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Drug Development Research

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https://www.readbyqxmd.com/read/28804913/on-bh3-mimetics-and-ca-2-signaling
#1
Pawel E Ferdek, Monika A Jakubowska
Preclinical Research BH3 mimetics are anticancer agents that reproduce the spatial arrangement of the BH3 domain of Bcl-2 family proteins. Just like the BH3-only proteins, these compounds bind to the hydrophobic cleft of the pro-survival Bcl-2 members such as Bcl-2 or Bcl-xL, and disrupt their heterodimerization with pro-apoptotic Bax or Bak, sensitizing cells to chemotherapy. In recent years, it has become clear that Bcl-2 family proteins are engaged in regulation of intracellular Ca(2+) homeostasis, including Ca(2+) release from the intracellular stores as well as Ca(2+) fluxes across the plasma membrane...
August 13, 2017: Drug Development Research
https://www.readbyqxmd.com/read/28799168/small-scaffolds-big-potential-developing-miniature-proteins-as-therapeutic-agents
#2
Justin M Holub
Preclinical Research Miniature proteins are a class of oligopeptide characterized by their short sequence lengths and ability to adopt well-folded, three-dimensional structures. Because of their biomimetic nature and synthetic tractability, miniature proteins have been used to study a range of biochemical processes including fast protein folding, signal transduction, catalysis and molecular transport. Recently, miniature proteins have been gaining traction as potential therapeutic agents because their small size and ability to fold into defined tertiary structures facilitates their development as protein-based drugs...
August 10, 2017: Drug Development Research
https://www.readbyqxmd.com/read/28786182/recent-advances-on-bioactive-constituents-in-ferula
#3
Yueting Zhou, Fang Xin, Guoqiang Zhang, Hexiang Qu, Desong Yang, Xiaoqiang Han
Preclinical Research The genus Ferula (Umbelliferea) is widely distributed across Central Asia and the Mediterranean. Some plants of the genus Ferula have been used as sources of pharmaceuticals for centuries. Ferula is a rich source of biologically active compounds, including coumarin derivatives, sesquiterpene-substituted compounds, daucane esters, humulane, and germacrane compounds, aromatic lactones and disulfide compounds. Therefore, utilizing these bioactive constituents with antimicrobial and insecticidal effects not only can provide a new strategy for developing drug and green pesticide, but also protect endangered plant resources...
August 8, 2017: Drug Development Research
https://www.readbyqxmd.com/read/28786125/recent-advances-in-glp-1-receptor-agonists-for-use-in-diabetes-mellitus
#4
Dominic N McBrayer, Yftah Tal-Gan
Preclinical Research Mimetics of Glucagon-like peptide 1 (GLP-1) represent a useful alternative or complementary treatment choice to insulin in the treatment of diabetes mellitus. The lack of hypoglycemia as a side effect when GLP-1 receptor agonists are used along with the tendency of these therapeutic agents to prevent or even reduce weight gain makes them valuable targets in therapy development. However, native GLP-1 and many of its early analogues have very short half-lives, requiring repeated treatment to maintain therapeutic levels...
August 8, 2017: Drug Development Research
https://www.readbyqxmd.com/read/28776721/synergistic-interaction-of-matricaria-chamomilla-extract-with-diclofenac-and-indomethacin-on-carrageenan-induced-paw-inflammation-in-rats
#5
Mario I Ortiz, Raquel Cariño-Cortés, Héctor A Ponce-Monter, Martha P González-García, Gilberto Castañeda-Hernández, Mireya Salinas-Caballero
Preclinical Research The coadministration of non-steroidal anti-inflammatory drugs (NSAIDs) with medicinal plant extracts may increase anti-inflammatory activity, thus permitting the use of lower NSAID doses and limiting the side effects. The aim of this study was to explore the interactions between an ethanolic extract of M. chamomilla extract (MCE) with two NSAIDs, diclofenac and indomethacin on carrageenan-induced paw inflammation and gastric injury in rats. Diclofenac, indomethacin and MCE, or combinations with MCE produced an anti-inflammatory effect...
August 4, 2017: Drug Development Research
https://www.readbyqxmd.com/read/28771761/metformin-protects-against-experimental-acrylamide-neuropathy-in-rats
#6
Samah S Oda
Preclinical Research To investigate the potential neuroprotective effects of metformin against experimental acrylamide neuropathy in rats, 24 rats were distributed into four equal groups (6 each). Group 1 was kept as a control. Group 2 (MET) was orally given metformin (200 mg/kg BW/day). Group 3 (ACR) was injected IP with acrylamide (50 mg/kg BW/day). Animals in group 4 (ACR + MET) were administered both MET and ACR at the same dose and route used in groups 2 and 3. Treatments were administered three times a week for three weeks...
