<p>Eight synthetic derivatives of embelin (<b>1a–1f</b> and <b>2a</b> and <b>2b</b>) were synthesized to investigate their <i>α</i>-glucosidase inhibitory activity and antibacterial activity against two bacterial strains, <i>Aeromonas hydrophila</i> and <i>Acinetobacter baumannii</i>. Four of these compounds (<b>1a</b>, <b>1d</b>, <b>2a</b>, and <b>2b</b>) were to our knowledge previously unreported. In terms of <i>α</i>-glucosidase inhibition, compounds <b>2a</b> and <b>2b</b> exhibited the most potent activity, with IC<sub>50</sub> values of 15.2 and 15.1 μM, respectively, surpassing the positive control agent (acarbose, IC<sub>50</sub> 332.5 ± 5.0 μM). Both compounds, <b>2a</b> and <b>2b</b>, showed moderate inhibition against A. hydrophila, with inhibition zones of 15 and 16 mm, respectively. Only compound <b>2a</b> exhibited an inhibition zone of 16 mm against A. baumannii. The other derivatives (<b>1a–1f</b>) showed no activity in either of the tested assays.</p>

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New Embelin Derivatives with Their Biological Activities

  • Thi-Kim-Dung Le,
  • Tran-Ngoc-Tu-Trinh Cao,
  • Thi-Bich-Ngan Nguyen,
  • Quach-Mai-Anh Nguyen,
  • Ngoc-Phuong-Nhi Ho,
  • Minh-Truong-Tho Ho,
  • Chuong Hoang Nguyen,
  • Duc-Dung Pham,
  • Thuc-Huy Duong,
  • Ngoc-Hong Nguyen,
  • Jirapast Sichaem

摘要

Eight synthetic derivatives of embelin (1a–1f and 2a and 2b) were synthesized to investigate their α-glucosidase inhibitory activity and antibacterial activity against two bacterial strains, Aeromonas hydrophila and Acinetobacter baumannii. Four of these compounds (1a, 1d, 2a, and 2b) were to our knowledge previously unreported. In terms of α-glucosidase inhibition, compounds 2a and 2b exhibited the most potent activity, with IC50 values of 15.2 and 15.1 μM, respectively, surpassing the positive control agent (acarbose, IC50 332.5 ± 5.0 μM). Both compounds, 2a and 2b, showed moderate inhibition against A. hydrophila, with inhibition zones of 15 and 16 mm, respectively. Only compound 2a exhibited an inhibition zone of 16 mm against A. baumannii. The other derivatives (1a–1f) showed no activity in either of the tested assays.