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<p>Metalloenzymes have emerged as substantial therapeutic targets in the pathogenesis of various human health conditions. Fluoroquinolones’ (FQs) derivatives of reduced nuclei harbor privileged scaffolds with versatile biological activities (antimicrobial, anti-inflammatory, selective antiproliferation and antilipolysis/antidiabesity). Highly functionalized lipophilic FQs (<b>6e, 4a,</b> and <b>6f</b>) with prominent in vitro DPPH radical scavenging capacities were fed orally (20 mg/kg body weight) for 3 days to adult male Wistar rats (200 ± 10) g of i.p.-CCl4 inflicted hepatic oxidative injury. In comparison to the untreated control group of CCl4 alone, rats treated with FQ compounds had a reduction in ALT levels (by 78.3%, 79.6%, and 77.9%, respectively), a reduction in AST levels (by 73.0%, 70.5%, and 61.6% respectively), and SOD levels resumed normality (by 142.8%, 168.6%, and 160%, respectively). Albumin levels were restored to normality (by 21.7%, 34.8%, and 34.9%, respectively), as well as the total antioxidative status (TAS) that was normalised alike (by 448.6%, 457.1%, and 468.6%, respectively). As chelation can be the highly plausible molecular antioxidation mechanism, the C-8-C-7 ethylene diamine divalent and trivalent chelator groups, lipophilicity, acidity, and size are among the key structural features required for FQs antioxidant effectiveness. Furthermore, FQs’ total H-B capabilities increase the total number of H-B donner/acceptors available for chelation.</p>

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Antioxidant activity and hepatoprotective effects of functionalized heterocyclic fluoroquinolone derivatives in carbon tetrachloride–induced liver injury in rats

  • 期刊论文

  • 发表日期：

    2025年8月7日

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  • Yusuf Al-Hiari,
  • Tareq Al-qirim,
  • Manal Suleiman,
  • Violet Kasabri,
  • Mohammad Alwahsh,
  • Hamza Abumansour

摘要

Metalloenzymes have emerged as substantial therapeutic targets in the pathogenesis of various human health conditions. Fluoroquinolones’ (FQs) derivatives of reduced nuclei harbor privileged scaffolds with versatile biological activities (antimicrobial, anti-inflammatory, selective antiproliferation and antilipolysis/antidiabesity). Highly functionalized lipophilic FQs (6e, 4a, and 6f) with prominent in vitro DPPH radical scavenging capacities were fed orally (20 mg/kg body weight) for 3 days to adult male Wistar rats (200 ± 10) g of i.p.-CCl4 inflicted hepatic oxidative injury. In comparison to the untreated control group of CCl4 alone, rats treated with FQ compounds had a reduction in ALT levels (by 78.3%, 79.6%, and 77.9%, respectively), a reduction in AST levels (by 73.0%, 70.5%, and 61.6% respectively), and SOD levels resumed normality (by 142.8%, 168.6%, and 160%, respectively). Albumin levels were restored to normality (by 21.7%, 34.8%, and 34.9%, respectively), as well as the total antioxidative status (TAS) that was normalised alike (by 448.6%, 457.1%, and 468.6%, respectively). As chelation can be the highly plausible molecular antioxidation mechanism, the C-8-C-7 ethylene diamine divalent and trivalent chelator groups, lipophilicity, acidity, and size are among the key structural features required for FQs antioxidant effectiveness. Furthermore, FQs’ total H-B capabilities increase the total number of H-B donner/acceptors available for chelation.