scispace - formally typeset
Search or ask a question
Author

Veena Kumari Vidya Rajan

Bio: Veena Kumari Vidya Rajan is an academic researcher from Shanmugha Arts, Science, Technology & Research Academy. The author has contributed to research in topics: Isozyme & Enzyme. The author has an hindex of 1, co-authored 1 publications receiving 28 citations.
Topics: Isozyme, Enzyme

Papers
More filters
Journal ArticleDOI
TL;DR: It has been identified that aliphatic and aromatic interactions are the most common in all the enzymes and in addition interactions unique to each one of these enzymes were identified.
Abstract: Cyclooxygenase (COXs) and Lipoxygenase (LOXs) pathways are the two major enzymatic pathways in arachidonic acid (AA) metabolism. The term eicosanoid is used to describe biologically active lipid mediators including prostaglandins, thromboxanes, leukotrienes and other oxygenated derivatives, which are produced primarily from AA. Eicosanoids generated in a tissue specific manner play a key role in inflammation and cancer. As AA is the substrate common to variety of COXs and LOXs, inhibition of one pathway results in diversion of the substrate to other pathways, which often is responsible for undesirable side effects. Hence there is need for development of not only isozyme specific inhibitors but also dual/multi enzyme inhibitors. Understanding the interactions of AA and characterizing its binding sites in these enzymes therefore is crucial for developing enzyme specific and multi enzyme inhibitors for enhancing therapeutic efficacy and/or overcoming side effects. AA binding sites in COXs and LOXs are identified and compared by the development of receptor based pharmacophore using MultiBind. Physico chemical properties were compared to understand the details of the binding sites in all the enzymes and to elucidate important amino acids that can be targeted for drug design. The alignment of AA binding sites in the seven enzymes COX-1, COX-2, 5-LOX, 12-LOX, 15-LOX and plant soybean LOX-1 and LOX-3 indicated a common pattern of five common interacting groups. In the same way, comparison of AA binding sites was done pair wise and by multiple alignment in various combinations. It has been identified that aliphatic and aromatic interactions are the most common in all the enzymes. In addition interactions unique to each one of these enzymes were identified. The complete analysis of AA binding sites in the seven enzymes was performed; 120 combinations for the seven enzymes were studied in detail. All the seven enzymes are structurally quite different, yet they share AA as the common binding partner. Comparisons in various combinations showed how they are similar and dissimilar with each other. This information will be helpful in designing specific as well as common inhibitors.

36 citations


Cited by
More filters
Journal ArticleDOI
TL;DR: Seven coumarin derivatives synthesized using various aromatic and heterocyclic amines were evaluated in vivo for anti-inflammatory and analgesic activity, and for ulcerogenic risk, and revealed that compound 33 and 35 are the most potent compounds in all the screening methods.

61 citations

Journal ArticleDOI
TL;DR: A series of newly synthesized 4-aryl-hydrazonopyrazolones were designed and their structures were confirmed by spectral and elemental analyses to explore the most active compounds, ulcerogenic effect on stomach in comparison with indomethacin and celecoxib in addition to histopathological investigations.

59 citations

Journal ArticleDOI
TL;DR: In silico, in vivo, and in vitro findings suggested that the synthesized indolizine compound 56 has a dual COX-2 and LOX inhibition characteristic and parallel in vivo anti-inflammatory activity in comparison to the standard drugs.

43 citations

Journal ArticleDOI
TL;DR: In this article, the role of arachidonic acid (AA) metabolism in cardiovascular health and disease as well as their potential therapeutic implication is reviewed, including the role played by different AA metabolites in the modulation of vascular tone and cardiovascular complications.
Abstract: Arachidonic acid (AA) is an essential fatty acid that is released by phospholipids in cell membranes and metabolized by cyclooxygenase (COX), cytochrome P450 (CYP) enzymes, and lipid oxygenase (LOX) pathways to regulate complex cardiovascular function under physiological and pathological conditions. Various AA metabolites include prostaglandins, prostacyclin, thromboxanes, hydroxyeicosatetraenoic acids, leukotrienes, lipoxins, and epoxyeicosatrienoic acids. The AA metabolites play important and differential roles in the modulation of vascular tone, and cardiovascular complications including atherosclerosis, hypertension, and myocardial infarction upon actions to different receptors and vascular beds. This article reviews the roles of AA metabolism in cardiovascular health and disease as well as their potential therapeutic implication.

33 citations

Journal ArticleDOI
TL;DR: In this paper, 41 hybrid compounds containing diaryl-1,5-diazole and morpholine structures acting as dual COX-2/5-LOX inhibitors have been designed, synthesized and biologically evaluated.

26 citations