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Research in Pharmaceutical Sciences

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https://www.readbyqxmd.com/read/29606972/renal-vascular-response-to-angiotensin-1-7-in-rats-the-role-of-mas-receptor
#1
Mehdi Nematbakhsh, Azam Mansouri
Recently a cross talk between angiotensin 1-7 (Ang1-7) receptor (MasR) and angiotensin II receptors types 1 and 2 (AT1R and AT2R) has been highlighted. The effects of MasR antagonist (A779) compared to the vehicle on the renal blood flow (RBF) and renal vascular resistance (RVR) responses to Ang1-7 (300 ng/kg/min) infusion in the absence of Ang II receptors in male and female rats were determined at controlled renal perfusion pressure. Ang1-7 infusion did not alter mean arterial pressure in male and female rats...
April 2018: Research in Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29606971/synthesis-and-cytotoxic-evaluation-of-some-novel-quinoxalinedione-diarylamide-sorafenib-analogues
#2
Mojtaba Khandan, Sedighe Sadeghian-Rizi, Ghadamali Khodarahmi, Farshid Hassanzadeh
A series of novel sorafenib analogues containing a quinoxalinedione ring and amide linker were synthesized. A total of 9 novel compounds in 6 synthetic steps were synthesized. Briefly, the amino group of p-aminophenol was first protected which then followed by O-arylation with 5-chloro-2-nitroaniline to provide compound d . Reduction of the nitro group of compound d and cyclization of the diamine group of compound e with oxalic acid afforded compound f which on deacetylation yeilded compound g . Then compound g was reacted with different acyl halides to afford the target compounds 1h-1p ...
April 2018: Research in Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29606970/the-protective-role-of-melatonin-in-cadmium-induced-proliferation-of-ovarian-cancer-cells
#3
Negar Ataei, Mahmoud Aghaei, Mojtaba Panjehpour
Cadmium (Cd), a ubiquitous environmental and occupational pollutant, acts as a metalloestrogen to induce cell proliferation. It is suggested that Cd may also contribute to the development of estrogen-related cancers like ovarian cancer which is the most lethal cancer in women. Furthermore, it was shown that melatonin has antiproliferative effect on estradiol (E2)-induced proliferation. The aim of the present study was to evaluate whether melatonin inhibits Cd-induced proliferation in ovarian cancer cell lines and also whether Cd and melatonin can modulate estrogen receptor α (ERα) expression...
April 2018: Research in Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29606969/bioassay-directed-isolation-of-quaternary-benzylisoquinolines-from-berberis-integerrima-with-bactericidal-activity-against-brucella-abortus
#4
Gholamhassan Azimi, Ali Hakakian, Mustafa Ghanadian, Ali Joumaa, Saeed Alamian
Berberis integerrima Bonge. (Syn: Berberis densiflora Boiss. & Buhse) is a shrub widely distributed in Middle East and central part of Asia. An ethnobotanical study revealed that indigenous and tribal people in Iran use B. integerrima root decoction for treatment of brucellosis. Therefore, the aim of this study was bioassay directed isolation of antibacterial compounds from this plant based on their in vitro bactericidal activity against Brucella abortus . Briefly, the ethanol extract of B. integerrima was fractioned and subjected to preliminary antibacterial screening tests against Brucella...
April 2018: Research in Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29606968/the-effect-of-betulinic-acid-on-leptin-adiponectin-hepatic-enzyme-levels-and-lipid-profiles-in-streptozotocin-nicotinamide-induced-diabetic-mice
#5
Akram Ahangarpour, Razieh Shabani, Yaghoob Farbood
Diabetes mellitus is developed by lack of insulin secretion or reduction of tissues sensitivity to insulin, which lead to serious complications. The aim of this study is to evaluate antihyperlipidemic effect of betulinic acid (BA) on streptozotocin-nicotinamide (STZ-NA) induced diabetic mice. In this experimental study, seventy adult male NMRI mice (20-25 g) were divided randomly into seven groups ( n = 10) of control, sham, diabetes, diabetes + BA (10, 20 and 40 mg/kg), and diabetes + metformin (200 mg/kg)...
