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Molecular Docking studies of Novel Flavones as Cyclooxygenase- 2 (Cox 2) Inhibitors
| Content Provider | Semantic Scholar |
|---|---|
| Author | Tendulkar, Reshma N. Mahajan, Supriya S. Shah, C. U. |
| Copyright Year | 2014 |
| Abstract | INTRODUCTION Cyclooxygenase (COX) is an enzyme that is responsible for the formation of prostanoids. The three main groups of prostanoids -prostaglandins, prostacyclins, and thromboxanes are each involved in the inflammatory response. [1] In the 1990s, researchers discovered that two different COX enzymes existed, now known as COX-1 and COX-2. Cyclooxygenase-1 (COX-1) is known to be present in most tissues. In the gastrointestinal tract, COX-1 maintains the normal lining of the stomach. The enzyme is also involved in kidney and platelet function. Cyclooxygenase-2 (COX-2) is present at sites of inflammation. [2] While both COX-1 and COX-2 convert arachidonic acid to prostaglandin, resulting in pain and inflammation; their other functions make inhibition of COX-1 undesirable while inhibition of COX-2 is considered desirable. Nonsteroidal anti-inflammatory drugs (NSAIDs), commonly prescribed to treat arthritis, work by inhibiting prostaglandins. [3] Traditional NSAIDs (Ibuprofen, Naproxen), however, can cause gastrointestinal problems including ulcers. Traditional NSAIDs are considered nonselective because they inhibit both COX-1 and COX-2. The inhibition of COX-2 by traditional NSAIDs accounts for the antiinflammatory effect of the drugs while the inhibition of COX-1 can lead to NSAIDs toxicity and associated side effects (ulcers, prolonged bleeding time, kidney problems). [3] Flavones are the compounds belong to a widely distributed group of natural products called flavonoids with a variety of pharmacological activities including antioxidant, anticancer and antiinflammatory activities. The anti-inflammatory activity is reported due to inhibition of lipooxygenase by the flavones. [4-5] Flavones are also known to suppress COX-2 transcription. [6] Literature reports that the anti-inflammatory and the anticancer activities of the flavones may be related to each other in view of the overexpression of COX-2 in some types of cancers. [7] In view of these literature findings, we decided to dock a series of flavones into the active site of COX-2 and study the binding pattern. Luteolin is a compound showing COX-2 inhibitory activity, [8] consisting of flavone moiety and SC-558 is selective Research Article |
| File Format | PDF HTM / HTML |
| Alternate Webpage(s) | http://www.speronline.com/japer/Articlefile/246.pdf |
| Language | English |
| Access Restriction | Open |
| Content Type | Text |
| Resource Type | Article |
