{"corpus_id":206970650,"paper_sha":"ebe4ad730ee73d00115b2ef13d1724b0d06f3172","doi":"10.1186/1471-2121-15-36","arxiv_id":null,"pmid":25303828,"pmcid":"4195704","mag_id":2163939713,"dblp_id":null,"acl_id":null,"title":"Cell specific apoptosis by RLX is mediated by NFκB in human colon carcinoma HCT-116 cells","year":2014,"publication_date":"2014-10-10","venue":"BMC Cell Biology","journal":{"name":"BMC Cell Biology","pages":"36 - 36","volume":"15"},"journal_issn":null,"journal_title":null,"publication_types":["JournalArticle"],"pubmed_pub_types":["Journal Article","Research Support, Non-U.S. Gov't"],"s2_fields_of_study":["Biology","Medicine"],"reference_count":23,"citation_count":19,"influential_citation_count":0,"is_open_access":true,"arxiv_categories":null,"arxiv_license":null,"arxiv_journal_ref":null,"mesh_headings":[{"d":"Acanthaceae","mj":false,"qs":[{"q":"chemistry","mj":false,"ui":"Q000737"}],"ui":"D027901"},{"d":"Alkaloids","mj":false,"qs":[{"q":"chemistry","mj":true,"ui":"Q000737"},{"q":"pharmacology","mj":true,"ui":"Q000494"}],"ui":"D000470"},{"d":"Antineoplastic Agents","mj":false,"qs":[{"q":"pharmacology","mj":true,"ui":"Q000494"}],"ui":"D000970"},{"d":"Apoptosis","mj":false,"qs":[{"q":"drug effects","mj":true,"ui":"Q000187"}],"ui":"D017209"},{"d":"Caspase 3","mj":false,"qs":[{"q":"genetics","mj":false,"ui":"Q000235"},{"q":"metabolism","mj":false,"ui":"Q000378"}],"ui":"D053148"},{"d":"Cell Movement","mj":false,"ui":"D002465"},{"d":"Colorectal Neoplasms","mj":false,"qs":[{"q":"drug therapy","mj":true,"ui":"Q000188"},{"q":"metabolism","mj":false,"ui":"Q000378"}],"ui":"D015179"},{"d":"Down-Regulation","mj":false,"qs":[{"q":"drug effects","mj":false,"ui":"Q000187"}],"ui":"D015536"},{"d":"HCT116 Cells","mj":false,"ui":"D045325"},{"d":"Humans","mj":false,"ui":"D006801"},{"d":"Membrane Potential, Mitochondrial","mj":false,"ui":"D053078"},{"d":"NF-kappa B","mj":false,"qs":[{"q":"metabolism","mj":true,"ui":"Q000378"}],"ui":"D016328"},{"d":"Up-Regulation","mj":false,"qs":[{"q":"drug effects","mj":false,"ui":"Q000187"}],"ui":"D015854"}],"chemicals":[{"n":"Alkaloids","ui":"D000470","reg":"0"},{"n":"Antineoplastic Agents","ui":"D000970","reg":"0"},{"n":"NF-kappa B","ui":"D016328","reg":"0"},{"n":"Caspase 3","ui":"D053148","reg":"EC 3.4.22.-"},{"n":"vasicinone","ui":"C052548","reg":"G6T5819NXM"}],"comments_corrections":null,"source_flags":5,"s2_open_access_pdf_url":"https://bmcmolcellbiol.biomedcentral.com/counter/pdf/10.1186/1471-2121-15-36","s2_open_access_landing_url":"https://www.semanticscholar.org/paper/ebe4ad730ee73d00115b2ef13d1724b0d06f3172","s2_open_access_license":"CCBY","s2_open_access_status":"GOLD","pmc_open_access_pdf_url":null,"pmc_open_access_landing_url":null,"pmc_open_access_license":null,"pmc_open_access_status":null,"unpaywall_open_access_pdf_url":null,"unpaywall_open_access_landing_url":null,"unpaywall_open_access_license":null,"unpaywall_open_access_status":null,"abstract":"BackgroundResistance 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.ResultsHere, 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.ConclusionsOverall, these findings indicate that RLX is a potent small molecule which triggers apoptosis, and promising potential candidate to be a chemotherapeutic agent.","claims":[{"public_id":"cl_dfe8624f9a88493156f2f37e3bba14a3","status":"active","text":"Combined RLX and BEZ-235 treatment in HCT-116 cells leads to down-regulation of NFκB protein expression (1 to 0.1 fold) and up-regulation of caspase-3 protein expression (1 to 2 fold).","confidence":0.9,"contributors":[{"id":1165,"public_id":"ezd9qvkvax","public_label":"The Reverser‮ (ezd9qvkvax)","roles":["extraction"],"url":"https://sah.borca.ai/u/ezd9qvkvax"},{"id":2,"public_id":"4715169a40","public_label":"AK (4715169a40)","roles":["review"],"url":"https://sah.borca.ai/u/4715169a40"},{"id":17,"public_id":"322360f1c1","public_label":"Killer Whale 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HCT-116 cells, evidenced by membrane blebbing, cell shrinkage, and chromatin condensation.","confidence":0.9,"contributors":[{"id":1165,"public_id":"ezd9qvkvax","public_label":"The Reverser‮ (ezd9qvkvax)","roles":["extraction"],"url":"https://sah.borca.ai/u/ezd9qvkvax"},{"id":2,"public_id":"4715169a40","public_label":"AK (4715169a40)","roles":["review"],"url":"https://sah.borca.ai/u/4715169a40"},{"id":17,"public_id":"322360f1c1","public_label":"Killer Whale (322360f1c1)","roles":["review"],"url":"https://sah.borca.ai/u/322360f1c1"}],"url":"https://sah.borca.ai/claims/cl_44d9f20e577e8fa3eb6d9770934bee31"}],"concepts":[{"public_id":"co_16bcf2c9aa3104024e6e56ec7a60455b","status":"active","name":"cell shrinkage","description":"Reduction in cell size during apoptosis, observed in HCT-116 cells.","types":["cellular phenomenon","apoptotic feature"],"aliases":["cellular shrinkage"],"contributors":[{"id":1165,"public_id":"ezd9qvkvax","public_label":"The Reverser‮ 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