{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,3,9]],"date-time":"2026-03-09T00:04:29Z","timestamp":1773014669410,"version":"3.50.1"},"reference-count":35,"publisher":"Wiley","issue":"9","license":[{"start":{"date-parts":[[2025,5,9]],"date-time":"2025-05-09T00:00:00Z","timestamp":1746748800000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"},{"start":{"date-parts":[[2025,5,9]],"date-time":"2025-05-09T00:00:00Z","timestamp":1746748800000},"content-version":"tdm","delay-in-days":0,"URL":"http:\/\/doi.wiley.com\/10.1002\/tdm_license_1.1"}],"content-domain":{"domain":["onlinelibrary.wiley.com"],"crossmark-restriction":true},"short-container-title":["Chemistry &amp;amp; Biodiversity"],"published-print":{"date-parts":[[2025,9]]},"abstract":"<jats:title>ABSTRACT<\/jats:title>\n                  <jats:p>Obesity is closely related to the occurrence and development of many diseases, such as diabetes, hypertension, and hyperlipidemia. As an important digestive enzyme, human pancreatic lipase (hPL) is involved in the metabolism and absorption of dietary fat and is a key target of overweight and obesity. Therefore, the inhibition of hPL enzyme is a feasible strategy for the prevention and treatment of obesity. In this study, we collected a series of marketed hypoglycemic and cardiovascular drugs and evaluated their inhibitory activity against hPL. Among them, ticagrelor (HC\u201014), prasugrel (HC\u201018), amlodipine (HC\u201026), simvastatin (HC\u201032), and lovastatin (HC\u201033) had strong inhibitory activity against hPL. In order to further clarify the inhibition mechanism, inhibition kinetics and molecular docking were carried out, and results revealed that HC\u201014 was a mixed inhibitory manner on hPL activity. HC\u201014 also showed similar inhibitory effect on human carboxylesterase 2 (hCES2), but poor inhibitory effect on other five serine hydrolases. Further studies showed that HC\u201014 significantly inhibited hPL activity in AR42J cells, resulting in dose\u2010dependent inhibition. Overall, the above results suggest that ticagrelor is a cardiovascular drug that inhibits hPL, which also provides an important reference for the search and development of other drugs for the treatment of obesity.<\/jats:p>","DOI":"10.1002\/cbdv.202500381","type":"journal-article","created":{"date-parts":[[2025,4,23]],"date-time":"2025-04-23T03:44:12Z","timestamp":1745379852000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":2,"title":["Discovery of Hypoglycemic and Cardiovascular Drugs as Effective Inhibitors on Human Pancreatic Lipase"],"prefix":"10.1002","volume":"22","author":[{"given":"Bing\u2010Jie","family":"Liang","sequence":"first","affiliation":[{"name":"Institute of Interdisciplinary Integrative Medicine Research Shanghai University of Traditional Chinese Medicine  Shanghai China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Le\u2010Xuan","family":"Dong","sequence":"additional","affiliation":[{"name":"Institute of Interdisciplinary Integrative Medicine Research Shanghai University of Traditional Chinese Medicine  Shanghai China"},{"name":"Shanghai Municipal Hospital of Traditional Chinese Medicine Shanghai University of Traditional Chinese Medicine  Shanghai China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Yang","family":"Yu","sequence":"additional","affiliation":[{"name":"College of Pharmacy Dalian Medical University  Dalian Liaoning Province China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Jing","family":"Zhang","sequence":"additional","affiliation":[{"name":"Institute of Interdisciplinary Integrative Medicine Research Shanghai University of Traditional Chinese Medicine  Shanghai China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Dan\u2010Dan","family":"Wang","sequence":"additional","affiliation":[{"name":"Collaborative Innovation Center of Tumor Marker Detection Technology, Equipment and Diagnosis Therapy Integration in Universities of Shandong, Shandong Province Key Laboratory of Detection Technology for Tumor Makers, School of Chemistry and Chemical Engineering Linyi University  Linyi Shandong Province China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Wen\u2010Yao","family":"He","sequence":"additional","affiliation":[{"name":"SPH Xing Ling Sci. &amp; Tech. 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