keyword
https://read.qxmd.com/read/38529713/mechanistic-insights-into-sodium-ion-mediated-ligand-binding-affinity-and-modulation-of-5-ht2b-gpcr-activity-implications-for-drug-discovery-and-development
#1
JOURNAL ARTICLE
Arushi Chauhan, Jitender Singh, Namrata Sangwan, Pramod K Avti
PURPOSE: The G-protein coupled receptor (GPCR) family, implicated in neurological disorders and drug targets, includes the sensitive serotonin receptor subtype, 5-HT2B. The influence of sodium ions on ligand binding at the receptor's allosteric region is being increasingly studied for its impact on receptor structure. METHODS: High-throughput virtual screening of three libraries, specifically the Asinex-GPCR library, which contains 8,532 compounds and FDA-approved (2466 compounds) and investigational compounds (2731)) against the modeled receptor [4IB4-5HT2B RM ] using the standard agonist/antagonist (Ergotamine/Methysergide), as previously selected from our studies based on ADMET profiling, and further on basis of binding free energy a single compound - dihydroergotamine is chosen...
March 26, 2024: Journal of Receptor and Signal Transduction Research
https://read.qxmd.com/read/38522494/in-vitro-immunotoxicity-effects-of-carbendazim-were-inhibited-by-n-acetylcysteine-in-microglial-bv-2-cells
#2
JOURNAL ARTICLE
Narjesse E L Mabrouk, Maha Mastouri, Gérard Lizard, Mahjoub Aouni, Hedi Harizi
Carbendazim (CBZ) is a benzimidazole fungicide widely used worldwide in industrial, agricultural, and veterinary practices. Although, CBZ was found in all brain tissues causing serious neurotoxicity, its impact on brain immune cells remain scarcely understood. Our study investigated the in vitro effects of CBZ on activated microglial BV-2 cells. Lipopolysaccharide (LPS)-stimulated BV-2 cells were exposed to increasing concentrations of CBZ and cytokine release was measured by ELISA, and Cytometric Bead Array (CBA) assays...
March 22, 2024: Toxicology in Vitro: An International Journal Published in Association with BIBRA
https://read.qxmd.com/read/38507311/emodin-ameliorates-myocardial-fibrosis-in-mice-by-inactivating-the-ros-pi3k-akt-mtor-axis
#3
JOURNAL ARTICLE
Wei Huang, Peiting Zhou, Xinyun Zou, Yunchuan Liu, Longfu Zhou, Yaolei Zhang
BACKGROUND: Emodin is a traditional medicine that has been shown to exert anti-inflammatory and anti-oxidative effects. Previous research has indicated that emodin can alleviate myocardial remodeling and inhibit myocardial hypertrophy and fibrosis. However, the mechanism by which emodin affects myocardial fibrosis (MF) has not yet been elucidated. METHODS: Fibroblasts were treated with ANGII, and a mouse model of MF was established by ligation of the left anterior descending coronary artery...
December 31, 2024: Clinical and Experimental Hypertension: CHE
https://read.qxmd.com/read/38486486/a-benzarone-derivative-inhibits-eya-to-suppress-tumor-growth-in-shh-medulloblastoma
#4
JOURNAL ARTICLE
Grace H Hwang, Maria F Pazyra-Murphy, Hyuk-Soo Seo, Sirano Dhe-Paganon, Sylwia A Stopka, Marina DiPiazza, Nizhoni Sutter, Thomas W Gero, Alison Volkert, Lincoln Ombelets, Georgia Dittemore, Matthew G Rees, Melissa M Ronan, Jennifer A Roth, Nathalie Y R Agar, David A Scott, Rosalind A Segal
UNLABELLED: Medulloblastoma is one of the most common malignant brain tumors of children, and 30% of medulloblastomas are driven by gain-of-function genetic lesions in the Sonic Hedgehog (SHH) signaling pathway. EYA1, a haloacid dehalogenase phosphatase and transcription factor, is critical for tumorigenesis and proliferation of SHH medulloblastoma (SHH-MB). Benzarone and benzbromarone have been identified as allosteric inhibitors of EYA proteins. Using benzarone as a point of departure, we developed a panel of 35 derivatives and tested them in SHH-MB...