August 3, 2017: Drug Development Research
https://www.readbyqxmd.com/read/28771757/supra-additive-interaction-of-docosahexaenoic-acid-and-naproxen-and-gastric-safety-on-the-formalin-test-in-rats
#7
Arlette Guadalupe Arroyo-Lira, Fernando Rodríguez-Ramos, Mario I Ortiz, Gilberto Castañeda-Hernández, Aracely Evangelina Chávez-Piña
Preclinical Research The aim of this work was to evaluate the effect of docosahexaenoic acid (DHA) on the pharmacokinetics and pharmacodynamics-nociception-of naproxen in rats, as well as to determine the gastric safety resulting from this combination versus naproxen alone. Female Wistar rats were orally administered DHA, naproxen or the DHA-naproxen mixture at fixed-ratio combination of 1:3. The antinociceptive effect was evaluated using the formalin test. The gastric injury was determined 3 h after naproxen administration...
August 3, 2017: Drug Development Research
https://www.readbyqxmd.com/read/28736996/phytochemical-investigation-antitumor-activity-and-hepatoprotective-effects-of-acrocarpus-fraxinifolius-leaf-extract
#8
Heba A S El-Nashar, Omayma A Eldahshan, Omama E Elshawi, Abdel Nasser B Singab
Preclinical Research Nine known phenolic compounds were isolated from an aqueous methanolic extract of Acrocarpus fraxinifolius Weight and Arn leaves (AFL) family Fabaceae. This extract of AFL contained approximately 169 mg gallic acid/g as assessed by HPLC. The AFL extract had marginal antitumor activity (IC50  > 200 µL/mL) but showed a concentration-dependent hepatoprotective effect against CCl4 -induced hepatotoxicity in vitro. Cell viability was increased, ALT and AST activity declined and reduced GSH concentration and SOD activity were restored as compared with silymarin...
July 24, 2017: Drug Development Research
https://www.readbyqxmd.com/read/28736839/the-neurotensin-nts1-receptor-agonist-pd149163-produces-antidepressant-like-effects-in-the-forced-swim-test-further-support-for-neurotensin-as-a-novel-pharmacologic-strategy-for-antidepressant-drugs
#9
Lawrence M Carey, Remington J Rice, Adam J Prus
Preclinical Research Neurotensin is a nonbrain penetrant neuropeptide neurotransmitter that alters dopaminergic and serotonergic neurotransmission. Previous animal behavioral studies have demonstrated that intra-ventral tegmental administration of neurotensin and system administration of the selective neurotensin NTS1 receptor agonist, PD149163 produce antidepressant-like effects in a forced swim test and a differential reinforcement of low rate task, respectively. The present study sought to expand upon these past findings by assessing systemic administration of PD149163 in a forced swim test, a primary antidepressant preclinical screening model, in mice...
July 24, 2017: Drug Development Research
https://www.readbyqxmd.com/read/28736816/antinociceptive-activity-of-ent-dihydrotucumanoic-acid-isolated-from-gymnosperma-glutinosum-spreng-less
#10
Angel Josabad Alonso-Castro, Marco Martin González-Chávez, Juan Ramón Zapata-Morales, Alexia Karina Verdinez-Portales, Amanda Sánchez-Recillas, Rolffy Ortiz-Andrade, Mario Isiordia-Espinoza, Fidel Martínez-Gutiérrez, Marco Antonio Ramírez-Morales, Fabiola Domínguez, María Elizabeth Juache-Flores, Roberto Martínez
Preclinical Research The diterpene ent-dihydrotumanoic acid (DTA) was among the compounds isolated from Gymnosperma glutinosum (Spreng) Less (Asteraceae). There are no reports regarding the pharmacological effects of DTA. Cytotoxicity against cancer cells (1-250 µM), and the antibacterial (50-1400 µM) activity of DTA were evaluated using the MTT assay, and the minimum inhibitory concentration test, respectively. The antidiarrheal (1-100 mg/kg p.o.) and anti-inflammatory (2 mg/ear) effects of DTA were evaluated using castor oil and 12-O-tetradecanoylphorbol-13-acetate, respectively...
