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Drug Design, Development and Therapy

Yang-Yang He, Yu Yan, Hui-Fang Zhang, Yi-Huang Lin, Yu-Cai Chen, Yi Yan, Ping Wu, Jian-Song Fang, Shu-Hui Yang, Guan-Hua Du
Systemic lupus erythematosus (SLE), with a high incidence rate and insufficient therapy worldwide, is a complex disease involving multiple organs characterized primarily by inflammation due to deposition of immunocomplexes formed by production of autoantibodies. The mechanism of SLE remains unclear, and the disease still cannot be cured. We used pristane to induce SLE in female BALB/c mice. Methyl salicylate 2-O-β-d-lactoside (MSL; 200, 400, and 800 mg/kg) was orally administered 45 days after pristane injection for 4...
2016: Drug Design, Development and Therapy
Xi Zhang, Yuge Ran, Kunjie Wang, Yuanxue Zhu, Jinghua Li
PURPOSE: Anti-programmed cell death receptor-1 (PD-1) antibodies have demonstrated antitumor activity in many cancer entities. Hepatic adverse events (AEs) are one of its major side effects, but the overall risks have not been systematically evaluated. Thus, we conducted this meta-analysis to investigate the overall incidence and risk of developing hepatic AEs in cancer patients treated with PD-1 inhibitors. METHODS: PubMed, Embase, and oncology conference proceedings were searched for relevant studies...
2016: Drug Design, Development and Therapy
Mingsheng Zhang, Enda Xue, Wei Shao
BACKGROUND: Nephroblastoma (Wilms' tumor [WT]) is the most common malignant renal cancer in children. Although the outcome of WT has significantly improved as a result of the combination of surgery, chemotherapy, and radiotherapy; in some cases WT results in severe complications. Thus, novel strategies that would decrease treatment burden are required. The aim of the current study was to investigate the synergistic antitumor effect of andrographolide (AND) in combination with vincristine (VCR) on WT cells...
2016: Drug Design, Development and Therapy
Jan M Keppel Hesselink, Flavia Chiosi, Ciro Costagliola
Resolvins are a novel class of lipid-derived endogenous molecules (autacoids) with potent immunomodulating properties, which regulate the resolution phase of an active immune response. These modulating factors are locally produced, influencing the function of cells and/or tissues, which are produced on demand and subsequently metabolized in the same cells and/or tissues. This review is focused on certain lipid autacoids with putative relevance for ophthalmology in general and for dry eye more specifically. We also briefly investigate the concept of aliamides and the role of palmitoylethanolamide in ophthalmology, and analyze in more detail the putative role and the preclinical and clinical development of resolvins as emerging treatments for dry eye and related disorders, with a focus on one of the lead resolvin derivatives - RX-10045...
2016: Drug Design, Development and Therapy
Stephen Flach, Marie Croft, Jie Ding, Ron Budhram, Todd Pankratz, Mike Pennick, Graeme Scarfe, Steven Troy, Jay Getsy
PURPOSE: Gastroesophageal reflux disease involves the reflux of gastric and/or duodenal content into the esophagus. Prokinetic therapies, such as the selective 5-hydroxytryptamine receptor 4 agonist revexepride, may aid gastric emptying. This Phase I study evaluated the pharmacokinetics and excretion pathways of [(14)C]revexepride in healthy individuals using a microtracer approach with accelerator mass spectrometry. PARTICIPANTS AND METHODS: Six healthy men received a single oral dose of 2 mg [(14)C]revexepride containing ~200 nCi of radioactivity; blood, urine, and fecal samples were collected over a 10-day period...
2016: Drug Design, Development and Therapy
Bincy Baby, Priya Antony, Walaa Al Halabi, Zahrah Al Homedi, Ranjit Vijayan
Polypharmacology, the discovery or design of drug molecules that can simultaneously interact with multiple targets, is gaining interest in contemporary drug discovery. Serine/threonine kinases are attractive targets for therapeutic intervention in oncology due to their role in cellular phosphorylation and altered expression in cancer. Quercetin, a naturally occurring flavonoid, inhibits multiple cancer cell lines and is used as an anticancer drug in Phase I clinical trial. Quercetin glycosides have also received some attention due to their high bioavailability and activity against various diseases including cancer...
2016: Drug Design, Development and Therapy
Jianming Wu, Xiao Ke, Na Ma, Wei Wang, Wei Fu, Hongcheng Zhang, Manxi Zhao, Xiaoping Gao, Xiaofeng Hao, Zhirong Zhang
BACKGROUND: It has been reported that formononetin (FMN), one of the main ingredients from famous traditional Chinese medicine "Huang-qi" (Astragalus membranaceus [Fisch] Bunge) for Qi-tonifying, exhibits the effects of immunomodulation and tumor growth inhibition via antiangiogenesis. Furthermore, A. membranaceus may alleviate the retinal neovascularization (NV) of diabetic retinopathy. However, the information of FMN on retinal NV is limited so far. In the present study, we investigated the effects of FMN on the hypoxia-induced retinal NV and the possible related mechanisms...
