Inotilone and related phenylpropanoid polyketides from Inonotus sp. and their identification as potent COX and XO inhibitors

Arthritis is a general term for severe inflammatory processes in joints or joint tissue. Nonsteroidal anti-inflammatory drugs , such as diclofenac and indomethacin, have emerged the most commonly used anti- inflammatory agents for the therapy of rheumatoid arthritis. Many of these drugs target cyclo...

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Main Authors: V. Kemami Wangun, Hilaire, Hartl, Albert, Trinh Tam, Kiet, Hertweck, Christian
Format: Article
Language:English
Published: Organic & Biomolecular Chemistry 2016
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Online Access:http://repository.vnu.edu.vn/handle/VNU_123/10561
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Institution: Vietnam National University, Hanoi
Language: English
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spelling oai:112.137.131.14:VNU_123-105612017-04-05T14:10:31Z Inotilone and related phenylpropanoid polyketides from Inonotus sp. and their identification as potent COX and XO inhibitors V. Kemami Wangun, Hilaire Hartl, Albert Trinh Tam, Kiet Hertweck, Christian cyclooxygenases (COX) xanthine oxidase (OX) new anti- inflammatory anti- arthritic therapeutics mushroom Inonotus Arthritis is a general term for severe inflammatory processes in joints or joint tissue. Nonsteroidal anti-inflammatory drugs , such as diclofenac and indomethacin, have emerged the most commonly used anti- inflammatory agents for the therapy of rheumatoid arthritis. Many of these drugs target cyclooxygenases (COX), which catalyze the first two steps in the biosynthesis of the prostaglandins from the substrate arachidonic acid. In this context, the selective inhibition of enzyme subtypes, COX-1 and COX-2, has become an important goal. In contrast to rheumatoid arthritis, gouty arthritis is mediated by the crystallisation of uric acid (UA) in the joints. Gout can be treated with drugs that either increase the urinary excretion of UA, or with xanthine oxidase (OX) inhibitors that block the terminal step of UA biosynthesis. The purine analogue allopurinnol is currently the only XO inhibitor in clinical use. Unfortunately, it seems to be associated with an infrequently but severe hypersensitivity. Thus, the search for new potent inhibitors of these enzymes, which could be useful as lead structures for new anti- inflammatory and anti- arthritic therapeutics, plays a pivotal role. Here we report on the isolation, structural elucidation and biological evaluation of natural anti- inflammatory COX and XO inhibitors from the mushroom Inonotus sp. 2016-05-23T09:32:17Z 2016-05-23T09:32:17Z 2006-05-09 Article 1447-0539 http://repository.vnu.edu.vn/handle/VNU_123/10561 en Organic & Biomolecular Chemistry;4 application/pdf Organic & Biomolecular Chemistry
institution Vietnam National University, Hanoi
building VNU Library & Information Center
country Vietnam
collection VNU Digital Repository
language English
topic cyclooxygenases (COX)
xanthine oxidase (OX)
new anti- inflammatory
anti- arthritic therapeutics
mushroom Inonotus
spellingShingle cyclooxygenases (COX)
xanthine oxidase (OX)
new anti- inflammatory
anti- arthritic therapeutics
mushroom Inonotus
V. Kemami Wangun, Hilaire
Hartl, Albert
Trinh Tam, Kiet
Hertweck, Christian
Inotilone and related phenylpropanoid polyketides from Inonotus sp. and their identification as potent COX and XO inhibitors
description Arthritis is a general term for severe inflammatory processes in joints or joint tissue. Nonsteroidal anti-inflammatory drugs , such as diclofenac and indomethacin, have emerged the most commonly used anti- inflammatory agents for the therapy of rheumatoid arthritis. Many of these drugs target cyclooxygenases (COX), which catalyze the first two steps in the biosynthesis of the prostaglandins from the substrate arachidonic acid. In this context, the selective inhibition of enzyme subtypes, COX-1 and COX-2, has become an important goal. In contrast to rheumatoid arthritis, gouty arthritis is mediated by the crystallisation of uric acid (UA) in the joints. Gout can be treated with drugs that either increase the urinary excretion of UA, or with xanthine oxidase (OX) inhibitors that block the terminal step of UA biosynthesis. The purine analogue allopurinnol is currently the only XO inhibitor in clinical use. Unfortunately, it seems to be associated with an infrequently but severe hypersensitivity. Thus, the search for new potent inhibitors of these enzymes, which could be useful as lead structures for new anti- inflammatory and anti- arthritic therapeutics, plays a pivotal role. Here we report on the isolation, structural elucidation and biological evaluation of natural anti- inflammatory COX and XO inhibitors from the mushroom Inonotus sp.
format Article
author V. Kemami Wangun, Hilaire
Hartl, Albert
Trinh Tam, Kiet
Hertweck, Christian
author_facet V. Kemami Wangun, Hilaire
Hartl, Albert
Trinh Tam, Kiet
Hertweck, Christian
author_sort V. Kemami Wangun, Hilaire
title Inotilone and related phenylpropanoid polyketides from Inonotus sp. and their identification as potent COX and XO inhibitors
title_short Inotilone and related phenylpropanoid polyketides from Inonotus sp. and their identification as potent COX and XO inhibitors
title_full Inotilone and related phenylpropanoid polyketides from Inonotus sp. and their identification as potent COX and XO inhibitors
title_fullStr Inotilone and related phenylpropanoid polyketides from Inonotus sp. and their identification as potent COX and XO inhibitors
title_full_unstemmed Inotilone and related phenylpropanoid polyketides from Inonotus sp. and their identification as potent COX and XO inhibitors
title_sort inotilone and related phenylpropanoid polyketides from inonotus sp. and their identification as potent cox and xo inhibitors
publisher Organic & Biomolecular Chemistry
publishDate 2016
url http://repository.vnu.edu.vn/handle/VNU_123/10561
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