keyword
https://read.qxmd.com/read/38484676/pro-inflammatory-enzyme-inhibition-of-lipoxygenases-by-flavonoid-rich-extract-from-artemisia-vulgaris
#1
JOURNAL ARTICLE
Jin Ru Lim, Lee Suan Chua, Azizul Azri Mustaffa
The peroxyl radicals generated by the activity of lipoxygenases (LOX) are mediators to trigger inflammatory diseases. Therefore, it is important to investigate potent LOX inhibitor for modulating the occurrence and resolving inflammatory processes. Artemisa vulgaris, is a herbal plant that is known for flavonoids, potentially inhibiting lipid peroxidation and scavenging radicals. The objectives of the present study were to obtain flavonoids rich extract from A. vulgaris, and determine the inhibitory mode of the extract against LOX...
March 10, 2024: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://read.qxmd.com/read/38466162/rapid-screening-and-isolation-of-5-lipoxygenase-inhibitors-in-inonotus-obliquus-and-mechanism-of-action-in-the-treatment-of-asthma
#2
JOURNAL ARTICLE
Haocheng Yun, Zhen Liu, Wanchao Hou, Qiang Liu, Yuyu Nong, Sainan Li, Chunming Liu
Accurate screening and targeted preparative isolation of active substances in natural medicines have long been two technical challenges in natural medicine research. This study outlines a new approach to improve the efficiency of natural product preparation, focusing on rapidly and accurately screening potential active ingredients in Inonotus obliquus as well as efficiently preparing 5-lipoxidase (5-LOX) inhibitors, to provide new ideas for the treatment of asthma with Inonotus obliquus. First, we used ultrafiltration (UF) mass spectrometry to screen for three potential inhibitors of 5-LOX in Inonotus obliquus...
March 2024: Journal of Separation Science
https://read.qxmd.com/read/38462728/antioxidant-constituents-from-ribes-glaciale-wall-bioassay-targeted-in-vitro-and-in-silico-evaluation
#3
JOURNAL ARTICLE
Rajendra Singh, Rohit Verma, Nitin Sati, Waseem Ahmad Ansari, Mohammad Faheem Khan
Bioassay targeted phyto-investigation of dried green walnut husk of Ribes glaciale Wall. yielded one new compound as β-D-glucopyrano (4'→3)-β-D-glucopyranose ( 1 ) and four known compounds namely scoparone ( 2 ), apigenin ( 3 ), β-sitosterol ( 4 ) and β-sitosterol-D-glucoside ( 5 ). The structure of new compound was elucidated with the help of 1D, 2D and HRESIMS analysis. The antioxidant activity of extract, fractions and pure were evaluated using 2, 2'-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) (ABTS), 2, 2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging and ferric ion reducing antioxidant power (FRAP) assays that found in the following order: butanol fr...
March 10, 2024: Natural Product Research
https://read.qxmd.com/read/38397818/formyl-peptide-receptor-2-dependent-cpla2-and-5-lox-activation-requires-a-functional-nadph-oxidase
#4
JOURNAL ARTICLE
Tiziana Pecchillo Cimmino, Iolanda Panico, Simona Scarano, Mariano Stornaiuolo, Gabriella Esposito, Rosario Ammendola, Fabio Cattaneo
Phospholipases (PL) A2 catalyzes the hydrolysis of membrane phospholipids and mostly generates arachidonic acid (AA). The enzyme 5-lipoxygenase (5-LOX) can metabolize AA to obtain inflammatory leukotrienes, whose biosynthesis highly depends on cPLA2 and 5-LOX activities. Formyl Peptide Receptor 2 (FPR2) belongs to a subfamily of class A GPCRs and is considered the most versatile FPRs isoform. Signaling triggered by FPR2 includes the activation of several downstream kinases and NADPH oxidase (NOX)-dependent ROS generation...
