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Drug Research

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https://www.readbyqxmd.com/read/28910831/multicomponent-synthesis-of-some-molecular-hybrid-containing-thiazole-pyrazole-as-apoptosis-inducer
#1
Parvin Kumar, Meenakshi Duhan, Kulbir Kadyan, Jitender Kumar Bhardwaj, Priyanka Saraf, Meenu Mittal
The present study describes a multicomponent synthesis of molecular hybrid containing pyrazole, thiazole moiety using hydrazone as a linker, which have been synthesized by condensation of 1-phenyl-3-(aryl)-1H-pyrazole-4-carbaldehydes 1a-b, thiosemicarbazide and α-bromoketones 2a-c.The target hybrid compounds, 1-((1-phenyl-3-aryl-1H-pyrazole-4-yl)methylene)-2-(4-arylthiazole-2-yl)hydrazine 3a-f are characterized by (1)H-NMR, (13)C NMR, FT-IR and mass. Apoptosis inducing ability and cytotoxic nature of all the hybrid compounds having thiazole, pyrazole and hydrazone were assessed by using biological assays viz morphological, fluorescence and tunel assays on granulosa cells of ovarian antral follicles of goat (Capra hircus) in vitro...
September 14, 2017: Drug Research
https://www.readbyqxmd.com/read/28898912/application-of-graphene-and-its-derivatives-in-cancer-diagnosis-and-treatment
#2
S Ghanbarzadeh, H Hamishehkar
Although chemotherapies are successful in some cases, systemic toxicity could be simultaneously observed due to the lack of drugs selectivity to cancerous tissues, leading to the failure of the chemotherapies. Furthermore, the therapeutic effects will be significantly improved if the anticancer drugs could be delivered to cancer cells with high selectivity. In recent years, there have been many advances in the field of diagnosis and treatment of cancer as a result of the development of novel materials with noticeable and often unique properties...
September 12, 2017: Drug Research
https://www.readbyqxmd.com/read/28898911/lactobacilus-delbrueckii-subsp-bulgaricus-modulates-the-secretion-of-th1-th2-and-treg-cell-related-cytokines-by-pbmcs-from-patients-with-atopic-dermatitis
#3
Abdolkarim Sheikhi, Hojjat Giti, Mohammad Reza Heibor, Abdollah Jafarzadeh, Mansour Shakerian, Narges Baharifar, Fereidon Niruzad, Ali Sadeghi Moghaddam, Parviz Kokhaei, Mohammad Baghaeifar
Background Atopic dermatitis (AD) is an inflammatory skin disease which may be due to the imbalance between Th1-, Th2 and Treg cell-related immune responses. Evidences suggest that appropriate stimulation with probiotics may correct the skewed immune response in children with AD. The aim was to determine the effects of the yogurt culture lactobacillus Bulgaricus on the secretion of Th1/Th2/Treg type cytokines by PBMCs from children with AD. MethodsL. Bulgaricus was cultivated on MRS broth. The PBMCs from 20 children with AD were separated by Ficoll-Hypaque centrifugation and co-cultured with different concentrations of UV killed bacteria in RPMI-1640 plus 10% FCS for 48/72 h...
September 12, 2017: Drug Research
https://www.readbyqxmd.com/read/28898910/balanced-coagonist-of-glp-1-and-glucagon-receptors-corrects-dyslipidemia-by-improving-fgf21-sensitivity-in-hamster-model
#4
Vishal Patel, Amit Joharapurkar, Samadhan Kshirsagar, Hiren M Patel, Dheerendra Pandey, Dipam Patel, Brijesh Sutariya, Maulik Patel, Rajesh Bahekar, Mukul R Jain
Hyperlipidemia is often associated with obesity and diabetes, and can lead to serious complications like atherosclerosis and fatty liver disease. Coagonist of GLP-1 and glucagon receptors is a therapy under clinical investigation for treatment of obesity and diabetes. In this study, we have characterized the mechanism of hypolipidemic effect of a balanced coagonist using high cholesterol-fed hamsters. Tyloxapol-induced hypertriglyceridemia, lipolysis in adipose tissue, and bile homeostasis were assessed after repeated dose treatment of the coagonist of GLP-1 and glucagon receptors (Aib2 C24 chimera 2, SC)...
