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.
Sorghum is an important cereal with diverse phenolic compounds that have potential health promoting benefits. The current study comparatively characterized the phenolic contents of two novel black-seeded sorghum lines (SC84 and PI570481) using different extraction systems (water, ethanol and their acidified counterparts) and evaluated their antioxidant and anti-inflammatory activities. Phenolic compositions were determined by spectrophotometric assays and HPLC analysis. Antioxidant activities were assessed by radical scavenging effects on nitric oxide (NO) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radicals, and the oxygen radical absorbance capacity (ORAC). Anti-inflammatory capacity was estimated by measuring levels of pro-inflammatory markers produced by lipopolysaccharide (LPS)-induced RAW 264.7 macrophages. Results showed that effects of solvent types and HCl on extraction efficiency differed among phenolic compounds and sorghum samples. Tannins were the most dominant polyphenols in the studied extracts (11.11–136.11 mg epicatechin equivalent/g sorghum). Sorghum extracts exerted more potent scavenging activity on DPPH than NO radicals. In LPS-activated RAW 264.7 cells, sorghum extracts dose-dependently inhibited the production of NO, interleukin-6 (IL-6), and intracellular reactive oxygen species (ROS), with ethanolic extracts showing greater anti-inflammatory activity. Positive correlations were noted between tannin content and DPPH radical scavenging activity, and anti-inflammatory capacity. These results suggest the potential role of tannin-rich sorghum extracts against inflammation and associated diseases.
Lactobacillus spp., as probiotics, have shown efficacy in the inhibition of pathogenic bacteria in the intestinal tract. In this study, we investigated the antibacterial activity of Lactobacillus casei NA-2, which was isolated from northeast sauerkraut in China. The results of co-culture suggested that L. casei NA-2 could inhibit the growth of Bacillus cereus, Staphylococcus aureus, Salmonella typhimurium and Escherichia coli O157:H7. Moreover, L. casei NA-2 could adhere to the four pathogenic bacteria potentially associated with its exopolysaccharide (EPS). EPS from L. casei NA-2 was then isolated and its activity determined. The results showed that EPS inhibited the biofilms of B. cereus, S. aureus, S. typhimurium and E. coli O157:H7, with the highest inhibition ratios of 95.5% ± 0.1%, 30.2% ± 3.3%, 14.3% ± 0.6%, and 16.9% ± 5.4%, respectively. Moreover, EPS was able to disperse B. cereus, S. aureus, S. typhimurium and E. coli O157:H7 by 94.1% ± 1.2%, 31.8% ± 8.6%, 40.8% ± 3.3% and 49.6% ± 3.8%, respectively. Results showed that EPS from L. casei NA-2 have potential antibacterial properties by inhibiting biofilm formation and dispersing pathogenic bacteria. In conclusion, the antibiofilm property of the EPS on the surface of L. casei NA-2 is one of the possible reasons for antibacterial activity of L. casei NA-2.