Antidiabetic, antioxidant, and anti-obesity effects of phenylthio-ethyl benzoate derivatives, and molecular docking study regarding alpha-amylase enzyme

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Jaradat N., Khasati A., Hawi M., Hawash M., Shekfeh S., Qneibi M., ...More

SCIENTIFIC REPORTS, vol.12, no.1, 2022 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 12 Issue: 1
  • Publication Date: 2022
  • Doi Number: 10.1038/s41598-022-07188-2
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Academic Search Premier, BIOSIS, CAB Abstracts, Chemical Abstracts Core, EMBASE, MEDLINE, Veterinary Science Database, Directory of Open Access Journals
  • Gazi University Affiliated: Yes


In addition to their wide therapeutic application, benzoates and benzoic acid derivatives are the most commonly utilized food preservatives. The purpose of this study was to estimate the antioxidant, anti-diabetic, and anti-obesity activities of four 2-(phenylthio)-ethyl benzoate derivatives utilizing standard biomedical assays. The results revealed that the 2a compound has potent antidiabetic activity through the inhibition of alpha-amylase and alpha-glycosidase with IC50 doses of 3.57 +/- 1.08 and 10.09 +/- 0.70 mu g/ml, respectively, compared with the positive control acarbose (IC50 = 6.47 and 44.79 mu g/ml), respectively. In addition, by utilizing the beta-carotene linoleic acid and DPPH methods, the 2a compound showed the highest antioxidant activity compared with positive controls. Moreover, the 2a compound showed potential anti-lipase activity with an IC50 dose of 107.95 +/- 1.88 mu g/ml compared to orlistat (IC50 = 25.01 +/- 0.78 mu g/ml). A molecular docking study was used to understand the interactions between four derivatives of (2-(phenylthio)-ethyl benzoate with alpha-amylase binding pocket. The present study concludes that the 2a compound could be exploited for further antidiabetic, antioxidant, and anti-obesity preclinical and clinical tests and design suitable pharmaceutical forms to treat these global health problems.