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Drug Research

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https://read.qxmd.com/read/30986883/determination-of-jw5473-in-rat-plasma-by-uplc-ms-ms-and-its-application-to-pharmacokinetic-study-of-jw5473
#1
Tae Kon Kim
A sensitive method for quantitation of JW5473 in rat plasma has been established using ultra performance liquid chromatography-electrospray ionization tandem mass spectrometry (UPLC-ESI/MS/MS). Tramadol was used as an internal standard. JW5473 and internal standard in plasma sample was extracted using acetonitrile (protein precipitation). A centrifuged upper layer was then evaporated and reconstituted with the mobile phase of 0.5% formic acid-acetonitrile (40:60, v/v). The reconstituted samples were injected into a C18 reversed-phase column...
April 15, 2019: Drug Research
https://read.qxmd.com/read/30934098/a-cautious-note-on-thalidomide-usage-in-cancer-treatment-genetic-profiling-of-the-tbx2-sub-family-gene-expression-is-required
#2
Georges Nemer, Athar Khalil
Thalidomide is still by excellence the mysterious drug that fascinated, blurred, misled, and changed the scientific community perspectives and policies. It was introduced in the 1950's as a sedative drug, then shortly withdrawn because of the devastating birth defects that affected tens of thousands throughout more than 40 countries. Back into the market in the mid 1990's and 2000's the drug is now being used to treat skin immune-related conditions and some cancers like multiple myeloma. Despite numerous beneficial effects which led to the development of new analogs, its direct mechanisms of action are still elusive...
April 1, 2019: Drug Research
https://read.qxmd.com/read/30912092/preparation-and-evaluation-of-ph-sensitive-novel-anticancer-drug-carrier-based-on-magnetic-chitosan-quartets
#3
Hossein Danafar, Farnaz Asadi, Ali Sharafi, Hamidreza Kheiri Manjili
Chitosan-coated magnetic nanoparticles are an appropriate drug delivery method which can improve the therapeutic properties of chemotherapy agents and also can be useful as MRI contrast agent for early cancer diagnosis. This research discovers the optimization of the possible therapeutic effects of Chitosan- citric acid- Fe3 O4 - CUR quartets. Chitosan as a natural polymer can use to encapsulate citric acid modified Fe3 O4 nanoparticles. The successful preparation of CUR-loaded nano-carriers was confirmed by X-ray diffraction (XRD), thermogravimetric analysis (TGA), differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), vibrating sample magnetometer (VSM) and transmission electron microscopy (TEM) techniques...
March 25, 2019: Drug Research
https://read.qxmd.com/read/30887484/pharmacokinetic-profile-of-curcumin-and-nanocurcumin-in-plasma-ovary-and-other-tissues
#4
Wawaimuli Arozal, Wenny Trias Ramadanty, Melva Louisa, Regina Puspa Utami Satyana, Gaviota Hartono, Serlie Fatrin, Sigit Purbadi, Ari Estuningtyas, Instiaty Instiaty
BACKGROUND: Curcumin is a natural diphenolic compound that is currently being investigated for various cancers, including ovarian cancer. Clinical application of curcumin has been limited due to its low solubility and bioavailability and rapid metabolism and degradation at physiological pH. Particle size is one factor that can affect the absorption process, which thus increases compound solubility and transport across the membrane. This study was conducted to determine the effects of modifying the particle size of curcumin on its pharmacokinetic parameters in blood and other organs...
March 18, 2019: Drug Research
https://read.qxmd.com/read/30822797/quantitation-of-ivosidenib-a-novel-mutant-idh1-inhibitoron-mice-dbs-application-to-a-pharmacokinetic-study
#5
Sreekanth Dittakavi, Rakesh Kumar Jat, Ramesh Mullangi
Ivosidenib is an approved drug for relapsed or refractory IDH1 mutant AML patients. The goal of the present work is to develop and validate an LC-MS/MS method for the quantitation of ivosidenib in mice dried blood spots (DBS) as per regulatory guideline in the linearity range of 1.10-3293 ng/mL. To date there is no bioanalytical method reported for quantitation of ivosidenib. The chromatographic resolution of ivosidenib and internal standard (warfarin) was achieved on a C18 column with an isocratic mobile phase...
