptive Effect of Racemic Flurbiprofen and Caffeine Co‐Administration in an Arthritic Gout‐Type Pain in Rats
The objective of this work was to evaluate the combination of rac‐Flur + caffeine oral in arthritic gout‐type pain in rats. The antinociceptive effects of the rac‐Flur alone and in combination with caffeine were analyzed on a pain‐induced functional impairment model in rat. rac‐Flur induced a dose‐dependent antinociceptive effect and caffeine did not present any effect. The combination of rac‐Flur and caffeine achieve a higher percentage of antinociceptive effect compared with the individual administration of rac‐Flur. The dose‐response curve (DRCs) shows that the combination of rac‐Flur (31.6 mg/kg...
Source: Drug Development Research - May 30, 2016 Category: Drugs & Pharmacology Authors: Ricardo Liévano‐Reyes, Hermínia Ines Pérez‐Méndez, Aida Solís‐Oba, Osmar Antonio Jaramillo‐Morales, Josué Vidal Espinosa‐Juárez, Francisco Javier López‐Muñoz Tags: Research Article Source Type: research
The Effect of Experimental Thyroid Dysfunction on Markers of Oxidative Stress in Rat Pancreas
In conclusion, our results showed that experimental hyperthyroidism induces oxidative stress in pancreas of rats, but hypothyroidism has no major impact on oxidative stress markers. Drug Dev Res, 2016. © 2016 Wiley Periodicals, Inc. (Source: Drug Development Research)
Source: Drug Development Research - April 30, 2016 Category: Drugs & Pharmacology Authors: Mojtaba Sajadian, Mohammad Hashemi, Saeedeh Salimi, Alireza Nakhaee Tags: Research Article Source Type: research