March 15, 2024: Cancer Research
https://read.qxmd.com/read/38485044/roles-of-heat-shock-protein-a12a-in-the-development-of-diabetic-cardiomyopathy
#5
JOURNAL ARTICLE
Yunxiao Jia, Yunhao Yu, Chenxi Gao, Yuehua Li, Chuanfu Li, Zhengnian Ding, Qiuyue Kong, Li Liu
Long-term hyperglycemia can lead to diabetic cardiomyopathy (DCM), a main lethal complication of diabetes. However, the mechanisms underlying DCM development have not been fully elucidated. Heat shock protein A12A (HSPA12A) is the atypic member of HSP70 family. In the present study, we found that the expression of HSPA12A was upregulated in hearts of mice with streptozotocin (STZ)-induced diabetes, while ablation of HSPA12A improved cardiac systolic and diastolic dysfunction and increased cumulative survival of diabetic mice...
March 12, 2024: Cell Stress & Chaperones
https://read.qxmd.com/read/38468466/dihydroergotamine-protects-against-ischemic-stroke-by-modulating-microglial-macrophage-polarization-and-inhibiting-inflammation-in-mice
#6
JOURNAL ARTICLE
Yangmin Zheng, Yue Hu, Feng Yan, Rongliang Wang, Zhen Tao, Junfen Fan, Ziping Han, Haiping Zhao, Ping Liu, Wei Zhuang, Yumin Luo
OBJECTIVES: The search for drugs that can protect the brain tissue and reduce nerve damage in acute ischemic stroke has emerged as a research hotspot. We investigated the potential protective effects and mechanisms of action of dihydroergotamine against ischemic stroke. METHODS: C57BL/6 mice were subjected to middle cerebral artery occlusion (MCAO), and dihydroergotamine at a dose of 10 mg/kg/day was intraperitoneally injected for 14 days. Adhesive removal and beam walking tests were conducted 1, 3, 5, 7, 10, and 14 days after MCAO surgery...
March 11, 2024: Neurological Research
https://read.qxmd.com/read/38459660/dihydrocapsaicin-suppresses-the-sting-mediated-accumulation-of-ros-and-nlrp3-inflammasome-and-alleviates-apoptosis-after-ischemia-reperfusion-injury-of-perforator-skin-flap
#7
JOURNAL ARTICLE
Yingying Lai, Ningning Yang, Xuankuai Chen, Xianhui Ma, Zhuliu Chen, Chengji Dong, Gaoxiang Yu, Yingying Huang, Donghao Shi, Pin Fang, Kejian Fu, Renhao Jiang, Cong Mao, Jian Ding, Weiyang Gao
Avascular necrosis frequently occurs as a complication following surgery involving the distal perforator flap. Dihydrocapsaicin (DHC) can protect tissue from ischemia-reperfusion (I/R) injury, but its specific role in multizone perforator flaps remains unclear. In this study, the prospective target of DHC in the context of I/R injury was predicted using network pharmacology analysis. Flap viability was determined through survival area analysis, laser Doppler blood flow, angiograms, and histological examination...
March 8, 2024: Phytotherapy Research: PTR
https://read.qxmd.com/read/38452694/penthorum-chinense-pursh-inhibits-ferroptosis-in-cellular-and-caenorhabditis-elegans-models-of-alzheimer-s-disease
#8
JOURNAL ARTICLE
Yuan-Yuan Yong, Lu Yan, Bin-Ding Wang, Dong-Sheng Fan, Min-Song Guo, Lu Yu, Jian-Ming Wu, Da-Lian Qin, Betty Yuen-Kwan Law, Vincent Kam-Wai Wong, Chong-Lin Yu, Xiao-Gang Zhou, An-Guo Wu
BACKGROUND: Ferroptosis, a unique type of cell death triggered by iron-dependent lipid peroxidation, plays a critical role in the pathogenesis of Alzheimer's disease (AD), a debilitating condition marked by memory loss and cognitive impairment due to the accumulation of beta-amyloid (Aβ) and hyperphosphorylated Tau protein. Increasing evidence suggests that inhibitors of ferroptosis could be groundbreaking in the treatment of AD. METHOD: In this study, we established in vitro ferroptosis using erastin-, RSL-3-, hemin-, and iFSP1-induced PC-12 cells...
