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Drug Development Research

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https://www.readbyqxmd.com/read/29732584/giving-priority-to-preclinical-pain-measures-resistant-to-existing-drugs-for-developing-innovative-analgesics
#1
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...
May 6, 2018: Drug Development Research
https://www.readbyqxmd.com/read/29732583/analgesic-and-anti-inflammatory-activities-of-epicatechin-gallate-from-bauhinia-hookeri
#2
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...
May 6, 2018: Drug Development Research
https://www.readbyqxmd.com/read/29989223/anti-inflammatory-and-antinociceptive-effects-of-tilifodiolide-isolated-from-salvia-tiliifolia-vahl-lamiaceae
#3
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
#4
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
#5
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/29719056/novel-primary-amine-diazeniumdiolates-chemical-and-biological-characterization
#6
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
#7
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
#8
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
#9
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
#10
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
#11
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
#12
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
https://www.readbyqxmd.com/read/29285772/computational-and-experimental-exploration-of-the-structure-activity-relationships-of-flavonoids-as-potent-glyoxalase-i-inhibitors
#13
Qosay A Al-Balas, Mohammad A Hassan, Nizar A Al-Shar'i, Tamam El-Elimat, Ammar M Almaaytah
Hit, Lead & Candidate Discovery Glyoxalase-I (Glo-I) enzyme has emerged as a potential target for cancer treatment. Several classes of natural products including coumarins and flavonoids have shown remarkable Glo-I inhibitory activity. In the present study, computational and experimental approaches were used to explore the structure-activity relationships of a panel of 24 flavonoids as inhibitors of the Glo-1 enzyme. Scutellarein with an IC50 value of 2.04 μM was identified as the most potent inhibitor among the series studied...
March 2018: Drug Development Research
https://www.readbyqxmd.com/read/29243848/analgesic-efficacy-of-preoperative-dexketoprofen-trometamol-a-systematic-review-and-meta-analysis
#14
Vicente Esparza-Villalpando, Amaury Pozos-Guillén, David Masuoka-Ito, César Gaitán-Fonseca, Daniel Chavarría-Bolaños
Post-Market Research Clinical evidence supports the use of dexketoprofen trometamol (DEX) to manage acute postoperative pain. However, controversies surround the impact of the use of this drug in preoperative analgesic protocols. The aim of the present meta-analysis was to evaluate the effectiveness of the preoperative administration of DEX under postoperative pain conditions. Electronic and manual searches were conducted through diverse electronic databases. A systematic review and meta-analysis to evaluate the analgesic efficacy of the preoperative administration of DEX was performed including Randomized Clinical Trials (RCTs) published between 2002 and 2017...
March 2018: Drug Development Research
https://www.readbyqxmd.com/read/29314177/assessment-of-the-antinociceptive-and-ulcerogenic-activity-of-the-tapentadol-diclofenac-combination-in-rodents
#15
Juan R Zapata-Morales, Ángel J Alonso-Castro, Vinicio Granados-Soto, Sergio Sánchez-Enriquez, Mario A Isiordia-Espinoza
Preclinical Research & Development The objective of the present study was to evaluate the tapentadol-diclofenac combination in three dose-ratios in the mouse acetic acid-induced visceral pain and their ulcerogenic activity on the stomachal mucous. Dose-response curves were generated for tapentadol, diclofenac, and their combination in the acetic acid-induced writhing test in mice. Moreover, the stomachs of animals were surgically removal and gastrointestinal ulcerogenic action of the combination was assessed...
February 2018: Drug Development Research
https://www.readbyqxmd.com/read/29243833/pharmacological-interaction-of-%C3%AE-bisabolol-and-diclofenac-on-nociception-inflammation-and-gastric-integrity-in-rats
#16
Mario I Ortiz, Raquel Cariño-Cortés, Héctor A Ponce-Monter, Gilberto Castañeda-Hernández, Aracely Evangelina Chávez-Piña
Preclinical Research & Development The combination of nonsteroidal anti-inflammatory drugs (NSAIDs) with herbal products having analgesic and anti-inflammatory effects may increase their beneficial effects and limit their side effects. In this study, the effects of an interaction between α-bisabolol and the NSAID, diclofenac on nociception (formalin test), inflammation (paw inflammation produced by carrageenan) and gastric injury in rat was assessed. Diclofenac, α-bisabolol, or diclofenac-α-bisabolol combinations produced antinociceptive and anti-inflammatory effects in rat (p < ...