2016: Drug Design, Development and Therapy
Jamileh Moghimi, Ali Asghar Rezaei, Raheb Ghorbani, Mohammad Reza Razavi, Daryoush Pahlevan
In the current study, the overall prevalence and the main underlying etiologies of inflammatory low back pain (ILBP) were determined, and the effectiveness of treatment with sulfasalazine was investigated in patients with inflammatory versus mechanical low back pain (LBP). In a prospective study conducted from July 2013 until August 2015, 1,779 consecutive patients within the age range of 18-50 years with a primary complaint of LBP referring to the rheumatology clinics were included. The patients were classified into two distinct groups: those suffering from ILBP (n=118) and those having mechanical LBP (n=1,661)...
2016: Drug Design, Development and Therapy
Yinxiang Lv, Yanan Huo, Xican Yu, Rongrong Liu, Shufen Zhang, Xiaoxiao Zheng, Xianning Zhang
Resistance to chemotherapeutic drugs is a major obstacle in non-small cell lung cancer (NSCLC) therapy. The molecular determinants of NSCLC resistance to doxorubicin are unknown. In the present study, we investigated whether topoisomerase IIβ binding protein 1 (TopBP1) was involved in the chemoresistance to doxorubicin in NSCLC cancer. We found that p53-deficient lung cancer cells (NCI-H1299) displayed the greatest resistance to doxorubicin compared with NCI-H358, A549, and HCC827 cells with p53 expression...
2016: Drug Design, Development and Therapy
Tomoki Tada, Kensaku Aki, Wataru Oboshi, Kazuyoshi Kawazoe, Toshiyuki Yasui, Eiji Hosoi
BACKGROUND: The hyperfunction and activation of platelets have been strongly implicated in the development and recurrence of arterial occlusive disease, and various antiplatelet drugs are used to treat and prevent such diseases. New antiplatelet drugs and many other drugs have been developed, but some drugs may have adverse effects on platelet functions. OBJECTIVE: The aim of this study was to establish an evaluation method for evaluating the effect and adverse effect of various drugs on platelet functions...
2016: Drug Design, Development and Therapy
Pietro Enea Lazzerini, Pier Leopoldo Capecchi, Giacomo Maria Guidelli, Enrico Selvi, Maurizio Acampa, Franco Laghi-Pasini
Rheumatoid arthritis (RA) is a chronic autoimmune inflammatory disease primarily affecting synovial joints and is characterized by persistent high-grade systemic inflammation. Proinflammatory cytokines, particularly interleukin-6 (IL-6), are of crucial importance in the pathogenesis of the disease, driving both joint inflammation and extra-articular comorbidities. Tocilizumab, a humanized IL-6 receptor-inhibiting monoclonal antibody, has been the first, and, to date, the only, IL-6 inhibitor approved for the treatment of RA...
2016: Drug Design, Development and Therapy
Marija Darkovska-Serafimovska, Emilija Janevik-Ivanovska, Icko Djorgoski, Zorica Arsova-Sarafinovska, Milka Zdravkovska, Trajan Balkanov, Nenad Ugresic
AIM: The aim of this study was to investigate the possibility of using (99m)technetium ((99m)Tc)-labeled tirofiban (a reversible antagonist of glycoprotein IIb/IIIa) for detection of deep venous thrombosis (DVT) in rats without causing an antiplatelet effect. METHODS: The ability of in vitro tirofiban to inhibit adenosine 5'-diphosphate (ADP)-induced platelet aggregation was evaluated using optical aggregometer. Binding of (99m)Tc-tirofiban to platelets was evaluated...
2016: Drug Design, Development and Therapy
Ao Zhou, Shuo Chen, Bin He, Weikang Zhao, Xiaojun Chen, Dianming Jiang
Bioactive mediators, cytokines, and chemokines have an important role in regulating and optimizing the synergistic action of materials, cells, and cellular microenvironments for tissue engineering. RADA self-assembling peptide hydrogels have been proved to have an excellent ability to promote cell proliferation, wound healing, tissue repair, and drug delivery. Here, we report that D-RADA16 and L-RADA16-RGD self-assembling peptides can form stable second structure and hydrogel scaffolds, affording the slow release of growth factor (transforming growth factor cytokine-beta 1 [TGF-beta 1])...
2016: Drug Design, Development and Therapy
Kok-Yong Chin
Osteoarthritis is a degenerative disease of the joint affecting aging populations worldwide. It has an underlying inflammatory cause, which contributes to the loss of chondrocytes, leading to diminished cartilage layer at the affected joints. Compounds with anti-inflammatory properties are potential treatment agents for osteoarthritis. Curcumin derived from Curcuma species is an anti-inflammatory compound as such. This review aims to summarize the antiosteoarthritic effects of curcumin derived from clinical and preclinical studies...