July 24, 2017: Drug Development Research
https://www.readbyqxmd.com/read/28718949/high-dosage-of-vitamin-d-regulates-the-energy-metabolism-and-increases-insulin-sensitivity-but-are-associated-with-high-levels-of-kidney-damage
#11
Rafael Calais Gaspar, José Diego Botezelli, Gabriel Keine Kuga, Vitor Rosetto Muñoz, Andressa Coope, Rodrigo Martins Pereira, Adelino Sanchez Ramos da Silva, Dennys Esper Cintra, Leandro Pereira de Moura, Eduardo Rochete Ropelle, José Rodrigo Pauli
Preclinical Research Metabolic disorders are responsible for more than 60% of all deaths worldwide. Calcitriol or vitamin D (vitD) deficiency is associated with a large proportion of these diseases is an important therapeutic target for exploration. This study evaluated the administration of high doses of vitD (3000 IU/kg) in obese and insulin-resistant C57BL/6J mice. Our results demonstrated that although high doses of vitD provided metabolic benefits such as increased insulin sensitivity and decreased body mass, this was associated with significant damage in the kidneys of obese mice...
July 18, 2017: Drug Development Research
https://www.readbyqxmd.com/read/28639316/synergism-between-naproxen-and-rutin-in-a-mouse-model-of-visceral-pain
#12
Angel Josabad Alonso-Castro, Joceline Estefanía Rangel-Velázquez, Mario A Isiordia-Espinoza, Luis Enrique Villanueva-Solís, Othoniel H Aragon-Martinez, Juan Ramón Zapata-Morales
Preclinical Research The aim of the present study was to evaluate the antinociceptive interaction between naproxen and the glycoside flavonoid, rutin in the acetic acid-induced writhing test in mice. Naproxen (5, 20, 50, and 100 mg/kg p.o.) or rutin (10, 25, 50, and 100mg/kg p.o.) were administered 60 min before the intraperitoneal administration with acetic acid. The dose-response curve of each individual compound and the experimental effective dose 50 (ED50 ) value were obtained to determinate different proportions of the combinations between the two compounds (naproxen-rutin 1:1, 3:1, and 3:1) in the writhing test...
June 22, 2017: Drug Development Research
https://www.readbyqxmd.com/read/28639277/serum-derived-transfer-factor-stimulates-the-innate-immune-system-to-improve-survival-traits-in-high-risk-pathogen-scenarios
#13
Bridget V Willeford, Trudy Shapiro-Dunlap, Kenneth O Willeford
Preclinical Research Transfer Factors (TFs) are low molecular weight (<5,000 daltons) biological response mediators. In the present study, a serum derived TF improved the ability of the recipient animal to survive high-risk infectious challenges (salmonellosis and canine parvoviral enteritis (CPV)) by altering the host's cytokine response profile. Mice mortally challenged with 5,000 colony-forming units of Salmonella experienced a group mortality of 73% while mice treated with a single 5 mg dose of the TF demonstrated a significant decrease in morbidity (7%, p ≤ 0...
June 22, 2017: Drug Development Research
https://www.readbyqxmd.com/read/28593649/the-effect-of-gabapentin-and-tramadol-in-cancer-pain-induced-by-glioma-cell-in-rat-femur
#14
Janette Nallely Corona-Ramos, Myrna Déciga-Campos, Mario Romero-Piña, Luis A Medina, Issac Martínez-Racine, Osmar A Jaramillo-Morales, Patricia García-López, Francisco Javier López-Muñoz
Preclinical Research The presence of pain as part of the cancer process is variable. Glioblastoma multiform (GBM) can produce bone metastasis, a condition that involves other pathological phenotypes including neuropathic and inflammatory pain. Tramadol and gabapentin are drugs used in the treatment of neuropathic pain. However, there are no studies evaluating their analgesic effects in bone metastasis. We produced a pain model induced by the inoculation of glioma cells (10(5) ) into the rat femur, by perforating the intercodiloid fossa...
June 7, 2017: Drug Development Research
https://www.readbyqxmd.com/read/28524398/anti-inflammatory-and-analgesic-activities-of-terminalia-muelleri-benth-combretaceae
#15
Nouran M Fahmy, Eman Al-Sayed, Mohamed M Abdel-Daim, Abdel Nasser Singab
Preclinical Research The anti-inflammatory and analgesic activities of a polyphenol-rich fraction (TMEF) obtained from Terminalia muelleri Benth. were measured. The analgesic activity of TMEF was tested using acetic acid-induced writhing and hot plate models in mice. The anti-inflammatory activity was assessed using carrageenan-induced paw edema model by measuring PGE2 , TNF-α, IL-1β, and IL-6 plasma levels as well as the paw thickness. TMEF was tested at doses of 100, 200, and 400 mg/kg p.o. and diclofenac sodium was used as a standard (100 mg/kg) in all experiments...