February 8, 2024: Antioxidants (Basel, Switzerland)
https://read.qxmd.com/read/38396917/conformational-dynamics-of-lipoxygenases-and-their-interaction-with-biological-membranes
#5
REVIEW
Fulvio Erba, Giampiero Mei, Velia Minicozzi, Annalaura Sabatucci, Almerinda Di Venere, Mauro Maccarrone
Lipoxygenases (LOXs) are a family of enzymes that includes different fatty acid oxygenases with a common tridimensional structure. The main functions of LOXs are the production of signaling compounds and the structural modifications of biological membranes. These features of LOXs, their widespread presence in all living organisms, and their involvement in human diseases have attracted the attention of the scientific community over the last decades, leading to several studies mainly focused on understanding their catalytic mechanism and designing effective inhibitors...
February 13, 2024: International Journal of Molecular Sciences
https://read.qxmd.com/read/38354820/integrated-analysis-and-separation-of-5-lipoxygenase-inhibitors-from-triterpenes-of-poria-cocos-using-bioaffinity-ultrafiltration-uplc-q-exactive-molecular-docking-and-target-based-multiple-complex-networks
#6
JOURNAL ARTICLE
Tong Wu, Wanchao Hou, Sainan Li, Chunming Liu, Yuchi Zhang
Poria cocos (Schw.) Wolf (P. cocos) has been widely used as medical plant in East Asia with remarkable anti-Alzheimer's disease (anti-AD) activity. However, the underlying mechanisms are still confused. In this study, based on the β-Amyloid deposition hypothesis of AD, an integrated analysis was conducted to screen and separation 5-lipoxygenase (5-LOX) inhibitors from triterpenoids of P. cocos and investigate the anti-AD mechanisms, containing bioaffinity ultrafiltration UPLC-Q-Exactive, molecular docking, and multiple complex networks...
February 12, 2024: Fitoterapia
https://read.qxmd.com/read/38347768/pharmacochemical-study-of-multitarget-amino-acids-hybrids-design-synthesis-in-vitro-and-in-silico-studies
#7
JOURNAL ARTICLE
Dimitra Hadjipavlou-Litina, Ioannis Fotopoulos, Eleni Pontiki
Neuro-inflammation is a complex phenomenon resulting in several disorders. ALOX-5, COX-2, pro-inflammatory enzymes, and amino acid neurotransmitters are tightly correlated to neuro- inflammatory pathologies. Developing drugs that interfere with these targets will offer treatment for various diseases. Herein, we extend our previous research by synthesizing a series of multitarget hybrids of cinnamic acids with amino acids recognized as neurotransmitters. The synthesis was based on an in silico study of a library of cinnamic amide hybrids with glycine, γ- aminobutyric, and L - glutamic acids...
February 9, 2024: Medicinal Chemistry
https://read.qxmd.com/read/38345035/integrated-computational-and-experimental-evaluation-of-phenolic-constituents-of-apricot-fruit-l-for-antiqourum-sensing-antibiofilm-antioxidant-and-15-lox-inhibitory-properties
#8
JOURNAL ARTICLE
Hafiz Abdul Rafey, Mohamed El-Shazly, Tooba Khalid, Tanveer Alam, Shah Iram Niaz, Omer Farooq
The present study investigated the antioxidant profile together with the antibacterial potential of Apricot L. with the aim to find a functional food based anti-infective lead. Additionally the study evaluated the biofilm and QS inhibitory potential of the plant using Pseudomonas aeruginosa (ATCC 15442) and Chromo bacterium Violaceum (DSM 30191) respectively. Several fractions of the peel of Apricot were subjected to initial antimicrobial and antibiofilm screening. Among all the fractions, methanol and ethyl acetate fractions displayed significant antimicrobial activity against the strains selected with MIC values 1...
February 12, 2024: Journal of Biomolecular Structure & Dynamics
https://read.qxmd.com/read/38315093/dual-cox-2-and-15-lox-inhibition-study-of-novel-4-arylidine-2-mercapto-1-phenyl-1h-imidazolidin-5-4h-ones-design-synthesis-docking-and-anti-inflammatory-activity
#9
JOURNAL ARTICLE
Nermine A Osman, Mostafa K Soltan, Samar Rezq, Joseph Flaherty, Damian G Romero, Ahmed S Abdelkhalek
Novel arylidene-5(4H)-imidazolone derivatives 4a-r were designed and evaluated as multidrug-directed ligands, that is, inflammatory, proinflammatory mediators, and reactive oxygen species (ROS) inhibitors. All of the tested compounds showed cyclooxygenase (COX)-1 inhibitory effect more than celecoxib and less than indomethacin and also demonstrated an improved inhibitory activity against 15-lipoxygenase (15-LOX). Compounds 4f, 4l, and 4p exhibited COX-2 selectivity comparable to that of celecoxib, while 4k was the most selective COX-2 inhibitor...
