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Drug Design, Development and Therapy

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https://www.readbyqxmd.com/read/28223780/erratum-evaluation-of-effects-of-various-drugs-on-platelet-functions-using-phorbol-12-myristate-13-acetate-induced-megakaryocytic-human-erythroid-leukemia-cells-corrigendum
#1
(no author information available yet)
[This corrects the article on p. 3099 in vol. 10.].
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28223779/effect-of-dexmedetomidine-in-preventing-etomidate-induced-myoclonus-a-meta-analysis
#2
REVIEW
Xueke Du, Chengmao Zhou, Linghui Pan, Changlong Li
OBJECTIVE: To investigate the effect of dexmedetomidine in the prevention of etomidate-induced myoclonus. METHODS: We searched for randomized controlled trials (RCTs) regarding the use of dexmedetomidine in preventing etomidate-induced myoclonus in the databases PubMed, EMBASE, the Cochrane Library, and CNKI. We extracted data and assessed the quality of the literature and adopted RevMan 5.2 to conduct meta-analysis on each effective index and employed funnel plot to test publication bias...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28223778/gancidin-w-a-potential-low-toxicity-antimalarial-agent-isolated-from-an-endophytic-streptomyces-suk10
#3
Noraziah Mohamad Zin, Mohd Shukri Baba, Abu Hassan Zainal-Abidin, Jalifah Latip, Noor Wini Mazlan, RuAngelie Edrada-Ebel
Endophytic Streptomyces strains are potential sources for novel bioactive molecules. In this study, the diketopiperazine gancidin W (GW) was isolated from the endophytic actinobacterial genus Streptomyces, SUK10, obtained from the bark of Shorea ovalis tree, and it was tested in vivo against Plasmodium berghei PZZ1/100. GW exhibited an inhibition rate of nearly 80% at 6.25 and 3.125 μg kg(-1) body weight on day four using the 4-day suppression test method on male ICR strain mice. Comparing GW at both concentrations with quinine hydrochloride and normal saline as positive and negative controls, respectively, 50% of the mice treated with 3...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28223777/phloretin-exerts-hypoglycemic-effect-in-streptozotocin-induced-diabetic-rats-and-improves-insulin-resistance-in-vitro
#4
Xin Shen, Nan Zhou, Le Mi, Zishuo Hu, Libin Wang, Xueying Liu, Shengyong Zhang
The present study investigated the possible antiobesity and hypoglycemic effects of phloretin (Ph). In an attempt to discover the hypoglycemic effect and potential mechanism of Ph, we used the streptozotocin-induced diabetic rats and (L6) myotubes. Daily oral treatment with Ph for 4 weeks significantly (P<0.05) reduced postprandial blood glucose and improved islet injury and lipid metabolism. Glucose consumption and glucose tolerance were improved by Ph via GOD-POD method. Western blot results revealed that the expression of Akt, PI3K, IRS-1, and GLUT4 were upregulated in skeletal muscle of type 2 diabetes (T2D) rats and in L6 myotubes by Ph...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28203057/kelussia-odoratissima-mozaff-activates-intrinsic-pathway-of-apoptosis-in-breast-cancer-cells-associated-with-s-phase-cell-cycle-arrest-via-involvement-of-p21-p27-in-vitro-and-in-vivo
#5
Hamed Karimian, Aditya Arya, Mehran Fadaeinasab, Mahboubeh Razavi, Maryam Hajrezaei, Ataul Karim Khan, Hapipah Mohd Ali, Mahmood Ameen Abdulla, Mohamad Ibrahim Noordin
BACKGROUND: The aim of this study was to evaluate the anticancer potential of Kelussia odoratissima. Several in vitro and in vivo biological assays were applied to explore the direct effect of an extract and bioactive compound of this plant against breast cancer cells and its possible mechanism of action. MATERIALS AND METHODS: K. odoratissima methanol extract (KME) was prepared, and MTT assay was used to evaluate the cytotoxicity. To identify the cytotoxic compound, a bioassay-guided investigation was performed on methanol extract...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28184152/drug-delivery-in-overcoming-the-blood-brain-barrier-role-of-nasal-mucosal-grafting
#6
REVIEW
Carlotta Marianecci, Federica Rinaldi, Patrizia Nadia Hanieh, Luisa Di Marzio, Donatella Paolino, Maria Carafa