September 12, 2017: Drug Research
https://www.readbyqxmd.com/read/28898909/anti-hyperglycaemic-effect-of-cleome-rutidosperma-in-alloxan-induced-diabetic-albino-rats
#5
Olayinka A Oridupa, Naomi O Ovwighose, Adebowale B Saba
The hypoglycaemic and antihyperglycaemic effects of methanol extract of leaves of Cleome rutidosperma (Cr) DC (Family: Capparidaceae) was investigated in Wistar rats. Fifty normoglycaemic male rats (120 g-200 g) were divided into groups A (hypoglycaemic study; n=20) and B (antihyperglycaemic study; n=30). Each experiment had one control group and three groups administered with Cr (100, 200 or 400 mg/kg) respectively. Group B had two additional groups of diabetic-untreated rats and glibenclamide-treated diabetic rats...
September 12, 2017: Drug Research
https://www.readbyqxmd.com/read/28898908/influence-of-high-dose-folic-acid-on-methotrexate-efficacies-and-safety-in-japanese-rheumatoid-arthritis-patients
#6
Shun Kameyama, Yuko Kase, Saori Kurihara, Fumiko Yoshida, Masamitu Noda, Toshimi Iiduka, Masami Horiguchi, Kentaro Sugiyama, Toshihiko Hirano
Backgrounds Folic acid dose at ≦5 mg/week has been recommended for rheumatoid arthritis (RA) patients to decrease risk of methotrexate adverse effects. However, higher doses of folic acid is used in some cases. We examined the influence of high-dose folic acid on methotrexate efficacies and safety in Japanese RA patients. Methods 502 RA patients of four hospitals prescribed methotrexate and folic acid were included. These patients were divided into two subgroups according to the threshold of folic acid dose by 5 mg/week...
September 12, 2017: Drug Research
https://www.readbyqxmd.com/read/28898907/effects-of-cobalamin-vitamin-b12-on-gentamicin-induced-nephrotoxicity-in-rat
#7
Saeed Hajihashemi, Zeinab Hamidizad, Ali Rahbari, Fatemeh Ghanbari, Zohre Aghaee Motealeghi
Background The main side effect of gentamicin is nephrotoxicity. The effect of cobalamin (Cob) was investigated on gentamicin nephrotoxicity in rats. Methods Renal injury induced by i.p. injection of gentamicin (100 mg/kg) for 8 consecutive days. Cobalamin (6 mg/kg/day, i.p) treatment was done for 8 consecutive days as co-treatment and post-treatment protocol. Results Cobalamin significantly increased creatinine clearance levels and renal blood flow which were reduced by gentamicin. Also, cobalamin significantly improved serum electrolytes (sodium and potassium) levels which were disturbed by gentamicin...
September 12, 2017: Drug Research
https://www.readbyqxmd.com/read/28898906/application-of-spray-drying-technique-for-flowability-enhancement-of-divalproex-sodium
#8
Saeed Ghanbarzadeh, Hadi Valizadeh, Shadi Yaqoubi, Arash Asdagh, Hamed Hamishehkar
Background Tablets and capsules are the most accepted and widely used solid dosage forms in the medical therapy. Flow property of the powders is playing a key role in the various pharmaceutical fields especially in the fomulation of tablets and capsules. The high hygroscopic crystalline structure of anhydrous Divalproex sodium (DVX) makes it to be appear as waxy white flakes with almost no powder flowability which cause serious problems during the tabletting and capsule filling procedures. Purpose The main objective of this study was to improve the flowability of DVX powder...
September 12, 2017: Drug Research
https://www.readbyqxmd.com/read/28898905/taguchi-experimental-design-for-optimization-of-recombinant-human-growth-hormone-production-in-cho-cell-lines-and-comparing-its-biological-activity-with-prokaryotic-growth-hormone
#9
Zahra Sadat Aghili, Sayyed Hamid Zarkesh-Esfahani
Growth hormone deficiency results in growth retardation in children and the GH deficiency syndrome in adults and they need to receive recombinant-GH in order to rectify the GH deficiency symptoms. Mammalian cells have become the favorite system for production of recombinant proteins for clinical application compared to prokaryotic systems because of their capability for appropriate protein folding, assembly, post-translational modification and proper signal. However, production level in mammalian cells is generally low compared to prokaryotic hosts...