April 2018: Research in Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29606967/effects-of-oregano-essential-oil-on-brain-tlr4-and-tlr2-gene-expression-and-depressive-like-behavior-in-a-rat-model
#6
Azam Amiresmaeili, Samira Roohollahi, Ali Mostafavi, Nayere Askari
The aim of the present study was to evaluate the effects of oregano essential oil (OEO) on the hippocampus and prefrontal cortex TLR 2/4 gene expression and depressive like behavior induced by chronic unpredictable stress (CUS). Sucrose preference and forced swim tests were adopted to examine the antidepressant effect. Control (CON), OEO, CUS, and CUS + OEO groups were used. The OEO and CUS + OEO groups received OEO (0.2 mL/kg, i.p.), CON and CUS received saline (0.2 mL/kg, i.p.), and the positive drug groups of CUS rats received fluoxetine (10 mg/kg) and diazepam (3 mg/kg) once daily for 14 days...
April 2018: Research in Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29606966/protective-effects-of-glucosamine-and-its-acetylated-derivative-on-serum-glucose-deprivation-induced-pc12-cells-death-role-of-reactive-oxygen-species
#7
Seyed Hadi Mousavi, Elham Bakhtiari, Azar Hosseini, Khadijeh Jamialahmadi
Finding products with antiapoptotic activities has been one of the approaches for the treatment of neurodegenerative disorders. Serum/glucose deprivation (SGD) has been used as a model for the investigation of the molecular mechanisms of neuronal ischemia. Recent studies indicated that glucosamine (GlcN) and N-acetyl glucosamine (GlcNAc) have many pharmacological effects including antioxidant activities. The present study aimed to investigate the protective effects of GlcN and GlcNAc against SGD-induced PC12 cells injury...
April 2018: Research in Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29606965/synthesis-and-antileishmanial-activity-of-antimony-v-complexes-of-hydroxypyranone-and-hydroxypyridinone-ligands
#8
Vafa Sheikhmoradi, Sedigheh Saberi, Lotfollah Saghaei, Nader Pestehchian, Afshin Fassihi
A novel series of antimony (V) complexes with the hydroxypyranone and hydroxypyridinone ligands were synthesized and characterized by1 HNMR, FT-IR and electron spin ionization mass spectroscopic (ESI-MS) techniques. The synthesis process involved protection of hydroxyl group followed by the reaction of the intermediate with primary amines and finally deprotection. All compounds were evaluated for in vitro activities against the amastigote and promastigote forms of Leishmania major . Most of the synthesized compounds exhibited good antileishmanial activity against both forms of L...
April 2018: Research in Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29606964/the-immunoinhibitory-and-apoptosis-inducing-activities-of-foeniculum-vulgare-on-human-peripheral-blood-lymphocytes
#9
Salimeh Ebrahimnezhad Darzi, Seyedeh Parvin Khazraei, Zahra Amirghofran
Foeniculum vulgare ( F. vulgare, Apiaceae) is an important plant currently used in folk medicine to treat various diseases including infections and inflammatory conditions. In this study we have investigated the immunomodulatory and apoptosis-inducing activities of the fractions from this plant. We prepared dichloromethane, hexane, butanol, and water fractions from the aerial parts of the plant. We examined the growth inhibitory effects of the fractions on proliferative lymphocytes by the BrdU incorporation assay...
April 2018: Research in Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29606963/synthesis-characterization-and-stability-study-of-desloratadine-multicomponent-crystal-formation
#10
Ahmad Ainurofiq, Rachmat Mauludin, Diky Mudhakir, Sundani Nurono Soewandhi
This study describes the formation of multicomponent crystal (MCC) of desloratadine (DES). The objective of this study was to discover the new pharmaceutical MCC of DES using several coformers. The MCC synthesis was performed between DES and 26 coformers using an equimolar ratio with a solvent evaporation technique. The selection of the appropriate solvent was carried out using 12 solvents. The preview of the MCC of DES was performed using polarized light microscopy (PLM). The formation of MCC was confirmed using powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), fourier transform infrared spectroscopy (FTIR), and scanning electron microscopy (SEM)...
April 2018: Research in Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29387115/synthesis-and-characterization-of-some-novel-diaryl-urea-derivatives-bearing-quinoxalindione-moiety
#11
Sedighe Sadeghian-Rizi, Ghadamali Khodarahmi, Amirhossein Sakhteman, Ali Jahanian-Najafabadi, Mahboubeh Rostami, Mahmoud Mirzaei, Farshid Hassanzadeh
Diaryl urea derivatives have exhibited a broad spectrum of biochemical effects and pharmaceutical applications. Several diaryl urea derivatives such as sorafenib, regorafenib, linifanib, and tivozanib and lenvatinib are in clinical trial or clinical use. Therefore, development of small molecules within the diaryl urea scaffold with the ability of binding to variety of enzymes and receptors in the biological system are an interesting topic for researchers. Sorafenib as a diaryl urea derivative is a well-known anticancer agent...
