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Drug Research

Veerasamy Ramya, Santhirakasu Vembu, Ganesan Ariharasivakumar, Manathusamy Gopalakrishnan
The purpose of the research is to synthesise a novel series of (E)-2-(4-(1H-indol-3-yl)-6-p-substituted phenylpyrimidin-2-yl)dimethylguanidine derivatives since 3-(1H-indol-3-yl)-1-p-substituted phenylprop-2-en-1-one and evaluate their molecular docking studies, antimicrobial, and anti-diabetic activities. Among all the synthesized compounds (11a-g), compound 11a exhibits excellent CDOCKER energy (-11.36 kcal/mol). The entire compounds (11a-g) confirm very good antimicrobial activity towards the tested microorganisms...
June 19, 2017: Drug Research
Ali Namvaran, Mehdi Fazeli, Safar Farajnia, Gholamreza Hamidian, Hassan Rezazadeh
Colorectal cancer is one the most important malignancies worldwide and finding new treatment option for this cancer is of high priority. Natural compounds are common source of drugs for treatment of various diseases including cancers. The aim of this study was to investigate the effects of Scrophularia oxysepala extract on Caco-2 cells and explore the possible role of caspase 3 pathway in inducing cell death in this cancer cells in compare with chemotherapy agents of cisplatin and capecitabine. The methanolic extract of Scrophularia oxysepala (SO) was prepared by drench method...
June 19, 2017: Drug Research
Farideh Mohammadian, Younes Pilehvar-Soltanahmadi, Shahriar Alipour, Mehdi Dadashpour, Nosratollah Zarghami
Background Gastric carcinoma still remains the second most common cause of cancer mortality in the world. Chrysin, as a flavone, has showed cancer chemopreventive activity. The cellular and molecular mechanisms of chrysin in cancer cells have not been fully understood. Objective In this study, we investigate expression levels of let-7a, miR-9, mir-18a, miR-21, miR-22, miR-34a, miR-126 and mir-221 to describe the anti-cancer effects of chrysin. Materials and Methods The cytotoxic effects of chrysin were assessed using MTT assay...
June 19, 2017: Drug Research
Ziyad Binkhathlan
Cremophor EL is a nonionic surfactant widely used in pharmaceutical formulations. Nonetheless, there are several reports on the influence of this excipient on the protein binding, pharmacokinetics, and pharmacodynamics of drugs. Valspodar is an investigational non-immunosuppressive derivative of cyclosporine A, used in clinical trials for treatment of multidrug resistant tumors. The formulation of valspodar (Amdray(®)) contains cremophor EL and ethanol as solubilizing agents. The main aim of the current study was to assess the plasma protein binding (in vitro) and the pharmacokinetic profile of valspodar in the cremophor EL-based formulation in comparison to a cremophor EL-free formulation following intravenous (i...
June 19, 2017: Drug Research
Reyhaneh Shayesteh, Mohammad Kamalinejad, Hasan Adiban, Azin Kardan, Fariborz Keyhanfar, Mohammad Reza Eskandari
Background Diabetes mellitus is a chronic endocrine disorder that is associated with significant mortality and morbidity due to microvascular and macrovascular complications. Diabetes complications accompanied with oxidative stress and carbonyl stress in different organs of human body because of the increased generation of free radicals and impaired antioxidant defense systems. In the meantime, reactive oxygen species (ROS) and reactive carbonyl species (RCS) have key mediatory roles in the development and progression of diabetes complications...
June 6, 2017: Drug Research
Angel S Galabov, Vesselina Vassileva, Vera Karabasheva
N'N'-anhydro-bis(β-hydroxy-ethyl)biguanide.HCl (abitylguanide) demonstrated a marked inhibitory effect on replication in cell cultures of a broad spectrum of human adenoviruses both standard laboratory strains and strains isolated from epidemic keratoconjunctivitis patients. The strongest inhibitory activity was found in viruses belonging to subgroup C (Rosen's subgroup III). The compound susceptible period of human adenovirus 5 replication in primary cell cultures of human embryo kidney cells included the total replication cycle and was especially pronounced during the exponential phase of the virus growth curve...
June 6, 2017: Drug Research
Marilena Vlachou, Angeliki Siamidi, Evanthia Diamantidi, Alexandra Iliopoulou, Ioannis Papanastasiou, V Ioannidou, Violeta Kourbeli, Angeliki-Sofia Foscolos, Anthony Vocat, Stewart T Cole, Vangelis Karalis, Tahsin Kellici, Thomas Mavromoustakos
The aim of the present investigation was to develop matrix tablet formulations for the in vitro controlled release of 2 new tuberculocidal adamantane aminoethers (compounds I and II), congeneric to the adamantane derivative SQ109, which is in final clinical trials, using carefully selected excipients, such as polyvinylpyrrolidone, sodium alginate and lactose. The tablets were prepared using the direct compression method and dissolution experiments were conducted using the US Pharmacopoeia type II apparatus (paddle method) in gastric and intestinal fluids...