March 1, 2019: Drug Research
https://read.qxmd.com/read/30822796/evaluation-of-rheum-turkestanicum-in-hexachlorobutadien-induced-renal-toxicity
#6
Mohammad Taher Boroushaki, Sahar Fanoudi, Arezoo Rajabian, Samaneh Boroumand, Azita Aghaee, Azar Hosseini
Hexachlorobutadien is nephrotoxic agent in rodents. The mechanism of toxicity includes generation of free radicals, depletion of thiol groups and production of toxic metabolites. Antioxidant compounds may reduce HCBD-nephrotoxicity. In this research we investigated the effect of Rheum turkeatanicum extract against HCBD-toxicity. The animals were divided to 4 groups which were including control (saline, 1 mL/kg), HCBD (100 mg/kg) and treatment groups which received extract at doses 100 and 200 mg/kg. The extract were administered as intraperitoneally (i...
March 1, 2019: Drug Research
https://read.qxmd.com/read/30780168/molecular-docking-and-3d-qsar-studies-of-c000000956-as-a-potent-inhibitor-of-bace-1
#7
Ogunleye Adewale Joseph, Kikiowo Babatomiwa, Adelakun Niyi, Omotuyi Olaposi, Inyang Olumide
BACKGROUND: BACE-1 is an aspartate protease that is responsible for the proteolysis of amyloid precursor proteins (APP) into beta-amyloid (Aβ), a neurotoxic peptide in patients with Alzheimer's disease (AD). As such, BACE-1 is a prime pharmacological target in the control of Aβ in the brain and its inhibition will be a sound approach in AD therapy. METHODS: The computational pipeline which comprised molecular docking (MD), Quantitative Structure Activity Relationship (QSAR) modelling and Absorption, Distribution, Metabolism, Excretion and Toxicity (ADMET) studies enabled the prediction of molecular interaction and relative inhibitory potentials of the hit compound...
February 19, 2019: Drug Research
https://read.qxmd.com/read/30776841/caveolins-an-assailant-or-an-ally-of-various-cellular-disorders
#8
Ritesh Kumar Srivastav, Tarique Mahmood Ansari, Mahesh Prasad, Vishal Kumar Vishwakarma, Paramdeep Bagga, Farogh Ahsan
Caveolae have impressive morphological highlights of the cytomembrane of mammalian cells which involve in wide diversity of cellular functions involving signaling pathways and cholesterol hastening. Caveolin proteins possess a 'scaffolding' domain which for caveolin-1 and caveolin-3 appear to act a dominant role in signal regulation through caveolae. Caveolin-1 is treated to be protein in the cytomembrane entrapped with caveolae in endothelial cells and vascular smooth muscle cells which diminish nitric oxide (NO) by fill up the calcium/calmodulin (Ca2+ /CaM) confining point of endothelial nitric oxide synthase (eNOS), decrease NO generation produce endothelial dysfunction and atherosclerotic injury development...
February 18, 2019: Drug Research
https://read.qxmd.com/read/30776840/vasoactive-agents-for-the-management-of-variceal-bleeding-a-mixed-treatment-comparison-network-meta-analysis-and-trial-sequential-analysis-of-randomized-clinical-trials
#9
Kannan Sridharan, Gowri Sivaramakrishnan
BACKGROUND: Vasoactives such as terlipressin, somatostatin, vasopressin, octreotide and nitrates are commonly used to treat variceal bleeding. The present study is a network meta-analysis comparing the efficacy and safety of the above vasoactive agents for treating variceal bleeding. METHODS: Electronic databases were searched for appropriate randomized clinical trials evaluating vasoactives in cirrhotic patients with variceal bleeding. Random-effects model was used to generate the pooled estimates...
February 18, 2019: Drug Research
https://read.qxmd.com/read/30722080/correction-synthesis-of-novel-diaziridinyl-quinone-isoxazole-hybrids-and-evaluation-of-their-anti-cancer-activity-as-potential-tubulin-targeting-agents
#10
P Ravi Kumar, Satyanarayana Yennam, K Raghavulu, Loka Reddy Velatooru, Siva Reddy Kotla, Vasudevarao Penugurti, Prasanta K Hota, Manoranjan Behera, A Jaya Shree
No abstract text is available yet for this article.
