Preparation and Sonodynamic Antitumor Effect of Protohemin‐Conjugated Multiwalled Carbon Nanotubes Functionalized with Carboxylic Group
In conclusion, MWCNTs‐Ph had increased antitumor efficiency and also decreased potential side effects. Drug Dev Res, 2016. © 2016 Wiley Periodicals, Inc. (Source: Drug Development Research)
Source: Drug Development Research - January 31, 2016 Category: Drugs & Pharmacology Authors: Chuan‐jin Wang, Wei Li Tags: Research Article Source Type: research
Apoptotic Cell Death Induced by ofLBP6A, Lipopolysaccharide Binding Protein Model Peptide, Derived from Paralichthy olivaceus on MKN‐28 Cells
Abstract
The aim of this study was to evaluate the anti‐cancer effects of lipopolysaccharide binding protein (LBP) analogs derived from the marine resource Paralichthy olivaceus on MKN‐28 gastric cancer cells. Five LBP analogs were used: ofLBP1N, ofLBP2A, ofLBP4N, ofLBP5A, and ofLBP6A. ofLBP6A induced cell death of MKN‐28 cells at a concentration of 40 μM. While the anti‐proliferation effects ofLBP6A showed on MKN‐28 cells at concentration of 40 μM, it did not affect non‐cancerous HEK‐293 cells at the same concentration. The mechanism study showed that ofLBP6A lead to the inhibition of cell prolifera...
Source: Drug Development Research - January 31, 2016 Category: Drugs & Pharmacology Authors: Chang‐Won Kang, Nan‐Hee Kim, Nam Gyu Park, Gun‐Do Kim Tags: Research Article Source Type: research
Synthesis of p‐O‐Alkyl Salicylanilide Derivatives as Novel EGFR Inhibitors
ABSTRACT
Epidermal growth factor receptor (EGFR), a validated target for anticancer drugs, plays a critical role in tumorigenesis and tumor development. A series of p‐O‐alkyl salicylanilide derivatives were designed and synthesized as novel EGFR inhibitors using a salicylic acid scaffold. A simulated six‐membered ring strategy formed through intramolecular hydrogen bonds was employed to mimic the planar quinazoline of the EGFR antagonist, gefitinib. The derived compounds with hydroxyl at the ortho position were more potent than ones with methoxyl group. In particular, compounds 5d and 5b displayed significant ...
Source: Drug Development Research - January 13, 2016 Category: Drugs & Pharmacology Authors: Li Zhang, Lin Hou, Wenyan Sun, Zidong Yu, Jibo Wang, Hua Gao, Guiming Yang Tags: Research Article Source Type: research
Analgesic Effect of the Newly Developed S(+)‐Flurbiprofen Plaster on Inflammatory Pain in a Rat Adjuvant‐Induced Arthritis Model
This article describes the properties of a novel topical NSAID (Nonsteroidal anti‐inflammatory drug) patch, SFPP (S(+)‐flurbiprofen plaster), containing the potent cyclooxygenase (COX) inhibitor, S(+)‐flurbiprofen (SFP). The present studies were conducted to confirm human COX inhibition and absorption of SFP and to evaluate the analgesic efficacy of SFPP in a rat adjuvant‐induced arthritis (AIA) model. COX inhibition by SFP, ketoprofen and loxoprofen was evaluated using human recombinant COX proteins. Absorption of SFPP, ketoprofen and loxoprofen from patches through rat skin was assessed 24 h after application. Th...
Source: Drug Development Research - January 13, 2016 Category: Drugs & Pharmacology Authors: Masanori Sugimoto, Yoshihisa Toda, Miyuki Hori, Akiko Mitani, Takahiro Ichihara, Shingo Sekine, Takuya Hirose, Hiromi Endo, Nobuko Futaki, Shinsuke Kaku, Noboru Otsuka, Hideo Matsumoto Tags: Research Article Source Type: research
Effect of α‐Hederin on IL‐2 and IL‐17 mRNA and miRNA‐133a Levels in Lungs of Ovalbumin‐Sensitized Male Rats
ABSTRACT
α‐hederin, a saponin that is a major constituent of English Ivy (Hedera helix) is effective in the treatment of asthma. In the present study, the effect of α‐hederin on lung tissue pathology and the levels of the inflammatory mediators; IL‐2 mRNA, IL‐17 mRNA, and MicroRNAs (miRNA)‐133a was evaluated in a rat ovalbumin (OVA)‐sensitized model of asthma. Rats were divided randomly into control (C), OVA‐sensitized (S), OVA‐sensitized pretreated with the antioxidant, thymoquinone (3 mg/kg, S + TQ) or OVA‐sensitized pretreated with α‐hederin (0.02 mg/kg, S + AH) groups. Levels of IL...