May 30, 2017: Drug Research
Alireza Nomani, Hamed Nosrati, Hamidreza Kheiri Manjili, Leila Khesalpour, Hossein Danafar
Biodegradable copolymeric polymersomes have been used for controlled drug delivery of proteins. These polymersomes important areas to overcome formulation associated problems of the proteins. The aim of this study was to develop polymersomes using biodegradable copolymers for delivery of bovine serum albumin (BSA) as a model protein. Encapsulated BSA by mPEG-PCL polymersomes led to formation of BSA-loaded mPEG-PCL polymersomes. The polymersomes synthesized with the protein-polymer ratio of 1:4 at 15 000 rpm gave maximum loading, minimum polydispersion with maximally sustained protein release pattern, among the prepared polymersomes...
May 30, 2017: Drug Research
Tae Kon Kim
In this study, a sensitive and reliable method for the quantitation of fenofibric acid in rat plasma was developed and validated using high performance liquid chromatography (HPLC). The plasma samples were prepared by deproteinization, and sildenafil was used as an internal standard. Chromatographic separation was achieved using a reversed-phase (C18) column. The mobile phase, 0.02 M ammonium acetate buffer:acetonitrile (35:65, v/v), was run at a flow rate of 1.0 mL/min, and the column eluent was monitored using an ultraviolet detector at 280 nm at room temperature...
May 30, 2017: Drug Research
Devaraj V Chandrashekar, Ponnayyan S Suresh, Rajnish Kumar, Ravi Kanth Bhamidipati, Ramesh Mullangi, Wolfgang Richter, Nuggehally R Srinivas
A highly sensitive, specific and rapid LC-ESI-MS/MS method has been developed and validated for the simultaneous quantification of bendamustine (BM) and γ-hydroxybendamustine (HBM) in small volume (20 µL) mice and dog plasma using phenacetin as an internal standard (IS) as per regulatory guidelines. Both the analytes and IS were extracted from mice and dog plasma using a liquid-liquid extraction method. Chromatography was achieved on Atlantis dC18 column using an isocratic mobile phase (0.2% formic acid:acetonitrile, 25:75) at a flow rate of 0...
May 30, 2017: Drug Research
Fatemeh Abbasitabar, Vahid Zare-Shahabadi
Quantitative structure-activity relationship (QSAR) models were derived for 179 analogues of artemisinin, a potent antimalarial agent. Molecular descriptors derived solely from molecular structure were used to represent molecular structure. Utilizing replacement method, a subset of 11 descriptors was selected. General regression neural network (GRNN) was used to construct the nonlinear QSAR models in all stages of study. The relative standard error percent in antimalarial activity predictions for the training set by the application of cross-validation (RMSE-CV) was 0...
May 30, 2017: Drug Research
Eunice Kazue Kano, Chang Chiann, Kazuo Fukuda, Valentina Porta
Bioavailability and bioequivalence study is one of the most frequently performed investigations in clinical trials. Bioequivalence testing is based on the assumption that 2 drug products will be therapeutically equivalent when they are equivalent in the rate and extent to which the active drug ingredient or therapeutic moiety is absorbed and becomes available at the site of drug action. In recent years there has been a significant growth in published papers that use in silico studies based on mathematical simulations to analyze pharmacokinetic and pharmacodynamic properties of drugs, including bioavailability and bioequivalence aspects...
May 23, 2017: Drug Research
Muhammad M Hammami, Syed N Alvi
Background Average bioequivalence has been criticized for not adequately addressing individual variations. Importance of subjects' blinding in bioequivalence studies has not been well studied. We explored the extent of intra-subject pharmacokinetic variability and effect of drug-ingestion unawareness in subjects taking single caffeine product. Methods A single-dose randomized cross-over design was used to compare pharmacokinetics of 200 mg caffeine, described as caffeine (overt) or as placebo (covert). Maximum concentration (Cmax), Cmax first time (Tmax), area-under-the-concentration-time-curve, to last measured concentration (AUCT), extrapolated to infinity (AUCI), or to Tmax of overt caffeine (AUCOverttmax), and Cmax/AUCI were calculated blindly using standard non-compartmental method...
