Structural characterization of: Momordica charantia L. (Cucurbitaceae) oligopeptides and the detection of their capability in non-small cell lung cancer A549 cells: Induction of apoptosis

Abstract

Oligopeptides are rarely reported from Chinese herbal medicine because they are often present in very low concentrations in a complex matrix. Twenty-eight oligopeptides were recently identified by high-performance liquid chromatography and quadrupole-time-of-flight-mass spectrometry (HPLC-Q-TOF-MS) from Momordica charantia L. (Cucurbitaceae), and a septapeptide, FHGKGHE (Phe-His-Gly-Lys-Gly-His-Glu), named MCLO-12, showed the best anticancer activity against the non-small cell lung cancer A549 cell line in vitro, with an IC50 value of 21.4 ± 2.21 mM. The anti-proliferative activity assay results showed that MCLO-12 induced apoptosis of A549 cells in a concentration-dependent manner. Treatment of the cells with MCLO-12 (10.7-42.8 mM mL-1) caused strong intracellular reactive oxygen species (ROS) up-regulating activities and activated caspase expression. MCLO-12 also suppressed the Trx system and subsequently activated a number of Trx-dependent pathways, including the ASK1, MAPK-p38 and JNK pathways. Thus, our research provides a good reference point for anti-NSCLC research into oligopeptides.