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Drug Design, Development and Therapy

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https://www.readbyqxmd.com/read/29440875/experimental-and-molecular-modeling-approach-to-optimize-suitable-polymers-for-fabrication-of-stable-fluticasone-nanoparticles-with-enhanced-dissolution-and-antimicrobial-activity
#1
Shaimaa Ahmed, Thirumala Govender, Inamullah Khan, Nisar Ur Rehman, Waqar Ali, Syed Muhammad Hassan Shah, Shahzeb Khan, Zahid Hussain, Riaz Ullah, Mansour S Alsaid
Background and aim: The challenges with current antimicrobial drug therapy and resistance remain a significant global health threat. Nanodrug delivery systems are playing a crucial role in overcoming these challenges and open new avenues for effective antimicrobial therapy. While fluticasone (FLU), a poorly water-soluble corticosteroid, has been reported to have potential antimicrobial activity, approaches to optimize its dissolution profile and antimicrobial activity are lacking in the literature...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29440874/clinical-potential-of-mechlorethamine-gel-for-the-topical-treatment-of-mycosis-fungoides-type-cutaneous-t-cell-lymphoma-a-review-on-current-efficacy-and-safety-data
#2
REVIEW
Kendall Liner, Celeste Brown, Laura Y McGirt
Nitrogen mustard is a chemotherapeutic agent that has a well-documented safety and efficacy profile in the treatment of cutaneous T-cell lymphoma. Development of nitrogen mustard formulations and treatment regimens has been studied extensively over the last 40 years. In the last 5 years, a new gel formulation has been developed that is associated with a decrease in delayed hypersensitivity reactions. The authors in this review found that while the gel formulation may result in a decrease of allergic contact dermatitis, this advantage has been replaced by a higher number of irritant contact reactions and a decrease in complete response rate...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29430172/dysregulation-of-neuregulin-1-erbb-signaling-in-the-hippocampus-of-rats-after-administration-of-doxorubicin
#3
Dehua Liao, Yujin Guo, Daxiong Xiang, Ruili Dang, Pengfei Xu, Hualin Cai, Lizhi Cao, Pei Jiang
Objective: Long-term use of doxorubicin (Dox) can cause neurobiological side effects associated with depression, but the underlying mechanisms remain equivocal. While recent evidence has indicated that Neuregulin-1 (NRG1) and its ErbB receptors play an essential role in neural function, much is still unknown concerning the biological link between the NRG1/ErbB pathway and the Dox-induced neurotoxicity. Therefore, we examined the protein expression of NRG1 and ErbB receptors in the hippocampus of rats following Dox treatment...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29416317/the-influence-of-prebiotic-or-probiotic-supplementation-on-antibody-titers-after-influenza-vaccination-a-systematic-review-and-meta-analysis-of-randomized-controlled-trials
#4
Tzu-Lin Yeh, Pei-Ching Shih, Shu-Jung Liu, Chao-Hsu Lin, Jui-Ming Liu, Wei-Te Lei, Chien-Yu Lin
Background: Influenza infection is a common disease with a huge disease burden. Influenza vaccination has been widely used, but concerns regarding vaccine efficacy exist, especially in the elderly. Probiotics are live microorganisms with immunomodulatory effects and may enhance the immune responses to influenza vaccination. Methods: We conducted a systematic review and meta-analysis to determine the influence of prebiotics/probiotics/synbiotics supplementation on vaccine responses to influenza vaccination...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29416316/durvalumab-an-investigational-anti-pd-l1-monoclonal-antibody-for-the-treatment-of-urothelial-carcinoma
#5
REVIEW
Izak Faiena, Amy L Cummings, Anna M Crosetti, Allan J Pantuck, Karim Chamie, Alexandra Drakaki
