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.

Phytochemical profile and biological activities of Momordica charantia L. (Cucurbitaceae): A review

“…The anticancer activity of terpenoids and sterols found in M. charantia are also reported by other authors Weng et al, 2013). The literatures indicates that M. charantia inhibits many types of cancer, including hepatocellular carcinoma , lung (Fan et al, 2015), bladder , colon (Dia and Krishnan 2016) and breast (L. yuan cancers. The mechanisms of action of bioactive compounds on cancer cells may be related to apoptosis through the regulation of enzymes with a cysteine residue capable of cleaving other proteins (caspase) and mitochondria Manoharan et al, 2014;Minina et al, 2017).…”

Novel therapeutics: response and resistance in ovarian cancer

“…BG-4 is a bioactive peptide isolated from the seeds of Momordica charantia and exhibits anti-cancer properties. 18 While addition of transforming growth factor β1 to ovarian cancer cell lines in the presence of paclitaxel and cisplatin resulted in chemotherapy resistance, the resistance was ameliorated by addition of BG-4. This was accompanied by reversal of transforming growth factor β1-induced epithelial to mesenchymal transition, suggesting a possible mechanism of BG-4 action (NT-91).…”

Bitter melon (Momordica charantia): a natural healthy vegetable

“…[34] Owing to these functional components, bitter melon possess wide range of pharmacological activities for instance, antioxidant, [32] antifungal, [35] antidiabetic, [36] ant obesity, stomachic, anticancer, hypotensive, and blood cholesterol lowering effects. [37,38] The diabetes mellitus and associated complications are true example of lifestyle related disorders. The sedentary lifestyle, high intake of dietary energy, and obesity are amongst various causes leading to metabolic syndrome and diabetes mellitus.…”