February 2018: Drug Development Research
https://www.readbyqxmd.com/read/29130540/anti-inflammatory-and-analgesic-activities-of-cupressuflavone-from-cupressus-macrocarpa-impact-on-pro-inflammatory-mediators
#17
Eman Al-Sayed, Haidy A Gad, Mohamed El-Shazly, Mohamed M Abdel-Daim, Abdel Nasser Singab
Hit, Lead & Candidate Discovery Inflammation is a complex biological process that is generally occurs in response to pathological triggers. Both neurodegenerative diseases and cancer have been linked to inflammation. The analgesic and anti-inflammatory effects of cupressuflavone (CUF) isolated from Cupressus macrocarpa were examined. The analgesic effects of CUF (40, 80 and 160 mg/kg po) were assessed in the acetic acid-induced writhing and hot plate models in mice with diclofenac sodium as the reference standard (100 mg/kg)...
February 2018: Drug Development Research
https://www.readbyqxmd.com/read/29076166/gastroprotective-effect-of-calealactone-b-lack-of-involvement-of-prostaglandins-nitric-oxide-and-sulfhydryls
#18
María Elena Sánchez-Mendoza, Yaraset López-Lorenzo, Audifás-Salvador Matus-Meza, Jesús Arrieta
Hit, Lead & Candidate Discovery The gastroprotective effect of calealactone B, isolated from Calea urticifolia was assessed in an ethanol-induced model of gastric lesioning. The possible involvement of prostaglandins, nitric oxide (NO) and sulfhydryl groups in the mechanism of action of calealactone B was also assessed. Calealactone B inhibited ethanol-induced gastric injuries with a maximal effect (95.3 ± 2.6%) at 30 mg kg-1 . A similar value was obtained at 10 mg kg-1 (83.5 ± 7.7%). Meanwhile, the reference anti-ulcer drug, carbenoxolone, an 11β-hydroxysteroid dehydrogenase (11β-HSD) inhibitor administered at 30 mg kg-1 showed 63...
February 2018: Drug Development Research
https://www.readbyqxmd.com/read/29044596/angelicin-potentiates-trail-induced-apoptosis-in-renal-carcinoma-caki-cells-through-activation-of-caspase-3-and-down-regulation-of-c-flip-expression
#19
Kyoung-Jin Min, Hee Jung Um, Seung Un Seo, Seon Min Woo, Shin Kim, Jong-Wook Park, Hyun-Shik Lee, Sang Hyun Kim, Yung Hyun Choi, Tae-Jin Lee, Taeg Kyu Kwon
Preclinical Research & Development Angelicin is a furocoumarin derived from Psoralea corylifolia L. fruit that has anti-inflammatory and anti-tumor activity. In the present study, the effect of angelicin in enhancing tumor necrosis factor-related apoptosis-inducing ligand (TRAIL)-induced apoptotic cell death was studied in Caki (renal carcinoma) cells. Angelicin alone and TRAIL alone had no effect on apoptosis, but in combination these compounds markedly induced apoptosis in the cancer cell lines while not inducing apoptosis in normal cells...
February 2018: Drug Development Research
https://www.readbyqxmd.com/read/28940250/synergistic-interaction-of-a-gabapentin-mangiferin-combination-in-formalin-induced-secondary-mechanical-allodynia-and-hyperalgesia-in-rats-is-mediated-by-activation-of-no-cyclic-gmp-atp-sensitive-k-channel-pathway
#20
Beatriz Godínez-Chaparro, Geovanna Nallely Quiñonez-Bastidas, Isabel Rocío Rojas-Hernández, Amaya Montserrat Austrich-Olivares, Alfonso Mata-Bermudez
Preclinical Research Gabapentin is an anticonvulsant used to treat neuropathic pain. Mangiferin is an antioxidant that has antinociceptive and antiallodynic effects in inflammatory and neuropathic pain models. The purpose of this study was to determine the interaction between mangiferin and gabapentin in the development and maintenance of formalin-induced secondary allodynia and hyperalgesia in rats. Gabapentin, mangiferin, or their fixed-dose ratio combination were administrated peripherally. Isobolographic analyses was used to define the nature of the interaction of antiallodynic and/or antihyperalgesic effects of the two compounds...
December 2017: Drug Development Research
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