Our expanding knowledge of immunotherapy for solid tumors has led to an explosion of clinical trials aimed at urothelial carcinoma. The primary strategy is centered on unleashing the immune system by releasing the inhibitory signals propagated by programmed cell death-1 (PD-1) and its ligand programmed cell death ligand-1 (PD-L1). Many antibody constructs have been developed to block these interactions and are used in clinical trials. The Food and Drug Administration has already approved a number of checkpoint inhibitors such as anti-cytotoxic T-lymphocyte-associated protein 4 (CTLA4) monoclonal antibodies including ipilimumab; anti-PD-1 monoclonal antibodies including nivolumab and pembrolizumab; anti-PD-L1 antibodies including atezolizumab, avelumab, and durvalumab...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29403265/bispecific-antibodies-design-therapy-perspectives
#6
REVIEW
Sergey E Sedykh, Victor V Prinz, Valentina N Buneva, Georgy A Nevinsky
Antibodies (Abs) containing two different antigen-binding sites in one molecule are called bispecific. Bispecific Abs (BsAbs) were first described in the 1960s, the first monoclonal BsAbs were generated in the 1980s by hybridoma technology, and the first article describing the therapeutic use of BsAbs was published in 1992, but the number of papers devoted to BsAbs has increased significantly in the last 10 years. Particular interest in BsAbs is due to their therapeutic use. In the last decade, two BsAbs - catumaxomab in 2009 and blinatumomab in 2014, were approved for therapeutic use...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29403264/anticonvulsant-and-reproductive-toxicological-studies-of-the-imidazole-based-histamine-h3r-antagonist-2-18-in-mice
#7
Salim M Bastaki, Yousef M Abdulrazzaq, Mohamed Shafiullah, Małgorzata Więcek, Katarzyna Kieć-Kononowicz, Bassem Sadek
The imidazole-based H3R antagonist 2-18 with high in vitro H3R antagonist affinity, excellent in vitro selectivity profile, and high in vivo H3R antagonist potency was tested for its anticonvulsant effect in maximal electroshock (MES)-induced convulsions in mice having valproic acid (VPA) as a reference antiepileptic drug (AED). Additionally, H3R antagonist 2-18 was evaluated for its reproductive toxicity in the same animal species. The results show that acute systemic administration (intraperitoneal; i.p.) of H3R antagonist 2-18 (7...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29398906/involvement-of-microrna-146a-in-diabetic-peripheral-neuropathy-through-the-regulation-of-inflammation
#8
Yonghao Feng, Long Chen, Qiong Luo, Men Wu, Yinghui Chen, Xiaohong Shi
Purpose: Recent evidence has shown the involvement of inflammation in the development of diabetic peripheral neuropathy (DPN). MicroRNA-146a (miR-146a) is closely involved in the inflammatory response. However, the role of miR-146a in the inflammatory reaction in DPN has not been clarified. This study was designed to explore the role of miR-146a in the regulation of inflammatory responses in DPN. Methods: Rats were randomly divided into three groups (n=6 per group): control group, type 2 diabetes mellitus (T2DM) group and DPN group...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29391780/diminishing-the-side-effect-of-mitomycin-c-by-using-ph-sensitive-liposomes-in-vitro-characterization-and-in-vivo-pharmacokinetics
#9
Yi-Ping Fang, Pei-Yu Hu, Yaw-Bin Huang
Introduction: Mitomycin C is an anticancer antibiotic agent that has the potential for broad-spectrum use against several cancers, including mammary cancers. Because its half-life is 17 min after a 30 mg intravenous bolus administration, the suitability of mitomycin C for wide use in the clinical setting is limited. Based on tumor pathophysiology, pH-sensitive liposomes could provide better tumor-targeted effects. The aim of this study was to investigate the possibility of diminishing the side effect of mitomycin C by using pH-sensitive liposomes...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29391779/biological-activity-quantitative-structure-activity-relationship-analysis-and-molecular-docking-of-xanthone-derivatives-as-anticancer-drugs
#10
Isnatin Miladiyah, Jumina Jumina, Sofia Mubarika Haryana, Mustofa Mustofa
