Anticancer, antimicrobial and antioxidant potential of sterically tuned bis-N-heterocyclic salts.
Noor Ul HudaShamsul IslamMuhammad ZiaKainaat WilliamFakhar I AbbasMuhammad Ihtisham UmarMuhammad Adnan IqbalAbdul MannanPublished in: Zeitschrift fur Naturforschung. C, Journal of biosciences (2019)
The current study was conducted to evaluate the antimicrobial, antioxidant, antileishmanial and cytotoxic potential of designed derivatives of 1,1'-(1,3-phenylenebis(methylene))bis(3-alkyl/aryl-1H-benzimidazol-3-ium) salts. The antibacterial potential of the test compounds was investigated against Staphylococcus aureus, Pseudomonas aeruginosa and two methicillin-resistant S. aureus (MRSA) strains (MRSA10, MRSA11), where compound 6 showed the best results. For brine shrimp lethality bioassay (BSLB), compound 6 again showed up to 100% mortality at 200 μg/mL and 56.7% mortality at 6.25 μg/mL. Antileishmanial assay was performed against Leishmania tropica at 20 μg/mL dosage, where 6 showed the most promising activity with 16.26% survival (83.74% mortality; IC50=14.63 μg/mL). The anticancer potential of the selected benzimidazole derivatives was evaluated against two selected cell lines (human colorectal cancer, HCT-116 and breast adenocarcinoma, MCF-7) using sulforhodamine B (SRB) assay. Compound 6 was found to be the most effective cytotoxic compound with 75% inhibition of HCT-116 proliferation at 1 mg/mL concentration. Succinctly, 6 exhibited impressive pharmacological potential that might be attributed to its higher lipophilic character owing to the longer N-substituted alkyl chains when compared to the other test compounds.
Keyphrases
- staphylococcus aureus
- methicillin resistant staphylococcus aureus
- ionic liquid
- pseudomonas aeruginosa
- biofilm formation
- oxidative stress
- endothelial cells
- high throughput
- risk factors
- cystic fibrosis
- type diabetes
- mass spectrometry
- signaling pathway
- cardiovascular disease
- coronary artery disease
- radiation therapy
- anti inflammatory
- drug resistant
- climate change
- atomic force microscopy
- molecular dynamics simulations
- breast cancer cells
- candida albicans
- pi k akt