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Drug Development Research

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https://www.readbyqxmd.com/read/30222190/neuroprotection-of-rhglp-1-in-diabetic-rats-with-cerebral-ischemia-reperfusion-injury-via-regulation-of-oxidative-stress-eaat2-and-apoptosis
#1
Yi Fang, Daoli Jiang, Yitong Wang, Qian Wang, Dongmei Lv, Jichao Liu, Chang Liu
Preclinical Research & Development The purpose of the present study is to evaluate the neuroprotective effect of recombinant human glucagon-like peptide-1 (rhGLP-1) as well as to explore corresponding mechanisms in diabetic rats with cerebral ischemia/reperfusion injury induced by middle cerebral artery occlusion (MCAO). Diabetes mellitus was induced by intraperitoneal injection of streptozotocin. The rats were pretreated with rhGLP-1 (20 μg/kg intraperitoneally, thrice a day) for 14 days. Thereafter, the rats were subjected to MCAO 90 min/reperfusion 24 hr...
September 17, 2018: Drug Development Research
https://www.readbyqxmd.com/read/30222185/the-compound-2-naphthalene-2-thio-5-8-dimethoxy-1-4-naphthoquinone-induces-apoptosis-via-reactive-oxygen-species-regulated-mitogen-activated-protein-kinase-protein-kinase-b-and-signal-transducer-and-activator-of-transcription-3-signaling-in-human-gastric-cancer
#2
Jia-Ru Wang, Gui-Nan Shen, Ying-Hua Luo, Xian-Ji Piao, Meng Shen, Chang Liu, Yue Wang, Ling-Qi Meng, Yi Zhang, Hao Wang, Jin-Qian Li, Wan-Ting Xu, Yang Liu, Hu-Nan Sun, Ying-Hao Han, Mei-Hua Jin, Long-Kui Cao, Cheng-Hao Jin
Hit, Lead & Candidate Discovery It is reported that 1,4-naphthoquinones and their derivatives have potent antitumor activity in various cancers, although their clinical application is limited by observed side effects. To improve the therapeutic efficacy of naphthoquinones in the treatment of cancer and to reduce side effects, we synthesized a novel naphthoquinone derivative, 2-(naphthalene-2-thio)-5,8-dimethoxy-1,4-naphthoquinone (NTDMNQ). In this study, we explored the effects of NTDMNQ on apoptosis in gastric cancer cells with a focus on reactive oxygen species (ROS) production...
September 17, 2018: Drug Development Research
https://www.readbyqxmd.com/read/30070718/can-light-based-approaches-overcome-antimicrobial-resistance
#3
Michael R Hamblin, Heidi Abrahamse
The relentless rise of antibiotic resistance is considered one of the most serious problems facing mankind. This mini-review will cover three cutting-edge approaches that use light-based techniques to kill antibiotic-resistant microbial species, and treat localized infections. First, we will discuss antimicrobial photodynamic inactivation using rationally designed photosensitizes combined with visible light, with the added possibility of strong potentiation by inorganic salts such as potassium iodide. Second, the use of blue and violet light alone that activates endogenous photoactive porphyrins within the microbial cells...
August 2, 2018: Drug Development Research
https://www.readbyqxmd.com/read/30188587/evaluation-of-samidorphan-a-%C3%AE-opioid-antagonist-in-a-drug-discrimination-assay-in-rats
#4
Mario P Sgro, Deah L Modlin, Daniel R Deaver, Mary J Kallman, Mark S Todtenkopf
Preclinical Research & Development Background: Samidorphan, a μ-opioid receptor antagonist, is in clinical development for central nervous system related diseases. The discriminative stimulus effects of samidorphan were assessed in rats trained to discriminate the effects of a known morphinan of abuse, morphine, from that of saline. METHODS: Escalating doses of samidorphan were substituted for morphine and rats were allowed to respond on two levers for food reward. Doses of samidorphan were chosen based on other pharmacodynamic assays in which samidorphan blocked the effects of morphine (such as blocking analgesia in a hot plate test; data not shown)...