February 16, 2024: Phytomedicine
https://read.qxmd.com/read/38452099/chronic-intermittent-hypoxia-aggravated-diabetic-cardiomyopathy-through-lkb1-ampk-nrf2-signaling-pathway
#9
JOURNAL ARTICLE
Bingbing Liu, Jianchao Si, Kerong Qi, Dongli Li, Tingting Li, Yi Tang, Ensheng Ji, Shengchang Yang
Chronic intermittent hypoxia (CIH) may play an important role in the development of diabetic cardiomyopathy (DCM). However, the exact mechanism of CIH-induced myocardial injury in DCM remains unclear. In vivo, the db/db mice exposed to CIH were established, and in vitro, the H9C2 cells were exposed to high glucose (HG) combined with intermittent hypoxia (IH). The body weight (BW), fasting blood glucose (FBG) and food intake were measured every two weeks. The glycolipid metabolism was assessed with the oral glucose tolerance test (OGTT) and insulin resistance (IR)...
2024: PloS One
https://read.qxmd.com/read/38424055/dioxygen-compatible-electron-donor-acceptor-catalytic-system-and-its-enabled-aerobic-oxygenation
#10
JOURNAL ARTICLE
Jialiang Wei, Junhong Meng, Caifang Zhang, Yameng Liu, Ning Jiao
The photochemical properties of Electron Donor-Acceptor (EDA) complexes present exciting opportunities for synthetic chemistry. However, these strategies often require an inert atmosphere to maintain high efficiency. Herein, we develop an EDA complex photocatalytic system through rational design, which overcomes the oxygen-sensitive limitation of traditional EDA photocatalytic systems and enables aerobic oxygenation reactions through dioxygen activation. The mild oxidation system transfers electrons from the donor to the effective catalytic acceptor upon visible light irradiation, which are subsequently captured by molecular oxygen to form the superoxide radical ion, as demonstrated by the specific fluorescent probe, dihydroethidine (DHE)...
February 29, 2024: Nature Communications
https://read.qxmd.com/read/38421470/edaravone-maintains-aqp4-polarity-via-os-mmp9-%C3%AE-dg-pathway-in-an-experimental-intracerebral-hemorrhage-mouse-model
#11
JOURNAL ARTICLE
Zhenhua Wang, Yuan Li, Zhixu Wang, Yuhui Liao, Qingqing Ye, Shilong Tang, Ting Wei, Pengyu Xiao, Juan Huang, Weitian Lu
Oxidative stress (OS) is the main cause of secondary damage following intracerebral hemorrhage (ICH). The polarity expression of aquaporin-4 (AQP4) has been shown to be important in maintaining the homeostasis of water transport and preventing post-injury brain edema in various neurological disorders. This study primarily aimed to investigate the effect of the oxygen free radical scavenger, edaravone, on AQP4 polarity expression in an ICH mouse model and determine whether it involves in AQP4 polarity expression via the OS/MMP9/β-dystroglycan (β-DG) pathway...
February 29, 2024: Molecular Neurobiology
https://read.qxmd.com/read/38413540/a-randomized-open-label-5-period-crossover-study-evaluating-the-pharmacokinetics-and-safety-of-a-single-dose-of-intranasal-dihydroergotamine-dhe-powder-sts101-intramuscular-dhe-mesylate-and-liquid-nasal-spray-dhe-in-healthy-adults
#12
JOURNAL ARTICLE
Richard B Lipton, Detlef Albrecht, Maria Bermudez, Jerry Hu, Elizabeth Hussey, Jeff Levy
OBJECTIVE: To compare the safety and pharmacokinetics (PK) of dihydroergotamine (DHE) after administration of intranasal DHE powder (STS101), liquid nasal spray (LNS) DHE mesylate, and intramuscular (IM) DHE mesylate injection in healthy participants. BACKGROUND: DHE is an effective acute migraine treatment; however, self-administration difficulties have prevented its broader role in the management of migraine. METHODS: This randomized, active-controlled, five-period crossover study was conducted over 5 weeks separated by 1-week washout periods...