Background: Xanthone derivatives have a wide range of pharmacological activities, such as those involving antibacterial, antiviral, antimalarial, anthelmintic, anti-inflammatory, antiprotozoal, and anticancer properties. Among these, we investigated the anticancer properties of xanthone. This research aimed to analyze the biological activity of ten novel xanthone derivatives, to investigate the most contributing-descriptors for their cytotoxic activities, and to examine the possible mechanism of actions of xanthone compound through molecular docking...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29391778/ipriflavone-promotes-proliferation-and-osteogenic-differentiation-of-periodontal-ligament-cells-by-activating-gpr30-pi3k-akt-signaling-pathway
#11
Yuanyuan Han, Xuxia Wang, Dan Ma, Xiaoxiao Wu, Panpan Yang, Jun Zhang
Objectives: This study was performed to investigate the effects and mechanism of ipriflavone (IP) on the proliferation and osteoblastic differentiation of periodontal ligament cells in vitro and periodontal tissue remodeling following orthodontic tooth movement (OTM) in vivo. Materials and methods: Human periodontal ligament cells (hPDLCs) were cultured in vitro and cell counting kit-8, alkaline phosphatase (ALP) activity assay, plate clone formation assay, and alizarin red staining were used to test proliferation and osteogenic differentiation of hPDLCs...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29391777/natural-products-an-important-resource-for-discovery-of-multitarget-drugs-and-functional-food-for-regulation-of-hepatic-glucose-metabolism
#12
REVIEW
Jian Li, Haiyang Yu, Sijian Wang, Wei Wang, Qian Chen, Yanmin Ma, Yi Zhang, Tao Wang
Imbalanced hepatic glucose homeostasis is one of the critical pathologic events in the development of metabolic syndromes (MSs). Therefore, regulation of imbalanced hepatic glucose homeostasis is important in drug development for MS treatment. In this review, we discuss the major targets that regulate hepatic glucose homeostasis in human physiologic and pathophysiologic processes, involving hepatic glucose uptake, glycolysis and glycogen synthesis, and summarize their changes in MSs. Recent literature suggests the necessity of multitarget drugs in the management of MS disorder for regulation of imbalanced glucose homeostasis in both experimental models and MS patients...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29391776/efficacy-and-side-effects-of-intravenous-theophylline-in-acute-asthma-a-systematic-review-and-meta-analysis
#13
Gulixian Mahemuti, Hui Zhang, Jing Li, Nueramina Tieliwaerdi, Lili Ren
Background and objective: Theophylline has been used for decades to treat both acute and chronic asthma. Despite its longevity in the practitioner's formulary, no detailed meta-analysis has been performed to determine the conditions, including concomitant medications, under which theophylline should be used for acute exacerbations of asthma. We aimed to quantify the usefulness and side effects of theophylline with or without ethylene diamine (aminophylline) in acute asthma, with particular emphasis on patient subgroups, such as children, adults, and concomitant medications...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29386886/renal-protective-effect-of-thalidomide-in-streptozotocin-induced-diabetic-rats-through-anti-inflammatory-pathway
#14
Hongxia Zhang, Yanlan Yang, Yanqin Wang, Baodong Wang, Rongshan Li
Background: Diabetic nephropathy (DN) is a major microvascular complication in diabetes. An increasing body of evidence has shown that DN is related to chronic inflammation, kidney hypertrophy, and fibrosis. While thalidomide has been shown to have anti-inflammatory and antifibrotic effects, the effects of thalidomide on the pathogenesis of DN are unclear. This study was undertaken to explore whether thalidomide has renal-protective effects in diabetic rats. Methods: Male Sprague Dawley rats were injected intraperitoneally with 50 mg/kg streptozotocin to induce diabetes...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29386885/peptides-derived-from-plasmodium-falciparum-leucine-rich-repeat-1-bind-to-serine-threonine-phosphatase-type-1-and-inhibit-parasite-growth-in-vitro
#15
Christine Pierrot, Xiguang Zhang, Gigliola Zhangi, Aline Fréville, Angelita Rebollo, Jamal Khalife
No abstract text is available yet for this article.