February 5, 2024: Archiv der Pharmazie
https://read.qxmd.com/read/38298631/anti-enzymatic-and-dna-docking-studies-of-montelukast-a-multifaceted-molecular-scaffold-with-in-vitro-investigations-molecular-expression-analysis-and-molecular-dynamics-simulations
#10
JOURNAL ARTICLE
Shawana Abdullah, Ambar Iqbal, Avinash Karkada Ashok, Farah Chafika Kaouche, Misbah Aslam, Safdar Hussain, Jameel Rahman, Muhammad Munawar Hayat, Muhammad Ashraf
Montelukast, an approved leukotriene receptor 1 (Cys-LT 1) antagonist with anti-inflammatory properties is used for the treatment of asthma and allergic rhinitis. In the present studies, montelukast was subjected to in vitro inhibitory assays followed by kinetic and in silico investigations. Montelukast demonstrated inhibitory activity against yeast α-glucosidase (IC50 44.31 ± 1.21 μM), jack bean urease (JB urease, IC50 8.72 ± 0.23 μM), human placental alkaline phosphatase (hPAP, IC50 17...
January 30, 2024: Heliyon
https://read.qxmd.com/read/38247498/-boesenbergia-rotunda-and-its-pinostrobin-for-atopic-dermatitis-dual-5-lipoxygenase-and-cyclooxygenase-2-inhibitor-and-its-mechanistic-study-through-steady-state-kinetics-and-molecular-modeling
#11
JOURNAL ARTICLE
Desy Liana, Chatchakorn Eurtivong, Anuchit Phanumartwiwath
Human 5-lipoxygenase (5-LOX) and cyclooxygenase-2 (COX-2) are potential targets for suppressing pruritic skin inflammation in atopic dermatitis (AD). In addition, Staphylococcus aureus colonization and oxidative stress worsen AD skin conditions. We aimed to investigate anti-inflammatory activity, using 5-LOX and COX-2 inhibitions, and the anti-staphylococcal, and antioxidant potentials of several medicinal plants bio-prospected from traditional medicine related to AD pathogenesis. Essential oils and hexane fractions were prepared and analyzed using gas chromatography-mass spectrometry...
January 5, 2024: Antioxidants (Basel, Switzerland)
https://read.qxmd.com/read/38151851/nordihydroguaiaretic-acid-affects-undifferentiated-and-differentiated-neuroblastoma-cells-differently-through-mechanisms-that-impact-on-cell-viability
#12
JOURNAL ARTICLE
Patricia Ferrera, César Espino De la Fuente-Muñoz, Clorinda Arias
AIM: We aimed to investigate the mechanisms involved in the neurotoxic effects of NDGA on differentiated and undifferentiated human neuroblastoma cells (MSN), assessing cell viability, changes in the actin cytoskeleton, cell migration and the expression of the 5-LOX enzyme and the inhibitor of cell cycle progression p21WAF1/CIP1. BACKGROUND: High expression and activity of the lipoxygenase enzyme (LOX) have been detected in several tumors, including neuroblastoma samples, suggesting the use of LOX inhibitors as potential therapy molecules...
December 26, 2023: CNS & Neurological Disorders Drug Targets
https://read.qxmd.com/read/38151349/-research-progress-in-drugs-targeting-5-lipoxygenase-for-age-related-diseases
#13
JOURNAL ARTICLE
Zhi-Jun Li, Yan-Hui Ma, Xi-Xi Hou, Tuan-Li Yao, Xiang-Yang Qin
With the acceleration of aging society, delaying aging or promoting healthy aging has become a major demand for human health. 5-Lipoxygenase (5-LOX) is a key enzyme catalyzing arachidonic acid into leukotrienes (LTs), which is a potent mediator of the inflammatory response. Previous studies showed that abnormal activation of 5-LOX and overproduction of LTs are closely related to the occurrence and development of aging-related inflammatory diseases. Therefore, inhibiting 5-LOX activation is a possibly potential strategy for treating age-related diseases...