Source: Drug Development Research - December 1, 2015 Category: Drugs & Pharmacology Authors: Hadi Ebrahimi, Maryam Fallahi, Amir Mahdi Khamaneh, Mohammad Ali Ebrahimi Saadatlou, Saeideh Saadat, Rana Keyhanmanesh Tags: Research Article Source Type: research
Synthesis and Cytotoxic Evaluation of Monocarbonyl Analogs of Curcumin as Potential Anti‐Tumor Agents
Abstract
A series of mono‐carbonyl curcumin analogs with different substituents at the 4/4’‐position of the phenyl group were synthesized and screened for in vitro cytotoxicity against a panel of human cancer cell lines using a methyl thiazolyl tetrazolium assay. Several of the curcumin analogs, especially B114, exhibited a wide‐spectrum of anti‐tumor properties in all tested cell lines, indicating their potential in as anti‐cancer lead compounds. Further toxicity testing in the NRK‐52E kidney cell line revealed that the analogs A111, A113, and B114 had comparable or higher safety than curcumin. These ...
Source: Drug Development Research - December 1, 2015 Category: Drugs & Pharmacology Authors: Zheer Pan, Chengwei Chen, Yeli Zhou, Feng Xu, Yaozeng Xu Tags: Research Article Source Type: research
The Practice of Medicinal Chemistry, 4th Edition.
Camille Wermuth,
David Aldous,
Pierre Raboisson and
Didier Rognan. Academic Press, London, 2015. ISBN Print 9780124172050 $150; eBook 9780124172135. $150. pp xxii + 880.
(Source: Drug Development Research)
Source: Drug Development Research - December 1, 2015 Category: Drugs & Pharmacology Authors: Michael Williams Tags: Book Review Source Type: research
Antihyperalgesic Activity of Rhodiola rosea in a Diabetic Rat Model
ABSTRACT
Rhodiola rosea L. (Crassulaceae) is used for enhancing physical and mental performance. Recent studies demonstrated that R. rosea had anti‐inflammatory activity in animal models, for example, carrageenan‐ and nystatin‐induced edema in rats, possibly by inhibiting phospholipase A2 and cyclooxygenases‐1 and ‐2. In addition, R. rosea had antinociceptive activity in thermal and chemical pain tests as well as mechanical hyperalgesia. The purpose of the present study was to assess the antihyperalgesic effect of an ethanol extract of Rhodiola rosea (R. rosea) in a diabetic rat model. Rats were administer...
Source: Drug Development Research - December 1, 2015 Category: Drugs & Pharmacology Authors: Myrna Déciga‐Campos, Maria Eva González‐Trujano, Rosa Ventura‐Martínez, Rosa Mariana Montiel‐Ruiz, Guadalupe Esther Ángeles‐López, Fernando Brindis Tags: Research Article Source Type: research
Resveratrol Ameliorates the Components of Hepatic Inflammation and Apoptosis in a Rat Model of Streptozotocin‐Induced Diabetes
This study was conducted to elucidate the potential role of resveratrol on hepatic inflammation and the apoptotic pathway components Bcl‐2, Bax and p53 in a streptozotocin (STZ)‐induced rat model of diabetes mellitus. Inflammatory and apoptotic biomarkers indicated a reduction in hepatic erythropoietin (1.26‐fold) and increased asymmetric dimethylarginine (3.9‐fold), visfatin (1.6‐fold), inflammatory interleukins and TNF–α contents (approximately twofold each) in the diabetic animals. Induction of inducible nitric oxide synthase gene (2.04‐fold) and protein expression (1.24‐fold) was also observed. Immunoh...
Source: Drug Development Research - December 1, 2015 Category: Drugs & Pharmacology Authors: Mehmet Bilgehan Pektaş, Gökhan Sadi, Halit Bugra Koca, Yasemin Yuksel, Ayhan Vurmaz, Tulay Koca, Murat Tosun Tags: Research Article Source Type: research
The connection Between Plasma Protein Binding and Acute Toxicity as Determined by the LD50 Value
ABSTRACT
A dataset of three drug classes (acids, bases, and neutrals) with LD50 values in mice was analysed to investigate a possible connection between high plasma protein binding and acute toxicity. Initially, it was found that high plasma protein binding was associated with toxicity for acids and neutrals, but after compensating for differences in lipophilicity, plasma protein binding was found not to be associated with toxicity. The therapeutic index established by the quotient between mouse LD50 and the defined daily dose was unaffected by both lipophilicity and plasma protein binding. Drug Dev Res. © 2015 Wil...