The blood-brain barrier (BBB) plays a fundamental role in protecting and maintaining the homeostasis of the brain. For this reason, drug delivery to the brain is much more difficult than that to other compartments of the body. In order to bypass or cross the BBB, many strategies have been developed: invasive techniques, such as temporary disruption of the BBB or direct intraventricular and intracerebral administration of the drug, as well as noninvasive techniques. Preliminary results, reported in the large number of studies on the potential strategies for brain delivery, are encouraging, but it is far too early to draw any conclusion about the actual use of these therapeutic approaches...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28182168/drugs-in-development-for-toxoplasmosis-advances-challenges-and-current-status
#7
REVIEW
P Holland Alday, Joseph Stone Doggett
Toxoplasma gondii causes fatal and debilitating brain and eye diseases. Medicines that are currently used to treat toxoplasmosis commonly have toxic side effects and require prolonged courses that range from weeks to more than a year. The need for long treatment durations and the risk of relapsing disease are in part due to the lack of efficacy against T. gondii tissue cysts. The challenges for developing a more effective treatment for toxoplasmosis include decreasing toxicity, achieving therapeutic concentrations in the brain and eye, shortening duration, eliminating tissue cysts from the host, safety in pregnancy, and creating a formulation that is inexpensive and practical for use in resource-poor areas of the world...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28182141/obinutuzumab-in-chronic-lymphocytic-leukemia-design-development-and-place-in-therapy
#8
REVIEW
Othman Al-Sawaf, Kirsten Fischer, Anja Engelke, Natali Pflug, Michael Hallek, Valentin Goede
For decades, treatment of chronic lymphocytic leukemia (CLL) has been based on chemotherapy. This changed when the first CD20 antibody rituximab was introduced. Since 2008, the combination of chemotherapy and CD20 antibodies has become the standard of care for most patients, and a significant fraction of patients had very long-lasting remissions after chemoimmunotherapy. Despite the improvement of response rates and overall survival (OS) by the use of chemoimmunotherapy, most CLL patients will relapse eventually...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28182127/impact-of-metoprolol-treatment-on-mental-status-of-chronic-heart-failure-patients-with-neuropsychiatric-disorders
#9
Xuelu Liu, Xueming Lou, Xianliang Cheng, Yong Meng
BACKGROUND: Metoprolol treatment is well established for chronic heart failure (CHF) patients, but the central nervous system side effects are often a potential drawback. OBJECTIVE: To investigate the impact of metoprolol treatment on change in mental status of CHF patients with clinical psychological disorders (such as depression, anxiety, and burnout syndrome). METHODS: From February 2013 to April 2016, CHF patients with clinical mental disorders received metoprolol (23...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28176948/theophylline-action-on-primary-human-bronchial-epithelial-cells-under-proinflammatory-stimuli-and-steroidal-drugs-a-therapeutic-rationale-approach
#10
Luca Gallelli, Daniela Falcone, Roberto Cannataro, Mariarita Perri, Raffaele Serra, Girolamo Pelaia, Rosario Maselli, Rocco Savino, Giuseppe Spaziano, Bruno D'Agostino
Theophylline is a natural compound present in tea. Because of its property to relax smooth muscle it is used in pharmacology for the treatment of airway diseases (ie, chronic obstructive pulmonary disease, asthma). However, this effect on smooth muscle is dose dependent and it is related to the development of side effects. Recently, an increasing body of evidence suggests that theophylline, at low concentrations, also has anti-inflammatory effects related to the activation of histone deacetylases. In this study, we evaluated the effects of theophylline alone and in combination with corticosteroids on human bronchial epithelial cells under inflammatory stimuli...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28176928/n-3-hydroxymethyl-%C3%AE-carboline-1-yl-ethyl-2-yl-l-phe-development-toward-a-nanoscaled-antitumor-drug-capable-of-treating-complicated-thrombosis-and-inflammation
