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Its effective antioxidant and anti-inflammatory properties position it as a promising functional food ingredient and nutraceutical candidate. Traditional production via plant extraction is limited by long growth cycles and low yields, while chemical synthesis uses toxic reagents and harsh conditions. Microbial biosynthesis offers a sustainable alternative. To date, baicalein titers of 367.8 mg\/L in Escherichia coli and 401.9 mg\/L in Pichia pastoris have been achieved through pathway optimization. However, a systematic review integrating its bioactivities and biosynthesis is still lacking. This review summarizes baicalein\u2019s sources, structure, pharmacological activities, and applications, with a focus on heterologous biosynthesis and pathway optimization. Future prospects are also proposed to promote its further biomedical applications and efficient production.<\/jats:p>","DOI":"10.1021\/acs.jafc.6c10769","type":"journal-article","created":{"date-parts":[[2026,9,21]],"date-time":"2026-09-21T14:04:55Z","timestamp":1789999495000},"page":"29812-29831","source":"Crossref","is-referenced-by-count":0,"title":["Pharmacological\nActivities, Biosynthetic Strategies,\nand Future Prospects: A Comprehensive Review of Baicalein"],"prefix":"10.1021","volume":"74","author":[{"given":"Zheng","family":"Liu","sequence":"first","affiliation":[{"name":"Jiangnan University , , 1800 Lihu Road , ,","place":["Wuxi, China, 214122"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yibo","family":"Shi","sequence":"additional","affiliation":[{"name":"Jiangnan University , , 1800 Lihu Road , ,","place":["Wuxi, China, 214122"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Chuanjun","family":"Hu","sequence":"additional","affiliation":[{"name":"Jiangnan University , , 1800 Lihu Road , ,","place":["Wuxi, China, 214122"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Hang","family":"Su","sequence":"additional","affiliation":[{"name":"Jiangnan University , , 1800 Lihu Road , ,","place":["Wuxi, China, 214122"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Xiaoyuan","family":"Yue","sequence":"additional","affiliation":[{"name":"Jiangnan University , , 1800 Lihu Road , ,","place":["Wuxi, China, 214122"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Liang","family":"Cheng","sequence":"additional","affiliation":[{"name":"Jiangnan University , , 1800 Lihu Road , ,","place":["Wuxi, China, 214122"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Wei","family":"Shen","sequence":"additional","affiliation":[{"name":"Jiangnan University , , 1800 Lihu Road , ,","place":["Wuxi, China, 214122"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-1054-2044","authenticated-orcid":true,"given":"Yuanyuan","family":"Xia","sequence":"additional","affiliation":[{"name":"Jiangnan University , , 1800 Lihu Road , ,","place":["Wuxi, China, 214122"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-8448-2040","authenticated-orcid":true,"given":"Li","family":"Zhou","sequence":"additional","affiliation":[{"name":"Jiangnan University , , 1800 Lihu Road , ,","place":["Wuxi, China, 214122"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-6173-8787","authenticated-orcid":true,"given":"Haiquan","family":"Yang","sequence":"additional","affiliation":[{"name":"Jiangnan University , , 1800 Lihu Road , ,","place":["Wuxi, China, 214122"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-0695-3382","authenticated-orcid":true,"given":"Xianzhong","family":"Chen","sequence":"additional","affiliation":[{"name":"Jiangnan University , , 1800 Lihu Road , ,","place":["Wuxi, China, 214122"]}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"316","published-online":{"date-parts":[[2026,9,21]]},"reference":[{"issue":"8","key":"2026093009073939900_cit1","doi-asserted-by":"publisher","first-page":"1639","DOI":"10.1016\/j.sjbs.2016.08.011","article-title":"Molecular characterization\nof flavonoid biosynthetic genes and accumulation of baicalin, baicalein,\nand wogonin in plant and hairy root of Scutellaria lateriflora.Saudi","volume":"25","author":"Tuan","year":"2018","journal-title":"J. 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Inorg.\nBiochem."},{"issue":"1","key":"2026093009073939900_cit24","doi-asserted-by":"publisher","first-page":"223","DOI":"10.3390\/molecules23010223","article-title":"Protective\nmechanism of the antioxidant baicalein toward hydroxyl\nradical-treated bone marrow-derived mesenchymal stem cells","volume":"23","author":"Tian","year":"2018","journal-title":"Molecules"},{"issue":"3","key":"2026093009073939900_cit25","doi-asserted-by":"publisher","first-page":"326","DOI":"10.1016\/j.jinorgbio.2008.11.003","article-title":"Iron-binding and anti-fenton\nproperties of baicalein\nand baicalin","volume":"103","author":"Perez","year":"2009","journal-title":"J. Inorg. Biochem."},{"issue":"4","key":"2026093009073939900_cit26","doi-asserted-by":"publisher","first-page":"256","DOI":"10.1016\/j.jpha.2016.04.001","article-title":"Effects of urea, metal\nions and surfactants on the binding of baicalein with bovine serum\nalbumin","volume":"6","author":"Roy","year":"2016","journal-title":"J. Pharm. 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Ethnopharmacol."},{"key":"2026093009073939900_cit40","doi-asserted-by":"publisher","first-page":"210","DOI":"10.1016\/j.jep.2014.08.031","article-title":"Safety, Tolerability,\nand pharmacokinetics of a single\nascending dose of baicalein chewable tablets in healthy subjects","volume":"156","author":"Li","year":"2014","journal-title":"J. Ethnopharmacol."},{"issue":"4","key":"2026093009073939900_cit41","doi-asserted-by":"publisher","DOI":"10.1126\/sciadv.1501780","article-title":"A specialized\nflavone\nbiosynthetic pathway has evolved in the medicinal plant, Scutellaria baicalensis","volume":"2","author":"Zhao","year":"2016","journal-title":"Sci. Adv."},{"key":"2026093009073939900_cit42","doi-asserted-by":"publisher","first-page":"255","DOI":"10.1016\/j.jep.2014.12.027","article-title":"Oroxylum indicum (L.) 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