August 2018: Drug Development Research
https://www.readbyqxmd.com/read/30188586/synergistic-interaction-between-docosahexaenoic-acid-and-diclofenac-on-inflammation-nociception-and-gastric-security-models-in-rats
#5
Christopher Allan Miranda-Lara, Mario I Ortiz, Fernando Rodríguez-Ramos, Aracely Evangelina Chávez-Piña
Preclinical Research & Development The addition of polyunsaturated fatty acids to nonsteroidal anti-inflammatory drugs can increase their antinociceptive activity and produce a gastroprotective effect. The aim of the present study was to examine the effects of the interaction between docosahexaenoic acid (DHA) and diclofenac on inflammation (fixed ratios 1:1, 1:3, and 3:1), nociception (fixed ratio 1:3), and gastric injury in rats. DHA, diclofenac, or combinations of DHA and diclofenac produced anti-inflammatory and antinociceptive effects in rat...
August 2018: Drug Development Research
https://www.readbyqxmd.com/read/30188585/anorectic-efficacy-and-safety-of-the-diethylpropion-topiramate-combination-in-rats
#6
Gabriela Y Cortés-Moreno, José E Roa-Coria, Ángel Zúñiga-Romero, Juan C Huerta-Cruz, Eleazar Lara-Padilla, Cecilia F Del Valle-Laisequilla, Héctor I Rocha-González, Juan G Reyes-García
Preclinical Research & Development Current drugs for obesity treatment have limited efficacy and considerable adverse effects. Combination of drugs with complementary mechanisms of action at lower doses may produce a greater efficacy with a better safety profile. This study was designed to assess the anorectic effect and safety of a diethylpropion + topiramate mixture in rats. The anorectic effect of drugs was measured using a sweetened milk consumption model, and the corresponding interaction was determined by isobolographic analysis, interaction index and confidence intervals...
August 2018: Drug Development Research
https://www.readbyqxmd.com/read/30188584/cyclodextrin-complexes-perspective-from-drug-delivery-and-formulation
#7
Shery Jacob, Anroop B Nair
Cyclodextrins (CDs) have been widely investigated as a unique pharmaceutical excipient for past few decades and is still explored for new applications. They are highly versatile oligosaccharides which possess multifunctional characteristics, and are mainly used to improve the physicochemical stability, solubility, dissolution rate, and bioavailability of drugs. Stability constant, factors affecting complexation, techniques to enhance complexation efficiency, the preparation methods for molecular inclusion complexes and release of guest molecules are discussed in brief...
August 2018: Drug Development Research
https://www.readbyqxmd.com/read/30188583/evaluation-of-phytomedicinal-potential-of-perillyl-alcohol-in-an-in-vitro-parkinson-s-disease-model
#8
Ehraz Anis, Mohd Faraz Zafeer, Fakiha Firdaus, Shireen Naaz Islam, Mahino Fatima, M Mobarak Hossain
Preclinical Research & Development Parkinson's disease (PD) is the second most common neurodegenerative disorder that affects approximately 10 million people worldwide. The risk of developing PD and similar neurodegenerative disorders increases with age and an estimated 4% people are diagnosed with the disease before reaching the age of 50. Oxidative stress, cytotoxicity, and mitochondrial dysfunction are common features exhibited in the development of PD. The 6-hyroxydopamine (6-OHDA) model of PD is one of the most well characterized and studied models of the disease...