#11
Jianhui Wu, Ming Zhao, Yuji Wang, Yaonan Wang, Haimei Zhu, Shurui Zhao, Lin Gui, Xiaoyi Zhang, Shiqi Peng
It is well documented that the surfaces of cancer cells, activated platelets and inflammatory cells are rich in P-selectin. N-(3-hydroxymethyl-β-carboline-1-yl-ethyl-2-yl)-l-Phe (HMCEF) is a P-selectin inhibitor capable of simultaneously inhibiting thrombosis and inflammation. Based on the knowledge that P-selectin is a common target for antithrombotic, anti-inflammatory and antitumor drugs, the aim of this study article was to estimate the possibility of HMCEF as a nanoscaled antitumor drug. Images of transmission electron micro scopy, scanning electron microscopy and atomic force microscopy proved that HMCEF forms nanoparticles with a diameter of <120 nm that promote delivery in blood circulation...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28176905/effect-of-roll-compaction-on-granule-size-distribution-of-microcrystalline-cellulose-mannitol-mixtures-computational-intelligence-modeling-and-parametric-analysis
#12
Pezhman Kazemi, Mohammad Hassan Khalid, Ana Pérez Gago, Peter Kleinebudde, Renata Jachowicz, Jakub Szlęk, Aleksander Mendyk
Dry granulation using roll compaction is a typical unit operation for producing solid dosage forms in the pharmaceutical industry. Dry granulation is commonly used if the powder mixture is sensitive to heat and moisture and has poor flow properties. The output of roll compaction is compacted ribbons that exhibit different properties based on the adjusted process parameters. These ribbons are then milled into granules and finally compressed into tablets. The properties of the ribbons directly affect the granule size distribution (GSD) and the quality of final products; thus, it is imperative to study the effect of roll compaction process parameters on GSD...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28176904/plitidepsin-design-development-and-potential-place-in-therapy
#13
REVIEW
Sara Alonso-Álvarez, Emilia Pardal, Diego Sánchez-Nieto, Miguel Navarro, Maria Dolores Caballero, Maria Victoria Mateos, Alejandro Martín
Plitidepsin is a cyclic depsipeptide that was first isolated from a Mediterranean marine tunicate (Aplidium albicans) and, at present, is manufactured by total synthesis and commercialized as Aplidin(®). Its antitumor activity, observed in preclinical in vitro and in vivo studies has prompted numerous clinical trials to be conducted over the last 17 years, alone or in combination with other anticancer agents. Single-agent plitidepsin has shown limited antitumor activity and a tolerable safety profile in several malignancies, such as noncutaneous peripheral T-cell lymphoma, melanoma, and multiple myeloma...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28144129/spotlight-on-mavrilimumab-for-the-treatment-of-rheumatoid-arthritis-evidence-to-date
#14
REVIEW
Chiara Crotti, Maria Gabriella Raimondo, Andrea Becciolini, Martina Biggioggero, Ennio Giulio Favalli
The introduction of biological therapies into clinical practice has dramatically modified the natural history of chronic inflammatory diseases, such as rheumatoid arthritis (RA). RA is a systemic autoimmune disease that causes articular damage and has a great negative impact on patients' quality of life. Despite the wide spectrum of available biological treatments, ~30% of RA patients are still unresponsive, resulting in high disability and increased morbidity and mortality. In the last few decades, the scientific knowledge on RA pathogenesis vastly improved, leading to the identification of new proinflammatory molecules as potential therapeutic targets...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28138224/comparison-of-the-long-term-efficacy-and-safety-of-generic-tacrobell-with-original-tacrolimus-prograf-in-kidney-transplant-recipients
#15
Seung Yeon Son, Hye Ryoun Jang, Jung Eun Lee, Heejin Yoo, Kyunga Kim, Jae Berm Park, Sung Joo Kim, Ha Young Oh, Wooseong Huh