2016: Drug Design, Development and Therapy
YoonJung Choi, SeungHwan Lee, Sang-Min Cho, Won-Ho Kang, Kyu-Yeol Nam, In-Jin Jang, Kyung-Sang Yu
BACKGROUND: A fixed-dose combination (FDC) of amlodipine and losartan has been used to reduce blood pressure in patients whose hypertension is not sufficiently controlled with either drug alone. The aim of this study was to evaluate the pharmacokinetic (PK) characteristics and tolerability of an FDC of 6.94 mg amlodipine besylate (5 mg as amlodipine)/50 mg losartan potassium compared to an FDC of 5 mg amlodipine camsylate/50 mg losartan potassium in healthy subjects. SUBJECTS AND METHODS: A randomized, open-label, single-dose, two-period, two-sequence crossover study was conducted on 46 healthy male subjects...
2016: Drug Design, Development and Therapy
Marion J Skalweit, Mei Li
Genetic screening of Pseudomonas aeruginosa (PSDA) and Acinetobacter baumannii (ACB) reveals genes that confer increased susceptibility to β-lactams when disrupted, suggesting novel drug targets. One such target is lytic transglycosylase. Bulgecin A (BlgA) is a natural product of Pseudomonas mesoacidophila and a lytic transglycosolase inhibitor that works synergistically with β-lactams targeting PBP3 for Enterobacteriaceae. BlgA also weakly inhibits di-Zn(2+) metallo-β-lactamases like L1 of Stenotrophomonas maltophilia...
2016: Drug Design, Development and Therapy
Shoaleh Shami, Karim Nasseri, Mousa Shirmohammadi, Farzad Sarshivi, Negin Ghadami, Ebrahim Ghaderi, Mokhtar Pouladi, Arvin Barzanji
INTRODUCTION: Shivering is among the unpleasant and potentially harmful side effects of spinal anesthesia. The aim of this randomized double-blind clinical trial was to compare the antishivering effect of two different doses of intrathecal pethidine on the incidence and intensity of shivering and other side effects in patients who underwent cesarean section. METHODS: In this study, 150 parturient females scheduled for nonemergent cesarean section were randomly allocated to three groups...
2016: Drug Design, Development and Therapy
Stephen J Balevic, C Egla Rabinovich
Uveitis refers to the presence of intraocular inflammation, and as a strict definition compromises the iris and ciliary body anteriorly and the choroid posteriorly (the uvea). Untreated, uveitis can lead to visual loss or blindness. The etiology of uveitis can include both infectious and noninfectious (usually immune-mediated) causes, the latter of which are often mediated predominantly by Th1 CD4(+) T-cells that secrete proinflammatory cytokines. Tumor necrosis factor-alpha (TNF-α) is a proinflammatory cytokine involved in the pathogenesis of uveitis, which at high concentrations can cause excess inflammation and tissue damage...
2016: Drug Design, Development and Therapy
Shao-Hui Lin, Wei Cui, Gui-Ling Wang, Shuai Meng, Ying-Chun Liu, Hong-Wei Jin, Liang-Ren Zhang, Ying Xie
Albumin-based nanoparticles (NPs) are a promising technology for developing drug-carrier systems, with improved deposition and retention profiles in lungs. Improved understanding of these drug-carrier interactions could lead to better drug-delivery systems. The present study combines computational and experimental methods to gain insights into the mechanism of binding of albuterol sulfate (AS) to bovine serum albumin (BSA) on the molecular level. Molecular dynamics simulation and surface plasmon resonance spectroscopy were used to determine that there are two binding sites on BSA for AS: the first of which is a high-affinity site corresponding to AS1 and the second of which appears to represent the integrated functions of several low-affinity sites corresponding to AS2, AS3, and AS8...
2016: Drug Design, Development and Therapy
Jee Sun Min, Doyun Kim, Jung Bae Park, Hyunjin Heo, Soo Hyeon Bae, Jae Hong Seo, Euichaul Oh, Soo Kyung Bae
BACKGROUND: Evaluating the potential risk of metabolic drug-drug interactions (DDIs) is clinically important. OBJECTIVE: To develop a physiologically based pharmacokinetic (PBPK) model for sarpogrelate hydrochloride and its active metabolite, (R,S)-1-{2-[2-(3-methoxyphenyl)ethyl]-phenoxy}-3-(dimethylamino)-2-propanol (M-1), in order to predict DDIs between sarpogrelate and the clinically relevant cytochrome P450 (CYP) 2D6 substrates, metoprolol, desipramine, dextromethorphan, imipramine, and tolterodine...
2016: Drug Design, Development and Therapy
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