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.
Highlights
Diabetes[15,16]
MAP30, momordica anti-HIV protein, inhibited proliferation of MDA-MB-231 breast cancer cells and increased survival in MDA-MB-231 breast cancer mice xenografts[17], methanolic extract of BG led to reduced proliferation and activated autophagy in CRC18 and sensitized Colorectal cancer (CRC) to the cytotoxic effect of doxorubicin[19] while BG lectin has been shown to induce G2/M cell cycle arrest, autophagy and apoptosis in hepatocellular cancer[20]
We showed that BG-4 is very potent in inhibiting proliferation of both colon cancer cells, promoted apoptosis as measured by flow cytometry and microscopy study and the mechanism of action involved is through downregulation of antiapoptotic proteins Bcl-2 and XIAP, upregulation of proapoptotic proteins Bax and caspase-3 and modification of cell cycle proteins p21 and cyclin dependent kinase 2 (CDK2)
Summary
Diabetes[15,16]. In addition, extracts from different parts of BG possessed anticancer properties. In HCT-116 human colon cancer cells, the percentage of cells undergoing apoptosis was increased from 5.4% (untreated) to 9.5% and 24.8% for 62.5 μg/mL and 125 μg/mL treatment, respectively. In HT-29 human colon cancer cells, the percentage of cells undergoing apoptosis was increased from 8.5% (untreated) to 19.6% and 31.9% for 62.5 μg/mL and 125 μg/mL treatment, respectively.
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