September 12, 2017: Drug Research
https://www.readbyqxmd.com/read/28898904/the-protective-effect-of-the-ethanol-leaf-extract-of-andrographis-paniculata-on-cisplatin-induced-acute-kidney-injury-in-rats-through-nrf2-kim-1-signalling-pathway
#10
Bisi Olajumoke Adeoye, Ebunoluwa Racheal Asenuga, Ademola Adetokunbo Oyagbemi, Temidayo Olutayo Omobowale, Adeolu A Adedapo
The ethanol leaf extract of Andrographis paniculata was used to ameliorate the renal toxicity induced by cisplatin in 28 rats divided into four groups of seven rats per group. Group A received normal saline for the duration of the experiment. Group B animals were treated with cisplatin (10 mg/kg i.p) on day 1 and 3 days after received normal saline for the next 7 days while groups C and D animals also received 10 mg/kg dose of cisplatin on day 1 but after 3 days were then respectively treated with 200 and 400 mg/kg doses of the extract of Andrographis paniculata for the remaining 7 days through oral administration...
September 12, 2017: Drug Research
https://www.readbyqxmd.com/read/28847024/incorporation-of-fluorinated-pyridine-in-the-side-chain-of-4-aminoquinolines-synthesis-characterization-and-antibacterial-activity
#11
Reza Ranjbar-Karimi, Alireza Poorfreidoni
A series of hybrid of 4-aminoquinoline and fluorinated pyridine derivatives were synthesized and their chemical structure were confirmed by (19)F-NMR, (1)H-NMR, (13)C-NMR and FT-IR. All compounds were tested against one Gram-positive and one Gram-negative bacteria to assess their in vitro antibacterial activity. Compounds 10a, 10b, 11a and 12b showed moderate antibacterial activity against Gram-positive bacterium, Staphylococcus aureus.
August 28, 2017: Drug Research
https://www.readbyqxmd.com/read/28847023/saliva-versus-plasma-bioequivalence-of-valsartan-hydrochlorothiazide-in-humans-validation-of-classes-ii-and-iv-drugs-of-the-salivary-excretion-classification-system
#12
Nasir Idkaidek, Haneen Agha, Tawfiq Arafat
Aim The aim of this study is to investigate the robustness of using non-invasive saliva instead of plasma for bioequivalence of valsartan and hydrochlorothiazide (HCT) in humans based on Salivary Excretion Classification System (SECS). Methods Plasma and resting saliva samples were collected over 24 h after oral administration of single dose 160 mg valsartan and 12.5 mg HCT to 12 healthy male volunteers after 10 h overnight fasting. Plasma and saliva concentrations were determined by validated liquid chromatography-mass spectrometry...
August 28, 2017: Drug Research
https://www.readbyqxmd.com/read/28847022/attenuation-of-morphine-induced-tolerance-and-dependence-by-pretreatment-with-cerebrolysin-in-male-rats
#13
Hamed Ghavimi, Sara Darvishi, Saeed Ghanbarzadeh
Background Dependence and tolerance to morphine are major problems which limit its chronic clinical application. Purpose This study was aimed to investigate the attenuation effect of Cerebrolysin, a mixture of potent growth factors (BDNF, GDNF, NGF, CNTF etc,), on the development of Morphine-induced dependence and tolerance. Methods Male Wistar rats were selected randomly and divided into different groups (n=8) including: a control group, groups received additive doses of morphine (5-25 mg/kg, ip, at an interval of 12 h until tolerance completion), and groups pretreated with Cerebrolysin (40, 80 and 160 mg/kg, ip, before morphine administration)...
August 28, 2017: Drug Research
https://www.readbyqxmd.com/read/28847021/characterisation-and-safety-of-intraperitoneal-perioperative-administration-of-antibacterial-agents-a-systematic-review
#14
Siv Fonnes, Barbara Juliane Holzknecht, Magnus Arpi, Jacob Rosenberg
Background Intraperitoneal drug administration applies treatment at the site of diseases with gynaecological, urological, or gastrointestinal origin. The objective of this systematic review was to investigate perioperative intraperitoneal administration of antibacterial agents to characterise the drugs used and their safety profile. Methods A protocol was registered at PROSPERO (CRD42016038956). A systematic review was conducted and reported according to Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA)...
August 28, 2017: Drug Research
https://www.readbyqxmd.com/read/28847020/effect-of-encapsulated-artemisia-aucheri-l-magnetic-nanogel-extract-on-shoulder-block-in-rat
#15
Siavash Beiranvand, Arash Karimi
Introduction Due to the severe pain generated after shoulder surgery, we aim to formulate and intravenously (IV) inject magnetic nanogel encapsulated Artemisia aucheri. L extract for inducing shoulder block in the rat. Methods Artemisia aucheri. L extract encapsulated magnetic nanoparticles (MNPs) was fabricated and tested in rat using paw withdrawal latencies (PWL) from thermal stimuli on the forepaw. The animals were divided into two groups; the untreated left forepaw (control group), and the test group with treated right forepaw...