February 5, 2019: Drug Research
https://read.qxmd.com/read/30665254/evaluation-of-anti-diarrheal-activity-of-methanol-root-bark-extract-of-milicia-excelsa-welw-c-c-berg-moraceae-in-rats
#11
Muritala Ayofe Adebayo, Oluwasegun Adekanmi Adedokun, Lateef Abiola Akinpelu, Paul Okwudili Okafor
Milicia excelsa (Moraceae) plant is used as an antidiarrheal agent in ethnomedicine but there is no scientific rationale for its claim. Hence, this study examined the acute toxicity (LD50 ) and anti-diarrheal effect of methanol root bark extract of Milicia excelsa per oral in rats as well as the probable phytoconstituents responsible for this effect. The LD50 was>5000 mg/kg, suggesting its safety. The extract significantly (p<0.05) reduced the total number of feces and wet feces in castor oil-induced diarrhea with percentage inhibitions of 41...
January 21, 2019: Drug Research
https://read.qxmd.com/read/30658353/simple-hplc-method-for-quantitative-determination-of-carbinoxamine-in-human-plasma-application-in-pharmacokinetic-studies-and-therapeutic-drug-monitoring
#12
Soha M El-Masry, Rasha M El-Morsi
A sensitive, specific and cost-effective HPLC method was developed for quantitative determination of carbinoxamine in human plasma using liquid chromatography with ultraviolet detection. A simple liquid-liquid extraction by ethyl acetate was used to extract carbinoxamine from human plasma. Satisfactory separation was achieved by a mobile phase consisting of 20 mM ammonium dihydrogen orthophosphate containing 0.01% triethyl amine (pH adjusted to 3 by using phosphoric acid) and acetonitrile in ratio of (75:25, v/v) at a flow rate of 0...
January 18, 2019: Drug Research
https://read.qxmd.com/read/30654398/synthesis-of-novel-diaziridinyl-quinone-isoxazole-hybrids-and-evaluation-of-their-anti-cancer-activity-as-potential-tubulin-targeting-agents
#13
P Ravi Kumar, Satyanarayana Yennam, K Raghavulu, Loka Reddy Velatooru, Siva Reddy Kotla, Vasudevarao Penugurthi, Prasanta K Hota, Manoranjan Behera, A Jaya Shree
Two series of diaziridinyl quinone isoxazole derivatives were prepared and evaluated for their cytotoxic activity against MCF7, HeLa, BT549, A549 and HEK293 cell lines and interaction with tubulin. Compounds (6A-M: ) showed promising activity against all the 5 human cancer cell lines. Compounds 6A: , 6E: and 6 M: were potent [IC50 ranging between 2.21 µg to 2.87 µg] on ER-positive MCF7 cell line similar to the commercially available drug molecule Doxorubicin. The results from docking models are in consistent with the experimental values which demonstrated the favourable binding modes of compounds 6A-M: to the interface of α- and β-tubulin dimer...
January 17, 2019: Drug Research
https://read.qxmd.com/read/30616250/2-benzylidene-1-indanone-analogues-as-dual-adenosine-a1-a2a-receptor-antagonists-for-the-potential-treatment-of-neurological-conditions
#14
HelenaDorathea Janse van Rensburg, LesetjaJ Legoabe, Gisella Terre'Blanche, MiethaM Van der Walt
Previous studies explored 2-benzylidine-1-tetralone derivatives as innovative adenosine A1 and A2A receptor antagonists for alternative non-dopaminergic treatment of Parkinson's disease. This study's aim is to investigate structurally related 2-benzylidene-1-indanones with substitutions on ring A and B as novel, potent and selective adenosine A1 and A2A receptor blockers. 2-Benzylidene-1-indanone derivatives were synthesised via acid catalysed aldol condensation reactions and evaluated via radioligand binding assays to ascertain structure activity relationships to govern A1 and A2A AR affinity...
