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Efforts geared toward effective therapeutic strategies with minimal side effects are underway. Peptides derived from natural resources have recently gained special attention as alternative chemotherapeutic agents due to their minimal adverse effects. In the present study, the aim was to isolate peptides from garlic (<jats:italic>Allium sativum<\/jats:italic>) and investigate their anticancer activity against leukemic cell lines. The protein extract of <jats:italic>A.\u00a0sativum<\/jats:italic> was pepsin\u2010digested to obtain protein hydrolysate followed by sequential purification methods. A novel anticancer peptide, VKLRSLLCS (VS\u20109), was identified and characterized by mass spectrometric analysis. The peptide was demonstrated to significantly inhibit the cell proliferation of MOLT\u20104 and K562 leukemic cell lines while exhibiting minimal inhibition against normal PBMC. Particularly, VS\u20109 could induce apoptosis and upregulate mRNA levels of <jats:italic>caspase 3<\/jats:italic>, <jats:italic>caspase 8<\/jats:italic>, <jats:italic>caspase 9<\/jats:italic>, and <jats:italic>Bax<\/jats:italic> while downregulating <jats:italic>Bcl\u20102<\/jats:italic>, <jats:italic>Bcl\u2010xL<\/jats:italic>, <jats:italic>and Bcl\u2010w<\/jats:italic>. Molecular docking of VS\u20109 with the anti\u2010apoptotic Bcl\u20102 protein family suggested that VS\u20109 could bind the binding groove of the BH3 domain on target proteins. Protein\u2013peptide interaction analysis by affinity chromatography and LC\u2010MS\/MS further showed that VS\u20109 could bind Bcl\u20102 proteins. Results suggest VS\u20109 as a potential garlic\u2010derived novel anticancer peptide possessing apoptosis\u2010inducing properties against leukemic cell lines via anti\u2010apoptotic Bcl\u20102 protein family.<\/jats:p>","DOI":"10.1111\/cbdd.13831","type":"journal-article","created":{"date-parts":[[2021,2,18]],"date-time":"2021-02-18T03:59:44Z","timestamp":1613620784000},"page":"1017-1028","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":29,"title":["A novel peptide isolated from garlic shows anticancer effect against leukemic cell lines via interaction with Bcl\u20102 family proteins"],"prefix":"10.1111","volume":"97","author":[{"given":"Karunaithas","family":"Rasaratnam","sequence":"first","affiliation":[{"name":"Department of Clinical Microscopy Faculty of Medical Technology Mahidol University Nakhon pathom Thailand"},{"name":"Department of Medical Laboratory Sciences Faculty of Allied Health Sciences University of Jaffna 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