Potent halogenated xanthone derivatives: synthesis, molecular docking and study on antityrosinase activity

Tyrosinase inhibitors can reduce melanin production for skin whitening, but some existing products may harm the skin. This study discovered six compounds that inhibit tyrosinase in the mushroom Agaricus bisporus by over 50%. Compound 11 displayed strong inhibition (92.2% and 86.7%) for L-tyrosine an...

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Main Authors: Baharuddin, Fatin Farhana, Mad Nasir, Nadiah, Tejo, Bimo Ario, Koh, Soo Peng, Ramakrishnan, Shuruti, Nordin, Nur Qurratu Ain A., Adzahar, Anis Nasuha, Devakrishnan, Pavithren, Mohd Razib, Salsabiilaa
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Published: Taylor and Francis Group 2023
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spelling oai:psasir.upm.edu.my:108720 http://psasir.upm.edu.my/id/eprint/108720/ Potent halogenated xanthone derivatives: synthesis, molecular docking and study on antityrosinase activity Baharuddin, Fatin Farhana Mad Nasir, Nadiah Tejo, Bimo Ario Koh, Soo Peng Ramakrishnan, Shuruti Nordin, Nur Qurratu Ain A. Adzahar, Anis Nasuha Devakrishnan, Pavithren Mohd Razib, Salsabiilaa Tyrosinase inhibitors can reduce melanin production for skin whitening, but some existing products may harm the skin. This study discovered six compounds that inhibit tyrosinase in the mushroom Agaricus bisporus by over 50%. Compound 11 displayed strong inhibition (92.2% and 86.7%) for L-tyrosine and L-DOPA substrates, while compound 13 showed high inhibition (96.0% and 62.0%) for both substrates. Molecular docking simulations revealed compounds 11 and 13 bind at the allosteric site of the enzyme. Xanthone derivatives, based on these findings, hold potential as safe skin whitening agents and for pigmentation-related diseases in the cosmetic industry. Taylor and Francis Group 2023-10-05 Article PeerReviewed Baharuddin, Fatin Farhana and Mad Nasir, Nadiah and Tejo, Bimo Ario and Koh, Soo Peng and Ramakrishnan, Shuruti and Nordin, Nur Qurratu Ain A. and Adzahar, Anis Nasuha and Devakrishnan, Pavithren and Mohd Razib, Salsabiilaa (2023) Potent halogenated xanthone derivatives: synthesis, molecular docking and study on antityrosinase activity. Journal of Asian Natural Products Research, 26 (5). pp. 575-582. ISSN 1028-6020; ESSN: 1477-2213 https://www.tandfonline.com/doi/full/10.1080/10286020.2023.2264784 10.1080/10286020.2023.2264784
institution UPM IR
collection UPM IR
description Tyrosinase inhibitors can reduce melanin production for skin whitening, but some existing products may harm the skin. This study discovered six compounds that inhibit tyrosinase in the mushroom Agaricus bisporus by over 50%. Compound 11 displayed strong inhibition (92.2% and 86.7%) for L-tyrosine and L-DOPA substrates, while compound 13 showed high inhibition (96.0% and 62.0%) for both substrates. Molecular docking simulations revealed compounds 11 and 13 bind at the allosteric site of the enzyme. Xanthone derivatives, based on these findings, hold potential as safe skin whitening agents and for pigmentation-related diseases in the cosmetic industry.
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author Baharuddin, Fatin Farhana
Mad Nasir, Nadiah
Tejo, Bimo Ario
Koh, Soo Peng
Ramakrishnan, Shuruti
Nordin, Nur Qurratu Ain A.
Adzahar, Anis Nasuha
Devakrishnan, Pavithren
Mohd Razib, Salsabiilaa
spellingShingle Baharuddin, Fatin Farhana
Mad Nasir, Nadiah
Tejo, Bimo Ario
Koh, Soo Peng
Ramakrishnan, Shuruti
Nordin, Nur Qurratu Ain A.
Adzahar, Anis Nasuha
Devakrishnan, Pavithren
Mohd Razib, Salsabiilaa
Potent halogenated xanthone derivatives: synthesis, molecular docking and study on antityrosinase activity
author_facet Baharuddin, Fatin Farhana
Mad Nasir, Nadiah
Tejo, Bimo Ario
Koh, Soo Peng
Ramakrishnan, Shuruti
Nordin, Nur Qurratu Ain A.
Adzahar, Anis Nasuha
Devakrishnan, Pavithren
Mohd Razib, Salsabiilaa
author_sort Baharuddin, Fatin Farhana
title Potent halogenated xanthone derivatives: synthesis, molecular docking and study on antityrosinase activity
title_short Potent halogenated xanthone derivatives: synthesis, molecular docking and study on antityrosinase activity
title_full Potent halogenated xanthone derivatives: synthesis, molecular docking and study on antityrosinase activity
title_fullStr Potent halogenated xanthone derivatives: synthesis, molecular docking and study on antityrosinase activity
title_full_unstemmed Potent halogenated xanthone derivatives: synthesis, molecular docking and study on antityrosinase activity
title_sort potent halogenated xanthone derivatives: synthesis, molecular docking and study on antityrosinase activity
publisher Taylor and Francis Group
publishDate 2023
_version_ 1819301821765648384
score 13.4562235