February 2018: Research in Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29387114/anti-inflammatory-activity-of-echium-amoenum-extract-on-macrophages-mediated-by-inhibition-of-inflammatory-mediators-and-cytokines-expression
#12
Najmeh Naseri, Kurosh Kalantar, Zahra Amirghofran
Echium amoenum (Boraginaceae) is an important remedy used for various illnesses. In this study, we investigated the anti-inflammatory effects of E. amoenum in the J774.1A macrophage cell line. We prepared ethyl acetate, dichloromethane and hexane extracts from E. amoenum flowers and examined their possible cytotoxic effects using MTT assay. Lipopolysaccharide (LPS)-stimulated macrophages were treated with the extracts after which we measured nitric oxide (NO) production by Griess method. Inducible NO synthase (iNOS), cyclooxygenase-2 (COX2), tumor necrosis factor (TNF)-α, interleukin (IL)-1β, and IL-6 gene expressions were examined by real time-PCR...
February 2018: Research in Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29387113/magnesium-sulfate-protects-the-heart-against-carbon-monoxide-induced-cardiotoxicity-in-rats
#13
Kaveh Tabrizian, Hamideh Khodayari, Ramin Rezaee, Hosseinali Jahantigh, Gholamreza Bagheri, Konstantinos Tsarouhas, Mahmoud Hashemzaei
Carbon monoxide (CO), a toxic gas produced via incomplete fossil fuel combustion, has several poisonous effects in the heart including induction of necrosis, apoptosis, and electrocardiogram (ECG) changes. Magnesium sulfate (MS) is a drug with cardioprotective effects especially when used after ischemia/reperfusion. In the current study, we aimed to evaluate MS cardioprotective effects following CO poisoning. Animals were exposed to CO 3000 ppm for 1 h and immediately after the exposure period and on the next 4 days (a total of 5 consecutive doses given on a daily basis), MS (75, 150 and 300 mg/kg) was injected intraperitoneally (i...
February 2018: Research in Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29387112/estrogen-stimulates-adenosine-receptor-expression-subtypes-in-human-breast-cancer-mcf-7-cell-line
#14
Azam Mohamadi, Mahmoud Aghaei, Mojtaba Panjehpour
Estrogen is a steroid hormone that plays a key role in the development and regulation of reproductive system. It has been shown that estrogen is related to breast cancer development through binding to its receptors. In order to uncover the estrogen effects on adenosine receptor expression, estrogen-positive MCF-7 cells were used to treat with agonist and antagonist of estrogen and then the mRNA expression of adenosine receptor subtypes were evaluated. Estrogen-positive MCF-7 cells were treated with various concentrations of 17β estradiol (E2) as an estrogen agonist, and ICI 182,780 as an estrogen antagonist...
February 2018: Research in Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29387111/chronic-exposure-to-arsenic-and-high-fat-diet-additively-induced-cardiotoxicity-in-male-mice
#15
Akram Ahangarpour, Leila Zeidooni, Azin Samimi, Soheila Alboghobeish, Laya Sadat Khorsandi, Mitra Moradi
Diet is one of the important risk factors that could potentially affect arsenic-induced cardiotoxicity. The present study was undertaken to investigate the effect of high fat diet on arsenic-induced cardiotoxicity in mice. Mice were divided into six different groups (n = 12), two control groups received either low fat diet (LFD) or high fat diet (HFD) along with deionized drinking water and four test groups given LFD + 25 ppm arsenic, LFD + 50 ppm arsenic, HFD + 25 ppm arsenic, and HFD + 50 ppm arsenic in drinking water for 5 months...
