title: BG-4, a novel anticancer peptide from bitter gourd (Momordica charantia), promotes apoptosis in human colon cancer cells.
abstract: Momordica charantia is a perennial plant with reported health benefits. BG-4, a novel peptide from Momordica charantia, was isolated, purified and characterized. The trypsin inhibitory activity of BG-4 is 8.6 times higher than purified soybean trypsin inhibitor. The high trypsin inhibitory activity of BG-4 may be responsible for its capability to cause cytotoxicity to HCT-116 and HT-29 human colon cancer cells with ED50 values of 134.4 and 217.0 μg/mL after 48 h of treatment, respectively. The mechanism involved in the cytotoxic effect may be associated with induction of apoptosis as evidenced by increased percentage of HCT-116 and HT-29 colon cancer cells undergoing apoptosis from 5.4% (untreated) to 24.8% (BG-4 treated, 125 μg/mL for 16 h) and 8.5% (untreated) to 31.9% (BG-4 treated, 125 μg/mL for 16 h), respectively. The molecular mechanistic explanation in the apoptosis inducing property of BG-4 is due to reduced expression of Bcl-2 and increased expression of Bax leading to increased expression of caspase-3 and affecting the expression of cell cycle proteins p21 and CDK2. This is the first report on the anti-cancer potential of a novel bioactive peptide isolated from Momordica charantia in vitro supporting the potential therapeutic property of BG-4 against colon cancer that must be addressed using in vivo models of colon carcinogenesis.
authors.affiliation: Department of Food Science and Technology, The University of Tennessee Institute of Agriculture, Knoxville TN 37996 USA.
authors.forename: Vermont P
authors.initials: VP
authors.lastname: Dia
authors.affiliation: USDA-ARS Plant Genetics Resources Unit, University of Missouri, Columbia, MO 65211 USA.
authors.forename: Hari B
authors.initials: HB
authors.lastname: Krishnan
mesh_terms: D000595:Amino Acid Sequence; D000970:Antineoplastic Agents / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D003110:Colonic Neoplasms / Q000473:pathology*; D000431:Ethanol / Q000737:chemistry; D006801:Humans; D013058:Mass Spectrometry; D008970:Molecular Weight; D029777:Momordica charantia / Q000737:chemistry*; D009363:Neoplasm Proteins / Q000378:metabolism; D010455:Peptides / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D010936:Plant Extracts / Q000494:pharmacology; D014361:Trypsin Inhibitors / Q000494:pharmacology; D014410:Tumor Stem Cell Assay; D014867:Water / Q000737:chemistry
chemical_list: D000970:Antineoplastic Agents; D009363:Neoplasm Proteins; D010455:Peptides; D010936:Plant Extracts; D014361:Trypsin Inhibitors; D014867:Water; D000431:Ethanol