Synthesis, biological evaluation and docking studies of aurone derivatives on Xanthine oxidase enzyme
Inhibition of xanthine oxidase (XO) activity is an effective therapeutic approach for the treatment of diseases such as gout and hyperuricemia. Additionally, the use of XO inhibitors can further be extended to injury treatments such as ischemic reperfusion in various organs such as heart, liver and...
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iium-742162019-09-19T07:12:26Z http://irep.iium.edu.my/74216/ Synthesis, biological evaluation and docking studies of aurone derivatives on Xanthine oxidase enzyme Rullah, Kamal Khye, Saw Phin Ang, Serene Mohd Aluwi, Mohd Fadhlizil Fasihi Lam, Kok Wai RS403 Materia Medica-Pharmaceutical Chemistry Inhibition of xanthine oxidase (XO) activity is an effective therapeutic approach for the treatment of diseases such as gout and hyperuricemia. Additionally, the use of XO inhibitors can further be extended to injury treatments such as ischemic reperfusion in various organs such as heart, liver and kidney. In this study, 7 aurone compounds were synthesized and tested on XO and compared with the positive control allopurinol. Compound 5e was identified as the most potent compound and was able to inhibit half of XO activity at 33.23 μM followed by compounds 5f and 5d at 210.22 μM and 302.0 μM, respectively. Finally, molecular docking study was conducted to understand the important binding interactions of the selected aurone with the active site of XO. UKM Press 2018 Article PeerReviewed application/pdf ms http://irep.iium.edu.my/74216/1/Kamal%20Rullah%2016.pdf Rullah, Kamal and Khye, Saw Phin and Ang, Serene and Mohd Aluwi, Mohd Fadhlizil Fasihi and Lam, Kok Wai (2018) Synthesis, biological evaluation and docking studies of aurone derivatives on Xanthine oxidase enzyme. Jurnal Sains Kesihatan Malaysia (JSKM), 16 (1). pp. 135-143. ISSN 2289-4535 http://ejournal.ukm.my/jskm/article/view/18825/7406 10.17576/JSKM-2018-1601-17 |
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RS403 Materia Medica-Pharmaceutical Chemistry Rullah, Kamal Khye, Saw Phin Ang, Serene Mohd Aluwi, Mohd Fadhlizil Fasihi Lam, Kok Wai Synthesis, biological evaluation and docking studies of aurone derivatives on Xanthine oxidase enzyme |
description |
Inhibition of xanthine oxidase (XO) activity is an effective therapeutic approach for the treatment of diseases such as gout and hyperuricemia. Additionally, the use of XO inhibitors can further be extended to injury treatments such as ischemic reperfusion in various organs such as heart, liver and kidney. In this study, 7 aurone compounds were synthesized and tested on XO and compared with the positive control allopurinol. Compound 5e was identified as the most potent compound and was able to inhibit half of XO activity at 33.23 μM followed by compounds 5f and 5d at 210.22 μM and 302.0 μM, respectively. Finally, molecular docking study was conducted to understand the important binding interactions of the selected aurone with the active site of XO. |
format |
Article |
author |
Rullah, Kamal Khye, Saw Phin Ang, Serene Mohd Aluwi, Mohd Fadhlizil Fasihi Lam, Kok Wai |
author_facet |
Rullah, Kamal Khye, Saw Phin Ang, Serene Mohd Aluwi, Mohd Fadhlizil Fasihi Lam, Kok Wai |
author_sort |
Rullah, Kamal |
title |
Synthesis, biological evaluation and docking studies of aurone derivatives on Xanthine oxidase enzyme |
title_short |
Synthesis, biological evaluation and docking studies of aurone derivatives on Xanthine oxidase enzyme |
title_full |
Synthesis, biological evaluation and docking studies of aurone derivatives on Xanthine oxidase enzyme |
title_fullStr |
Synthesis, biological evaluation and docking studies of aurone derivatives on Xanthine oxidase enzyme |
title_full_unstemmed |
Synthesis, biological evaluation and docking studies of aurone derivatives on Xanthine oxidase enzyme |
title_sort |
synthesis, biological evaluation and docking studies of aurone derivatives on xanthine oxidase enzyme |
publisher |
UKM Press |
publishDate |
2018 |
url |
http://irep.iium.edu.my/74216/ http://irep.iium.edu.my/74216/ http://irep.iium.edu.my/74216/ http://irep.iium.edu.my/74216/1/Kamal%20Rullah%2016.pdf |
first_indexed |
2023-09-18T21:45:08Z |
last_indexed |
2023-09-18T21:45:08Z |
_version_ |
1777413399275110400 |