February 2018: Research in Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29387110/the-effect-of-two-different-crosslinkers-on-in-vitro-characteristics-of-ciprofloxacin-loaded-chitosan-implants
#16
Esti Hendradi, Dewi Melani Hariyadi, Muhammad Faris Adrianto
The objective of this study was to determine and evaluate a controlled release implant of ciprofloxacin using bovine hydroxyapatite (BHA)-chitosan composite and glutaraldehyde or genipin as crosslinking agents. Ciprofloxacin implants were prepared using BHA, chitosan, ciprofloxacin at 30:60:10 and using three different concentrations of glutaraldehyde or genipin (0.3, 0.5, or 0.7%) as crosslinkers. Implants were formed as mini-tablet with 4.0 mm diameter weighing 100 mg using compression method. Further, the prepared ciprofloxacin implants were characterized for porosity, density, water absorption capacity, swelling, degradation, compressive strength, compatibility (Fourier transforms-infrared spectroscopy (FT-IR)), morphology (scanning electron microscope (SEM)), X-ray diffraction (X-RD), and in vitro drug release...
February 2018: Research in Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29387109/anti-tuberculosis-and-cytotoxic-evaluation-of-the-seaweed-sargassum-boveanum
#17
Vajihe Akbari, Saeed Zafari, Afsaneh Yegdaneh
Marine seaweeds produce a variety of compounds with different biological activities, including antituberculosis and anticancer effects. The aim of this study was to investigate anti-tuberculosis activity of Sargassum boveanum ( S. boveanum ) and cytotoxicity of different fractions of this seaweed. S. boveanum was collected from Persian Gulf. The plant was extracted by maceration with methanol-ethyl acetate solvent. The extract was evaporated and partitioned by Kupchan method to yield hexane, tricholoroethane, chloroform, and butanol partitions...
February 2018: Research in Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29387108/the-effects-of-hydroalcoholic-extract-of-allium-elburzense-wendelbo-bulb-on-dexamethasone-induced-dyslipidemia-hyperglycemia-and-oxidative-stress-in-rats
#18
Leila Safaeian, Behzad Zolfaghari, Sajad Karimi, Ardeshir Talebi, Mohammadreza Aghaye Ghazvini
Recent evidences have suggested the beneficial cardiovascular effects of some plants belonging to the genus Allium . The present study is an attempt to investigate the effects of hydroalcoholic extract of Allium elburzense bulb on dexamethasone-induced dyslipidemia in rats. Total phenolic content of A. elburzense bulb hydroalcoholic extract was determined using Folin-Ciocalteu method. Thirty-six male Wistar albino rats in 6 groups were studied. Group 1 (dyslipidemic control) received dexamethasone (10 mg/kg/day, s...
February 2018: Research in Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29387107/mitochondrial-and-caspase-pathways-are-involved-in-the-induction-of-apoptosis-by-nardosinen-in-mcf-7-breast-cancer-cell-line
#19
Amirhosein Shahali, Mustafa Ghanadian, Seyyed Mehdi Jafari, Mahmoud Aghaei
Natural products isolated from plants provide a valuable source for expansion of new anticancer drugs. Nardosinen (4,9-dihydroxy-nardosin-6-en) is a natural sesquiterpene extracted from Juniperus foetidissima . Recently, we have reported the cytotoxic effects of nardosinen in various cancer cells. The aim of the current study was to investigate the anticancer features of nardosinen as well as its possible molecular mechanisms of the nardosinen cytotoxic effect on breast tumor cells. MTT assay showed that nardosinen notably inhibited cell proliferation in a dose-dependent manner in MCF-7 breast cancer cells...
February 2018: Research in Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29387106/design-synthesis-cytotoxicity-evaluation-and-docking-studies-of-1-2-4-triazine-derivatives-bearing-different-arylidene-hydrazinyl-moieties-as-potential-mtor-inhibitors
#20
Sara Ranjbar, Najmeh Edraki, Mahsima Khoshneviszadeh, Alireza Foroumadi, Ramin Miri, Mehdi Khoshneviszadeh
Mammalian target of rapamycin (mTOR) is a phosphoinositide 3-kinase-related protein kinase which controls cell growth and is frequently deregulated in many cancers. Therefore, mTOR inhibitors are used as antineoplastic agents for cancer treatment. In this study, 1,2,4-triazine derivatives containing different arylidene-hydrazinyl moieties were designed and synthesized. Cytotoxicity of the compounds was evaluated on HL-60 and MCF-7 cell lines by MTT assay. S1 , S2 and S3 exhibited good cytotoxic activity on both cell lines with an IC50 range of 6...
February 2018: Research in Pharmaceutical Sciences
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