Source: Drug Development Research - December 1, 2015 Category: Drugs & Pharmacology Authors: Andreas Svennebring Tags: Research Article Source Type: research
Evaluation of a Postoperative Pain‐Like State on Motivated Behavior in Rats: Effects of Plantar Incision on Progressive‐Ratio Food‐Maintained Responding
ABSTRACT
There has been recent interest in characterizing the effects of pain‐like states on motivated behaviors in order to quantify how pain modulates goal‐directed behavior and the persistence of that behavior. The current set of experiments assessed the effects of an incisional postoperative pain manipulation on food‐maintained responding under a progressive‐ratio (PR) operant schedule. Independent variables included injury state (plantar incision or anesthesia control) and reinforcer type (grain pellet or sugar pellet); dependent variables were tactile sensory thresholds and response breakpoint. Once re...
Source: Drug Development Research - October 23, 2015 Category: Drugs & Pharmacology Authors: Emily Warner, Rebecca Krivitsky, Katherine Cone, Phillip Atherton, Travis Pitre, Janell Lanpher, Denise Giuvelis, Ivy Bergquist, Tamara King, Edward J. Bilsky, Glenn W. Stevenson Tags: Research Article Source Type: research
Safety of Anti‐TNF Therapies in Immune‐Mediated Inflammatory Diseases: Focus on Infections and Malignancy
ABSTRACT
The efficacy of anti‐TNF agents in the treatment of multiple immune‐mediated inflammatory diseases (IMIDs) has increased their daily use. However, concerns remain regarding their long‐term safety profile. Using a literature‐based review of the infectious and malignant complications of anti‐TNF biologics in IMIDs including psoriasis, Rheumatoid Arthritis, and inflammatory bowel disease, this review presents current evidence relative to the safety of anti‐TNF agents in the context infections and malignancy in adults with IMIDs. Treatment with anti‐TNF biologics is an effective treatment option w...
Source: Drug Development Research - October 20, 2015 Category: Drugs & Pharmacology Authors: Rui Pereira, Paula Lago, Raquel Faria, Tiago Torres Tags: Review Article Source Type: research
Schisandrae Fructus Inhibits IL‐1β‐Induced Matrix Metalloproteinases and Inflammatory Mediators Production in SW1353 Human Chondrocytes by Suppressing NF‐κB and MAPK Activation
This study investigated the antiosteoarthritis properties of an ethanol extract of SF on IL‐1β‐stimulated SW1353 chondrocytes. SF attenuated IL‐1β‐induced expression and activity of matrix metalloproteinase (MMP)‐1, MMP‐3, and MMP‐13 and also reduced the elevated levels of cyclooxygenase‐2 and inducible nitric oxide synthase associated with the inhibition of prostaglandin E2 and nitric oxide production in IL‐1β‐stimulated SW1353 chondrocytes. In addition, SF markedly suppressed the nuclear translocation of nuclear factor‐kappa B (NF‐κB) by blocking inhibitor κB‐alpha degradation and inhibited...
Source: Drug Development Research - October 7, 2015 Category: Drugs & Pharmacology Authors: Jin‐Woo Jeong, Hye Hyeon Lee, Eun‐Ok Choi, Ki Won Lee, Ki Young Kim, Sung Goo Kim, Su Hyun Hong, Gi‐Young Kim, Cheol Park, Ho Kyoung Kim, Young Whan Choi, Yung Hyun Choi Tags: Research Article Source Type: research
A New Role for an Old Drug: Metformin Targets MicroRNAs in Treating Diabetes and Cancer
ABSTRACT
MicroRNAs (miRNAs) are a family of short, noncoding, 19–23 base pair RNA molecules. Due to their unique role in gene regulation in various tissues, miRNAs play important roles in regulating insulin secretion, metabolic disease, and cancer biology. Emerging evidence demonstrates that miRNAs could also be novel diagnostic markers for a variety of disease states. Additionally, miRNAs have been found to function either as oncogenes, or tumor suppressor genes in cerian cancers. An increasing number of studies have been conducted investigating new drugs targeting miRNAs as a potential anticancer therapy. Metfor...
Source: Drug Development Research - September 10, 2015 Category: Drugs & Pharmacology Authors: Joseph Yi Zhou, Biao Xu, Lixin Li Tags: Research Overview Source Type: research
Small‐Molecule Regulators of MicroRNAs in Biomedicine
ABSTRACT
MicroRNAs (miRNAs) can regulate gene expression at the post‐transcriptional level and have been implicated in the development of various human diseases, including cancer. The regulatory networks of miRNAs play a vital role not only in normal physiology but also in pathology and may represent novel targets for drug discovery. Regulation of miRNAs and the elucidation of miRNA networks will advance miRNA‐targeted research but are challenging due to a shortage of appropriate tools. Using different assay systems, diverse small molecules with unique miRNA regulatory activity have been identified. These bioact...
Source: Drug Development Research - September 1, 2015 Category: Drugs & Pharmacology Authors: Tingting Xia, Jinbo Li, Hao Cheng, Chenyu Zhang, Yan Zhang Tags: Research Review Source Type: research
