Computational and experimental exploration of the structure –activity relationships of flavonoids as potent glyoxalase‐I inhibitors
Drug Development Research, EarlyView. (Source: Drug Development Research)
Source: Drug Development Research - December 29, 2017 Category: Drugs & Pharmacology Source Type: research
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Drug Development Research, Ahead of Print. (Source: Drug Development Research)
Source: Drug Development Research - December 29, 2017 Category: Drugs & Pharmacology Source Type: research
Analgesic efficacy of preoperative dexketoprofen trometamol: A systematic review and meta ‐analysis
Drug Development Research, EarlyView. (Source: Drug Development Research)
Source: Drug Development Research - December 15, 2017 Category: Drugs & Pharmacology Source Type: research
Pharmacological interaction of α‐bisabolol and diclofenac on nociception, inflammation, and gastric integrity in rats
Drug Development Research,Volume 79, Issue 1, Page 29-37, February 2018. (Source: Drug Development Research)
Source: Drug Development Research - December 15, 2017 Category: Drugs & Pharmacology Source Type: research
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Drug Development Research, Ahead of Print. (Source: Drug Development Research)
Source: Drug Development Research - December 15, 2017 Category: Drugs & Pharmacology Source Type: research
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Drug Development Research,Volume 79, Issue 1, Page 29-37, February 2018. (Source: Drug Development Research)
Source: Drug Development Research - December 15, 2017 Category: Drugs & Pharmacology Source Type: research
Pharmacological interaction of α‐bisabolol and diclofenac on nociception, inflammation, and gastric integrity in rats
In this study, the effects of an interaction between α‐bisabolol and the NSAID, diclofenac on nociception (formalin test), inflammation (paw inflammation produced by carrageenan) and gastric injury in rat was assessed. Diclofenac, α‐bisabolol, or diclofenac–α‐bisabolol combinations produced antinociceptive and anti‐inflammatory effects in rat (p < .05). The systemic administration of diclofenac, but not α‐bisabolol, produced gastric damage while the diclofenac–α‐bisabolol combinations produced limited gastric damage. Effective dose (ED40) values were determined for each individual drug and analy...
Source: Drug Development Research - December 15, 2017 Category: Drugs & Pharmacology Authors: Mario I. Ortiz, Raquel Cari ño‐Cortés, Héctor A. Ponce‐Monter, Gilberto Castañeda‐Hernández, Aracely Evangelina Chávez‐Piña Tags: RESEARCH ARTICLE Source Type: research
Issue Information – TOC
(Source: Drug Development Research)
Source: Drug Development Research - December 11, 2017 Category: Drugs & Pharmacology Tags: Issue Information – TOC Source Type: research
Ursolic acid derivatives as potential antidiabetic agents: In vitro, in vivo, and in silico studies
Abstract
Protein tyrosine phosphatase 1B (PTP‐1B) has attracted interest as a novel target for the treatment of type 2 diabetes, this because its role in the insulin‐signaling pathway as a negative regulator. Thus, the aim of current work was to obtain seven ursolic acid derivatives as potential antidiabetic agents with PTP‐1B inhibition as main mechanism of action. Furthermore, derivatives 1–7 were submitted in vitro to enzymatic PTP‐1B inhibition being 3, 5, and 7 the most active compounds (IC50 = 5.6, 4.7, and 4.6 μM, respectively). In addition, results were corroborated with in silico docking studi...
Source: Drug Development Research - December 1, 2017 Category: Drugs & Pharmacology Authors: Ricardo Guzm án‐Ávila, Virginia Flores‐Morales, Paolo Paoli, Guido Camici, Juan José Ramírez‐Espinosa, Litzia Cerón‐Romero, Gabriel Navarrete‐Vázquez, Sergio Hidalgo‐Figueroa, Maria Yolanda Rios, Rafael Villalobos‐Molina, Samuel Estrad Tags: RESEARCH ARTICLE Source Type: research
Assessment of the antinociceptive and ulcerogenic activity of the tapentadol –diclofenac combination in rodents
The objective of the present study was to evaluate the tapentadol–diclofenac combination in three dose‐ratios in the mouse acetic acid‐induced visceral pain and their ulcerogenic activity on the stomachal mucous. Dose‐response curves were generated for tapentadol, diclofenac, and their combination in the acetic acid‐induced writhing test in mice. Moreover, the stomachs of animals were surgically removal and gastrointestinal ulcerogenic action of the combination was assessed. The isobolographic analysis, interaction index, and ANOVA were used to analyze the data. The isobolographic analysis and interaction index s...
Source: Drug Development Research - December 1, 2017 Category: Drugs & Pharmacology Authors: Juan R. Zapata ‐Morales, Ángel J. Alonso‐Castro, Vinicio Granado‐Soto, Sergio Sánchez‐Enriquez, Mario A. Isiordia‐Espinoza Tags: RESEARCH ARTICLE Source Type: research
Computational and experimental exploration of the structure –activity relationships of flavonoids as potent glyoxalase‐I inhibitors
Abstract
Glyoxalase‐I (Glo‐I) enzyme has emerged as a potential target for cancer treatment. Several classes of natural products including coumarins and flavonoids have shown remarkable Glo‐I inhibitory activity. In the present study, computational and experimental approaches were used to explore the structure–activity relationships of a panel of 24 flavonoids as inhibitors of the Glo‐1 enzyme. Scutellarein with an IC50 value of 2.04 μM was identified as the most potent inhibitor among the series studied. Di‐ or tri‐hydroxylation of the benzene rings A and B accompanied with a C2/C3 double bond in rin...
Source: Drug Development Research - December 1, 2017 Category: Drugs & Pharmacology Authors: Qosay A. Al ‐Balas, Mohammad A. Hassan, Nizar A. Al‐Shar'i, Tamam El‐Elimat, Ammar M. Almaaytah Tags: RESEARCH ARTICLE Source Type: research
Analgesic efficacy of preoperative dexketoprofen trometamol: A systematic review and meta ‐analysis
Abstract
Clinical evidence supports the use of dexketoprofen trometamol (DEX) to manage acute postoperative pain. However, controversies surround the impact of the use of this drug in preoperative analgesic protocols. The aim of the present meta‐analysis was to evaluate the effectiveness of the preoperative administration of DEX under postoperative pain conditions. Electronic and manual searches were conducted through diverse electronic databases. A systematic review and meta‐analysis to evaluate the analgesic efficacy of the preoperative administration of DEX was performed including Randomized Clinical Trials (...
Source: Drug Development Research - December 1, 2017 Category: Drugs & Pharmacology Authors: Vicente Esparza ‐Villalpando, Amaury Pozos‐Guillén, David Masuoka‐Ito, César Gaitán‐Fonseca, Daniel Chavarría‐Bolaños Tags: RESEARCH ARTICLE Source Type: research
Anti ‐inflammatory and analgesic activities of cupressuflavone from Cupressus macrocarpa: Impact on pro‐inflammatory mediators
Drug Development Research,Volume 79, Issue 1, Page 22-28, February 2018. (Source: Drug Development Research)
Source: Drug Development Research - November 11, 2017 Category: Drugs & Pharmacology Source Type: research
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Drug Development Research,Volume 79, Issue 1, Page 22-28, February 2018. (Source: Drug Development Research)
Source: Drug Development Research - November 11, 2017 Category: Drugs & Pharmacology Source Type: research
Issue Information – TOC
(Source: Drug Development Research)
Source: Drug Development Research - November 8, 2017 Category: Drugs & Pharmacology Tags: Issue Information – TOC Source Type: research