August 2018: Drug Development Research
https://www.readbyqxmd.com/read/29989223/anti-inflammatory-and-antinociceptive-effects-of-tilifodiolide-isolated-from-salvia-tiliifolia-vahl-lamiaceae
#9
Marco Martin González-Chávez, Angel Josabad Alonso-Castro, Juan Ramón Zapata-Morales, Víctor Arana-Argáez, Julio Cesar Torres-Romero, Yessica Elisa Medina-Rivera, Ernesto Sánchez-Mendoza, Salud Pérez-Gutiérrez
Salvia tiliifolia Vahl (Lamiaceae) is used for the empirical treatment of pain and inflammation. The diterpenoid tilifodiolide (TFD) was isolated from Salvia tiliifolia. The in vitro anti-inflammatory effects of TFD (0.1-200 µM) were assessed using murine macrophages stimulated with LPS and estimating the levels of pro-inflammatory mediators for 48 h. The in vivo anti-inflammatory activity of TFD was assessed using the carrageenan-induced paw edema test for 6 h. The antinociceptive effects of TFD were evaluated using the formalin test and the acetic acid induced-writhing test...
June 2018: Drug Development Research
https://www.readbyqxmd.com/read/29989222/evaluation-of-oral-pharmacokinetics-in-vitro-metabolism-blood-partitioning-and-plasma-protein-binding-of-novel-antidiabetic-agent-s009-0629-in-rats
#10
Guru Raghavendra Valicherla, Kishan Shamjibhai Italiya, Chandra Prakash Gupta, Shachi Mishra, Mohammed Riyazuddin, Anees Ahmed Syed, Sandeep Kumar Singh, Sudhir Shahi, Gaurav Taneja, Mohammad Wahajuddin, Atul Goel, Jiaur Rahaman Gayen
S009-0629 [methyl-8-(methylthio)-2-phenyl-6-p-tolyl-4,5-dihydro-2H-benzo[e]indazole-9-carboxylate] is a novel antidiabetic agent with PTP1B inhibitory activity. In this study, we have investigated the in vitro metabolic stability, plasma protein binding, blood partitioning, and oral pharmacokinetic study of S009-0629 in rats. The plasma protein binding, blood partitioning, and metabolic stability were determined by HPLC method. The oral pharmacokinetic study was analyzed by liquid chromatography coupled mass spectrometry (LC-MS/MS) method...
June 2018: Drug Development Research
https://www.readbyqxmd.com/read/29989221/in-silico-and-in-vivo-investigation-of-ferrocene-incorporated-acyl-ureas-and-homoleptic-cadmium-carboxylate-derivatives-for-anticonvulsant-anxiolytic-and-sedative-potential
#11
Sadia Adil, Arif-Ullah Khan, Haroon Badshah, Faiza Asghar, Muhammad Usman, Amin Badshah, Saqib Ali
In this study different derivatives of ferrocene-incorporated acyl ureas and homoleptic cadmium carboxylates were investigated for potential anticonvulsant, anxiolytic and sedative properties, using in-silico and in-vivo techniques. The molecular docking studies reveled that ferrocene compounds derivative 1-(4-bromobenzoyl)-3-(4-ferrocenylphenyl) urea (PB1) and cadmium compounds derivative bis (diphenylacetato) cadmium (II) (DPAA) exhibit binding affinities against various neurotherapeutic molecular targets involved in epilepsy, anxiety, and sedation...
June 2018: Drug Development Research
https://www.readbyqxmd.com/read/29732584/giving-priority-to-preclinical-pain-measures-resistant-to-existing-drugs-for-developing-innovative-analgesics
#12
Yukinori Nagakura
Preclinical Research & Development Chronic pain is a major health and socioeconomic burden because of its high prevalence, negative influence on patients' physical and/or emotional conditions, and huge costs to society. The responses of chronic pain patients to analgesic therapies vary substantially from individual to individual, and no more than a minority of chronic pain patients with various etiologies such as neuropathy and inflammation are, in fact, successfully relieved by existing drugs including opioid analgesics, nonopioid analgesics, antiepileptics, and antidepressants...