May 23, 2017: Drug Research
Niyaz Ahmad, Rizwan Ahmad, Atta Abbas Naqvi, Md Aftab Alam, Rehan Abdur Rub, Farhan Jalees Ahmad
Background Quercetin (Qur) and its major in vivo bioactive metabolites i. e., 3'-O-methyl quercetin, 4'-O-methyl quercetin and quercetin 7-O-β-D-glucuronide, may be used to treat cerebral ischemia however the poor aqueous solubility and less intestinal absorption of Qur results low bioavailability. Purpose To improve Qur bioavailability through preparation of nanoformulation and to develop and validate a sensitive quantification method for Qur detection in brain homogenate. Methods Qur-containing self-nanoemulsifying drug delivery system (Qur-SNEDDS) was developed to form oil-in-water nanoemulsions in situ...
May 23, 2017: Drug Research
Zohreh Sattar, Mehrdad Iranshahi
Ferula hermonis, a well-known species of the genus Ferula found in Lebanon and Syria, has a brilliant history in traditional medicine as it has been used for the treatment of erectile dysfunction in men and menopausal disturbances in women. Thanks to modern pharmacological and clinical investigations, F. hermonis is a valuable medicinal and condimental plant that may be used for the treatment of impotence and diabetes, the prevention of osteoporosis, and possesses anti-microbial and anti-inflammatory properties...
May 18, 2017: Drug Research
Chrysa Daousani, Vangelis D Karalis
In the past, dosage regimens authorized for adults were extrapolated to children relying mainly on empirical dosage adjustments. However, children are not small adults, but a distinct and heterogeneous group in terms of physiology, disease occurrence, pharmacokinetics, pharmacodynamics and also psychological, cognitive, and behavioral aspects. Even though it would be helpful to know the physiological changes and the special drug treatment needs in children, this task could not be performed due to ethical reasons...
May 18, 2017: Drug Research
Stephanie Zergiebel, Christian Fleck, Hans-Dieter Arndt, Christoph Enzensperger, Andreas Seeling
Dibenzo- and benzindolo-azecines represent a class of potential neuroleptics. To characterize the effectiveness at the dopamine and 5-HT2A-receptor representative structures were synthesized and tested by radio ligand binding studies, in vivo and in vitro studies.Neuroleptic potency and the risk of side effects of the prodrug 7-methyl-5,6,7,8,9,14-hexahydrodibenzo[d,g]azecin-3-yl isobutyrate, an ester derivative of the most promising azecine 7-methyl-5,6,7,8,9,14-hexahydrodibenzo[d,g]azecin-3-ol (LE404), was tested in vivo concerning conditioned avoidance response inhibition, locomotor activity and triggering of catalepsy vs...
May 18, 2017: Drug Research
Mohan Pethe, Samir Yelwatkar, Smita Manchalwar, Vijay Gujar
Aim and Objective The current study sought to investigate antidiabetic, hypolipidimic, antioxidant and histopathological effects of floral extract of Hibiscus rosa sinensis in Alloxan induced Diabetes in rats. Materials and Methods Study was conducted on 6 groups with 6 wistar rats in each group for the period of 4 weeks. Group I: served as normal control (NC), rats administered with gum acacia 1 ml daily, group II: consider as diabetic control (DC) treated with alloxon 150 mg/kg body wt. Whereas Hibiscus rosa-sinensis flower extract was given orally in group III (DE1), group IV (DE2), group V (DE3) at doses of 50, 100 and 200 mg/kg body weight dissolved in distilled water respectively...
May 18, 2017: Drug Research
Solomon Umukoro, Somtochukwu I Ogboh, Osarume Omorogbe, Abdul-Lateef A Adekeye, Matthew O Olatunde
Objectives Depression is a complex neuropsychiatric disorder, which affects the quality of life of the sufferers and treatment approach is associated with serious adverse effects and sometimes therapeutic failures. Cymbopogon citratus leaf (CC) has been reported to exert anti-depressant effect but its mechanism of action is yet to be elucidated hence, the need for this study. Methods The anti-depressant-like effect of Cymbopogon citratus aqueous leaf was evaluated using forced swim test (FST), tail suspension test (TST) and yohimbine-induced lethality test (YLT) in aggregated mice...
May 12, 2017: Drug Research
Forough Saki, Abdolkarim Sheikhi, Gholam Hosein Ranjbar Omrani, Hamid Karimi, Mohammad Hossein Dabbaghmanesh, Seyed Nouraddin Mousavinasab
Type I diabetes mellitus (T1DM) patients are at risk of osteoporosis and fracture due to the osteoblast and osteoclast malfunction. Osteopontin (OPN) as the major non-collagenous bone matrix protein is produced by osteoblasts and osteoclasts and involve in bone resorption, formation and remodeling. To evaluate the serum levels of OPN, bone mineral density (BMD) and correlation in patients with T1DM this study was designed. In this case-control study, 87 children with T1DM and 87 age/sex-matched healthy subjects were enrolled...
May 12, 2017: Drug Research
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