February 27, 2024: Headache
https://read.qxmd.com/read/38409327/redox-regulation-of-m-6-a-methyltransferase-mettl3-in-%C3%AE-cells-controls-the-innate-immune-response-in-type-1-diabetes
#13
JOURNAL ARTICLE
Dario F De Jesus, Zijie Zhang, Natalie K Brown, Xiaolu Li, Ling Xiao, Jiang Hu, Matthew J Gaffrey, Garrett Fogarty, Sevim Kahraman, Jiangbo Wei, Giorgio Basile, Tariq M Rana, Clayton Mathews, Alvin C Powers, Audrey V Parent, Mark A Atkinson, Sirano Dhe-Paganon, Decio L Eizirik, Wei-Jun Qian, Chuan He, Rohit N Kulkarni
Type 1 diabetes (T1D) is characterized by the destruction of pancreatic β-cells. Several observations have renewed the interest in β-cell RNA sensors and editors. Here, we report that N6 -methyladenosine (m6 A) is an adaptive β-cell safeguard mechanism that controls the amplitude and duration of the antiviral innate immune response at T1D onset. m6 A writer methyltransferase 3 (METTL3) levels increase drastically in β-cells at T1D onset but rapidly decline with disease progression. m6 A sequencing revealed the m6 A hypermethylation of several key innate immune mediators, including OAS1, OAS2, OAS3 and ADAR1 in human islets and EndoC-βH1 cells at T1D onset...
February 26, 2024: Nature Cell Biology
https://read.qxmd.com/read/38400621/vascular-protein-disulfide-isomerase-a1-mediates-endothelial-dysfunction-induced-by-angiotensin-ii-in-mice
#14
JOURNAL ARTICLE
Agnieszka Kij, Anna Bar, Izabela Czyzynska-Cichon, Kamil Przyborowski, Bartosz Proniewski, Lukasz Mateuszuk, Zuzanna Kurylowicz, Agnieszka Jasztal, Elzbieta Buczek, Anna Kurpinska, Joanna Suraj-Prazmowska, Brygida Marczyk, Karolina Matyjaszczyk-Gwarda, Andreas Daiber, Matthias Oelze, Maria Walczak, Stefan Chlopicki
AIM: Protein disulfide isomerases (PDIs) are involved in platelet aggregation and intravascular thrombosis, but their role in regulating endothelial function is unclear. Here, we characterized the involvement of vascular PDIA1 in angiotensin II (Ang II)-induced endothelial dysfunction in mice. METHODS: Endothelial dysfunction was induced in C57BL/6JCmd male mice via Ang II subcutaneous infusion, and PDIA1 was inhibited with bepristat. Endothelial function was assessed in vivo with magnetic resonance imaging and ex vivo with a myography, while arterial stiffness was measured as pulse wave velocity...
February 23, 2024: Acta Physiologica
https://read.qxmd.com/read/38390944/high-glucose-induces-oxidative-stress-that-alters-glycocalyx-proteoglycan-levels-in-primary-rat-retinal-microvascular-endothelial-cells-and-in-isolated-ophthalmic-arteries
#15
JOURNAL ARTICLE
Ivan A Alvarez, Minsup Lee, Randa S Eshaq, Wendy Leskova, Norman R Harris
Our purpose in this study was to identify the role played by oxidative stress in the changes to proteoglycans that occur under hyperglycemic conditions, using primary rat retinal microvascular endothelial cells (RRMEC) and cultured ophthalmic arteries. The cells and blood vessels obtained from rats were cultured in normal glucose (5.6 mM) and high glucose (25 mM) with or without N-acetylcysteine (NAC), an antioxidant. Intracellular oxidative stress was determined by measuring dihydroethidium (DHE) fluorescence and malondialdehyde (MDA)-modified protein levels...