June 2018: Drug Development Research
https://www.readbyqxmd.com/read/29732583/analgesic-and-anti-inflammatory-activities-of-epicatechin-gallate-from-bauhinia-hookeri
#13
Eman Al-Sayed, Mohamed M Abdel-Daim
Hit, Lead & Candidate Discovery The acetic acid-induced writhing and hot plate models in mice were utilized to determine the analgesic effect of epicatechin gallate (ECG) isolated from Bauhinia hookeri. The anti-inflammatory activity of ECG was determined using carrageenan-induced paw edema model. The pro-inflammatory mediators (PGE2 , TNF-α, IL-1β, and IL-6) were estimated in the plasma of different treatment groups. ECG was tested at doses of 100, 200, and 400 mg/kg p.o. and diclofenac sodium was used as a standard drug (100 mg/kg) in all experiments...
June 2018: Drug Development Research
https://www.readbyqxmd.com/read/29719056/novel-primary-amine-diazeniumdiolates-chemical-and-biological-characterization
#14
Melany P Puglisi, Michael J Bradaric, John Pontikis, Jonathan Cabai, Theodore Weyna, Patrick Tednes, Robert Schretzman, Karl Rickert, Zhao Cao, Daniela Andrei
Hit, Lead & Candidate Discovery Diazeniumdiolates, also known as NONOates, are extensively used in biochemical, physiological, and pharmacological studies due to their ability to release nitric oxide (NO. ) and/or their congeneric nitroxyl (HNO). The purpose of this work was to synthesize a series of primary amine-based diazeniumdiolates as HNO/NO donors and to determine their efficacy as anticancer and antifungal agents in vivo. The seven compounds (3a-3g) were successfully synthesized and characterized, one of which had been previously reported in the literature (3g)...
May 2018: Drug Development Research
https://www.readbyqxmd.com/read/29697151/an-updated-overview-with-simple-and-practical-approach-for-developing-in-vitro-in-vivo-correlation
#15
Shery Jacob, Anroop B Nair
Preclinical Research & Development An in vitro-in vivo correlation (IVIVC) is as a predictive mathematical model that demonstrates a key role in the development, advancement, evaluation and optimization of extended release, modified release and immediate release pharmaceutical formulations. A validated IVIVC model can serve as a surrogate for bioequivalence studies and subsequently save time, effort and expenditure during pharmaceutical product development. This review discusses about different levels of correlations, general approaches to develop an IVIVC by mathematical modelling, validation, data analysis and various applications...
May 2018: Drug Development Research
https://www.readbyqxmd.com/read/29663513/a-variant-of-grk5-is-associated-with-the-therapeutic-efficacy-of-repaglinide-in-chinese-han-patients-with-type-2-diabetes-mellitus
#16
Zhenhai Shang, Feifei Han, Xueyan Zhou, Zejun Bao, Jing Zhu, Tao Wang, Qian Lu, Lei Du, Wei Li, Dongmei Lv, Xiaoxing Yin
Post-Market Research We aimed to investigate the impact of G protein-coupled receptor kinase 5 (GRK5) rs10886471 polymorphism on repaglinide efficacy in Chinese patients with type 2 diabetes mellitus (T2DM). A total of 300 T2DM patients and 210 healthy controls were genotyped for GRK5 rs10886471 on a three-dimensional polyacrylamide gel-based DNA microarray. Eighty-five patients with the same genotypes of cytochrome P450 (CYP) 2C8*3 139Arg and organic anion-transporting polypeptide 1B1 (OATP1B1) 521TT were randomly selected to orally take repaglinide for eight consecutive weeks...
