{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,25]],"date-time":"2026-09-25T06:26:30Z","timestamp":1790317590693,"version":"4.1.0"},"reference-count":39,"publisher":"Wiley","issue":"9","license":[{"start":{"date-parts":[[2017,8,11]],"date-time":"2017-08-11T00:00:00Z","timestamp":1502409600000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"funder":[{"DOI":"10.13039\/501100003663","name":"Small and Medium Business Administration","doi-asserted-by":"publisher","award":["C0036335"],"award-info":[{"award-number":["C0036335"]}],"id":[{"id":"10.13039\/501100003663","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Chemistry &amp; Biodiversity"],"published-print":{"date-parts":[[2017,9]]},"abstract":"<jats:p>Melanin is the major factor that determines skin color and protects from ultraviolet radiation. In present study we evaluated the anti\u2010melanogenesis effect of acetazolamide (<jats:styled-content style=\"fixed-case\">ACZ<\/jats:styled-content>) using four different approaches: enzyme kinetic, <jats:italic>in\u00a0vitro<\/jats:italic>,<jats:italic> in\u00a0vivo<\/jats:italic> and <jats:italic>in silico<\/jats:italic>. <jats:styled-content style=\"fixed-case\">ACZ<\/jats:styled-content> demonstrated significant inhibitory activity (<jats:italic><jats:styled-content style=\"fixed-case\">IC<\/jats:styled-content><\/jats:italic><jats:sub>50<\/jats:sub> 7.895\u00a0\u00b1\u00a00.24\u00a0\u03bc<jats:sc>m<\/jats:sc>) against tyrosinase as compared to the standard drug kojic acid (<jats:italic><jats:styled-content style=\"fixed-case\">IC<\/jats:styled-content><\/jats:italic><jats:sub>50<\/jats:sub> 16.84\u00a0\u00b1\u00a00.64\u00a0\u03bc<jats:sc>m<\/jats:sc>) and kinetic analyses showed that <jats:styled-content style=\"fixed-case\">ACZ<\/jats:styled-content> is a non\u2010competitive inhibitor without cytotoxic effect. In <jats:italic>in\u00a0vitro<\/jats:italic> experiments, A375 human melanoma cells were treated with 20 or 40\u00a0\u03bc<jats:sc>m<\/jats:sc> of <jats:styled-content style=\"fixed-case\">ACZ<\/jats:styled-content> with or without 50\u00a0\u03bc<jats:sc>m<\/jats:sc> of <jats:sc>l<\/jats:sc>\u2010<jats:styled-content style=\"fixed-case\">DOPA<\/jats:styled-content>. <jats:italic>Western<\/jats:italic> blot results showed that <jats:styled-content style=\"fixed-case\">ACZ<\/jats:styled-content> significantly (<jats:italic>P\u00a0<\/jats:italic>&lt;<jats:italic>\u00a0<\/jats:italic>0.05) decreased the expression level of tyrosinase at 40\u00a0\u03bc<jats:sc>m<\/jats:sc>. Zebrafish embryos were treated with 10, 20 or 40\u00a0\u03bc<jats:sc>m<\/jats:sc> of <jats:styled-content style=\"fixed-case\">ACZ<\/jats:styled-content> and of positive control kojic acid. At 72\u00a0h of treatment with <jats:styled-content style=\"fixed-case\">ACZ<\/jats:styled-content> and kojic acid, <jats:styled-content style=\"fixed-case\">ACZ<\/jats:styled-content> significantly (<jats:italic>P\u00a0<\/jats:italic>&lt;<jats:italic>\u00a0<\/jats:italic>0.001) decreased the embryos pigmentation to 40.8% of untreated embryos at the dose of 40\u00a0\u03bc<jats:sc>m<\/jats:sc> of <jats:styled-content style=\"fixed-case\">ACZ<\/jats:styled-content> while kojic acid decreased only 25.0% of pigmentation at the same dose of kojic acid. <jats:italic>In silico<\/jats:italic> docking were performed against tyrosinase using PyRx tool. Docking studies suggested that His244, Asn260 and His85 are the major interacting residues in the binding site of the protein. In conclusion, our results suggest that <jats:styled-content style=\"fixed-case\">ACZ<\/jats:styled-content> is a good candidate for the inhibition of melanin and it could be used as a lead for developing the drugs for hyperpigmentary disorders and skin whitening.<\/jats:p>","DOI":"10.1002\/cbdv.201700117","type":"journal-article","created":{"date-parts":[[2017,5,29]],"date-time":"2017-05-29T12:26:45Z","timestamp":1496060805000},"source":"Crossref","is-referenced-by-count":29,"title":["Acetazolamide Inhibits the Level of Tyrosinase and Melanin: An Enzyme Kinetic, <i>In Vitro<\/i>,<i> In Vivo<\/i>, and <i>In Silico<\/i> Studies"],"prefix":"10.1002","volume":"14","author":[{"given":"Qamar","family":"Abbas","sequence":"first","affiliation":[{"name":"Department of Biological Sciences College of Natural Sciences Kongju National University 56 Gongjudehak\u2010Ro 56 Gongju Chungnam 32588 Korea"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Hussain","family":"Raza","sequence":"additional","affiliation":[{"name":"Department of Biological Sciences College of Natural Sciences Kongju National University 56 Gongjudehak\u2010Ro 56 Gongju Chungnam 32588 Korea"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Mubashir","family":"Hassan","sequence":"additional","affiliation":[{"name":"Department of Biological Sciences College of Natural Sciences Kongju National University 56 Gongjudehak\u2010Ro 56 Gongju Chungnam 32588 Korea"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Abdul Rehman","family":"Phull","sequence":"additional","affiliation":[{"name":"Department of Biological Sciences College of Natural Sciences Kongju National University 56 Gongjudehak\u2010Ro 56 Gongju Chungnam 32588 Korea"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Song Ja","family":"Kim","sequence":"additional","affiliation":[{"name":"Department of Biological Sciences College of Natural Sciences Kongju National University 56 Gongjudehak\u2010Ro 56 Gongju Chungnam 32588 Korea"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Sung\u2010Yum","family":"Seo","sequence":"additional","affiliation":[{"name":"Department of Biological Sciences College of Natural Sciences Kongju National University 56 Gongjudehak\u2010Ro 56 Gongju Chungnam 32588 Korea"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2017,8,11]]},"reference":[{"key":"e_1_2_8_2_1","doi-asserted-by":"publisher","DOI":"10.1111\/j.1600-0749.2004.00198.x"},{"key":"e_1_2_8_3_1","doi-asserted-by":"publisher","DOI":"10.1111\/exd.12765"},{"key":"e_1_2_8_4_1","doi-asserted-by":"publisher","DOI":"10.1002\/ptr.1954"},{"key":"e_1_2_8_5_1","doi-asserted-by":"crossref","first-page":"23707","DOI":"10.1016\/S0021-9258(18)35895-2","article-title":"Mutational Mapping of the Catalytic Activities of Human Tyrosinase","volume":"267","author":"Tripathi R. 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