花生四烯酸代谢途径综述及几种具有COX-2抑制作用的杂环衍生物的最新进展

Q4 Pharmacology, Toxicology and Pharmaceutics
Swagatam Sahoo, Ragghee Bhattacharya, Manish Yadav, Debasis Sai Panda, Tunul Guria, Kirtimaya Mishra
{"title":"花生四烯酸代谢途径综述及几种具有COX-2抑制作用的杂环衍生物的最新进展","authors":"Swagatam Sahoo, Ragghee Bhattacharya, Manish Yadav, Debasis Sai Panda, Tunul Guria, Kirtimaya Mishra","doi":"10.25258/ijddt.13.3.49","DOIUrl":null,"url":null,"abstract":"Inflammation crucial part of the immune response associated with a broad range of immunological diseases. The arachidonic acid (AA) pathway, which is an essential inflammatory mediator present at the internal surface of the cellular matrix, is hydrolyzed by phospholipase A2, which leads to the development of metabolites such as cytochrome P450 (CYP), lipoxygenases (LOXs), cyclooxygenases (Coxs) and enzymes which further develops into bioactive mediators such as prostanoids, leukotrienes (LTs) and more. Cyclooxygenases produce prostaglandins, available as 2 isomorphs, COX-1(constitutive) & COX-2(inducible), targeted by NSAIDs used to treat inflammation. Yet, they have a number of negative effects that lead to market withdrawal. Research has been done to look at novel COX-2 inhibitors and safety precautions. By structural alteration at COX-2 strong receiving site, structural along with functional research on a number of selective COX-2 blockers results in the creation of novel structures that are more potent and selective against inflammation while having a very low risk of side effects. This is made possible by computer-assisted medication design. This review gives an explanation regarding the biological functionalization of several COX-2 derivatives obtained by the help of in vitro, in vivo & molecular docking for better understanding of the structures and bonding accountable for an action","PeriodicalId":13851,"journal":{"name":"International Journal of Drug Delivery Technology","volume":"43 1","pages":"0"},"PeriodicalIF":0.0000,"publicationDate":"2023-09-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"An Overview of Arachidonic Acid Metabolic Pathway and Recent Updates on a Few Heterocyclic Derivatives showing COX-2 Inhibition\",\"authors\":\"Swagatam Sahoo, Ragghee Bhattacharya, Manish Yadav, Debasis Sai Panda, Tunul Guria, Kirtimaya Mishra\",\"doi\":\"10.25258/ijddt.13.3.49\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"Inflammation crucial part of the immune response associated with a broad range of immunological diseases. The arachidonic acid (AA) pathway, which is an essential inflammatory mediator present at the internal surface of the cellular matrix, is hydrolyzed by phospholipase A2, which leads to the development of metabolites such as cytochrome P450 (CYP), lipoxygenases (LOXs), cyclooxygenases (Coxs) and enzymes which further develops into bioactive mediators such as prostanoids, leukotrienes (LTs) and more. Cyclooxygenases produce prostaglandins, available as 2 isomorphs, COX-1(constitutive) & COX-2(inducible), targeted by NSAIDs used to treat inflammation. Yet, they have a number of negative effects that lead to market withdrawal. Research has been done to look at novel COX-2 inhibitors and safety precautions. By structural alteration at COX-2 strong receiving site, structural along with functional research on a number of selective COX-2 blockers results in the creation of novel structures that are more potent and selective against inflammation while having a very low risk of side effects. This is made possible by computer-assisted medication design. This review gives an explanation regarding the biological functionalization of several COX-2 derivatives obtained by the help of in vitro, in vivo & molecular docking for better understanding of the structures and bonding accountable for an action\",\"PeriodicalId\":13851,\"journal\":{\"name\":\"International Journal of Drug Delivery Technology\",\"volume\":\"43 1\",\"pages\":\"0\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2023-09-25\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"International Journal of Drug Delivery Technology\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.25258/ijddt.13.3.49\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q4\",\"JCRName\":\"Pharmacology, Toxicology and Pharmaceutics\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"International Journal of Drug Delivery Technology","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.25258/ijddt.13.3.49","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"Pharmacology, Toxicology and Pharmaceutics","Score":null,"Total":0}
引用次数: 0

摘要

炎症是与广泛的免疫疾病相关的免疫反应的重要组成部分。花生四烯酸(AA)途径是存在于细胞基质内表面的重要炎症介质,被磷脂酶A2水解,导致代谢产物如细胞色素P450 (CYP)、脂氧合酶(LOXs)、环氧合酶(cox)和进一步发展为生物活性介质如前列腺素、白三烯(lt)等的酶的发展。环加氧酶产生前列腺素,有两种异构体:COX-1(组成型)和COX-1;COX-2(诱导型),被用于治疗炎症的非甾体抗炎药靶向。然而,它们有一些导致市场退出的负面影响。研究人员对新型COX-2抑制剂和安全预防措施进行了研究。通过改变COX-2强受体位点的结构,对一些选择性COX-2阻滞剂的结构和功能研究导致了新的结构的产生,这些结构更有效和选择性地抗炎症,同时具有非常低的副作用风险。这是通过计算机辅助药物设计实现的。本文综述了几种COX-2衍生物在体外和体内的生物功能化。分子对接可以更好地理解一个作用的结构和键合
本文章由计算机程序翻译,如有差异,请以英文原文为准。
An Overview of Arachidonic Acid Metabolic Pathway and Recent Updates on a Few Heterocyclic Derivatives showing COX-2 Inhibition
Inflammation crucial part of the immune response associated with a broad range of immunological diseases. The arachidonic acid (AA) pathway, which is an essential inflammatory mediator present at the internal surface of the cellular matrix, is hydrolyzed by phospholipase A2, which leads to the development of metabolites such as cytochrome P450 (CYP), lipoxygenases (LOXs), cyclooxygenases (Coxs) and enzymes which further develops into bioactive mediators such as prostanoids, leukotrienes (LTs) and more. Cyclooxygenases produce prostaglandins, available as 2 isomorphs, COX-1(constitutive) & COX-2(inducible), targeted by NSAIDs used to treat inflammation. Yet, they have a number of negative effects that lead to market withdrawal. Research has been done to look at novel COX-2 inhibitors and safety precautions. By structural alteration at COX-2 strong receiving site, structural along with functional research on a number of selective COX-2 blockers results in the creation of novel structures that are more potent and selective against inflammation while having a very low risk of side effects. This is made possible by computer-assisted medication design. This review gives an explanation regarding the biological functionalization of several COX-2 derivatives obtained by the help of in vitro, in vivo & molecular docking for better understanding of the structures and bonding accountable for an action
求助全文
通过发布文献求助,成功后即可免费获取论文全文。 去求助
来源期刊
International Journal of Drug Delivery Technology
International Journal of Drug Delivery Technology Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
0.70
自引率
0.00%
发文量
0
期刊介绍: International Journal of Drug Delivery Technology (IJDDT) provides the forum for reporting innovations, production methods, technologies, initiatives and the application of scientific knowledge to the aspects of pharmaceutics, including controlled drug release systems, drug targeting etc. in the form of expert forums, reviews, full research papers, and short communications.
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
copy
已复制链接
快去分享给好友吧!
我知道了
右上角分享
点击右上角分享
0
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:604180095
Book学术官方微信