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Total 791 results found since Jan 2013.

Hybrid molecules of scutellarein and 3, 5, 6-trimethylpyrazine-2-formic acid linked with polar amino acid for ischemic stroke
AbstractScutellarin has been found to possess a certain protective activity against oxidative damage, and scutellarein has been proved to be the main absorption component of scutellarin in the small intestine. Tertramethylpyrazine is a commonly used antiplatelet drug, and its active metabolite 3, 5, 6-trimethylpyrazine-2-formic acid displays similar pharmacological activities with lower toxicity. Based on the principle of molecular hybridization and previous work, five hybrid molecules of scutellarein and 3, 5, 6-trimethylpyrazine-2-formic acid linked with polar amino acids were synthesized, and their anti-oxidative and an...
Source: Medicinal Chemistry Research - April 22, 2022 Category: Chemistry Source Type: research

Synthesis and biological evaluation of hybrids from optically active ring-opened 3-N-butylphthalide derivatives and 4-fluro-edaravone as potential anti-acute ischemic stroke agents
Bioorg Med Chem. 2022 Jun 20;69:116891. doi: 10.1016/j.bmc.2022.116891. Online ahead of print.ABSTRACTThe treatment of acute ischemic stroke (AIS) remains a tough challenge in clinic. Here, we report the anti-AIS activity of R- and S-FMPB generated from hybridization of ring-opened R- and S-3-N-butylphthalide (R- and S-NBP) derivatives (R- and S-APB) with 4-fluro-edaravone (4-F-Eda), respectively. S-FMPB (10 mg/kg, iv) significantly improved the neurological score and alleviated cerebral infarction and edema of rats suffered from transient middle cerebral artery occlusion (tMCAO), superior to RS- and R-FMPB, as well as bet...
Source: Bioorganic and Medicinal Chemistry - June 28, 2022 Category: Chemistry Authors: Jian Jia Jianbing Wu Duorui Ji Weijie Jiao Xiaoli Wang Zhangjian Huang Yihua Zhang Source Type: research

Comparison between one and two-dimensional liquid chromatographic approaches for the determination of plasmatic stroke biomarkers by isotope dilution and tandem mass spectrometry
Analyst, 2023, Accepted Manuscript DOI: 10.1039/D2AN01750D, PaperAdela Cort és Giménez-Coral, Pablo Rodriguez-Gonzalez, Adriana Gonzalez-Gago, Eva Cernuda Morollón, Elena López-Cancio, Belén Prieto García, Jose Ignacio Garcia Alonso This work presents the evaluation of one and two dimensional liquid chromatography for the quantification of three stroke outcome predictors in plasma. Isotopically labelled analogues of L-arginine (L-Arg), asymmetric dimethylarginine... The content of this RSS Feed (c) The Royal Society of Chemistry
Source: RSC - Analyst latest articles - December 16, 2022 Category: Chemistry Authors: Adela Cort és Giménez-Coral Source Type: research

Design and synthesis of novel GluN2A NMDAR positive allosteric modulators via scaffold hopping strategy as anti-stroke therapeutic agents
This study reported a series of GluN1/2A positive allosteric modulators as neuroprotective agents, and provided a potential opportunity to discover new drugs for stroke treatment.PMID:36934527 | DOI:10.1016/j.bmc.2023.117236
Source: Bioorganic and Medicinal Chemistry - March 19, 2023 Category: Chemistry Authors: Xin Chen Hongyu Zhu Xuequan Liu Qihong Li Mingxin Dong Source Type: research

Exploring Mechanisms of Houshiheisan in Treating Ischemic Stroke with Network Pharmacology and Independent Cascade Model
CONCLUSION: This study advocated potential drug development with targets in the AGE signaling pathway, with emphasis on neuroprotective, anti-inflammatory, and anti-apoptotic functions. The molecular docking simulation indicated that the ligand-target combination selection method based on the IC model was effective and reliable.PMID:37565556 | DOI:10.2174/1386207326666230810094557
Source: Combinatorial Chemistry and High Throughput Screening - August 11, 2023 Category: Chemistry Authors: Bo Cao Jiao Jin Zhiyu Tang Qiong Luo Jinbing An Wei Pang Source Type: research

The Role of Nicotinamidephosphoribosyltransferase in Cerebral Ischemia.
Abstract As recombinant tissue plasminogen activator is the only drug approved for the clinical treatment of acute ischemic stroke, there is an urgent unmet need for novel stroke treatments. Endogenous defense mechanisms against stroke may hold the key to new therapies for stroke. A large number of studies suggest that nicotinamidephosphoribosyl-transferase (NAMPT) is an attractive candidate to improve post-stroke recovery. NAMPT is a multifunctional protein and plays important roles in immunity, metabolism, aging, inflammation, and stress responses. NAMPT exists in both the intracellular and extracellular space. ...
Source: Current Topics in Medicinal Chemistry - June 10, 2015 Category: Chemistry Authors: Chen X, Zhao S, Song Y, Shi Y, Leak RK, Cao G Tags: Curr Top Med Chem Source Type: research

Plasma Branched-Chain Amino Acids and Incident Cardiovascular Disease in the PREDIMED Trial Lipids, Lipoproteins, and Cardiovascular Risk Factors
CONCLUSIONS: Higher concentrations of baseline BCAAs were associated with increased risk of CVD, especially stroke, in a high cardiovascular risk population. A Mediterranean-style diet had a negligible effect on 1-year changes in BCAAs, but it may counteract the harmful effects of BCAAs on stroke.
Source: Clinical Chemistry - March 27, 2016 Category: Chemistry Authors: Ruiz-Canela, M., Toledo, E., Clish, C. B., Hruby, A., Liang, L., Salas-Salvado, J., Razquin, C., Corella, D., Estruch, R., Ros, E., Fito, M., Gomez-Gracia, E., Aros, F., Fiol, M., Lapetra, J., Serra-Majem, L., Martinez-Gonzalez, M. A., Hu, F. B. Tags: Lipids, Lipoproteins, and Cardiovascular Risk Factors Source Type: research

Converter domain mutations in myosin alter structural kinetics and motor function Molecular Biophysics
Myosins are molecular motors that use a conserved ATPase cycle to generate force. We investigated two mutations in the converter domain of myosin V (R712G and F750L) to examine how altering specific structural transitions in the motor ATPase cycle can impair myosin mechanochemistry. The corresponding mutations in the human β-cardiac myosin gene are associated with hypertrophic and dilated cardiomyopathy, respectively. Despite similar steady-state actin-activated ATPase and unloaded in vitro motility–sliding velocities, both R712G and F750L were less able to overcome frictional loads measured in the loaded motility assay...
Source: Journal of Biological Chemistry - February 1, 2019 Category: Chemistry Authors: Laura K. Gunther, John A. Rohde, Wanjian Tang, Shane D. Walton, William C. Unrath, Darshan V. Trivedi, Joseph M. Muretta, David D. Thomas, Christopher M. Yengo Tags: Enzymology Source Type: research

AMPK inhibitor BML-275 induces neuroprotection through decreasing cyt c and AIF expression after transient brain ischemia
This study supports the hypothesis that anti-apoptosis is one of potential neuroprotective strategies for the treatment of stroke.PMID:34837819 | DOI:10.1016/j.bmc.2021.116522
Source: Bioorganic and Medicinal Chemistry - November 27, 2021 Category: Chemistry Authors: Yue Hu Yao-Dong Dong Yan-Chao Wu Qiu-Xu Wang Xiang Nan Da-Li Wang Source Type: research