August 28, 2017: Drug Research
https://www.readbyqxmd.com/read/28738427/nanoemulsion-an-advanced-vehicle-for-efficient-drug-delivery
#16
Asad Ali, Vaseem Ahamad Ansari, Usama Ahmad, Juber Akhtar, Afroz Jahan
Advanced drug delivery system has now gained preference over the conventional drug delivery system. One such research is nanoemulsion which is famous among the researchers because of ease of formation, stability, clarity, increased absorption rate leading to increasing in bioavailability and potential to form a formulation with both lipophilic as well as the hydrophilic drug. Long lasting stability (up to years) and ability to encapsulate both lipophilic and hydrophilic drug has given this colloidal system a valuable position in drug delivery...
July 24, 2017: Drug Research
https://www.readbyqxmd.com/read/28738426/long-term-effects-of-liraglutide-in-japanese-patients-with-type-2-diabetes-among-the-subgroups-with-different-renal-functions-results-of-2-year-prospective-study
#17
Takeyuki Hiramatsu, Akiko Ozeki, Hideaki Ishikawa, Shinji Furuta
Aims Very few studies have ever examined the effects of long-term (>1 year) administration of liraglutide in patients with type 2 diabetes mellitus (T2DM) and renal impairment. Therefore, we conducted a 2-year study to prospectively examine the effects of liraglutide in those patients. Methods A total of 148 patients with T2DM were enrolled and treated with liraglutide (0.6 or 0.9 mg/day). 97 patients completed the 2-year study without protocol deviations. These patients were divided into 3 groups according to the baseline estimated glomerular filtration ratio (eGFR) (in mL/min/1...
July 24, 2017: Drug Research
https://www.readbyqxmd.com/read/28738425/preparation-and-characterization-of-pegylated-iron-oxide-gold-nanoparticles-for-delivery-of-sulforaphane-and-curcumin
#18
Hossein Danafar, Ali Sharafi, Sonia Askarlou, Hamidreza Kheiri Manjili
Natural products have been used for the treatment of various diseases such as cancer. Curcumin (CUR) and sulforaphane (SF) have anti-cancer effects, but their application is restricted because of their low water solubility and poor oral bioavailability. To improve the bioavailability and solubility of SF and CUR, we performed an advanced delivery of SF and CUR with PEGylated gold coated Fe3O4 magnetic nanoparticles (PEGylated Fe3O4@Au NPs) to endorse SF and CUR maintenance as an effective and promising antitumor drugs...
July 24, 2017: Drug Research
https://www.readbyqxmd.com/read/28724167/in-vitro-controlled-release-of-two-new-tuberculocidal-adamantane-aminoethers-from-solid-pharmaceutical-formulations-ii
#19
Marilena Vlachou, Angeliki Siamidi, Dimitrios Spaneas, Dimitrios Lentzos, Polixeni Ladia, Konstantina Anastasiou, Ioannis Papanastasiou, Angeliki-Sofia Foscolos, Markos-Orestis Georgiadis, 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 two new tuberculocidal adamantane aminoethers (compounds III and IV), congeneric to the adamantane derivative SQ109, which is in final clinical trials, and aminoethers (I) and (II), 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...
July 19, 2017: Drug Research
https://www.readbyqxmd.com/read/28724166/iron-pharmacokinetics-in-women-with-iron-deficiency-anaemia-following-a-single-oral-dose-of-a-novel-formulation-of-tardyferon-prolonged-release-ferrous-sulphate
#20
Andrew Leary, Laurence Barthe, Thierry Clavel, Claudie Sanchez, Zahida Issiakhem, Bruno Paillard, Jean-Marc Edmond
Numerous iron-containing preparations are available on the market; these vary in dosage, salt, chemical state of iron (ferric or ferrous) and in the iron delivery process (immediate or prolonged-release). Tardyferon® is a prolonged-release tablet containing 80 mg ferrous sulphate. The formulation has recently been modified; changes to the excipients which constitute the inert formulation matrix have allowed a decrease in tablet size for easier swallowing. The aim of this multicenter open-label study was to characterize the serum pharmacokinetics of iron in non-pregnant women aged 23-45 years with iron deficiency anaemia (IDA) following single oral administration of 160 mg Tardyferon® under fasting conditions...
July 19, 2017: Drug Research
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