Kojic acid-derived tyrosinase inhibitors: synthesis and bioactivity
Tyrosinase is a key enzyme for melanin biosynthesis, catalyzing the oxidation of L-tyrosine to L-dopaquinone. The tyrosinase inhibition is an effective approach to control hyperpigmentation in human skin and enzymatic browning in fruits and vegetables. Kojic acid is a naturally-occurring tyrosinase...
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| Format: | Article |
| Language: | English |
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Mazandaran University of Medical Sciences
2015-01-01
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| Series: | Pharmaceutical and Biomedical Research |
| Subjects: | |
| Online Access: | http://pbr.mazums.ac.ir/browse.php?a_code=A-10-26-1&slc_lang=en&sid=1 |
| _version_ | 1818974552289443840 |
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| author | Seyedeh Mahdieh Hashemi Saeed Emami |
| author_facet | Seyedeh Mahdieh Hashemi Saeed Emami |
| author_sort | Seyedeh Mahdieh Hashemi |
| collection | DOAJ |
| description | Tyrosinase is a key enzyme for melanin biosynthesis, catalyzing the oxidation of L-tyrosine to L-dopaquinone. The tyrosinase inhibition is an effective approach to control hyperpigmentation in human skin and enzymatic browning in fruits and vegetables. Kojic acid is a naturally-occurring tyrosinase inhibitor which has been clinically used to treat the hyperpigmentation of skin. However, kojic acid as a hydrophilic small-molecule has insufficient inhibitory activity and stability, with considerable toxicity. To overcome these drawbacks, synthetic derivatives of kojic acid were developed, which exhibited enhanced tyrosinase inhibitory activity and more favorable stability relative to kojic acid. In this context, the synthesis and biological activity of kojic acid derivatives as tyrosinase inhibitors have been highlighted. |
| first_indexed | 2024-12-20T15:41:52Z |
| format | Article |
| id | doaj.art-9e686aa7da674451b60009f4e84a3cdf |
| institution | Directory Open Access Journal |
| issn | 2423-4486 2423-4494 |
| language | English |
| last_indexed | 2024-12-20T15:41:52Z |
| publishDate | 2015-01-01 |
| publisher | Mazandaran University of Medical Sciences |
| record_format | Article |
| series | Pharmaceutical and Biomedical Research |
| spelling | doaj.art-9e686aa7da674451b60009f4e84a3cdf2022-12-21T19:35:10ZengMazandaran University of Medical SciencesPharmaceutical and Biomedical Research2423-44862423-44942015-01-0111117Kojic acid-derived tyrosinase inhibitors: synthesis and bioactivitySeyedeh Mahdieh Hashemi0Saeed Emami1 Department of Medicinal Chemistry and Pharmaceutical Sciences Research Center, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran Department of Medicinal Chemistry, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran Tyrosinase is a key enzyme for melanin biosynthesis, catalyzing the oxidation of L-tyrosine to L-dopaquinone. The tyrosinase inhibition is an effective approach to control hyperpigmentation in human skin and enzymatic browning in fruits and vegetables. Kojic acid is a naturally-occurring tyrosinase inhibitor which has been clinically used to treat the hyperpigmentation of skin. However, kojic acid as a hydrophilic small-molecule has insufficient inhibitory activity and stability, with considerable toxicity. To overcome these drawbacks, synthetic derivatives of kojic acid were developed, which exhibited enhanced tyrosinase inhibitory activity and more favorable stability relative to kojic acid. In this context, the synthesis and biological activity of kojic acid derivatives as tyrosinase inhibitors have been highlighted.http://pbr.mazums.ac.ir/browse.php?a_code=A-10-26-1&slc_lang=en&sid=1Kojic acid 4H-pyran-4-one derivatives enzyme inhibitors structural modifications |
| spellingShingle | Seyedeh Mahdieh Hashemi Saeed Emami Kojic acid-derived tyrosinase inhibitors: synthesis and bioactivity Pharmaceutical and Biomedical Research Kojic acid 4H-pyran-4-one derivatives enzyme inhibitors structural modifications |
| title | Kojic acid-derived tyrosinase inhibitors: synthesis and bioactivity |
| title_full | Kojic acid-derived tyrosinase inhibitors: synthesis and bioactivity |
| title_fullStr | Kojic acid-derived tyrosinase inhibitors: synthesis and bioactivity |
| title_full_unstemmed | Kojic acid-derived tyrosinase inhibitors: synthesis and bioactivity |
| title_short | Kojic acid-derived tyrosinase inhibitors: synthesis and bioactivity |
| title_sort | kojic acid derived tyrosinase inhibitors synthesis and bioactivity |
| topic | Kojic acid 4H-pyran-4-one derivatives enzyme inhibitors structural modifications |
| url | http://pbr.mazums.ac.ir/browse.php?a_code=A-10-26-1&slc_lang=en&sid=1 |
| work_keys_str_mv | AT seyedehmahdiehhashemi kojicacidderivedtyrosinaseinhibitorssynthesisandbioactivity AT saeedemami kojicacidderivedtyrosinaseinhibitorssynthesisandbioactivity |