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Design, Synthesis, Spectroscopic Characterization, and in Vitro Pharmacological Evaluation of Novel 2-(5-Alkoxybenzimidazol-2-ylthio)-N-arylacetamide Derivatives as Antimicrobial and Antioxidant Agents
Subject area: Biological & Medical Sciences · Area of research: Pharmacy
Abstract
Background: Gentamicin remains an important and inexpensive aminoglycoside antibiotic, but its clinical value is limited by dose-dependent injury to the proximal tubular epithelium, a process driven largely by oxidative stress. Sugarcane (Saccharum officinarum L.) leaves are rich in flavonoids, including luteolin, yet the contribution of luteolin to the reported renal benefits of sugarcane has not been tested directly. Objective: To isolate luteolin from sugarcane leaves and evaluate its nephroprotective activity against gentamicin-induced nephrotoxicity in rats. Methods: Shade-dried leaves were extracted with ethanol in a Soxhlet apparatus, and luteolin was isolated by silica-gel column chromatography with gradient elution. Identity was supported by thin-layer chromatography against authentic luteolin, melting point, and ultraviolet and infrared spectroscopy. After an acute oral toxicity study, thirty Wistar rats were divided into five groups of six: normal control, gentamicin control (80 mg/kg, i.p., 8 days), standard antioxidant, and low-dose and high-dose luteolin-rich fraction given orally with gentamicin. Serum creatinine, blood urea nitrogen (BUN), uric acid, kidney malondialdehyde (MDA), relative kidney weight, body weight and renal histology were assessed. Results: The ethanolic extract yield was about 9–10% w/w, and the isolate showed an Rf of 0.62 against 0.61 for standard luteolin and UV maxima near 253 and 350 nm. No mortality or toxic signs occurred in the acute study. Gentamicin raised creatinine (0.72 to 3.18 mg/dL), BUN (18.4 to 62.5 mg/dL), uric acid (1.9 to 5.8 mg/dL), kidney MDA (2.1 to 7.9 nmol/mg) and relative kidney weight (0.62 to 1.05%), and caused tubular necrosis, casts and inflammation. The high dose of luteolin-rich fraction restored these values towards normal (creatinine 1.24 mg/dL, BUN 26.8 mg/dL, MDA 3.1 nmol/mg), gave about 80% protection, and preserved tubular architecture, comparable to the standard. The low dose gave intermediate protection. Conclusions: Luteolin from sugarcane leaves protects against gentamicin nephrotoxicity in a dose-dependent manner, most probably by suppressing lipid peroxidation. Confirmation of purity by spectroscopic methods and mechanistic studies are warranted.
Keywords
luteolin; Saccharum officinarum; sugarcane leaves; gentamicin; nephrotoxicity; oxidative stress; malondialdehyde; nephroprotection
References
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How to cite this paper
@article{1723900,
author = {Rajendra Kumar Yadav, Santosh Kumar Shukla},
title = {Design, Synthesis, Spectroscopic Characterization, and in Vitro Pharmacological Evaluation of Novel 2-(5-Alkoxybenzimidazol-2-ylthio)-N-arylacetamide Derivatives as Antimicrobial and Antioxidant Agents},
journal = {Iconic Research And Engineering Journals},
year = {2026},
volume = {10},
number = {4},
pages = {1455-1464},
issn = {2456-8880},
url = {https://www.irejournals.com/formatedpaper/1723900.pdf},
abstract = {Background: Gentamicin remains an important and inexpensive aminoglycoside antibiotic, but its clinical value is limited by dose-dependent injury to the proximal tubular epithelium, a process driven largely by oxidative stress. Sugarcane (Saccharum officinarum L.) leaves are rich in flavonoids, including luteolin, yet the contribution of luteolin to the reported renal benefits of sugarcane has not been tested directly.
Objective: To isolate luteolin from sugarcane leaves and evaluate its nephroprotective activity against gentamicin-induced nephrotoxicity in rats.
Methods: Shade-dried leaves were extracted with ethanol in a Soxhlet apparatus, and luteolin was isolated by silica-gel column chromatography with gradient elution. Identity was supported by thin-layer chromatography against authentic luteolin, melting point, and ultraviolet and infrared spectroscopy. After an acute oral toxicity study, thirty Wistar rats were divided into five groups of six: normal control, gentamicin control (80 mg/kg, i.p., 8 days), standard antioxidant, and low-dose and high-dose luteolin-rich fraction given orally with gentamicin. Serum creatinine, blood urea nitrogen (BUN), uric acid, kidney malondialdehyde (MDA), relative kidney weight, body weight and renal histology were assessed.
Results: The ethanolic extract yield was about 9–10% w/w, and the isolate showed an Rf of 0.62 against 0.61 for standard luteolin and UV maxima near 253 and 350 nm. No mortality or toxic signs occurred in the acute study. Gentamicin raised creatinine (0.72 to 3.18 mg/dL), BUN (18.4 to 62.5 mg/dL), uric acid (1.9 to 5.8 mg/dL), kidney MDA (2.1 to 7.9 nmol/mg) and relative kidney weight (0.62 to 1.05%), and caused tubular necrosis, casts and inflammation. The high dose of luteolin-rich fraction restored these values towards normal (creatinine 1.24 mg/dL, BUN 26.8 mg/dL, MDA 3.1 nmol/mg), gave about 80% protection, and preserved tubular architecture, comparable to the standard. The low dose gave intermediate protection.
Conclusions: Luteolin from sugarcane leaves protects against gentamicin nephrotoxicity in a dose-dependent manner, most probably by suppressing lipid peroxidation. Confirmation of purity by spectroscopic methods and mechanistic studies are warranted.},
keywords = {luteolin; Saccharum officinarum; sugarcane leaves; gentamicin; nephrotoxicity; oxidative stress; malondialdehyde; nephroprotection},
month = {October},
}