This study aimed to evaluate the long-term efficacy and safety of a generic tacrolimus (Tacrobell [TCB]) compared to the original tacrolimus (Prograf [PGF]) in kidney transplant recipients. In this retrospective observational study, we analyzed the data from 444 patients who took TCB as a first-line immunosuppressive drug and 245 patients who took PGF. The 5-year graft survival rate was 92% for patients in the PGF group and 97% for patients in the TCB group, respectively. Cox proportional hazards for a one-sided, noninferiority model showed noninferiority (upper confidence interval [CI] limit of the hazard ratio [HR]<1...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28138223/computational-intelligence-models-to-predict-porosity-of-tablets-using-minimum-features
#16
Mohammad Hassan Khalid, Pezhman Kazemi, Lucia Perez-Gandarillas, Abderrahim Michrafy, Jakub Szlęk, Renata Jachowicz, Aleksander Mendyk
The effects of different formulations and manufacturing process conditions on the physical properties of a solid dosage form are of importance to the pharmaceutical industry. It is vital to have in-depth understanding of the material properties and governing parameters of its processes in response to different formulations. Understanding the mentioned aspects will allow tighter control of the process, leading to implementation of quality-by-design (QbD) practices. Computational intelligence (CI) offers an opportunity to create empirical models that can be used to describe the system and predict future outcomes in silico...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28138222/facilitated-saliva-secretion-and-reduced-oral-inflammation-by-a-novel-artificial-saliva-system-in-the-treatment-of-salivary-hypofunction
#17
Minkyung Kang, Hyounggeun Park, Joon-Ho Jun, Miwon Son, Myung Joo Kang
Saliva substitutes and/or lubricants are commonly employed to lessen dry mouth symptoms by stimulating and/or substituting for the secretion of saliva. In this study, a novel artificial saliva containing inorganic salts, including sodium chloride and potassium chloride, and bactericidal agents, including potassium thiocyanate and lactoperoxidase, was formulated in the form of a solution (DM-sol) or gel (DM-gel). Those in vivo therapeutic efficacies were assessed in terms of saliva secretion and anti-inflammatory activity in rats and mice, respectively...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28138221/immunotherapy-for-the-treatment-of-colorectal-tumors-focus-on-approved-and-in-clinical-trial-monoclonal-antibodies
#18
REVIEW
Alex Françoso, Patricia Ucelli Simioni
Colorectal cancer is considered a disease of the elderly population. Since the number of geriatric patients continues to rise, monoclonal antibody therapy is the most promising therapy in the recent research. Presently, the monoclonal antibodies most frequently used in the treatment of colorectal tumors are bevacizumab, cetuximab, panitumumab, and ramucirumab. Bevacizumab is a monoclonal antibody that acts on VEGF. Cetuximab and panitumumab act on EGFR. Ramucirumab binds directly to the ligand-binding pocket of VEGFR-2 to block the binding of VEGF-A, VEGF-C, and VEGF-D...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28138220/erratum-golimumab-in-radiographic-and-nonradiographic-axial-spondyloarthritis-a-review-of-clinical-trials-corrigendum
#19
(no author information available yet)
[This corrects the article on p. 2087 in vol. 10.].
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28138219/resveratrol-inhibits-transforming-growth-factor-%C3%AE-2-induced-epithelial-to-mesenchymal-transition-in-human-retinal-pigment-epithelial-cells-by-suppressing-the-smad-pathway
#20
Ching-Long Chen, Yi-Hao Chen, Ming-Cheng Tai, Chang-Min Liang, Da-Wen Lu, Jiann-Torng Chen
Proliferative vitreoretinopathy (PVR) is the main cause of failure following retinal detachment surgery. Transforming growth factor (TGF)-β2-induced epithelial-to-mesenchymal transition (EMT) plays an important role in the development of PVR, and EMT inhibition decreases collagen gel contraction and fibrotic membrane formation, resulting in prevention of PVR. Resveratrol is naturally found in red wine and has inhibitory effects on EMT. Resveratrol is widely used in cardioprotection, neuroprotection, chemotherapy, and antiaging therapy...
2017: Drug Design, Development and Therapy
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