February 6, 2024: Pathophysiology: the Official Journal of the International Society for Pathophysiology
https://read.qxmd.com/read/38360728/fucoidan-modulates-sirt1-and-nlrp3-to-alleviate-hypertensive-retinopathy-in-vivo-and-in-vitro-insights
#16
JOURNAL ARTICLE
Jing Li, Xiaochen Wang, Jie Bai, Huangzhao Wei, Wenbo Wang, Shuai Wang
BACKGROUND: Hypertension influences the inflammatory pathological changes in the retina. The function of the inflammasomes is significant. To see if Sirtuin 1 (SIRT1) regulates angiotensin II (Ang II)-induced hypertensive retinopathy and inflammation by modulating NOD-like receptor thermal protein domain associated protein 3 (NLRP3) inflammasome activation and the potential protective effects of fucoidan (FO) in mouse retinal vascular endothelial cells (mRECs) and mice retina. METHODS: The diagnosis of hypertensive retinopathy was made after three weeks of Ang II infusion (3000 ng/kg/min)...
February 15, 2024: Journal of Translational Medicine
https://read.qxmd.com/read/38314817/high-throughput-screening-assessment-of-reactive-oxygen-species-ros-generation-using-dihydroethidium-dhe-fluorescence-dye
#17
JOURNAL ARTICLE
Rahul Kumar, Rama R Gullapalli
Reactive oxygen species (ROS) play a key role in the regulation of cellular metabolism in physiological and pathological processes. Physiological ROS production plays a central role in the spatial and temporal modulation of normal cellular functions such as proliferation, signaling, apoptosis, and senescence. In contrast, chronic ROS overproduction is responsible for a wide spectrum of diseases, such as cancer, cardiovascular disease, and diabetes, among others. Quantifying ROS levels in an accurate and reproducible manner is thus essential to understanding normal cellular functionality...
January 19, 2024: Journal of Visualized Experiments: JoVE
https://read.qxmd.com/read/38313995/benefits-and-risks-of-medications-used-in-the-management-of-hypotension-a-review
#18
REVIEW
Thangwaritorn Skylynn, Thomas Abel, Lee Christopher, Ghafary Suliman, Rivera Dominic, Varughese Joel, Zeyu Yu, Sudhakar Pemminati
This comprehensive literature review addresses the scarcity and limited study of hypotension treatments compared to abundant antihypertensive drugs. Hypotension, categorized as absolute, relative, or orthostatic, has diverse causes. This review explores various treatments, including drugs affecting the sympathetic nervous system, such as midodrine, dihydroergotamine, and ergotamine, which have shown efficacy in managing hypotension. Dopamine agonists/antagonists and other drugs such as ephedrine, norepinephrine, and fludrocortisone are also discussed, each with distinct mechanisms and applications...
January 2024: Curēus
https://read.qxmd.com/read/38313499/correction-to-targeting-the-spike-repurposing-mithramycin-and-dihydroergotamine-to-block-sars-cov-2-infection
#19
Soledad Stagnoli, Gabriele Macari, Pietro Corsi, Barbara Capone, Ander Vidaurrazaga, June Ereño-Orbea, Ana Ardá, Fabio Polticelli, Jesus Jimenez-Barbero, Nicola Ga Abrescia, Ivan Coluzza
[This corrects the article DOI: 10.1021/acsomega.3c02921.].
January 30, 2024: ACS Omega
https://read.qxmd.com/read/38307660/status-migrainosus
#20
REVIEW
Salwa Kamourieh, Todd Rozen, Jane M Anderson
Status migrainosus is one of the recognized complications of migraine with or without aura, defined as a persistent debilitating migraine attack lasting for more than 72h with little reprieve, leading to functional disability. The individual impact of status migrainosus and the substantial healthcare burden are highlighted. Current case series which inform our understanding of this condition are examined with two groups emergent, those with classic status migrainosus and those with episodic status migrainosus...
2024: Handbook of Clinical Neurology
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