title: Cell specific apoptosis by RLX is mediated by NFκB in human colon carcinoma HCT-116 cells.
abstract: BACKGROUND
  Resistance to chemotherapy represents a major obstacle in correcting colorectal carcinomas (CRC). Inspite of recent advances in the treatment of metastatic disease, the prognosis of the patients remains poor. RLX, a vasicinone analogue has been reported to possess potent bronchodilator, anti-asthmatic and anti-inflammatory properties. However, its anti-cancer activity is unknown.
  
  
  RESULTS
  Here, we report for the first time that RLX has anti-cancer property against panel of human cancer cell lines and most potent activity was found against HCT-116 cells with IC50 value of 12 μM and have further investigated the involvement of NFκB and caspase-3 in RLX action in CRC apoptosis. Following RLX and BEZ-235 treatment in HCT-116, we observed significant down-regulation of NFκB (1 to 0.1 fold) and up-regulation of caspase-3 (1 to 2 fold) protein expressions. Additionally, morphological studies revealed membrane blebbing, cell shrinkage, chromatin condensation and finally apoptosis in HCT-116 cells.
  
  
  CONCLUSIONS
  Overall, these findings indicate that RLX is a potent small molecule which triggers apoptosis, and promising potential candidate to be a chemotherapeutic agent.
authors.forename: Asif Khurshid
authors.initials: AK
authors.lastname: Qazi
authors.forename: Aashiq
authors.initials: A
authors.lastname: Hussain
authors.forename: Mushtaq A
authors.initials: MA
authors.lastname: Aga
authors.forename: Shakir
authors.initials: S
authors.lastname: Ali
authors.forename: Subhash Chandra
authors.initials: SC
authors.lastname: Taneja
authors.forename: Parduman Raj
authors.initials: PR
authors.lastname: Sharma
authors.forename: Ajit Kumar
authors.initials: AK
authors.lastname: Saxena
authors.forename: Dilip M
authors.initials: DM
authors.lastname: Mondhe
authors.affiliation: Cancer Pharmacology Division, CSIR-Indian Institute of Integrative Medicine, Jammu 180001, India. ahdar@iiim.ac.in.
authors.forename: Abid
authors.initials: A
authors.lastname: Hamid
mesh_terms: D027901:Acanthaceae / Q000737:chemistry; D000470:Alkaloids / Q000737:chemistry* / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D053148:Caspase 3 / Q000235:genetics / Q000378:metabolism; D002465:Cell Movement; D015179:Colorectal Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D015536:Down-Regulation / Q000187:drug effects; D045325:HCT116 Cells; D006801:Humans; D053078:Membrane Potential, Mitochondrial; D016328:NF-kappa B / Q000378:metabolism*; D015854:Up-Regulation / Q000187:drug effects
chemical_list: D000470:Alkaloids; D000970:Antineoplastic Agents; D016328:NF-kappa B; D053148:Caspase 3; C052548:vasicinone