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29379271/sinomenine-reduces-neuronal-cell-apoptosis-in-mice-after-traumatic-brain-injury-via-its-effect-on-mitochondrial-pathway
#16
Chuanjing Fu, Qi Wang, Xiaofu Zhai, Juemin Gao
Background: Sinomenine (SIN) has been shown to have protective effects against brain damage following traumatic brain injury (TBI). However, the mechanisms and its role in these effects remain unclear. This study was conducted to investigate the potential mechanisms of the protective effects of SIN. Methods: The weight-drop model of TBI in Institute of Cancer Research (ICR) mice were treated with SIN or a vehicle via intraperitoneal administration 30 min after TBI...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29343944/quantitative-assessment-of-the-effects-of-chitosan-intervention-on-blood-pressure-control
#17
Haohai Huang, Ying Zou, Honggang Chi
Background: Chitosan is a popular dietary fiber often used to reduce dietary fat absorption to control weight and blood lipids. However, its effects on blood pressure (BP) have not been fully elucidated. We evaluated the effects of chitosan administration on systolic blood pressure (SBP) and diastolic blood pressure (DBP) through a pooled analysis of available randomized controlled trials (RCTs). Materials and methods: Electronic searches were conducted in Medline, Cochrane Library, Scopus, and EMBASE to identify relevant human placebo-control RCTs...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29343943/the-oral-bioavailability-excretion-and-cytochrome-p450-inhibition-properties-of-epiberberine-an-in-vivo-and-in-vitro-evaluation
#18
Ning Chen, Xiao-Yan Yang, Chang-E Guo, Xin-Ning Bi, Jian-Hua Chen, Hong-Ying Chen, Hong-Pin Li, Hong-Ying Lin, Yu-Jie Zhang
Epiberberine (EPI) is a novel and potentially effective therapeutic and preventive agent for diabetes and cardiovascular disease. To evaluate its potential value for drug development, a specific, sensitive and robust high-performance liquid chromatography-tandem mass spectrometry assay for the determination of EPI in rat biological samples was established. This assay was used to study the pharmacokinetics, bioavailability and excretion of EPI in rats after oral administration. In addition, a cocktail method was used to compare the inhibition characteristics of EPI on cytochrome P450 (CYP450) isoforms in human liver microsomes (HLMs) and rat liver microsomes (RLMs)...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29343942/portulaca-oleracea-l-alleviates-liver-injury-in-streptozotocin-induced-diabetic-mice
#19
Guoyin Zheng, Fengfeng Mo, Chen Ling, Hao Peng, Wei Gu, Min Li, Zhe Chen
Purslane is a widespread succulent herb that exhibits various pharmacological effects. The purpose of this study was to evaluate the protective effect of Portulaca oleracea L. (purslane) on streptozotocin-induced diabetes in mice. Oral glucose-tolerance tests were carried out to assess blood glucose levels and body weight and food intake were recorded. The biochemical parameters anti-aspartate aminotransferase, alanine aminotransferase, insulin, triglycerides, total cholesterol, IL-6, IL-1β, and TNFα were also measured...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29343941/clinical-features-of-hypophosphatemic-osteomalacia-induced-by-long-term-low-dose-adefovir-dipivoxil
#20
Sheng Zhu, Yu-Hui Yang, Rong-Wei Gao, Ran Li, Yu-Zhen Zou, Lei Feng, Bo Zhang
Objective: To investigate the predictors of hypophosphatemic osteomalacia induced by adefovir dipivoxil (ADV) and to monitor for early detection. Patients and methods: Hospitalized patients who were diagnosed with ADV-related hypo-phosphatemic osteomalacia were recruited and retrospectively analyzed in our hospital from January 2012 to December 2016. A telephone interview was conducted at 1, 3, 6, 9, 12, and 24 months after cessation of ADV. Results: In the 8 patients enrolled in the study, the hypophosphatemic osteomalacia symptoms developed at an average of 5...
2018: Drug Design, Development and Therapy
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