{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,7,29]],"date-time":"2026-07-29T06:40:03Z","timestamp":1785307203030,"version":"3.55.0"},"reference-count":34,"publisher":"MDPI AG","issue":"14","license":[{"start":{"date-parts":[[2022,7,19]],"date-time":"2022-07-19T00:00:00Z","timestamp":1658188800000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"DOI":"10.13039\/501100002367","name":"Youth Innovation on Promotion Association, Chinese Academy of Science","doi-asserted-by":"publisher","award":["2019425"],"award-info":[{"award-number":["2019425"]}],"id":[{"id":"10.13039\/501100002367","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100002367","name":"Youth Innovation on Promotion Association, Chinese Academy of Science","doi-asserted-by":"publisher","award":["2022D03018"],"award-info":[{"award-number":["2022D03018"]}],"id":[{"id":"10.13039\/501100002367","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100002367","name":"Youth Innovation on Promotion Association, Chinese Academy of Science","doi-asserted-by":"publisher","award":["2019-XBQNXZ-B-015"],"award-info":[{"award-number":["2019-XBQNXZ-B-015"]}],"id":[{"id":"10.13039\/501100002367","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100002367","name":"Youth Innovation on Promotion Association, Chinese Academy of Science","doi-asserted-by":"publisher","award":["2021-JCTD-001"],"award-info":[{"award-number":["2021-JCTD-001"]}],"id":[{"id":"10.13039\/501100002367","id-type":"DOI","asserted-by":"publisher"}]},{"name":"Special Training Program of Natural Science Foundation of Xinjiang Autonomous Region","award":["2019425"],"award-info":[{"award-number":["2019425"]}]},{"name":"Special Training Program of Natural Science Foundation of Xinjiang Autonomous Region","award":["2022D03018"],"award-info":[{"award-number":["2022D03018"]}]},{"name":"Special Training Program of Natural Science Foundation of Xinjiang Autonomous Region","award":["2019-XBQNXZ-B-015"],"award-info":[{"award-number":["2019-XBQNXZ-B-015"]}]},{"name":"Special Training Program of Natural Science Foundation of Xinjiang Autonomous Region","award":["2021-JCTD-001"],"award-info":[{"award-number":["2021-JCTD-001"]}]},{"DOI":"10.13039\/501100002367","name":"West Light Foundation of the Chinese Academy of Science","doi-asserted-by":"publisher","award":["2019425"],"award-info":[{"award-number":["2019425"]}],"id":[{"id":"10.13039\/501100002367","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100002367","name":"West Light Foundation of the Chinese Academy of Science","doi-asserted-by":"publisher","award":["2022D03018"],"award-info":[{"award-number":["2022D03018"]}],"id":[{"id":"10.13039\/501100002367","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100002367","name":"West Light Foundation of the Chinese Academy of Science","doi-asserted-by":"publisher","award":["2019-XBQNXZ-B-015"],"award-info":[{"award-number":["2019-XBQNXZ-B-015"]}],"id":[{"id":"10.13039\/501100002367","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100002367","name":"West Light Foundation of the Chinese Academy of Science","doi-asserted-by":"publisher","award":["2021-JCTD-001"],"award-info":[{"award-number":["2021-JCTD-001"]}],"id":[{"id":"10.13039\/501100002367","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["IJMS"],"abstract":"<jats:p>Vitiligo is a common chronic dermatological abnormality that afflicts tens of millions of people. Furocoumarins isolated from Uygur traditional medicinal material Psoralen corylifolia L. have been proven to be highly effective for the treatment of vitiligo. Although many furocoumarin derivatives with anti-vitiligo activity have been synthesized, their targets with respect to the disease are still ambiguous. Fortunately, the JAKs were identified as potential targets for the disease and its inhibitors have been proved to be effective in the treatment of vitiligo in many clinical trials. Thus, sixty-five benzene sulfonate and benzoate derivatives of furocoumarins (7a\u20137ad, 8a\u20138ag) with superior anti-vitiligo activity targeting JAKs were designed and synthesized based on preliminary research. The SAR was characterized after the anti-vitiligo-activity evaluation in B16 cells. Twenty-two derivatives showed more potent effects on melanin synthesis in B16 cells than the positive control (8-MOP). Among them, compounds 7y and 8 not only could increase melanin content, but they also improved the catecholase activity of tyrosinase in a concentration-dependent manner. The docking studies indicated that they were able to interact with amino acid residues in JAK1 and JAK2 via hydrogen bonds. Furthermore, candidate 8 showed a moderate inhibition of CXCL\u221210, which plays an important role in JAK\u2013STAT signaling. The RT-PCR and Western blotting analyses illustrated that compounds 7y and 8 promoted melanogenesis by activating the p38 MAPK and Akt\/GSK-3\u03b2\/\u03b2-catenin pathways, as well as increasing the expressions of the MITF and tyrosinase-family genes. Finally, furocoumarin derivative 8 was recognized as a promising candidate for the fight against the disease and worthy of further research in vivo.<\/jats:p>","DOI":"10.3390\/ijms23147959","type":"journal-article","created":{"date-parts":[[2022,7,19]],"date-time":"2022-07-19T23:10:22Z","timestamp":1658272222000},"page":"7959","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":16,"title":["Study of Novel Furocoumarin Derivatives on Anti-Vitiligo Activity, Molecular Docking and Mechanism of Action"],"prefix":"10.3390","volume":"23","author":[{"ORCID":"https:\/\/orcid.org\/0000-0001-5943-6771","authenticated-orcid":false,"given":"Chao","family":"Niu","sequence":"first","affiliation":[{"name":"State Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, CAS Key Labortory of Chemistry of Plant Resources in Arid Zone, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi 830011, China"},{"name":"University of Chinese Academy of Sciences, Beijing 100049, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Deng","family":"Zang","sequence":"additional","affiliation":[{"name":"State Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, CAS Key Labortory of Chemistry of Plant Resources in Arid Zone, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi 830011, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-4652-6879","authenticated-orcid":false,"given":"Haji Akber","family":"Aisa","sequence":"additional","affiliation":[{"name":"State Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, CAS Key Labortory of Chemistry of Plant Resources in Arid Zone, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi 830011, China"},{"name":"University of Chinese Academy of Sciences, Beijing 100049, China"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2022,7,19]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"883","DOI":"10.1016\/j.jaad.2015.07.039","article-title":"Vitiligo is not a cosmetic disease","volume":"73","author":"Ezzedine","year":"2015","journal-title":"J. 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