Article ; Online: Lipoxygenase inhibitory synthetic derivatives of methyl gallate regulate gene expressions of COX-2 and cytokines to reduce animal model arthritis.
2023 Volume 13, Issue 1, Page(s) 10644
Abstract: Mammalian lipoxygenases (LOXs) are involved in the biosynthesis of mediators of anaphylactic reactions and have been implicated in cell maturation, the pathogenesis of bronchial asthma, atherosclerosis, rheumatoid arthritis, cardiovascular diseases, ... ...
Abstract | Mammalian lipoxygenases (LOXs) are involved in the biosynthesis of mediators of anaphylactic reactions and have been implicated in cell maturation, the pathogenesis of bronchial asthma, atherosclerosis, rheumatoid arthritis, cardiovascular diseases, Alzheimer's disease and osteoporosis. Hence LOX inhibition in chronic conditions can lead to reducing the disease progression, which can be a good target for treating these diseases. The present study deals with designing methyl gallate derivatives and their anti-inflammatory effect by in silico, in vitro and in vivo methods. Designed derivatives were docked against LOX enzyme, and molecular dynamic simulations were carried out. Following the synthesis of derivatives, in vitro LOX inhibition assay, enzyme kinetics and fluorescence quenching studies were performed. One of the derivatives of methyl gallate (MGSD 1) was demonstrated as an anti-inflammatory agent for the treatment of rheumatoid arthritis in the animal model. Amelioration of Freund's complete adjuvant (FCA)-induced arthritis by methyl gallate and its derivative with a concentration of 10-40 mg.kg |
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MeSH term(s) | Animals ; Cytokines ; Lipoxygenase ; Cyclooxygenase 2/genetics ; Tumor Necrosis Factor-alpha ; Diclofenac ; Arthritis, Rheumatoid ; Lipoxygenases ; Gene Expression ; Mammals |
Chemical Substances | Cytokines ; Lipoxygenase (EC 1.13.11.12) ; Cyclooxygenase 2 (EC 1.14.99.1) ; Tumor Necrosis Factor-alpha ; methyl gallate (623D3XG80C) ; Diclofenac (144O8QL0L1) ; Lipoxygenases (EC 1.13.11.-) |
Language | English |
Publishing date | 2023-06-30 |
Publishing country | England |
Document type | Journal Article |
ZDB-ID | 2615211-3 |
ISSN | 2045-2322 ; 2045-2322 |
ISSN (online) | 2045-2322 |
ISSN | 2045-2322 |
DOI | 10.1038/s41598-023-37613-z |
Database | MEDical Literature Analysis and Retrieval System OnLINE |
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