Characterization and Investigation of Novel Benzodioxol Derivatives as Antidiabetic Agents: An In Vitro and In Vivo Study in an Animal Model

Mohammed Hawash*, Derar Al-Smadi, Anil Kumar, Barbara Olech, Paulina Maria Dominiak, Nidal Jaradat, Sarah Antari, Sarah Mohammed, Ala’a Nasasrh, Murad Abualhasan, Ahmed Musa, Shorooq Suboh, İrfan Çapan, Mohammad Qneibi, Hiba Natsheh*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

Abstract

In this study, we synthesized benzodioxol carboxamide derivatives and investigated their antidiabetic potential. The synthesized compounds (Ia-Ic and IIa-IId) underwent characterization via HRMS, 1H-, 13CAPT-NMR, and MicroED. Their efficacy against α-amylase was assessed in vitro, while MTS assays were employed to gauge cytotoxicity across cancer and normal cell lines. Additionally, the antidiabetic impact of compound IIc was evaluated in vivo using a streptozotocin-induced diabetic mice model. Notably, IIa and IIc displayed potent α-amylase inhibition (IC50 values of 0.85 and 0.68 µM, respectively) while exhibiting a negligible effect on the Hek293t normal cell line (IC50 > 150 µM), suggesting their safety. Compound IId demonstrated significant activity against four cancer cell lines (26–65 µM). In vivo experiments revealed that five doses of IIc substantially reduced mice blood glucose levels from 252.2 mg/dL to 173.8 mg/dL in contrast to the control group. The compelling in vitro anticancer efficacy of IIc and its safety for normal cells underscores the need for further in vivo assessment of this promising compound. This research highlights the potential of benzodioxol derivatives as candidates for the future development of synthetic antidiabetic drugs.

Original languageAmerican English
Article number1486
JournalBiomolecules
Volume13
Issue number10
DOIs
StatePublished - 6 Oct 2023
Externally publishedYes

Bibliographical note

Publisher Copyright:
© 2023 by the authors.

Keywords

  • benzodioxol
  • cytotoxicity
  • in vivo
  • mice
  • microED
  • streptozotocin
  • α-amylase

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