January 7, 2019: Drug Research
https://read.qxmd.com/read/30616249/study-of-dna-binding-activity-and-antibacterial-effect-of-escitalopram-oxalate-an-extensively-prescribed-antidepressant
#15
Reza Valipour, Mehmet Bertan Yilmaz, Ebrahim Valipour
Escitalopram oxalate (EO) is considered as one of the extensively prescribed antidepressant drug in Turkey and some other countries, therefore this research was aimed to study the interaction of the drug with DNA and study of the substance effect on bacterial growth. The absorption value of the drug solution at 238 nm was increased when DNA was added gradually to it and it showed hyperchromism effect. The value obtained for DNA binding constant (Kb) was 0.035  M -1 . When we added the CuCl2 2H2O to the mixture, any breakage was not shown in double strand DNA in comparison with control DNA...
January 7, 2019: Drug Research
https://read.qxmd.com/read/30616248/effect-of-artemisia-aucheri-l-and-bupivacaine-encapsulated-nanoparticles-on-nociceptive-pain
#16
Mahmoud Reza Moradkhani, Arash Karimi
AIM: The purpose of this study was to evaluate the antinociceptive interaction between bupivacaine and Artemisia aucheri. L encapsulated nanoparticles. METHODS AND MATERIALS: The effect of bupivacaine and Artemisia aucheri.L alone, and their encapsulated co-administration was assessed using the 3% formalin test in rat. Increasing doses of bupivacaine (31.6, 100, 178, and 316 mg/kg) or Artemisia aucheri.L (5.6, 10, 17.8, and 31.6 mg/kg) were given i.p. 10 min before 3% formalin administration...
January 7, 2019: Drug Research
https://read.qxmd.com/read/30609434/mechanistic-pathways-of-atp-sensitive-potassium-channels-referring-to-cardio-protective-effects-and-cellular-functions
#17
Vishal Kumar Vishwakarma, Prabhat Kumar Upadhyay, Hridaya Shanker Chaurasiya, Ritesh Kumar Srivasatav, Tarique Mahmood Ansari, Vivek Srivastava
A study of potassium channels correlates the fundamentals of mechanistic pathways and various physiological functions. The knowledge of these pathways provides the background, how to determine unit cell functions and to affect cardio protection. ATP sensitive potassium channels adjust excitability of membrane and functions as per metabolic status of cell. A lot of energy consumption primarily occurred in skeletal muscles which also express high number of potassium channels. The increase in calcium release and high heat production is occurred due to loss of potassium channels...
January 4, 2019: Drug Research
https://read.qxmd.com/read/30609433/spinal-serotonin-and-5ht6-receptor-levels-during-development-of-neuropathy-and-influence-of-blockade-of-these-receptors-on-thermal-hyperalgesia-in-diabetic-mice
#18
Cagda Celik Sari, Ozgur Gunduz, Ahmet Ulugol
Little is known about the role of 5-HT6 receptors in the pathophysiology of neuropathic pain. The aim of this study is firstly, to investigate the influence of spinal and systemic 5-HT6 receptors on thermal hyperalgesia, one of the most significant symptoms of neuropathy occurring in diabetes; and secondly to determine spinal lumbar serotonin and 5-HT6 receptor levels during development of diabetic neuropathy in mice. Diabetes was produced in Balb/c mice with a single injection of streptozocin (150 mg/kg, i...
January 4, 2019: Drug Research
https://read.qxmd.com/read/30577045/editorial
#19
(no author information available yet)
No abstract text is available yet for this article.
January 2019: Drug Research
https://read.qxmd.com/read/30572351/synthesis-and-anticonvulsant-studies-of-thiazolidinone-and-azetidinone-derivatives-from-indole-moiety
#20
Sachin Saini
2-Amino-5-(3'-indolomethylene)-1, 3 , 4 - oxadiazole (3): undergoes facile condensation with various aromatic aldehydes to gave 2-substitiuted arylidenylamino-5-(3'- indolomethylene) - 1, 3 , 4 - oxadiazole (4-8): . Cyclocondensation of (4-8): with thioglycolic acid and triethylamine yielded 3-[5'-(3"- indolomethylene)- 1', 3', 4'- oxadiazol-2'-yl]- 2- (substituted aryl)-4- thiazolidinones (9-13): and 1-[5'-(3"- indolomethylene) -1', 3', 4'- oxadiazol - 2'- yl ] -4-(substituted aryl) -2- azetidinones (14-18): ...
December 20, 2018: Drug Research
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