May 2018: Drug Development Research
https://www.readbyqxmd.com/read/29573360/potential-amelioration-of-nicotine-induced-toxicity-by-nanocurcumin
#17
Krishna Chattopadhyay, Anwesha Samanta, Subrata Mukhopadhyay, Brajadulal Chattopadhyay
Clinical Research Curcumin, a nontoxic bioactive agent of turmeric significantly reduces nicotine-induced toxicity both at cellular and genetic levels. The clinical implication of native curcumin is hindered in the target cells due to its low aqueous solubility, poor bioavailability and poor pharmacokinetics. The problem was tried to overcome by preparing nanocurcumin with a view to improve its aqueous solubility and better therapeutic efficacy against nicotine-induced toxicity. The prepared nanocurcumin was characterized by Ultraviolet-visible spectroscopy; Field emission scanning electron microscopy (FE-SEM); X-ray diffraction (XRD); and Fourier transform infrared spectroscopy (FTIR)...
May 2018: Drug Development Research
https://www.readbyqxmd.com/read/29380405/the-potential-of-radiolabeled-chemotherapeutics-in-tumor-diagnosis-preliminary-investigations-with-68-ga-gemcitabine
#18
Subhajit Ghosh, Tapas Das, Haladhar D Sarma, Ashutosh Dash
Preclinical Research & Development Gemcitabine, a nucleoside analog, is a well-known chemotherapeutic drug that is used either alone or with other agents to treat a wide variety of cancers. The aim of the present work was to evaluate the potential of 68 Ga-labeled gemcitabine for its application in positron emission tomography (PET) imaging of tumorous lesions. Gemcitabine was coupled with p-NCS-benzyl-DOTA in order to facilitate radiolabeling with 68 Ga. The gemcitabine-p-NCS-benzyl-DOTA was radiolabeled with 68 Ga, obtained from a 68 Ge/68 Ga radionuclide generator...
May 2018: Drug Development Research
https://www.readbyqxmd.com/read/29570223/an-investigation-of-the-monoamine-oxidase-inhibition-properties-of-pyrrolo-3-4-f-indole-5-7-dione-and-indole-5-6-dicarbonitrile-derivatives
#19
Zhanna V Chirkova, Mariya V Kabanova, Sergey I Filimonov, Igor G Abramov, Anél Petzer, Idalet Engelbrecht, Jacobus P Petzer, Kyrill Yu Suponitsky, Alexander V Veselovsky
Hit, Lead & Candidate Discovery In recent studies, we have shown that pyrrolo[3,4-f]indole-5,7-dione and indole-5,6-dicarbonitrile derivatives act as good potency in vitro inhibitors of the monoamine oxidase (MAO) enzymes. To expand on these series and to further derive structure-activity relationships (SARs) for MAO inhibition, in the present study we synthesized additional homologs and related analogs of these chemical classes. Analyzes of the MAO inhibition properties of the synthesized compounds show that among the pyrrolo[3,4-f]indole-5,7-dione derivatives good potency MAO inhibitors exist as exemplified by 10, which possesses IC50 values for the inhibition of MAO-A and MAO-B of 0...
March 2018: Drug Development Research
https://www.readbyqxmd.com/read/29380400/ursolic-acid-derivatives-as-potential-antidiabetic-agents-in-vitro-in-vivo-and-in-silico-studies
#20
Ricardo Guzmán-Ávila, Virginia Flores-Morales, Paolo Paoli, Guido Camici, Juan José Ramírez-Espinosa, Litzia Cerón-Romero, Gabriel Navarrete-Vázquez, Sergio Hidalgo-Figueroa, Maria Yolanda Rios, Rafael Villalobos-Molina, Samuel Estrada-Soto
Hit, Lead & Candidate Discovery Protein tyrosine phosphatase 1B (PTP-1B) has attracted interest as a novel target for the treatment of type 2 diabetes, this because its role in the insulin-signaling pathway as a negative regulator. Thus, the aim of current work was to obtain seven ursolic acid derivatives as potential antidiabetic agents with PTP-1B inhibition as main mechanism of action. Furthermore, derivatives 1-7 were submitted in vitro to enzymatic PTP-1B inhibition being 3, 5, and 7 the most active compounds (IC50  = 5...
March 2018: Drug Development Research
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