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Emerging evidence suggests that esculetin has a wide range of pharmacological activities. Based on its fundamental properties, including antioxidant, antiinflammatory, antiapoptotic, anticancer, antidiabetic, neuroprotective, and cardiovascular protective activities, as well as antibacterial activity, among others, esculetin is expected to be a therapeutic drug for specific disease indications, such as cancer, diabetes, atherosclerosis, Alzheimer's disease (AD), Parkinson's disease (PD), nonalcoholic fatty liver disease (NAFLD), and other diseases. The oral bioavailability of esculetin was shown by studies to be low. The extensive glucuronidation was described to be the main metabolic pathway of esculetin and C\u20107 phenolic hydroxyl to be its major metabolic site. With the development of scientific research technology, the pharmacological effects of esculetin are identified and its potential for the treatment of diseases is demonstrated. The underlining mechanisms of action and biological activities as well as the pharmacokinetic data of the analyzed compound reported so far are highlighted in this review with the aim of becoming a proven, and applicable insight and reference for further studies on the utilization of esculetin.\n                  <\/jats:p>","DOI":"10.1002\/ptr.7311","type":"journal-article","created":{"date-parts":[[2021,11,22]],"date-time":"2021-11-22T19:54:16Z","timestamp":1637610856000},"page":"279-298","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":110,"title":["Esculetin: A review of its pharmacology and pharmacokinetics"],"prefix":"10.1002","volume":"36","author":[{"given":"Linlin","family":"Zhang","sequence":"first","affiliation":[{"name":"School of Pharmacy Chengdu University of Traditional Chinese Medicine Chengdu China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-3891-8098","authenticated-orcid":false,"given":"Qingxuan","family":"Xie","sequence":"additional","affiliation":[{"name":"School of Pharmacy Chengdu University of Traditional Chinese Medicine Chengdu China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Xiaofang","family":"Li","sequence":"additional","affiliation":[{"name":"School of Pharmacy Chengdu University of Traditional Chinese Medicine Chengdu China"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2021,11,22]]},"reference":[{"key":"e_1_2_10_2_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.apjtm.2016.01.014"},{"key":"e_1_2_10_3_1","doi-asserted-by":"publisher","DOI":"10.1002\/acn3.282"},{"key":"e_1_2_10_4_1","doi-asserted-by":"publisher","DOI":"10.1186\/s12943-016-0550-2"},{"key":"e_1_2_10_5_1","doi-asserted-by":"publisher","DOI":"10.1007\/s13105-011-0103-5"},{"key":"e_1_2_10_6_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bbrc.2015.04.034"},{"key":"e_1_2_10_7_1","doi-asserted-by":"publisher","DOI":"10.1161\/01.RES.75.3.539"},{"key":"e_1_2_10_8_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.etp.2010.02.006"},{"key":"e_1_2_10_9_1","doi-asserted-by":"publisher","DOI":"10.1007\/s13277-015-4286-1"},{"key":"e_1_2_10_10_1","first-page":"617","article-title":"Amplification and functional characterization of MUC1 promoter and gene\u2010virotherapy via a targeting adenoviral vector expressing hSSTR2 gene in MUC1\u2010positive Panc\u20101 pancreatic cancer cells in vitro","volume":"15","author":"Chen L.","year":"2005","journal-title":"International Journal of Molecular Medicine"},{"key":"e_1_2_10_11_1","doi-asserted-by":"publisher","DOI":"10.3109\/10715762.2015.1087643"},{"key":"e_1_2_10_12_1","doi-asserted-by":"publisher","DOI":"10.1161\/01.RES.0000040420.17366.2E"},{"key":"e_1_2_10_13_1","doi-asserted-by":"publisher","DOI":"10.3892\/ijo.2014.2700"},{"key":"e_1_2_10_14_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.cbi.2016.10.013"},{"key":"e_1_2_10_15_1","doi-asserted-by":"publisher","DOI":"10.1002\/ijc.24563"},{"key":"e_1_2_10_16_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.advenzreg.2007.11.016"},{"issue":"29","key":"e_1_2_10_17_1","first-page":"3173","article-title":"Coumarins as promising scaffold for the treatment of age\u2010related diseases\u2014An overview of the last five years","volume":"17","author":"Delogu G. 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