Startseite Anticancer, antimicrobial and antioxidant potential of sterically tuned bis-N-heterocyclic salts
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Anticancer, antimicrobial and antioxidant potential of sterically tuned bis-N-heterocyclic salts

  • Noor ul Huda , Shamsul Islam , Muhammad Zia , Kainaat William , Fakhar i Abbas , Muhammad Ihtisham Umar , Muhammad Adnan Iqbal ORCID logo EMAIL logo und Abdul Mannan EMAIL logo
Veröffentlicht/Copyright: 30. November 2018
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Abstract

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.

Award Identifier / Grant number: 1085

Funding statement: Dr. Muhammad Adnan Iqbal is thankful to the Higher Education Commission of Pakistan, Funder Id: 10.13039/501100004681 (HEC) for Start up Research Grant (SRGP) Project Number 1085/Letter Number 21-1085/SRGP/R&D.

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Received: 2018-06-21
Revised: 2018-10-18
Accepted: 2018-10-29
Published Online: 2018-11-30
Published in Print: 2018-12-19

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