Momordicine-I, a bitter melon bioactive metabolite, displays anti-tumor activity in head and neck cancer involving c-Met and downstream signaling

Subhayan Sur, Robert Steele, T. Scott Isbell, Kalyan Nagulapalli Venkata, Mostafa E. Rateb, Ratna B. Ray*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

2 Downloads (Pure)

Abstract

Head and neck cancer (HNC) is one of the most aggressive cancers, and treatments are quite challenging due to the difficulty in early diagnosis, lack of effective chemotherapeutic drugs, adverse side effects and therapy resistance. We identified momordicine-I (M-I), a bioactive secondary metabolite in bitter melon (Momordica charantia), by performing liquid chromatography-high resolution electrospray ionization mass spectrometry (LC-HRESIMS) analysis. M-I inhibited human HNC cell (JHU022, JHU029, Cal27) viability in a dose-dependent manner without an apparent toxic effect on normal oral keratinocytes. Mechanistic studies showed that M-I inhibited c-Met and its downstream signaling molecules c-Myc, survivin, and cyclin D1 through the inactivation of STAT3 in HNC cells. We further observed that M-I was non-toxic and stable in mouse (male C57Bl/6) blood, and a favorable pharmacokinetics profile was observed after IP administration. M-I treatment reduced HNC xenograft tumor growth in nude mice and inhibited c-Met and downstream signaling. Thus, M-I has potential therapeutic implications against HNC.
Original languageEnglish
Article number1432
Number of pages15
JournalCancers
Volume13
Issue number6
DOIs
Publication statusPublished - 21 Mar 2021

Keywords

  • momordicine-I
  • bitter melon (Momordica charantia)
  • head and neck cancer
  • C-MET signaling
  • therapy

Fingerprint

Dive into the research topics of 'Momordicine-I, a bitter melon bioactive metabolite, displays anti-tumor activity in head and neck cancer involving c-Met and downstream signaling'. Together they form a unique fingerprint.

Cite this