December 25, 2023: Sheng Li Xue Bao: [Acta Physiologica Sinica]
https://read.qxmd.com/read/38145834/thirty-years-with-three-dimensional-structures-of-lipoxygenases
#14
REVIEW
Ernst H Oliw
The X-ray crystal structures of soybean lipoxygenase (LOX) and rabbit 15-LOX were reported in the 1990s. Subsequent 3D structures demonstrated a conserved U-like shape of the substrate cavities as reviewed here. The 8-LOX:arachidonic acid (AA) complex showed AA bound to the substrate cavity carboxylate-out with C10 at 3.4 Å from the iron metal center. A recent cryo-electron microscopy (EM) analysis of the 12-LOX:AA complex illustrated AA in the same position as in the 8-LOX:AA complex. The 15- and 12-LOX complexes with isoenzyme-specific inhibitors/substrate mimics confirmed the U-fold...
December 23, 2023: Archives of Biochemistry and Biophysics
https://read.qxmd.com/read/38145424/design-synthesis-and-pharmacological-evaluation-of-indazole-carboxamides-of-n-substituted-pyrrole-derivatives-as-soybean-lipoxygenase-inhibitors
#15
JOURNAL ARTICLE
Vasiliki Lavrentaki, Antonios Kousaxidis, Panagiotis Theodosis-Nobelos, Georgios Papagiouvannis, Konstantinos Koutsopoulos, Ioannis Nicolaou
In this paper, we attempted to develop a novel class of compounds against lipoxygenase, a key enzyme in the biosynthesis of leukotrienes implicated in a series of inflammatory diseases. Given the absence of appropriate human 5-lipoxygenase crystallographic data, solved soybean lipoxygenase-1 and -3 structures were used as a template to generate an accurate pharmacophore model which was further used for virtual screening purposes. Eight compounds (1-8) have been derived from the in-house library consisting of N-substituted pyrroles conjugated with 5- or 6-indazole moieties through a carboxamide linker...
December 25, 2023: Molecular Diversity
https://read.qxmd.com/read/38138448/development-of-novel-pyrrole-derivatives-and-their-cinnamic-hybrids-as-dual-cox-2-lox-inhibitors
#16
JOURNAL ARTICLE
Viola Noti, Eleni Pontiki, Dimitra Hadjipavlou-Litina
Molecular hybridization has emerged as a promising approach in the treatment of diseases exhibiting multifactorial etiology. With regard to this, dual cyclooxygenase-2/lipoxygenase (COX-2/LOX) inhibitors could be considered a safe alternative to traditional non-steroidal anti-inflammatory drugs (tNSAIDs) and selective COX-2 inhibitors (coxibs) for the treatment of inflammatory conditions. Taking this into account, six novel pyrrole derivatives and pyrrole-cinnamate hybrids were developed as potential COX-2 and soybean LOX (sLOX) inhibitors with antioxidant activity...
December 5, 2023: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://read.qxmd.com/read/38056389/molecular-hybrids-of-substituted-phenylcarbamoylpiperidine-and-1-2-4-triazole-methylacetamide-as-potent-15-lox-inhibitors-design-synthesis-dft-calculations-and-molecular-docking-studies
#17
JOURNAL ARTICLE
Zahid Nawaz, Naheed Riaz, Muhammad Saleem, Ambar Iqbal, Syeda Abida Ejaz, Bushra Bashir, Saima Muzaffar, Muhammad Ashraf, Aziz-Ur-Rehman, Muhammad Sajjad Bilal, Bala Krishna Prabhala, Salvia Sajid
Inflammation is a multifaceted phenomenon triggered by potentially active mediators acutely released arachidonic acid metabolites partially in lipoxygenase (LOX) pathway which are primarily accountable for causing several diseases in humans. It is widely believed that an inhibitor of the LOX pathway represents a rational approach for designing more potent antiinflammatory leads with druggable super safety profiles. In our continual efforts in search for anti-LOX molecules, the present work was to design a new series of N-alkyl/aralkyl/aryl derivatives (7a-o) of 4-phenyl-5-(1-phenylcarbamoylpiperidine)-4H-1,2,4-triazole-3-thiol which was commenced in seriate formation of phenylcarbamoyl derivative (1), hydrazide (2), semicarbazide (3) and 4-phenyl-5-(1-phenylcarbamoylpiperidine)-4H-1,2,4-triazole-3-thiol (4)...