May 19, 2017: Drug Development Research
https://www.readbyqxmd.com/read/28524372/herbal-formula-baogan-yihao-bgyh-prevented-dimethylnitrosamine-dmn-induced-liver-injury-in-rats
#16
Xiujie Liu, Jing Su, Yu Shi, Ying Guo, Imran Suheryani, Shicong Zhao, Yulin Deng, Weiwei Meng, Yan Chen, Lili Sun, Rongji Dai
Preclinical Research Baogan Yihao (BGYH) is a traditional Chinese herbal medicine for the treatment of chronic liver diseases. In this study, the effects of BGYH on dimethylnitrosamine (DMN)-induced liver fibrosis were investigated using a rat model. BGYH alleviate liver damage, as indicated by decreased levels of AST, ALT, γ-GT, and AKP. BGYH also prevented collagen deposition and reduced pathological tissue injury in liver tissue. In fibrosis, high levels of α-SMA and TGF-β in liver tissue were markedly attenuated by BGYH...
May 19, 2017: Drug Development Research
https://www.readbyqxmd.com/read/28608491/toxicity-and-protective-effect-of-phenolic-enriched-ethylacetate-fraction-of-ocimum-gratissimum-linn-leaf-against-acute-inflammation-and-oxidative-stress-in-rats
#17
Abayomi M Ajayi, Solomon Umukoro, Benneth Ben-Azu, Bulus Adzu, Olusegun G Ademowo
Preclinical Research Ocimum gratissimum L. leaves have attracted considerable attention from researchers because of their medicinal value that include anti-inflammatory, analgesic, antimicrobial, and antioxidant activities. In the present study, the toxicity and the protective effect of phenolic extract of O. gratissimum leaf (EAFOg) against acute inflammation and oxidative stress in rats was assessed. EAFOg, enriched in phenols had no cytotoxic effect against CHO-k1 cells, and no lethality against brine shrimp eggs or mice at a dose of 2000 mg/kg...
June 2017: Drug Development Research
https://www.readbyqxmd.com/read/28608490/antiestrogenic-activity-of-triptolide-in-human-breast-cancer-cells-mcf-7-and-immature-female-mouse
#18
Yi Tang, Jun Wang, Jinghua Cheng, Lijun Wang
Preclinical Research To investigate the antiestrogenic activity of triptolide in human breast cancer cell line MCF-7 and immature female C57BL/6 mouse. The effects of triptolide on cell proliferation, cell cycle, and the expression of estrogen receptor alpha (ERα) and progesterone receptor (PR) were examined in MCF-7 cells. In vivo antiestrogenic effects of triptolide were observed after cotreatment of mice with E2 and triptolide for 4 days. Triptolide dose- and time-dependently inhibited cell growth in untreated or E2 -treated MCF-7 cells, which was associated with increased S phase arrest...
June 2017: Drug Development Research
https://www.readbyqxmd.com/read/28449192/anti-inflammatory-effects-of-pegylated-human-adrenomedullin-in-a-mouse-dss-induced-colitis-model
#19
Sayaka Nagata, Motoo Yamasaki, Kazuo Kitamura
Preclinical Research Human adrenomedullin (hAM), a hypotensive peptide, also has anti-inflammatory effects. hAM can reduce the severity of the dextran sulphate sodium (DSS)- and 2,4,6-trinitrobenzene sulfonic acid (TNBS)-induced colitis in animal models. Furthermore, in a clinical study, hAM treatment reduced the Disease Activity Index in ulcerative colitis. However, these therapeutic effects required continuous administration of hAM as the half-life of native hAM is quite short in blood. To resolve this problem, hAM N-terminal was conjugated with two kinds of polyethylene glycol (PEG); 5 kDa PEG or 60 kDa PEG (5 kDa PEG-hAM and 60 kDa PEG-hAM respectively)...
April 27, 2017: Drug Development Research
https://www.readbyqxmd.com/read/28370133/isobolographic-analyses-of-proglumide-celecoxib-interaction-in-rats-with-painful-diabetic-neuropathy
#20
Samuel Suarez-Mendez, Carlos A Tovilla-Zarate, Luis F Ortega-Varela, Deysi Y Bermudez-Ocaña, Jorge L Blé-Castillo, Thelma B González-Castro, Alma M Zetina-Esquivel, Juan C Diaz-Zagoya, Isela Esther Juárez-Rojop
Preclinical Research The aim of the present study was to analyze the antihyperalgesic and antiallodynic interaction between the non-selective cholecystokinin (CCK) antagonist receptor, proglumide, and the selective cyclooxygenase-2 inhibitor, celecoxib in streptozotocin (STZ)-induced diabetic rats. Hyperalgesia was evaluated in the formalin test and tactile allodynia using von Frey filaments. Isobolographic analyses were employed to define the nature of the compound interactions, using a fixed dose ratio (0...
April 3, 2017: Drug Development Research
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