November 23, 2023: Bioorganic Chemistry
https://read.qxmd.com/read/38025070/phytochemical-characterization-of-typha-domingensis-and-the-assessment-of-therapeutic-potential-using-in-vitro-and-in-vivo-biological-activities-and-in-silico-studies
#18
JOURNAL ARTICLE
Rizwana Dilshad, Kashif-Ur-Rehman Khan, Saeed Ahmad, Asif Ansari Shaik Mohammad, Asmaa E Sherif, Huma Rao, Maqsood Ahmad, Bilal Ahmad Ghalloo, M Yasmin Begum
Typha domingensis , a medicinal plant with significant traditional importance for curing various human diseases, has potentially bioactive compounds but was less explored previously. Therefore, this study aims to investigate the therapeutic potential of T. domingensis by evaluating the phytochemical profile through high-performance liquid chromatography (HPLC) techniques and its biological activities ( in vitro and in vivo ) from the methanolic extract derived from the entire plant (TDME). The secondary metabolite profile of TDME regulated by reverse phase ultra-high-performance liquid chromatography-mass spectrometry (RP-UHPLC-MS) revealed some bioactive compounds by -ve and +ve modes of ionization...
2023: Frontiers in Chemistry
https://read.qxmd.com/read/37993774/dna-methylation-and-lipid-metabolism-are-involved-in-ga-induced-maize-aleurone-layers-pcd-as-revealed-by-transcriptome-analysis
#19
JOURNAL ARTICLE
Yequn Wu, Jiaqi Hou, Ruifei Ren, Zhenfei Chen, Mengxia Yue, Le Li, Haoli Hou, Xueke Zheng, Lijia Li
BACKGROUND: The aleurone layer is a part of many plant seeds, and during seed germination, aleurone cells undergo PCD, which is promoted by GA from the embryo. However, the numerous components of the GA signaling pathway that mediate PCD of the aleurone layers remain to be identified. Few genes and transcriptomes have been studied thus far in aleurone layers to improve our understanding of how PCD occurs and how the regulatory mechanism functions during PCD. Our previous studies have shown that histone deacetylases (HDACs) are required in GA-induced PCD of aleurone layer...
November 22, 2023: BMC Plant Biology
https://read.qxmd.com/read/37985602/synthesis-molecular-docking-analgesic-anti-inflammatory-and-ulcerogenic-evaluation-of-thiophene-pyrazole-candidates-as-cox-5-lox-and-tnf-%C3%AE-inhibitors
#20
JOURNAL ARTICLE
M J Nagesh Khadri, Ramith Ramu, N Akshaya Simha, Shaukath Ara Khanum
The thiophene bearing pyrazole derivatives (7a-j) were synthesized and examined for their in vitro cyclooxygenase, 5-lipoxygenase, and tumour inducing factor-α inhibitory activities followed by the in vivo analgesic, anti-inflammatory, and ulcerogenic evaluations. The synthesized series (7a-j) were characterized using 1 H NMR, 13 C NMR, FT-IR, and mass spectral analysis. Initially, the compounds (7a-j) were evaluated for their in vitro cyclooxygenase, 5-lipoxygenase, and tumour inducing factor-α inhibitory activities and the compound (7f) with two phenyl substituents in the pyrazole ring and chloro substituent in the thiophene ring and the compound (7g) with two phenyl substituents in the pyrazole ring and bromo substituent in the thiophene ring were observed as potent compounds among the series...
November 20, 2023: Inflammopharmacology
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